CN101416955B - Improved cataplasm ground-mass and use thereof - Google Patents
Improved cataplasm ground-mass and use thereof Download PDFInfo
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- CN101416955B CN101416955B CN2008102331249A CN200810233124A CN101416955B CN 101416955 B CN101416955 B CN 101416955B CN 2008102331249 A CN2008102331249 A CN 2008102331249A CN 200810233124 A CN200810233124 A CN 200810233124A CN 101416955 B CN101416955 B CN 101416955B
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Abstract
The invention discloses an improved substrate of a cataplasma and the application thereof to loxoprofen sodium cataplasma. The substrate of the cataplasma adopts the combined application of two or more cross-linking agents and achieves the purposes of increasing the viscosity of a paste and improving the ductibility and moldability of the paste. The application of the substrate can reduce the variety and usage of thickening accessories or can increase the viscosity of the cataplasma to the extent required by a viscous force even without adding special thickening agents. The substrate has advantages in ensuring the good ductibility and moldability of the cataplasma and quickly establishing analytical methods, and the like, thus being significant for the further promotion and application of the cataplasma.
Description
Technical field
The use in conjunction of the substrate of the cataplasma that the present invention relates to improve, this substrate cross-linking agent by utilizing two or more, thus reach the performances such as the adhesiveness of improving cataplasma, mastic ductility, mouldability.Cataplasma of the present invention refers to have in the development and application field cross-linking type cataplasma of bright prospects, comprises take sodium polyacrylate, polyacrylic acid, partly is neutralized polyacrylic acid and novel high polymer material as the improvement of the cataplasma performance of framework material.The invention still further relates to the utilization of catablasm base material of the present invention in the medicine cataplasma, such as the loxoprofen sodium cataplasma.
Background technology
How to improve the adhesiveness of aqueous cataplasma, can take into account again simultaneously mouldability, the ductility of cataplasma, it is a great problem that the puzzlement cataplasma is used always, many cataplasma products in addition in the process of using because poor adhesion, skin tracing ability are bad, usually cause occurring in use attaching not firm, need repeatedly impose the situations such as external force overlays, bring very big inconvenience to use, and affect drug effect.Simultaneously be unfavorable for that also medicine discharges stably, the performance of drug effect also will be had a greatly reduced quality, thereby causes the patient to this dosage form trust crisis, finally causes social sanction's degree of this dosage form to descend, and affects the further propagation and employment of this dosage form.
On addressing this problem, main path has three at present, one, adopt new material, the method is not only the development of this dosage form, also be that formulation art is constantly brought forth new ideas and the direction that develops, but because a kind of invention of new adjuvant will be a long-term process with using, can not reach in a short time and solve this dosage form purpose that has problems at present.Its two, adopt to increase the adjuvant of adhesion and the consumption of adjuvant.Because cataplasma is comprised of tens kinds of functional adjuvants, mouldability, factors affecting stability for this dosage form are more, therefore increase kind and the consumption of adjuvant, can cause damage for mouldability, the stability of preparation to a certain extent, also can increase simultaneously the difficulty of establishment of the analytical method of preparation.Its three, adopt to increase the adhesiveness that the pressure sensitive adhesive sticker increases preparation.Cataplasma generally adopts aqueous matrix as carrier, be difficult for causing the anaphylaxis of body, this is a large characteristic and advantage of cataplasma always, but because in order to reach satisfied sticking effect, adopt pressure sensitive adhesive, increased like this probability of cataplasma because of pressure sensitive adhesive sensitization, made losing without this advantage of anaphylaxis of cataplasma.Therefore adopting a small amount of adjuvant or existing preparation prescription is carried out the adhesiveness that rational allocation reaches increases cataplasma, can take into account again mouldability, the ductility of cataplasma simultaneously, will be the main direction that addresses this problem at present.The inventor finishes the present invention for this reason, has overcome defects.
Summary of the invention:
The invention provides a kind of substrate of cataplasma of improvement, it is characterized in that this substrate is comprised of the excipient of associating cross-linking agent, water and suitable cataplasma, wherein, said associating cross-linking agent comprises cross-linking agent dihydroxyaluminum aminoacetate and at least a other cross-linking agent.Said water is deionized water, the excipient of said suitable cataplasma comprises: wetting agent such as glycerol, transdermal enhancer such as azone, solvent such as PEG400, filler such as titanium dioxide, framework material, thickening agent such as gelatin, sodium carboxymethyl cellulose, absorbent such as polyvinylpolypyrrolidone XL-10, aromatic such as Oleum menthae, cross-linking regulator such as disodium salt disodium, pH value regulator such as tartaric acid, antiseptic such as methyl hydroxybenzoate, wherein framework material is selected from polyacrylic acid, sodium polyacrylate, part is neutralized one or both in the polyacrylic acid, or two or more, preferred part is neutralized polyacrylic acid.The adjuvant that these all types of excipient all are this area routines and conventional consumption.
In one embodiment, above-mentioned catablasm base material of the present invention, its excipient include but not limited to glycerol, azone, PEG400, titanium dioxide, one or more are selected from polyacrylic acid, sodium polyacrylate, part and are neutralized polyacrylic framework material, gelatin, polyvinylpolypyrrolidone XL-10, Oleum menthae, sodium carboxymethyl cellulose, disodium salt disodium, tartaric acid or methyl hydroxybenzoate.
In some specific embodiments, the substrate of the cataplasma of improvement of the present invention, mainly the adjuvant by following weight portion forms: glycerol 20-50 part, azone 1-3 part, PEG400 10-5 part, titanium dioxide 0.3-1.5 part, framework material 2-7 part, gelatin 1-3 part, polyvinylpolypyrrolidone XL-10 0.5-1 part, associating cross-linking agent 0.02-11 part, Oleum menthae 0.1-1 part, sodium carboxymethyl cellulose 1-3 part, disodium salt disodium 0.02-0.05 part, tartaric acid 0.5-1.0 part, methyl hydroxybenzoate 0.1-0.4 part, deionized water 16-201 part, preferred 30-75 part, wherein, said associating cross-linking agent comprises cross-linking agent dihydroxyaluminum aminoacetate and at least a other cross-linking agent.
