CN102284012B - Gel plaster containing curcumin and bletilla hyacinthina gum and preparation method thereof - Google Patents
Gel plaster containing curcumin and bletilla hyacinthina gum and preparation method thereof Download PDFInfo
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Abstract
The invention provides a gel plaster containing curcumin and bletilla hyacinthina gum, which comprises the following components in parts by weight: 0.2-0.5 part of curcumin, 1.0-2.5 parts of bletilla hyacinthina gum, 2.0-5.0 parts of polyacrylic acid, 0.4-1.4 parts of adhesive, 25.0-65.0 parts of humectant, 0.1-0.2 part of aluminum hydroxide, 0-5.0 parts of solid dispersion material, 0-1.5 parts of permeation promoter and 35.0-58.0 parts of water. The adhesive is selected from polyvinylpyrrolidone, hydroxypropyl methylcellulose, polyvinyl alcohol and the like; the humectant is selected from glycerol, propylene glycol, polyethylene glycol and the like; the solid dispersion material is selected from polyvinylpyrrolidone, mannitol, polyethylene glycol, poloxamer and the like; and the permeation promoter is selected from hydroxypropyl-beta-cyclodextrin, borneol, pennyroyal, olive oil and the like. The curcumin in the gel plaster can be transdermally absorbed and slowly and continuously released, and can stably be taken for a long time; and the bletilla hyacinthina gum can protect the skin, and reduce the irritation of the drugs to the skin.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to a kind of gel adhesive that contains curcumin and Bletilla glucomannan and preparation method thereof.
Background technology
Curcumin is a kind of natural pigment, is mainly derived from the rhizome of zingiberaceous plant Rhizoma Curcumae Longae Curcuma longa L., is the main active in Rhizoma Curcumae Longae.Modern pharmacological research shows, curcumin has physiological function and the effects such as function of gallbladder promoting, blood fat reducing, antiinflammatory, rheumatism, antibiotic, anticancer, antioxidation, removing free radical, can be widely used in medical science, food, cosmetic field (Mei Quanxi etc., modern Chinese medicine pharmacology handbook, China Traditional Chinese Medicine Publishing House, 1998,490-491).Yet, curcumin has unstability and water-insoluble, be easy to fade in air, existing pharmaceutical dosage form is mainly ejection preparation, microemulsion formulation and soft capsule preparation (Cui Jing etc., the development of curcumin microemulsion and property research thereof, Chinese Pharmaceutical Journal, 2005,40 (24): 1877-1880), bioavailability is also unsatisfactory, has limited its applying in food industry and pharmaceutical preparation.
Transdermal delivery system has been obtained remarkable progress adhering to controlled-release material and the percutaneous short aspect such as means and methods of oozing in recent years, and some of them have been used for clinical and have formed commodity, have shown gratifying prospect.Percutaneous dosing is for the whole body therapeutic of the treatment of local skin disease and some disease all significant (Liang Wenquan etc., percutaneous dosing product development present situation, external treatment with Chinese medicine magazine, 2005,14 (1): 3).And the curcumin percutaneous drug administration preparation, the key issue of existence is how to guarantee the stability of medicine, the percutaneous rate of medicine and the adhesion property of patch.In addition, medicine discharged from substrate and promote Drug Percutaneous Absorption, being still the person that needs the preparation work further problem (Cui Fude, pharmaceutics, People's Health Publisher, the 2005:425-433 of research; Pan Weisan, the new drug preparation technique, Chemical Industry Press, 2004:201-202).And the application success of curcumin in transdermal delivery system is to the exploitation of Chinese medicine significant (Liu Qiang etc., the progress of Chinese medicine percutaneous drug-delivery preparation and development trend, external treatment with Chinese medicine magazine, 2004,13 (1): 31-33).
The Pseudobulbus Bletillae (Rhizoma Bletillae) is the dry tuber of the orchid Pseudobulbus Bletillae (Rhizoma Bletillae) (Bletilla striata (Thunb) Reichb.f); has astringing to arrest bleeding; the effects such as detumescence and promoting granulation can be treated hemorrhage, pneumonopathy, burn etc., also can be used for having in cosmetics the effect of protection skin, slow down aging.Bletilla glucomannan is the water-soluble polysaccharide that is rich in the Pseudobulbus Bletillae (Rhizoma Bletillae), and it joins mannan by the glucose that 4 molecule mannose and 1 molecule glucose form, and relative molecular mass is in 100,000-200,000 left and right.Bletilla glucomannan has multiple biological activity; clinical in effects such as antiinflammatory coagulant blood, antitumor, anticomplementary activity, immunosuppressant; can be used as pharmaceutical adjunct; as filmogen, suspending agent, emulsifying agent etc.; also can be used in daily chemical products; the instead of chemical thickening agent; and have functions such as reducing zest, protection skin, slow down aging; extremely promising biomedical material (Wang Jun etc.; the clinical practice of Bletilla glucomannan, Journal of Chinese Hospital Pharmacy, 2004; 24 (9), 556-557).
