CN102727454B - Evodiamine dispersion tablets and preparation method thereof - Google Patents
Evodiamine dispersion tablets and preparation method thereof Download PDFInfo
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- CN102727454B CN102727454B CN2012101667649A CN201210166764A CN102727454B CN 102727454 B CN102727454 B CN 102727454B CN 2012101667649 A CN2012101667649 A CN 2012101667649A CN 201210166764 A CN201210166764 A CN 201210166764A CN 102727454 B CN102727454 B CN 102727454B
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Abstract
The present invention provides a drug for treating hyperuricemia and gout, ie., evodiamine dispersion tablets. The evodiamine dispersion tablets are the preparation prepared from the following raw materials and additives, by weight, 7-13 parts of evodiamine, 30-50 parts of a solid dispersion water-soluble carrier material, 70-90 parts of a filler, and 8-14 parts of a disintegrating agent. The present invention further provides a preparation method and uses of the dispersion tablets. The evodiamine dispersion tablets of the present invention have characteristics of short disintegration time and high dispersion uniformity. According to the present invention, the dissolution of the insoluble drug evodiamine in the solid preparation can be significantly improved, the absorption of the evodiamine in the human body is prompted, the bioavailability of the drug is increased, and new selections are provided for clinical medication for treatments of hyperuricemia and gout.
Description
Technical field
The present invention relates to a kind of rutaecarpin dispersible tablet and preparation method thereof.
Background technology
Rutaecarpin is Fructus Evodiae main pharmacodynamics composition, and modern pharmacological research shows, rutaecarpin has the pharmacological activities such as blood vessel dilating, antiinflammatory, analgesia, fat-reducing, regulate body temperature, antitumor and anticancer transfer, has wide DEVELOPMENT PROSPECT.By long-term experiment, find, rutaecarpin also has the effect of significantly falling blood uric acid and the foot swelling of anti-animal acute gouty arthritis, applicable to the treatment (Song Ying of hyperuricemia and gout, Deng, the pharmacodynamic study of rutaecarpin treatment gout, Pharmacology and Clinics of Chinese Materia Medica, 6 phases in 2011).But rutaecarpin is insoluble in water, if it is prepared into to common oral preparation, can cause the dissolution of rutaecarpin low, oral absorption is incomplete, and bioavailability is low, is unfavorable for the performance meeting of therapeutical effect.And on the clinical treatment of hyperuricemia and gout, often need release rapid.
Dispersible tablet is fast dissolving dosage form commonly used, and this dosage form mainly is applicable to insoluble drug and the low medicine of bioavailability.It has good dispersing state, disintegration time is short, drug-eluting is rapid, absorption is fast, bioavailability is high, untoward reaction is few, the mode of taking is various and easy to carry, especially is applicable to the advantages such as old people and dysphagia patients.
At present, yet there are no rutaecarpin is prepared into to the report that disperses sheet.
Summary of the invention
The object of the present invention is to provide a kind ofly be uniformly dispersed, dissolution rate is fast, bioavailability is high rutaecarpin dispersible tablet.Another object of the present invention is to provide the preparation method of this dispersible tablet.
The invention provides a kind of rutaecarpin dispersible tablet, it is the preparation be prepared from by the supplementary material that comprises following weight proportion:
Rutaecarpin 7-13 part, solid dispersion water-solubility carrier material 30-50 part, filler 70-90 part, disintegrating agent 8-14 part;
Wherein, described solid dispersion water-solubility carrier material is selected from one or more the combination in Macrogol 4000, polyethylene glycol 6000, PLURONICS F87, polyvinylpyrrolidone, mannitol, polyethylene oxide;
Described filler is selected from one or more the combination in microcrystalline Cellulose, mannitol, lactose, dextrin, amylum pregelatinisatum;
Described disintegrating agent is selected from one or more the combination in microcrystalline Cellulose (MCC), cross-linking sodium carboxymethyl cellulose (CCMC-Na), carboxymethyl starch sodium (CMS-Na), low-substituted hydroxypropyl cellulose (L-HPc), crospolyvinylpyrrolidone (PVPP).
Wherein, described solid dispersion water-solubility carrier material is PLURONICS F87; Filler is microcrystalline Cellulose: lactose=(1-3): (1-3) w/w; Disintegrating agent is PVPP:CMS-Na=(1-3): (1-3) w/w or PVPP:L-HPc=(1-3): (1-3) w/w.
Further, it is the preparation be prepared from by the supplementary material that comprises following weight proportion:
10 parts of rutaecarpins, 40 parts of PLURONICS F87s, 82 parts of filleies, 11 parts of disintegrating agents;
Wherein, filler is microcrystalline Cellulose: lactose=1:1w/w; Disintegrating agent is PVPP:CMS-Na=1:1w/w or PVPP:L-HPc=1:1w/w.
Further, it also contains following adjuvant: 5 parts of lubricants, 2 parts of correctivess.
Wherein, described lubricant is selected from one or more the combination in micropowder silica gel, magnesium stearate, Pulvis Talci, Polyethylene Glycol, corn starch; Described correctives is selected from one or more the combination in mannitol, steviosin, aspartame.