The substrate of the cataplasma of improvement of the present invention adopts the use in conjunction of two or more cross-linking agent to reach the adhesion that improves mastic (catablasm base material), improves mouldability and the ductility of mastic.
Crosslinked the referring to of the so-called associating of the present invention reaches the associating utilization by at least two kinds of cross-linking agent mixing, and wherein at least a cross-linking agent is dihydroxyaluminum aminoacetate, and wherein, dihydroxyaluminum aminoacetate: the weight ratio scope of other cross-linking agent is 1:1～1000, preferred 1:1～500.
The substrate of the cataplasma of the invention described above, said framework material be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more, preferred part is neutralized sodium polyacrylate NP700 (Viscomate NP700, clear and the electrician of Japan), part is neutralized sodium polyacrylate NP600 (Viscomate NP600, clear and the electrician of Japan) and partly be neutralized sodium polyacrylate NP800 (Viscomate NP800, the clear and electrician of Japan).
The catablasm base material of the invention described above, said other cross-linking agent is selected from one or more in calcium hydroxide, magnesium aluminate, aluminium hydroxide, gel aluminum hydroxide, aluminum chloride, aluminium potassium sulfate, aluminum nitrate, calcium chloride, lime nitrate, aluminum glycinate, aluminium-magnesium silicate and the hydrotalcite, preferred aluminium hydroxide, gel aluminum hydroxide (dry powder), aluminium-magnesium silicate or its mixture.
In one embodiment, the substrate of the cataplasma of improvement of the present invention, mainly the adjuvant by following weight portion is made: glycerol 20-50 part, azone 1-3 part, PEG400 10-5 part, titanium dioxide 0.3-1.5 part, part is neutralized sodium polyacrylate NP700 2-7 part, gelatin 1-3 part, polyvinylpolypyrrolidone XL-10 0.5-1 part, dihydroxyaluminum aminoacetate 0.01-0.03 part aluminium-magnesium silicate 2.5-5 part or aluminium hydroxide 3-10 part or gel aluminum hydroxide 0.01-5 part, Oleum menthae 0.1-1 part, sodium carboxymethyl cellulose 1-3 part, disodium salt disodium 0.02-0.05 part, tartaric acid 0.5-1.0 part, methyl hydroxybenzoate 0.1-0.4 part, deionized water 16-201 part, preferred 30-75 part, wherein, said associating cross-linking agent comprises cross-linking agent dihydroxyaluminum aminoacetate and at least a other cross-linking agent.
Among the present invention, the unit of said weight portion can be gram (g), kilogram (kg), kilogram, milligram unit of weights such as (mg), can select according to the actual needs corresponding unit of weight.
The present invention also provides a kind of method of catablasm base material of preparation improvement, and its process comprises:
A, with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, the titanium dioxide of adding through grinding, make its dispersion, obtain mixed system, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind gelatin, framework material, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
B, dihydroxyaluminum aminoacetate and another kind of cross-linking agent are dispersed in water, obtain mixed cross-linker;
C, with the tartaric acid water dissolution, make tartaric acid solution for subsequent use;
D, the mixed cross-linker of step b is joined in the system of step a under stirring, stir; Then,
E, the tartaric acid solution of step c is joined in the steps d, stirring gets final product.
Gelatin, framework material are crossed 80～200 mesh sieves in the said method, wherein, framework material be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more, preferred part is neutralized sodium polyacrylate NP600, NP700, NP800 (Viscomate NP600, NP700, NP800).
In the said method, described another kind of cross-linking agent is aluminium-magnesium silicate or aluminium hydroxide.
The present invention also comprises the application of catablasm base material of the present invention in preparation cataplasma medicine, the active constituents of medicine that is applicable to catablasm base material of the present invention mainly is hydrophilic medicament, as: leflunomide, cetirizine hydrochloride, granisetron, felbinac, methyl salicylate, indomethacin, diclofenac, ketoprofen, flurbiprofen, aspirin, loxoprofen sodium etc. are active component.In the present invention, will set forth take the loxoprofen sodium cataplasma as representative the application of substrate of the present invention.
The present invention also provides a kind of cataplasma of loxoprofen sodium, comprises loxoprofen sodium, associating cross-linking agent, water (preferred deionized water) and excipient, and its feature is comprised of dihydroxyaluminum aminoacetate and another kind of at least cross-linking agent at the associating cross-linking agent.
The cataplasma of above-mentioned loxoprofen sodium, another kind of cross-linking agent is selected from one or more in calcium hydroxide, magnesium aluminate, aluminium hydroxide, aluminum chloride, aluminium potassium sulfate, aluminum nitrate, calcium chloride, lime nitrate, aluminum glycinate, aluminium-magnesium silicate and the hydrotalcite, preferred aluminium hydroxide, aluminium-magnesium silicate or its mixture; Excipient comprises: wetting agent such as glycerol, transdermal enhancer such as azone, solvent such as PEG400, filler such as titanium dioxide, framework material, thickening agent such as gelatin, sodium carboxymethyl cellulose, absorbent such as polyvinylpolypyrrolidone XL-10, aromatic such as Oleum menthae, cross-linking regulator such as disodium salt disodium, pH value regulator such as tartaric acid, antiseptic such as methyl hydroxybenzoate, wherein framework material be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more, preferred part is neutralized polyacrylic acid.