Summary of the invention
The object of the present invention is to provide a kind ofly to be distributed in skin surface with higher concentration, good stability, dissolubility is high, bioavailability good, improve the gel adhesive that contains curcumin and Bletilla glucomannan of patient's medication compliance.
Another object of the present invention is to provide the above-mentioned preparation method that contains the gel adhesive of curcumin and Bletilla glucomannan.
For achieving the above object, the technical solution used in the present invention is:
A kind of gel adhesive that contains curcumin and Bletilla glucomannan comprises the component of following weight proportion:
Curcumin 0.2～0.5 Bletilla glucomannan 1.0～2.5 framework materials 2.0～5.0
Adhesive 0.4～1.4 wetting agent 25.0～65.0 cross-linking agent 0.1～0.2
Wherein said framework material is polyacrylic acid.Described adhesive is for being selected from one or more in polyvinylpyrrolidone (PVP), hypromellose (HPMC), starch, polyvinyl alcohol (PVA), gelatin, arabic gum, Polyethylene Glycol; Described wetting agent is to be selected from one or more in glycerol, propylene glycol, sorbitol, Polyethylene Glycol, ethylene glycol, 1,3 butylene glycol.Described cross-linking agent is aluminium hydroxide.Described solid dispersion is to be selected from one or more in polyvinylpyrrolidone, hypromellose, chitosan, mannitol, Polyethylene Glycol, poloxamer, preferably polyethylene ketopyrrolidine or mannitol.Described penetrating agent is to be selected from one or more in HP-β-CD, Borneolum Syntheticum, Oleum menthae, olive oil, carbamide.The weight proportion of above-mentioned solid dispersion is preferably 1.0～5.0, penetrating agent preferred 0.5～1.5.
In a kind of preferred implementation, described gel adhesive comprises the component of following weight proportion:
Wherein the weight proportion of solid dispersion more preferably 1.0～5.0, and penetrating agent is 0.5～1.5.
Bletilla glucomannan of the present invention can prepare by the following method: will add in the distilled water of 10～12 times of volumes (in ml) after 1 weight portion (in g) Pseudobulbus Bletillae (Rhizoma Bletillae) pulverizing medicinal materials, be heated to 50 ℃ and stirred 1 hour, filter, collect extracting solution; Then the medicinal residues distilled water that adds respectively 5～6 times of volumes (in ml) repeats to extract 1～3 time; Merge extractive liquid, is concentrated into half volume, adds 95% ethanol to regulate ethanol mass concentration to 70%, separates out precipitation, and centrifugal, collecting precipitation is used washing with alcohol, in 80 ℃ of dryings, obtains Bletilla glucomannan.
The present invention also provides the above-mentioned preparation method that contains the gel adhesive of curcumin and Bletilla glucomannan, comprises step:
1) preparation of curcumin solid dispersion: according to the prescription consumption proportion, curcumin is dissolved in appropriate organic solvent, mix with the solid dispersion, fully stir under 60 ℃ of condition of water bath heating, organic solvent is removed in evaporation, lets cool to room temperature, dry 5h in 45～55 ℃ of vacuum drying ovens again, pulverize, sieve, and get final product;
2) preparation of substrate: according to the prescription consumption proportion, Bletilla glucomannan, wetting agent, cross-linking agent are stirred under 25 ℃～35 ℃ water bath condition, then add framework material, adhesive, penetrating agent, fully stir, and get final product;
3) preparation of pastille glue: according to the prescription consumption proportion, with curcumin or step 1) curcumin solid dispersion of preparation is added in substrate after with appropriate solvent (water or glycerol) dissolving dispersion, adds remaining water, stir, de-bubbled, and get final product;
4) preparation of gel adhesive: pastille glue is applied on backing layer, dry 0.5～3.5h under 40～60 ℃, the upper cover protective layer cuts, and get final product.
In one embodiment, step 1) in, curcumin can be dissolved in the volatile organic solvents such as dehydrated alcohol, acetone, vacuum drying normally approximately 50 ℃ carried out approximately 5 hours, sieving can be the sieve of 80 orders, 100 orders or other different pore sizes.
In one embodiment, step 2) the aqueous solution form of 0.5～10wt% that in, adhesive can be prepared is in advance added, and by its dilution is gluey aqueous solution, is conducive to each component and mixes quickly and evenly.For example, preferably, polyvinylpyrrolidone is to add with the aqueous solution form of 1.5～8.5wt%, and polyvinyl alcohol is to add with the aqueous solution form of 1.5～9.5wt%, and hypromellose is to add with the aqueous solution form of 0.5～3.5wt%.