The cataplasma of above-mentioned loxoprofen sodium, its excipient include but not limited to glycerol, azone, PEG400, titanium dioxide, framework material, gelatin, polyvinylpolypyrrolidone XL-10, Oleum menthae, sodium carboxymethyl cellulose, disodium salt disodium, tartaric acid or methyl hydroxybenzoate.Wherein, framework material be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more.
In specific embodiments, the cataplasma of loxoprofen sodium of the present invention, the cross-linking agent, deionized water and the multiple adjuvant that is selected from glycerol, azone, PEG400, titanium dioxide, framework material, gelatin, polyvinylpolypyrrolidone XL-10, Oleum menthae, sodium carboxymethyl cellulose, disodium salt disodium, tartaric acid, methyl hydroxybenzoate that comprise loxoprofen sodium, formed by dihydroxyaluminum aminoacetate and aluminium hydroxide or aluminium-magnesium silicate.Wherein, framework material be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more, preferred part is neutralized polyacrylic acid NP600, NP700, NP800.
The loxoprofen sodium cataplasma of the invention described above comprises that further loxoprofen sodium is by HP-β-CD (hydroxypropyl beta cyclodextrin) enclose.
In one embodiment, the cataplasma of loxoprofen sodium of the present invention, raw material by following weight portion forms: loxoprofen sodium 0.5-3 part, glycerol 20-50 part, azone 1-3 part, PEG400 10-3 part, titanium dioxide 0.3-1.5 part, framework material 2-7 part, gelatin 1-3 part, polyvinylpolypyrrolidone XL-10 0.5-1 part, associating cross-linking agent 0.02-10 part, Oleum menthae 0.1-1 part, sodium carboxymethyl cellulose 1-3 part, disodium salt disodium 0.02-0.05 part, tartaric acid 0.5-1.0 part, methyl hydroxybenzoate 0.1-0.4 part, deionized water 16-201 part, preferred 30-75 part, wherein, said associating cross-linking agent is comprised of cross-linking agent dihydroxyaluminum aminoacetate and at least a other cross-linking agent; Wherein, randomly loxoprofen sodium can be used first HP-β CD enclose.
Loxoprofen sodium cataplasma of the present invention, described other cross-linking agent is selected from one or more in calcium hydroxide, magnesium aluminate, aluminium hydroxide, gel aluminum hydroxide, aluminum chloride, aluminium potassium sulfate, aluminum nitrate, calcium chloride, lime nitrate, aluminum glycinate, aluminium-magnesium silicate and the hydrotalcite, preferred aluminium hydroxide, gel aluminum hydroxide, aluminium-magnesium silicate or its mixture.
Loxoprofen sodium cataplasma of the present invention, described framework material be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more, preferred part is neutralized polyacrylic acid NP700.
In another embodiment, loxoprofen sodium cataplasma of the present invention, mainly the raw material by following weight portion is made: loxoprofen sodium 0.5-3 part, glycerol 20-50 part, azone 1-3 part, PEG400 10-3 part, titanium dioxide 0.3-1.5 part, framework material 2-7 part, gelatin 1-3 part, polyvinylpolypyrrolidone XL-10 0.5-1 part, dihydroxyaluminum aminoacetate 0.01-0.03 part, aluminium-magnesium silicate 2.5-5 part or aluminium hydroxide 3-10 part or gel aluminum hydroxide 0.01-5 part, Oleum menthae 0.1-1 part, sodium carboxymethyl cellulose 1-3 part, disodium salt disodium 0.02-0.05 part, tartaric acid 0.5-1.0 part, methyl hydroxybenzoate 0.1-0.4 part, deionized water 16-201 part, preferred 30-75 part, wherein, randomly loxoprofen sodium can be used first HP-β CD enclose.
The present invention also provides a kind of method for preparing the loxoprofen sodium cataplasma: its process may further comprise the steps:
The preparation of a loxoprofen sodium HP-β CD clathrate is got HP-β CD and is dissolved in the deionized water, adds loxoprofen sodium and make it dissolving under stirring, and rotating speed stirred 1 hour, and loxoprofen sodium is carried out enclose, obtained loxoprofen sodium CD clathrate.
B with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then add glycerol, azone, Oleum menthae, EDTA-2Na and stir evenly the formation glycerol mixture, the titanium dioxide of adding through grinding, it is scattered in the above-mentioned glycerol mixture, and then sodium carboxymethyl cellulose is scattered in the glycerol mixture, being scattered in the glycerol mixture behind gelatin, framework material, the polyvinylpolypyrrolidone XL-10 mix homogeneously, obtain mixed system again;
C is dispersed in deionized water with dihydroxyaluminum aminoacetate and another kind of cross-linking agent, obtains mixed cross-linker;
D tartaric acid is for subsequent use with water dissolution;
E joins the mixed cross-linker of step c in the mixed system of step b under stirring, stir, and then add the loxoprofen sodium CD clathrate of step a, stir, the tartaric acid that adds at last steps d stirs and namely gets the loxoprofen sodium cataplasma.
In the said method, another kind of cross-linking agent is selected from one or more in calcium hydroxide, magnesium aluminate, aluminium hydroxide, gel aluminum hydroxide, aluminum chloride, aluminium potassium sulfate, aluminum nitrate, calcium chloride, lime nitrate, aluminum glycinate, aluminium-magnesium silicate and the hydrotalcite, preferred aluminium hydroxide, aluminium-magnesium silicate or its mixture.Gelatin among the step b, framework material are crossed 200 mesh sieves, wherein be selected from polyacrylic acid, sodium polyacrylate, part be neutralized in the polyacrylic acid one or both or two or more, preferred part is neutralized polyacrylic acid NP700.Among the present invention, described gel aluminum hydroxide is dry powder.