In one embodiment, step 2), Bletilla glucomannan also can without extraction, directly add in described gel adhesive with the form of Pseudobulbus Bletillae (Rhizoma Bletillae) medicinal powder.When using with the form of common bletilla, its consumption is about as much as 3～4 times of Bletilla glucomannan consumption.
In one embodiment, step 3), de-bubbled can adopt the method such as ultrasonic, standing or centrifugal to carry out.
In one embodiment, step 4) in, backing layer can be cellulose acetate, spun rayon cloth or medical adhesive-bonded fabric etc., and protective layer can be polypropylene film, polyethylene film, cellophane or mylar etc.
Beneficial effect of the present invention is, the mechanism such as matrix type and adhesive decentralized are combined, and promotes Transdermal absorption and the sustained release of medicine.As active component, synergism strengthens drug effect with curcumin and Bletilla glucomannan, and Bletilla glucomannan can be protected skin simultaneously, and reducing stimulates; Gelatinous Bletilla glucomannan also can be used as adhesion material, adheres on skin with the framework material polyacrylic acid and as the drug depot controlled release drug, makes the active component effect of described gel adhesive lasting, can stablize for a long time administration.In addition, can also add solid dispersion and penetrating agent by selectivity.The solid dispersion makes medicine that higher dissolubility be arranged in the substrate when guaranteeing to make medicine stability, is discharged into skin surface by substrate smoothly; Penetrating agent makes medicine see through horny layer from skin surface, diffuses into corium.The use in conjunction of above-mentioned each component makes the curcumin in gel adhesive reach the purpose of Transdermal absorption and slow sustained release, and reduces medicine to the zest of skin, reaches the purpose of protection skin.
The gel adhesive that contains curcumin and Bletilla glucomannan of the present invention can be used for the treatment of various diseases, comprises the auxiliary treatment of arthroncus, arthritis, skin carcinoma or the auxiliary treatment of breast carcinoma etc.The in-vitro evaluation experimental result shows, preparation of the present invention reaches more than 93% at the 2h medicine realeasing rate; Drug accumulation transdermal amount reaches 40 μ gcm
-2Above, after medicine is prepared into solid dispersion, accumulation transdermal amount reaches 347 μ gcm
-2, significantly improve the accumulation transdermal amount of medicine.Said preparation can be stablized administration in 32h.
Description of drawings
Fig. 1 is the cumulative release percentage rate Q-t curve of gel adhesive sample of the present invention.
Fig. 2 is the accumulation transdermal amount Q-time t curve of gel adhesive sample of the present invention.
Fig. 3 is the accumulation transdermal amount Q-t of gel adhesive sample of the present invention
1/2Curve.
The specific embodiment
Following preferred embodiment only is provided for further understanding the features and advantages of the invention, and should not be construed as limitation of the present invention.Wherein curcumin is provided by Tianjin recovery fine chemistry industry institute, lot number CBO346-5G-N, available from branch, pharmacy of Tongrentang Linyi, Beijing, other materials and reagent are common commercially available prod to the Pseudobulbus Bletillae (Rhizoma Bletillae) (Bletilla striata (Thunb) Reichb.f) unless otherwise specified.
[embodiment 1] preparation Bletilla glucomannan
Take approximately 20g of common bletilla, adding distil water 240mL, heating in water bath to 50 ℃ insulation dipping stirs and extracted 1 hour, through four layers of filtered through gauze, gets extracting solution.Medicinal residues again adding distil water approximately 80～120ml repeat as stated above to extract twice, merge the filtrate of three times, be concentrated into half volume, add 95% ethanol and make the alcohol amount of containing reach 70wt%, separate out rapidly a large amount of white precipitates this moment, centrifugal, reclaim ethanol, the collecting precipitation thing, with a small amount of washing with alcohol 3 times, volatilize ethanol, and about 80 ℃ dryings, obtain approximately 5.6g of Bletilla glucomannan.
[embodiment 2] preparation contains the gel adhesive of curcumin and Bletilla glucomannan
Prescription:
| Component | Consumption (g) | Effect |
| Curcumin | 0.4 | Active component |
| Bletilla glucomannan | 2.5 | Active component, adhesive |
| Polyacrylic acid | 3.0 | Framework material, adhesive |
| Polyvinylpyrrolidone (PVP) | 0.8 | Substrate, adhesive |
| Polyvinyl alcohol (PVA) | 0.3 | Substrate, adhesive |
| Hypromellose (HPMC) | 0.2 | Substrate, adhesive |
| Glycerol | 15.0 | Substrate, wetting agent |
| Propylene glycol | 15.0 | Substrate, wetting agent |
| Polyethylene Glycol | 5.0 | Substrate, wetting agent |
| Aluminium hydroxide (Al (OH) 3) | 0.1 | Substrate, cross-linking agent |
| Water | 57.7 | Substrate |
| Amount to | 100 |
Preparation method:
1) preparation of substrate: according to above-mentioned prescription consumption proportion, Bletilla glucomannan, glycerol (can stay a little glycerol as the solvent of step 3), propylene glycol, Polyethylene Glycol, aluminium hydroxide are stirred under 35 ℃ of water bath condition, add again polyacrylic acid, PVP (can be formulated as in advance the approximately PVP aqueous solution form of 5wt%, also claim " glue "), PVA (can be formulated as in advance the approximately PVA aqueous solution form of 5wt%), HPMC (can be formulated as in advance the approximately HPMC aqueous solution form of 2wt%), stir, obtain substrate.
2) preparation of pastille glue: after curcumin is disperseed with appropriate solvent (dehydrated alcohol, water or glycerol) dissolving, be added in substrate, add remaining water, stir, ultrasonic or standing de-bubbled obtains pastille glue.
3) preparation of gel adhesive: pastille glue is applied on medical adhesive-bonded fabric, and in the about 0.5h of 60 ℃ of dryings, upper cover cellophane protective layer cuts and get final product.
[embodiment 3] preparation contains the gel adhesive of curcumin and Bletilla glucomannan
Prescription:
| Component | Consumption (g) | Effect |
| Curcumin | 0.4 | Active component |
| Bletilla glucomannan | 2.0 | Active component, adhesive |
| PVP k-30 | 4.0 | The solid dispersion |
| Polyacrylic acid | 4.0 | Framework material, adhesive |
| Polyvinylpyrrolidone (PVP) | 0.6 | Substrate, adhesive |
| Polyvinyl alcohol (PVA) | 0.1 | Substrate, adhesive |
| Hypromellose (HPMC) | 0.3 | Substrate, adhesive |
| Glycerol | 25.0 | Substrate, wetting agent |
| Propylene glycol | 15.0 | Substrate, wetting agent |
| Polyethylene Glycol | 10.0 | Substrate, wetting agent |
| Aluminium hydroxide | 0.2 | Substrate, cross-linking agent |
| Water | 38.4 | Substrate |
| Amount to | 100 |
Preparation method:
1) preparation of curcumin solid dispersion: according to above-mentioned prescription consumption proportion, curcumin is dissolved in appropriate dehydrated alcohol, add PVPk-30 to mix, ultrasonic 5min makes dissolving, fully stirs under 60 ℃ of condition of water bath heating, dehydrated alcohol is removed in evaporation, let cool to room temperature, then in 50 ℃ of vacuum drying ovens dry 5h, take out to pulverize, cross 80 mesh sieves, be stored in exsiccator standby.
2) preparation of substrate: according to above-mentioned prescription consumption proportion, Bletilla glucomannan, glycerol (can stay a little glycerol as the solvent of step 3), propylene glycol, Polyethylene Glycol, aluminium hydroxide are stirred under 25 ℃ of water bath condition, the HPMC of glue form of PVA, 2wt% of glue form that adds again glue form PVP, the 5wt% of polyacrylic acid, 5wt%, stir, obtain substrate.
3) preparation of pastille glue: after curcumin solid dispersion is disperseed with appropriate solvent (water or glycerol) dissolving, be added in substrate, add remaining water, stir, the ultrasonic degas bubble obtains pastille glue.
4) preparation of gel adhesive: pastille glue is applied on medical adhesive-bonded fabric, and in the about 0.5h of 60 ℃ of dryings, upper cover cellophane protective layer cuts and get final product.
[embodiment 4] preparation contains the gel adhesive of curcumin and Bletilla glucomannan
Prescription:
| Component | Consumption (g) | Effect |
| Curcumin | 0.4 | Active component |
| Bletilla glucomannan | 1.0 | Active component |
| Mannitol | 3.0 | The solid dispersion |
| Polyacrylic acid | 5.0 | Framework material, adhesive |
| Polyvinylpyrrolidone (PVP) | 0.3 | Substrate, adhesive |
| Polyvinyl alcohol (PVA) | 0.1 | Substrate, adhesive |
| Hypromellose (HPMC) | 0.1 | Substrate, adhesive |
| Glycerol | 35 | Substrate, wetting |
| Propylene glycol | ||
| 10 | Substrate, wetting | |
| Polyethylene Glycol | ||
| 10 | Substrate, wetting agent | |
| Aluminium hydroxide | 0.1 | Substrate, cross-linking agent |
| Water | 35.0 | Substrate |
| Amount to | 100 |
Preparation method:
1) preparation of curcumin solid dispersion: according to above-mentioned consumption proportion, curcumin is dissolved in appropriate dehydrated alcohol, add mannitol, fully stir under 60 ℃ of condition of water bath heating, dehydrated alcohol is removed in evaporation, lets cool to room temperature, dry 5h in 50 ℃ of vacuum drying ovens again, take out and pulverize, cross 80 mesh sieves, be stored in exsiccator standby.