The substrate of cataplasma of the present invention and loxoprofen sodium cataplasma are characterised in that: adopt dihydroxyaluminum aminoacetate and another kind of cross-linking agent, such as aluminium hydroxide or aluminium-magnesium silicate, the mode of use in conjunction is improved the performance of cataplasma, as the cross-linking agent that is most widely used at present---dihydroxyaluminum aminoacetate, it has superior cross-linking effect, although the dihydroxyaluminum aminoacetate of trace can cause the rapid shaping of cataplasma mastic, but the formed mastic adhesion of dihydroxyaluminum aminoacetate is also lower, must increase the tackify composition, such as PVPK90 (30 POVIDONE K 30 BP/USP 90), PVPK30 (PVP K30), PVA (polyvinyl alcohol) etc. increase the viscosity of mastic.Be that the mastic that cross-linking agent forms can reach very strong adhesion in the situation that do not add viscosifier and adopt aluminium hydroxide or aluminium-magnesium silicate, but the mastic intensity that forms a little less than.In view of the foregoing, the present invention find to adopt dihydroxyaluminum aminoacetate respectively with aluminium hydroxide, the aluminium-magnesium silicate use in conjunction mode as cross-linking agent, the performance of cataplasma especially is being greatly improved aspect adhesion and the intensity, make adhesion and the mouldability of mastic can be according to actual needs, regulate the ratio (dihydroxyaluminum aminoacetate: other cross-linking agent=0.01:0.01～0.01:10, preferred 0.01:0.01～0.01:5) realize of dihydroxyaluminum aminoacetate and aluminium hydroxide or aluminium-magnesium silicate.Prescription research is more simplified, and the performance of cataplasma is greatly improved.
Characteristics and advantage that the present invention has are as follows:
1. prescription is oversimplified, reduced prescription moulding process screening difficulty, can better hold the character of cataplasma agent.Because the use in conjunction of cross-linking agent has reduced the application of tackify supplementary product kind and quantity to a certain extent, therefore in prescription research, reduced the influence factor who affects the mastic molding, brought facility for prescription research.
2. reduce auxiliary product quantities in the prescription, more be conducive to the establishment of analysis of pharmaceutical dosage forms method.
3. increase the affinity of medicine and substrate, increased the drug loading of medicine.Because the application of tackify supplementary product kind and quantity reduces, and has reduced the possibility that the tackify supplementary product consumption is affected by pharmaceutical properties, and then has increased the affinity of medicine and substrate, has increased the drug loading of medicine.
4. viscous force is controlled, and can regulate and control in a big way, has increased the working place of preparation preparation.Because two kinds of cross-linking agent features make adhesiveness adjusting, ductility adjusting, the mouldability of preparation regulate and all mainly be controlled by cross-linking agent ratio and consumption, are more convenient for controlling adhesiveness and the intensity of mastic.
5. shorten the developmental research time of cataplasma, the potential market that increases product is worth.
Specific embodiment
By embodiment the present invention is done further understanding, but can not limit the scope of the invention.
1. Piglet s colibacillosis
1.1 evaluation criterion and method
| Group | The grouping standard | Evaluation index | Comparative approach |
| 1〉the dihydroxyaluminum aminoacetate group 2〉aluminium-magnesium silicate group 3〉aluminium hydroxide group 4〉dihydroxyaluminum aminoacetate+aluminium-magnesium silicate group 5〉dihydroxyaluminum aminoacetate+aluminium hydroxide group | Using kind with cross-linking agent divides | Adhesion strength, embossability, outward appearance | That multiply by weight coefficient take each step meansigma methods of every group of preparation and compare as PTS |
Initial bonding strength (weight 0.4)
By " 2005 editions Firsts of Chinese pharmacopoeia, first method is measured among the appendix XII E
[1], get 3 every batch of test samples, remove backing layer, place on 15 ° the inclined-plane, the steel ball of 3 kinds of different sizes (diameter be respectively 4,5,6mm) is freely rolled down from beveled top end, and 3 test samples of each batch all can cling steel ball at test section, and the adhesion strength experimental result is qualified.
Initial bonding strength〉4mm 0 minute
Initial bonding strength 4mm 〉=or＜5mm 60 minutes
Initial bonding strength 5mm 〉=or＜6mm 80 minutes
Initial bonding strength 〉=6mm 100 minutes
Embossability (weight 0.4)
By " 2005 editions Firsts of Chinese pharmacopoeia, among the appendix II under the embossability step method measure
[1], 3 batches of test samples are placed respectively 37 ℃, in the climatic chamber of relative humidity 64%, take out behind the 30min, be fixed in 60.The steel plate inclined-plane on, place 24h after, the cream face is without the trickling phenomenon, embossability is good.
The cream surface current dropped down not molding 0 minute
Cream face short-distance movement, cream face molding 50 minutes
The cream face is without trickling phenomenon 100 minutes
Outward appearance (weight 0.2)
The smooth in appearance degree is good, protecting film was easily taken off from 100 minutes
Smoothness is general, protecting film was more easily taken off from 60 minutes
Smoothness is relatively poor, protecting film difficulty take off from 20 minutes
1.2, sample preparation and test:
The dihydroxyaluminum aminoacetate group, prescription
Glycerol 25g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP700 5g gelatin 1.5g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.05g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium (EDTA-2Na) 0.05g methyl hydroxybenzoate 0.4g deionized water 55.8g
Preparation technology:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, obtain glycerol mixture, to add after the titanium dioxide grinding and be scattered in the above-mentioned glycerol mixture, obtain mixed system, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gelatin and NP700 are crossed behind 200 mesh sieves and polyvinylpolypyrrolidone XL-10 mix homogeneously, redispersion gets final product in above-mentioned system;
B is dispersed in dihydroxyaluminum aminoacetate in the 5g water, and is for subsequent use;
It is for subsequent use that c gets tartaric acid solution with tartaric acid with the 40.8g water dissolution;
E joins the mixed cross-linker of step b in the mixed system of step a under stirring, and with 5g water flushing cup, washing liquid is poured in the mixed system of step a and stirred, and then the tartaric acid solution of step c joined in the mixed system of step a, and with 5g water flushing cup, washing liquid is poured into to stir in the mixed system of step a namely gets catablasm base material.