2) preparation of substrate: according to above-mentioned consumption proportion, Bletilla glucomannan, glycerol, propylene glycol, Polyethylene Glycol, aluminium hydroxide are stirred under 30 ℃ of water bath condition, the HPMC of glue form of PVA, 1wt% of glue form of PVP, 6wt% that adds again the glue form of polyacrylic acid, 5wt%, stir, obtain substrate.
3) preparation of pastille glue: after curcumin solid dispersion is disperseed with appropriate solvent (water or glycerol) dissolving, be added in substrate, add remaining water, stir, the ultrasonic degas bubble obtains pastille glue.
4) preparation of gel adhesive: pastille glue is applied on medical adhesive-bonded fabric, dry approximately 3.0h under 40 ℃, upper cover cellophane protective layer cuts and get final product.
[embodiment 5] preparation contains the gel adhesive of curcumin and Bletilla glucomannan
Prescription:
| Component | Consumption (g) | Effect |
| Curcumin | 0.2 | Active component |
| Bletilla glucomannan | 1.5 | Active component |
| Polyethylene glycol 6000 | 2.0 | The solid dispersion |
| Polyacrylic acid | 3.5 | Framework material, adhesive |
| Polyvinylpyrrolidone (PVP) | 0.1 | Substrate, adhesive |
| Polyvinyl alcohol (PVA) | 0.3 | Substrate, adhesive |
| Hypromellose (HPMC) | 0.3 | Substrate, |
| Glycerol | ||
| 20 | Substrate, wetting agent | |
| Propylene glycol | 5 | Substrate, wetting agent |
| Polyethylene Glycol | 15 | Substrate, wetting agent |
| Oleum menthae | 1.0 | Substrate, penetrating agent |
| Borneolum Syntheticum | 0.5 | Substrate, penetrating agent |
| Aluminium hydroxide | 0.1 | Substrate, cross-linking agent |
| Water | 50.5 | Substrate |
| Amount to | 100 |
Preparation method:
1) preparation of curcumin solid dispersion: according to above-mentioned consumption proportion, curcumin is dissolved in appropriate dehydrated alcohol, add polyethylene glycol 6000, fully stir under 60 ℃ of condition of water bath heating, dehydrated alcohol is removed in evaporation, lets cool to room temperature, dry 5h in 50 ℃ of vacuum drying ovens again, take out and pulverize, cross 80 mesh sieves, be stored in exsiccator standby.
2) preparation of substrate: according to above-mentioned consumption proportion, Bletilla glucomannan, glycerol, propylene glycol, Polyethylene Glycol, aluminium hydroxide are stirred under 30 ℃ of water bath condition, the HPMC of glue form of PVA, 3.5wt% of glue form of PVP, 8wt% that adds again the glue form of polyacrylic acid, 5wt%, Oleum menthae, Borneolum Syntheticum, stir, obtain substrate.
3) preparation of pastille glue: after curcumin solid dispersion is disperseed with appropriate solvent (water or glycerol) dissolving, be added in substrate, add remaining water, stir, the ultrasonic degas bubble obtains pastille glue.
4) preparation of gel adhesive: pastille glue is applied on medical adhesive-bonded fabric, dry approximately 3.0h under 40 ℃, upper cover cellophane protective layer cuts and get final product.
[embodiment 6] preparation contains the gel adhesive of curcumin and Bletilla glucomannan
Prescription:
| Component | Consumption (g) | Effect |
| Curcumin | 0.5 | Active component |
| Bletilla glucomannan | 2.0 | Active component |
| PLURONICS F87 | 5.0 | The solid dispersion |
| Polyacrylic acid | 4.5 | Framework material, adhesive |
| Polyvinylpyrrolidone (PVP) | 0.2 | Substrate, adhesive |
| Polyvinyl alcohol (PVA) | 0.2 | Substrate, adhesive |
| Hypromellose (HPMC) | 0.2 | Substrate, adhesive |
| Glycerol | 30.0 | Substrate, wetting agent |
| Propylene glycol | 5.0 | Substrate, wetting agent |
| Polyethylene Glycol | 5.0 | Substrate, wetting agent |
| HP-β-CD | 0.5 | Substrate, penetrating agent |
| Olive oil | 0.5 | Substrate, penetrating agent |
| Aluminium hydroxide | 0.2 | Substrate, cross-linking agent |
| Water | 46.2 | Substrate |
| Amount to | 100 |
Preparation method:
1) preparation of curcumin solid dispersion: according to above-mentioned consumption proportion, curcumin is dissolved in appropriate dehydrated alcohol, add polyethylene glycol 6000, fully stir under 60 ℃ of condition of water bath heating, dehydrated alcohol is removed in evaporation, lets cool to room temperature, dry 5h in 50 ℃ of vacuum drying ovens again, take out and pulverize, cross 80 mesh sieves, be stored in exsiccator standby.
2) preparation of substrate: according to above-mentioned consumption proportion, Bletilla glucomannan, glycerol, propylene glycol, Polyethylene Glycol, aluminium hydroxide are stirred under 25 ℃ of water bath condition, HPMC, HP-β-CD, the olive oil of glue form of PVA, 1wt% of glue form of PVP, 6wt% that adds again the glue form of polyacrylic acid, 5wt%, stir, obtain substrate.
3) preparation of pastille glue: after curcumin solid dispersion is disperseed with appropriate solvent (water or glycerol) dissolving, be added in substrate, add remaining water, stir, the ultrasonic degas bubble obtains pastille glue.
4) preparation of gel adhesive: pastille glue is applied on medical adhesive-bonded fabric, dry approximately 2.0h under 50 ℃, upper cover cellophane protective layer cuts and get final product.
[embodiment 7] preparation contains the gel adhesive of curcumin and Bletilla glucomannan
Prescription:
| Component | Consumption (g) | Effect |
| Curcumin | 0.3 | Active component |
| Bletilla glucomannan | 1.5 | Active component, adhesive |
| Polyacrylic acid | 3.0 | Framework material, adhesive |
| Polyvinylpyrrolidone (PVP) | 0.6 | Substrate, adhesive |
| Polyvinyl alcohol (PVA) | 0.3 | Substrate, adhesive |
| Hypromellose (HPMC) | 0.3 | Substrate, adhesive |
| Glycerol | 20.0 | Substrate, wetting agent |
| Propylene glycol | 10.0 | Substrate, wetting agent |
| Polyethylene Glycol | 10.0 | Substrate, wetting agent |
| Oleum menthae | 1.0 | Substrate, penetrating agent |
| Aluminium hydroxide | 0.2 | Substrate, cross-linking agent |
| Water | 52.8 | Substrate |
| Amount to | 100 |
Preparation method:
1) preparation of substrate: according to above-mentioned consumption proportion, Bletilla glucomannan, glycerol, propylene glycol, Polyethylene Glycol, aluminium hydroxide are stirred under 30 ℃ of water bath condition, the HPMC of glue form of PVA, 1wt% of glue form of PVP, 6wt% that adds again the glue form of polyacrylic acid, Oleum menthae, 5wt%, stir, obtain substrate.
2) preparation of pastille glue: after curcumin is disperseed with suitable quantity of water or glycerol dissolving, be added in substrate, add remaining water, stir, the ultrasonic degas bubble obtains pastille glue.
3) preparation of gel adhesive: pastille glue is applied on medical adhesive-bonded fabric, dry approximately 2.0h under 50 ℃, upper cover cellophane protective layer cuts and get final product.
The recruitment evaluation of [embodiment 8] gel adhesive
1, extracorporeal releasing experiment (Chinese Pharmacopoeia 2005 editions, two appendix XD, the three therapeutic methods of traditional Chinese medicine)
Get embodiment 1,2,3 gel adhesive is denoted as sample A, B and C, throws off protective layer and is fixed between two-layer video disc, emission surface is up.As accepting medium, the accepting medium temperature is 32 ± 0.5 ℃ with 30% ethanol-normal saline solution, and the accepting medium volume is 200mL, and mixing speed is 100rmin
-1Sampling after the experiment beginning after 0.45 μ m filtering with microporous membrane, after every sub-sampling, is added the blank acceptable solution of isothermal.Cumulative release amount by each time period of Analysis result calculation of each sample point.Each time point drug accumulation discharges percentage rate Q and is listed in the table below 1.With time t, each point cumulative release percentage rate Q is figure, obtains the release in vitro curve, as shown in Figure 1.
Table 1 contains the extracorporeal releasing experiment result (n=6) of the gel adhesive of curcumin and Bletilla glucomannan
2, percutaneous abilities is investigated
Get embodiment 1,2,3 gel adhesive is denoted as sample A, B and C, carries out the transdermal test.