Initial bonding strength, embossability and the outward appearance of the substrate that test obtains, mark respectively as follows:
| Every | Average | Score after the weighting | Add up to (after the weighting) |
| Initial bonding strength embossability outward appearance | 60 100 60 | 24 37.36.7 | 68 |
The aluminium-magnesium silicate group
Prescription
Glycerol 25g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP7005g gelatin 1.0g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g aluminium-magnesium silicate 3g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium 0.05g methyl hydroxybenzoate 0.4g deionized water 54.9g
Preparation technology:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, obtain glycerol mixture, aluminium-magnesium silicate is scattered in the glycerol mixture, with adding after the titanium dioxide grinding and being scattered in the above-mentioned glycerol mixture, obtain mixed system again, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gelatin and NP700 are crossed behind 200 mesh sieves and polyvinylpolypyrrolidone XL-10 mix homogeneously, and redispersion gets final product in above-mentioned system;
It is for subsequent use that b gets tartaric acid solution with tartaric acid with the 40.0g water dissolution;
C joins the tartaric acid solution of step b in the mixed system of step a, and with remaining water flushing cup, and washing liquid is poured into to stir in the mixed system of step a namely gets catablasm base material.
Initial bonding strength, embossability and the outward appearance of the substrate that test obtains, mark respectively as follows:
| Every | Average | Score after the weighting | Add up to (after the weighting) |
| Initial bonding strength embossability outward appearance | 66.7100 60 | 26.7 20 12 | 58.7 |
The aluminium hydroxide group
Prescription:
Glycerol 25g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP7005g gelatin 1.0g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g aluminium hydroxide 10g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium (EDTA-2Na) 0.05g methyl hydroxybenzoate 0.4g deionized water 46.6g
Preparation technology:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, obtain glycerol mixture, aluminium hydroxide is scattered in the glycerol mixture, with adding after the titanium dioxide grinding and being scattered in the above-mentioned glycerol mixture, obtain mixed system again, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gelatin and NP700 are crossed behind 200 mesh sieves and polyvinylpolypyrrolidone XL-10 mix homogeneously, and redispersion gets final product in above-mentioned system;
It is for subsequent use that b gets tartaric acid solution with tartaric acid with the 31.6g water dissolution;
C joins the tartaric acid solution of step b in the mixed system of step a, and with 15g water flushing cup, and washing liquid is poured into to stir in the mixed system of step a namely gets catablasm base material.
Initial bonding strength, embossability and the outward appearance of the substrate that test obtains, mark respectively as follows:
| Every | Average | Score after the weighting | Add up to (after the weighting) |
| Initial bonding strength embossability outward appearance | 86.7100 60 | 34.7 20 12 | 66.7 |
Dihydroxyaluminum aminoacetate+aluminium-magnesium silicate group
Prescription:
Glycerol 25g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP7005g gelatin 1.0g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.02 aluminium-magnesium silicate 2.5g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium (EDTA-2Na) 0.05g methyl hydroxybenzoate 0.4g deionized water 51.1g
Preparation technology:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, obtain glycerol mixture, dihydroxyaluminum aminoacetate and aluminium-magnesium silicate are scattered in the glycerol mixture, to add after the titanium dioxide grinding and be scattered in the above-mentioned glycerol mixture again, obtain mixed system, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gelatin and NP700 are crossed behind 200 mesh sieves and polyvinylpolypyrrolidone XL-10 mix homogeneously, and redispersion gets final product in above-mentioned system;
It is for subsequent use that b gets tartaric acid solution with tartaric acid with the 40.1g water dissolution;
C joins the tartaric acid solution of step b in the mixed system of step a, and with 11g water flushing cup, and washing liquid is poured into to stir in the mixed system of step a namely gets catablasm base material.
Initial bonding strength, embossability and the outward appearance of the substrate that test obtains, mark respectively as follows:
| Every | Average | Score after the weighting | Add up to (after the weighting) |
| Initial bonding strength embossability outward appearance | 66.7100 73.3 | 26.7 40 14.7 | 81.4 |
Dihydroxyaluminum aminoacetate+aluminium hydroxide group
Prescription: glycerol 25g azone 2.0g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP700 5g gelatin 1.0g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.02 aluminium hydroxide 10g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium (EDTA-2Na) 0.05g methyl hydroxybenzoate 0.4g deionized water 52.6g
Preparation technology:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, obtain glycerol mixture, dihydroxyaluminum aminoacetate and aluminium hydroxide are scattered in the glycerol mixture, to add after the titanium dioxide grinding and be scattered in the above-mentioned glycerol mixture again, obtain mixed system, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gelatin and NP700 are crossed behind 200 mesh sieves and polyvinylpolypyrrolidone XL-10 mix homogeneously, and redispersion gets final product in above-mentioned system;
It is for subsequent use that b gets tartaric acid solution with tartaric acid with the 37.6g water dissolution;
C joins the tartaric acid solution of step b in the mixed system of step a, and with 15g water flushing cup, washing liquid is poured into the catablasm base material that stirs to get in the mixed system of step a.
Initial bonding strength, embossability and the outward appearance of the substrate that test obtains, mark respectively as follows:
| Every | Average | Score after the weighting | Add up to (after the weighting) |
| Initial bonding strength embossability outward appearance | 93.383.3 100 | 37.3 33.320 | 90.6 |
The result compares:
From top result separately, can see, the cross-linking agent use in conjunction has been compared the good effect of improving in the performance that improves the aspects such as mastic initial bonding strength, embossability, outward appearance with alone cross-linking agent, the overall performance that demonstrates the catablasm base material of the crosslinked prescription of associating obviously is better than the substrate of single cross-linking agent prescription.In above-mentioned experiment, in order to make experiment have more comparability, do not add in addition the tackify composition for the experiment with dihydroxyaluminum aminoacetate only.