Adopt the Franze diffusion cell of improvement, device transdermal area is 1.766cm
2, the volume of acceptance pool is 17mL, ON cycle water-bath, 32 ± 1 ℃ of constant temperature.Get mouse skin and be fixed between acceptance pool and supply pool, patch is cut into suitable size, be affixed on above-mentioned synthetic membrane, acceptance pool is take the normal saline of 30% dehydrated alcohol as accepting medium, makes itself and contact skin.Acceptance pool and supply chamber is closely fixing, drain bubble, add stirrer with 150rmin
-1Speed stir, respectively at 1,2,4,6,8,12,20, the 32h 3mL that take a sample from acceptance pool is placed in test tube, need further be diluted with constant temperature (32 ℃) acceptable solution by the patch of solid dispersion making, add simultaneously 32 ℃ of acceptable solution 3mL.Measure absorbance in the 425nm place, substitution regression equation calculation concentration, and try to achieve unit are accumulative total infiltration capacity according to following formula, Q=(CnVn+ ∑ CiVi)/S, wherein Cn is the concentration of n sub-sampling, and Vn is the volume of n sub-sampling, and Ci is the concentration of i sub-sampling, Vi is the volume of i sub-sampling, and S is the transdermal area.To time (t) mapping, obtain equation with unit are accumulative total infiltration capacity (Qr), calculate percutaneous rate Js.
In each gel adhesive, the accumulation transdermal amount Q of each time point t is as shown in table 2 below.To accumulation transdermal amount (Qr) mapping, obtain the release in vitro curve with the time (t), see Fig. 2.With time t
1/2To each point accumulation transdermal amount Q mapping, see Fig. 3.Unit are accumulative total infiltration capacity (Qr)-t curve is pressed respectively zero level Q-t and Higuchi equation Q-t
1/2Carry out models fitting, calculate infiltration rate, the results are shown in Table 3.
Table 2 contains the gel adhesive transdermal test in vitro experimental result (n=6) of curcumin and Bletilla glucomannan
Table 3 contains the gel adhesive models fitting regression equation of curcumin and Bletilla glucomannan
| Prescription | The zero level equation | R 2 | Js/μg.cm -2.h -1 | The Higuchi equation | R 2 | Js/μg.cm -2.h -1 |
| A | Q＝1.189t+1.819 | 0.9828 | 1.189 | Q＝66.269t 1/2-0.444 | 0.9697 | 66.269 |
| B | Q＝3.999t+31.391 | 0.8813 | 3.999 | Q＝28.33t 1/2-8.638 | 0.9721 | 28.33 |
| C | Q＝9.075t+96.907 | 0.7898 | 9.075 | Q＝7.978t 1/2-8.769 | 0.9231 | 7.987 |
Can find out from the above results, gel adhesive of the present invention can reach more than 93% at the 2h medicine realeasing rate; Drug accumulation transdermal amount reaches 40 μ gcm
-2Above, after medicine is prepared into solid dispersion, accumulation transdermal amount reaches 347 μ gcm
-2, significantly improve the accumulation transdermal amount of medicine.Said preparation can be stablized administration in 32h.
Gel adhesive of the present invention can be cut into suitable size in clinical practice, every subsides contain the different sizes such as curcumin 10mg, 20mg, and each one pastes the external application affected part.
Be more than that description to preferred embodiment of the present invention does not limit the present invention, those skilled in the art can make according to the present invention various changes and distortion, only otherwise break away from spirit of the present invention, all should belong to the category of claims of the present invention.
Claims (8)
1. gel adhesive that contains curcumin and Bletilla glucomannan comprises the component of following weight proportion:
Curcumin 0.2～0.5 Bletilla glucomannan 1.0～2.5 framework materials 2.0～5.0
Adhesive 0.4～1.4 wetting agent 25.0～65.0 cross-linking agent 0.1～0.2
Solid dispersion 0～5.0 penetrating agent 0～1.5 water 35.0～58.0
Wherein said framework material is polyacrylic acid; Described adhesive is to be selected from one or more in polyvinylpyrrolidone, hypromellose, starch, polyvinyl alcohol, gelatin, arabic gum, Polyethylene Glycol; Described wetting agent is to be selected from one or more in glycerol, propylene glycol, sorbitol, Polyethylene Glycol, ethylene glycol, 1,3 butylene glycol; Described cross-linking agent is aluminium hydroxide; Described solid dispersion is to be selected from one or more in polyvinylpyrrolidone, hypromellose, chitosan, mannitol, Polyethylene Glycol, poloxamer; Described penetrating agent is to be selected from one or more in HP-β-CD, Borneolum Syntheticum, Oleum menthae, olive oil, carbamide;
It is characterized in that:
Described gel adhesive comprises the component of following weight proportion:
Curcumin 0.2～0.5 Bletilla glucomannan 1.0～2.5 polyacrylic acid 2.0～5.0
Polyvinylpyrrolidone 0.2～0.8 polyvinyl alcohol 0.1～0.3 hypromellose 0.1～0.3
Glycerol 15.0～35.0 propylene glycol 5.0～15.0 Polyethylene Glycol 5.0～15.0
Solid dispersion 0～5.0 aluminium hydroxide 0.1～0.2 penetrating agent 0～1.5
Water 35.0～58.0.