2. substrate prescription embodiment
Embodiment 1
Prescription
Glycerol 20g azone 2g PEG400 10g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP7005g gelatin 3g polyvinylpolypyrrolidone XL-10 1g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.02g aluminium-magnesium silicate 2.5g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g deionized water 52.7g
Preparation method:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding azone, glycerol, Oleum menthae, disodium salt disodium stirs evenly, obtain glycerol mixture, dihydroxyaluminum aminoacetate and aluminium-magnesium silicate are scattered in glycerol mixture, to add after the titanium dioxide grinding and be scattered in the above-mentioned glycerol mixture again, obtain mixed system, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gelatin and NP700 are crossed behind 200 mesh sieves and polyvinylpolypyrrolidone XL-10 mix homogeneously, and redispersion gets final product in above-mentioned system;
It is for subsequent use that b gets tartaric acid solution with tartaric acid with the 47g water dissolution;
C joins the tartaric acid solution of step b in the mixed system of step a, and with 4.7g water flushing cup, and washing liquid is poured into to stir in the mixed system of step a gets final product.
Embodiment 2
Prescription
Glycerol 50g azone 2g PEG400 5g titanium dioxide 0.3g partly is neutralized sodium polyacrylate NP6002g gelatin 2g polyvinylpolypyrrolidone XL-10 1g tartaric acid 1.0g dihydroxyaluminum aminoacetate 0.02g aluminium hydroxide 3.2g Oleum menthae 1.0g sodium carboxymethyl cellulose 2g disodium salt disodium 0.02g methyl hydroxybenzoate 0.4g deionized water 30.0g
Preparation method:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding azone, glycerol, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and aluminium hydroxide are scattered in the glycerol step, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture again, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 200 order gelatin, 200 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
B tartaric acid is for subsequent use with the 25g water dissolution;
C joins the tartaric acid of step b in the system of a step under stirring, and washes cup with 5g water, washing liquid is poured into to stir in the ab mixed system get final product.
Embodiment 3
Prescription
Glycerol 25g azone 1g PEG400 10g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP6005g gelatin 1.5g polyvinylpolypyrrolidone XL-10 1g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.02g aluminium-magnesium silicate 2.5g Oleum menthae 0.5g sodium carboxymethyl cellulose 1g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g deionized water 51.2g
Preparation method:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and the grinding of aluminium-magnesium silicate adding titanium dioxide are scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 200 order gelatin, 200 order NP700, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
B tartaric acid is for subsequent use with the 42.2g water dissolution;
C joins the tartaric acid of b step in the system of a step under stirring, and washes cup with 9g water, washing liquid is poured into to stir in the ab mixed system get final product.
Embodiment 4
Prescription
Glycerol 20g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP7005g gelatin 2g polyvinylpolypyrrolidone XL-10 1g tartaric acid 1.0g dihydroxyaluminum aminoacetate 0.02g aluminium hydroxide 5g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g deionized water 55.8g
Preparation method:
A with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and aluminium-magnesium silicate are scattered in the glycerol mixture, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 200 order gelatin, 200 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
B tartaric acid is for subsequent use with the 50g water dissolution;
C joins step b tartaric acid in the system of a step under stirring, with 5.8g water flushing cup, washing liquid is poured in the mixed system of step a and b, and stirring gets final product.
3. the preparation of loxoprofen sodium cataplasma.
Embodiment 5
Prescription
Loxoprofen sodium 1.143g, (being equivalent to anhydride 1.0g) glycerol 30g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate, (NP700) 5g gelatin 2g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.02g aluminium-magnesium silicate 2.5g Oleum menthae 0.5g sodium carboxymethyl cellulose 3g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g HP-β CD 6.49g deionized water 40.5g
Preparation method:
The preparation of a HP-β CD clathrate is got HP-β CD 32.45g and is dissolved in the 50g water, adds loxoprofen sodium 5.711g under stirring, makes it dissolving, stirs 1 hour with 500 rev/mins rotating speeds, and loxoprofen sodium is carried out enclose
B with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and aluminium-magnesium silicate are scattered in the glycerol mixture, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 100 order gelatin, 100 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
C tartaric acid is for subsequent use with the 25g water dissolution;
The clathrate 17.63g that d gets step a joins in the system of step b under stirring, and with 5.5g water flushing cup, washing liquid poured in step a, the b mixed system stir, then the tartaric acid of step c being poured into stirs in step a, the b mixed system gets final product.
Embodiment 6
Prescription
Loxoprofen sodium 0.5715g (being equivalent to anhydride 0.5g) glycerol 30g azone 3g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate NP600 5g gelatin 2g polyvinylpolypyrrolidone XL-10 1g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.02g aluminium-magnesium silicate 2.5g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g HP-β CD 3.245g deionized water 43.9g
Preparation method:
The preparation of a HP-β CD clathrate is got HP-β CD 32.45g and is dissolved in the 50g water, adds loxoprofen sodium 5.711g under stirring, makes it dissolving, stirs 1 hour with 500 rev/mins rotating speeds, and loxoprofen sodium is carried out enclose;
B with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and aluminium-magnesium silicate are scattered in the glycerol mixture, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 200 order gelatin, 200 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
C tartaric acid is for subsequent use with the 30g water dissolution;
The clathrate 8.32g that d gets step a joins in the system of step b under stirring, and with 3.9g water flushing cup, washing liquid poured in step a, the b mixed system stir, then the tartaric acid of step c being poured into stirs in step a, the b mixed system gets final product.
Embodiment 7
Prescription
Loxoprofen sodium 1.143g (being equivalent to anhydride 1.0g) glycerol 30g azone 2g PEG400 5g titanium dioxide 1.5g partly is neutralized sodium polyacrylate NP700 5g gelatin 2g polyvinylpolypyrrolidone XL-10 1g tartaric acid 1g dihydroxyaluminum aminoacetate 0.02g aluminium hydroxide 5g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g HP-β CD 6.49g deionized water 37.1g
Preparation method:
The preparation of a HP-β CD clathrate is got HP-β CD 32.45g and is dissolved in the 50g water, adds loxoprofen sodium 5.711g under stirring, makes it dissolving, stirs 1 hour with 500 rev/mins rotating speeds, and loxoprofen sodium is carried out enclose;
B with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and aluminium hydroxide are scattered in the glycerol mixture, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 200 order gelatin, 200 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
C tartaric acid is for subsequent use with the 19g water dissolution;
The clathrate 17.63g that d gets step a joins in the system of step b under stirring, and with 8.1g water flushing cup, washing liquid poured in step a, the b mixed system stir, then the tartaric acid of step c being poured into stirs in step a, the b mixed system gets final product.
Embodiment 8
Prescription
Loxoprofen sodium 0.5715g (being equivalent to anhydride 0.5g) glycerol 37g azone 2g PEG400 5g titanium dioxide is recognized 0.5g and partly is neutralized sodium polyacrylate NP600 6g gelatin 1g polyvinylpolypyrrolidone XL-10 1g tartaric acid 1g dihydroxyaluminum aminoacetate 0.015g aluminium hydroxide 10g Oleum menthae 0.5g sodium carboxymethyl cellulose 2g disodium salt disodium 0.05g methyl hydroxybenzoate 0.1g HP-β CD 3.25g deionized water 30g
Preparation method:
The preparation of a HP-β CD clathrate is got HP-β CD 32.45g and is dissolved in the 50g water, adds loxoprofen sodium 5.711g under stirring, makes it dissolving, stirs 1 hour with 500 rev/mins rotating speeds, and loxoprofen sodium is carried out enclose.Get at last the 8.32g clathrate as a step.
B with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and aluminium hydroxide are scattered in the glycerol mixture, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 200 order gelatin, 200 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
C tartaric acid is for subsequent use with the 20g water dissolution;
The clathrate 8.32g that d gets step a joins in the system of step b under stirring, and with 5g water flushing cup, washing liquid poured in step a, the b mixed system stir, then the tartaric acid of step c being poured into stirs in step a, the b mixed system gets final product.
Embodiment 9
Prescription
Loxoprofen sodium 1.143g, (being equivalent to anhydride 1.0g) glycerol 30g azone 2g PEG400 5g titanium dioxide 0.5g partly is neutralized sodium polyacrylate, (NP700) 5g gelatin 2g polyvinylpolypyrrolidone XL-10 0.5g tartaric acid 0.5g dihydroxyaluminum aminoacetate 0.01g gel aluminum hydroxide, (dry powder) 0.01g Oleum menthae 0.1g sodium carboxymethyl cellulose 3g disodium salt disodium 0.05g methyl hydroxybenzoate 0.2g HP-β CD 6.49g deionized water 44g
Preparation method:
The preparation of a HP-β CD clathrate is got HP-β CD 32.45g and is dissolved in the 50g water, adds loxoprofen sodium 5.711g under stirring, makes it dissolving, stirs 1 hour with 500 rev/mins rotating speeds, and loxoprofen sodium is carried out enclose
B with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, EDTA-2Na stirs evenly, dihydroxyaluminum aminoacetate and gel aluminum hydroxide are scattered in the glycerol mixture, adding the titanium dioxide grinding is scattered in the above-mentioned glycerol mixture, then sodium carboxymethyl cellulose is scattered in the above-mentioned system, gets final product being scattered in the above-mentioned system behind 100 order gelatin, 100 order NP600, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
C tartaric acid is for subsequent use with the 24g water dissolution;
The clathrate 17.63g that d gets step a joins in the system of step b under stirring, and with 10g water flushing cup, washing liquid poured in step a, the b mixed system stir, then the tartaric acid of step c being poured into stirs in step a, the b mixed system gets final product
The catablasm base material that above embodiment is obtained and loxoprofen sodium cataplasma are by indexs such as aforesaid their initial bonding strength of method test, embossability, outward appearances, and its result is as follows:
| Group | The initial bonding strength score | The embossability score | The outward appearance score | Total points |
| The substrate of embodiment 1 | 32.0 | 40.0 | 20.0 | 92.0 |
| The substrate of embodiment 2 | 34.7 | 40.0 | 20.0 | 94.7 |
| The substrate of embodiment 3 | 37.3 | 40.0 | 20.0 | 97.3 |
| The substrate of embodiment 4 | 37.3 | 40.0 | 20.0 | 97.3 |
| Embodiment 5 loxoprofen sodium cataplasmas | 26.7 | 40.0 | 14.7 | 81.4 |
| Embodiment 6 loxoprofen sodium cataplasmas | 24.0 | 40.0 | 17.3 | 81.3 |
| Embodiment 7 loxoprofen sodium cataplasmas | 37.3 | 33.3 | 20.0 | 90.6 |
| Embodiment 8 loxoprofen sodium cataplasmas | 32.0 | 33.3 | 17.3 | 82.6 |
| Embodiment 9 loxoprofen sodium cataplasmas | 24.0 | 40 | 20 | 84.0 |
Annotate: score value is gained after the weighting
Conclusion: the data from above table are found out, adopt bar cloth substrate and the loxoprofen sodium cataplasma of the associating cross-linking agent preparation of dihydroxyaluminum aminoacetate, the bar cloth substrate that obviously is better than single cross-linking agent in the performance of the several respects such as adhesion strength, embossability, outward appearance, so use in conjunction of cross-linking agent, the performance indications of cataplasma have been improved to a certain extent, be worth further promoting the use, be conducive to improve quality and the curative effect of cataplasma.