2. gel adhesive as claimed in claim 1, is characterized in that, described Bletilla glucomannan is to prepare by the following method: will add in the distilled water of 10～12 times of volumes after 1 weight portion Pseudobulbus Bletillae (Rhizoma Bletillae) pulverizing medicinal materials, be heated to 50 ℃ and stirred 1 hour, filter, collect extracting solution; Then the medicinal residues distilled water that adds respectively 5～6 times of volumes repeats to extract 1～3 time; Merge extractive liquid, is concentrated into half volume, adds 95% ethanol to regulate ethanol mass concentration to 70%, separates out precipitation, and centrifugal, collecting precipitation is used washing with alcohol, in 80 ℃ of dryings, obtains Bletilla glucomannan.
3. gel adhesive as claimed in claim 1, is characterized in that, described gel adhesive comprises the component of following weight proportion:
Curcumin 0.4, Bletilla glucomannan 2.5, polyacrylic acid 3.0, polyvinylpyrrolidone 0.8, polyvinyl alcohol 0.3 hypromellose 0.2, glycerol 15.0, propylene glycol 15.0, Polyethylene Glycol 5.0, aluminium hydroxide 0.1, water 57.7.
4. gel adhesive as claimed in claim 1, is characterized in that, described gel adhesive comprises the component of following weight proportion:
Curcumin 0.4, Bletilla glucomannan 2.0, polyacrylic acid 4.0, polyvinylpyrrolidone 0.6, polyvinyl alcohol 0.1, hypromellose 0.3, glycerol 25.0, propylene glycol 15.0, Polyethylene Glycol 10.0, aluminium hydroxide 0.2, polyvinylpyrrolidone k-30 4.0, water 38.4.
5. gel adhesive as claimed in claim 1, is characterized in that, described gel adhesive comprises the component of following weight proportion:
Curcumin 0.4, Bletilla glucomannan 1.0, polyacrylic acid 5.0, polyvinylpyrrolidone 0.3, polyvinyl alcohol 0.1, hypromellose 0.1, glycerol 35.0, propylene glycol 10.0, Polyethylene Glycol 10.0, aluminium hydroxide 0.1, mannitol 3.0, water 35.0.
6. method for preparing gel adhesive claimed in claim 1 comprises step:
1) preparation of curcumin solid dispersion: according to the prescription consumption proportion, curcumin is dissolved in appropriate organic solvent dehydrated alcohol or acetone, mix with the solid dispersion, fully stir under 60 ℃ of condition of water bath heating, organic solvent is removed in evaporation, lets cool to room temperature, dry 5h in 45～55 ℃ of vacuum drying ovens again, take out and pulverize, sieve, and get final product;
2) preparation of substrate: according to the prescription consumption proportion, Bletilla glucomannan, wetting agent, cross-linking agent are stirred under 25 ℃～35 ℃ water bath condition, then add framework material, adhesive, penetrating agent, fully stir, and get final product;
3) preparation of pastille glue: according to the prescription consumption proportion, with curcumin or step 1) curcumin solid dispersion of preparation is added in substrate after disperseing with suitable quantity of water or glycerol dissolving, adds remaining water, stir, and de-bubbled, and get final product;
4) preparation of gel adhesive: pastille glue is applied on backing layer, dry 0.5～3.5h under 40～60 ℃, the upper cover protective layer cuts, and get final product.
7. method as claimed in claim 6, is characterized in that, described step 2) in adhesive be to add with the aqueous solution form of 0.5～10wt%.
8. method as claimed in claim 7, it is characterized in that, described step 2) in, adhesive is selected from polyvinylpyrrolidone, polyvinyl alcohol and hypromellose, and polyvinylpyrrolidone is to add with the aqueous solution form of 1.5～8.5wt%, polyvinyl alcohol is to add with the aqueous solution form of 1.5～9.5wt%, and hypromellose is to add with the aqueous solution form of 0.5～3.5wt%.
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| CN115364270A (en) * | 2022-04-11 | 2022-11-22 | 北京化工大学 | Preparation method of antibacterial and antioxidant fiber film dressing containing traditional Chinese medicines |
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Effective date of registration: 20210907 Address after: 276000 east of 150m Road south of the intersection of Huaxia Road and federal Road, economic and Technological Development Zone, Linyi City, Shandong Province Patentee after: Shandong Fuyang Technology Development Co.,Ltd. Address before: 276000 Shuangling Road, Lanshan District, Linyi City, Shandong Province Patentee before: LINYI University |