List of references:
[1] Chinese Pharmacopoeia Commission. one one of Pharmacopoeia of People's Republic of China .2005 version [s]. Beijing: Chemical Industry Press, 2005: appendix X II E
Claims (11)
1. the substrate of the cataplasma of an improvement, it is characterized in that this substrate is comprised of the excipient of associating cross-linking agent, water and suitable cataplasma, wherein, said associating cross-linking agent comprises dihydroxyaluminum aminoacetate cross-linking agent and at least a other cross-linking agent, wherein, the weight ratio scope of dihydroxyaluminum aminoacetate and other cross-linking agent is 0.01: 0.05～0.01: 10, and described other cross-linking agent is aluminium hydroxide, gel aluminum hydroxide, aluminium-magnesium silicate or its mixture.
2. the substrate of the cataplasma of an improvement is characterized in that mainly being comprised of the adjuvant of following weight portion:
Glycerol 20-50 part, azone 1-3 part, PEG400 10-5 part, titanium dioxide 0.3-1.5 part, framework material 2-7 part, gelatin 1-3 part, polyvinylpolypyrrolidone XL-10 0.5-1 part, associating cross-linking agent 0.02-10 part, sodium carboxymethyl cellulose 1-3 part, disodiumedetate 0.02-0.05 part, tartaric acid 0.5-1.0 part, methyl hydroxybenzoate 0.1-0.4 part, deionized water 30-75 part, wherein, said associating cross-linking agent comprises dihydroxyaluminum aminoacetate cross-linking agent and at least a other cross-linking agent, wherein, the weight ratio scope of dihydroxyaluminum aminoacetate and other cross-linking agent is 0.01: 0.05～0.01: 10, and described other cross-linking agent is aluminium hydroxide, gel aluminum hydroxide, aluminium-magnesium silicate or its mixture.
3. the substrate of cataplasma according to claim 2, the framework material that it is characterized in that indication are selected from polyacrylic acid, sodium polyacrylate and part and are neutralized in the polyacrylic acid one or more.
4. cataplasma that contains loxoprofen sodium, comprise loxoprofen sodium, associating cross-linking agent, water and excipient, it is characterized in that the associating cross-linking agent is comprised of dihydroxyaluminum aminoacetate and at least a other cross-linking agent, wherein, the weight ratio scope of dihydroxyaluminum aminoacetate and other cross-linking agent is 0.01: 0.05～0.01: 10, and described other cross-linking agent is aluminium hydroxide, gel aluminum hydroxide, aluminium-magnesium silicate or its mixture.
5. cataplasma that contains loxoprofen sodium is characterized in that this cataplasma mainly is comprised of the raw material of following weight portion:
Loxoprofen sodium 0.5-3 part, associating cross-linking agent 0.02-10 part, glycerol 20-50 part, azone 1-3 part, PEG400 10-5 part, titanium dioxide 0.3-1.5 part, framework material 2-7 part, gelatin 1-3 part, polyvinylpolypyrrolidone XL-10 0.5-1 part, Oleum menthae 0.1-1 part, sodium carboxymethyl cellulose 1-3 part, disodiumedetate 0.02-0.05 part, tartaric acid 0.5-1.0 part, methyl hydroxybenzoate 0.1-0.4 part, deionized water 30-75 part, wherein, said associating cross-linking agent is comprised of cross-linking agent dihydroxyaluminum aminoacetate and at least a other cross-linking agent, wherein, the weight ratio scope of dihydroxyaluminum aminoacetate and other cross-linking agent is 0.01: 0.05～0.01: 10, and described other cross-linking agent is aluminium hydroxide, gel aluminum hydroxide, aluminium-magnesium silicate or its mixture.
6. the cataplasma that contains loxoprofen sodium according to claim 5, the framework material that it is characterized in that indication are selected from polyacrylic acid, sodium polyacrylate, part and are neutralized in the polyacrylic acid one or more.
7. the method for the substrate of the cataplasma of each described improvement of preparation claim 1-2, its process comprises:
A, with the methyl hydroxybenzoate dispersing and dissolving in PEG400, then adding glycerol, azone, Oleum menthae, disodiumedetate stirs evenly, the titanium dioxide of adding through grinding, it is uniformly dispersed, obtain mixed system, then sodium carboxymethyl cellulose is scattered in the aforementioned system, gets final product being scattered in the above-mentioned system behind gelatin, framework material, the polyvinylpolypyrrolidone XL-10 mix homogeneously again;
B, dihydroxyaluminum aminoacetate and another kind of cross-linking agent are dispersed in water, obtain the associating cross-linking agent;
C, tartaric acid water dissolution get tartaric acid solution;
D, the associating cross-linking agent of step b is joined in the system of step a under stirring, stir;
E, the tartaric acid solution of step c is joined in the steps d mixed system, uniform stirring makes the substrate of the cataplasma of improvement.
8. method for preparing the cataplasma that contains loxoprofen sodium of claim 4 or 5 comprises it is characterized in that the method for claim 7: add loxoprofen sodium in the mixed system of its steps d, obtain containing the cataplasma of loxoprofen sodium.
9. substrate according to claim 1, said excipient comprises: wetting agent, transdermal enhancer, filler, framework material, thickening agent, absorbent, aromatic, pH value regulator or antiseptic.
10. cataplasma according to claim 4, said excipient comprises: wetting agent, transdermal enhancer, filler, framework material, thickening agent, absorbent, aromatic, pH value regulator or antiseptic.
11. according to claim 9 described substrate or cataplasma claimed in claim 10, said excipient comprises glycerol, azone, PEG400, titanium dioxide, framework material, gelatin, polyvinylpolypyrrolidone XL-10, Oleum menthae, sodium carboxymethyl cellulose, disodiumedetate, tartaric acid or methyl hydroxybenzoate.
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