Further preferably, it is the preparation be prepared from by the supplementary material that comprises following weight proportion:
10 parts of rutaecarpins, 40 parts of PLURONICS F87s, 41 parts of microcrystalline Cellulose, 41 parts of lactose, 5.5 parts of L-HPc, 5.5 parts of PVPP, 2.5 parts of magnesium stearate, 2.5 parts of micropowder silica gels, 2 parts of Aspartane.
The present invention also provides the preparation method of above-mentioned rutaecarpin dispersible tablet, and it comprises following operating procedure:
(1) take supplementary material by the prescription proportioning;
(2), after getting rutaecarpin and being crushed to particle diameter 1 ~ 10 μ m, with solid dispersion water-solubility carrier material mixing, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, after mixing with filler, disintegrating agent, tabletting or granulate after tabletting again.
Wherein, described fusion method concrete operations are as follows: solid dispersion water-solubility carrier material is heated to molten condition, after rutaecarpin is mixed homogeneously, is cooled to curingly, after drying, pulverize, obtain solid dispersion.
Further, be cooled to-10-30 ℃ solidifies.
The present invention also provides the purposes of upper rutaecarpin dispersible tablet in the medicine of preparation treatment hyperuricemia, gout.
The present invention is by screening resulting rutaecarpin dispersible tablet to multiple auxiliary materials, disintegration time is short, dispersing uniformity is high, can significantly improve the dissolution of rutaecarpin in solid preparation, be conducive to rutaecarpin absorption in vivo, and then improved the bioavailability of medicine, for the clinical application for the treatment of hyperuricemia, gout provides new selection.
The specific embodiment
The preparation of embodiment 1 rutaecarpin dispersible tablet of the present invention
The rutaecarpin dispersible tablet comprises following percentage by weight component, to make 1000
Preparation method: (1) takes supplementary material by the prescription proportioning;
(2) get rutaecarpin, after being crushed to particle diameter 1～10 μ m, then mix with PLURONICS F87, adopt fusion method to prepare solid dispersion;
Fusion method of the present invention can carry out according to conventional method, or adopts following operating procedure:
Poloxamer, in 80 ℃ of water bath with thermostatic control meltings, is stirred after adding rutaecarpin, freezing the solidifying under-20 ℃ that incline and rapidly, and move to, take out dry, pulverize, sieving for standby.
(3) get the solid dispersion that step (2) prepares, pulverized after 80 mesh sieves with microcrystalline Cellulose, lactose, L-HPc, PVPP, Aspartane, magnesium stearate and micropowder silica gel, mix evenly after direct compression.
The function of this rutaecarpin dispersible tablet cure mainly for: blood uric acid, antiinflammatory, analgesia are fallen.Treatment for hyperuricemia, gout.
The preparation of embodiment 2 rutaecarpin dispersible tablet of the present invention
The rutaecarpin dispersible tablet comprises following percentage by weight component, to make 1000
Preparation method: (1) takes supplementary material by the prescription proportioning;
(2) after getting rutaecarpin and being crushed to particle diameter 1～10 μ m, then mix with PEG-6000, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, mix rear direct compression with microcrystalline cellulose, lactose, L-HPc, PVPP, Aspartane, magnesium stearate and micropowder silica gel after pulverizing 80 mesh sieves
The preparation of embodiment 3 Fructus Evodiae dispersible tablet of the present invention
The rutaecarpin dispersible tablet comprises following percentage by weight component, to make 1000
Preparation method: (1) takes supplementary material by the prescription proportioning;
(2) after getting rutaecarpin and being crushed to particle diameter 1～10 μ m, then mix with PEG-4000, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, mix rear direct compression with microcrystalline cellulose, L-HPc, PVPP, Aspartane, magnesium stearate and micropowder silica gel after pulverizing 80 mesh sieves
The preparation of embodiment 4 Fructus Evodiae dispersible tablet of the present invention
The rutaecarpin dispersible tablet comprises following percentage by weight component, to make 1000
Preparation method: (1) takes supplementary material by the prescription proportioning;
(2) after getting rutaecarpin and being crushed to particle diameter 1～10 μ m, then mix with PLURONICS F87, PEG-6000, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, pulverized the preparation that mixes rear direct compression embodiment 5 Fructus Evodiae dispersible tablet of the present invention after 80 mesh sieves with microcrystalline cellulose, lactose, L-HPc, PVPP, Aspartane, magnesium stearate and micropowder silica gel
The rutaecarpin dispersible tablet comprises following percentage by weight component, to make 1000
Preparation method: (1) takes supplementary material by the prescription proportioning;
(2) after getting rutaecarpin and being crushed to particle diameter 1～10 μ m, then mix with PEG-4000, PEG-6000, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, mix rear direct compression with microcrystalline cellulose, lactose, L-HPc, PVPP, Aspartane, magnesium stearate and micropowder silica gel after pulverizing 80 mesh sieves.
Embodiment 6 dispersible tablet character are investigated
Rutaecarpin dispersible tablet in embodiment 1 to 5 has been carried out to dispersing uniformity, dissolution in vitro test, and its test method and result are as follows.
1, dispersing uniformity
Experimental condition: get 6 of rutaecarpin dispersible tablets, shine dispersing uniformity inspection technique (two appendix IA of Chinese Pharmacopoeia version in 2010) in the 100ml water of 15 ~ 25 ℃, jolting 3 minutes, all also, by No. 2 sieves, its result of the test sees the following form 1 in disintegrate:
Table 1 dispersing uniformity result of the test
| Embodiment | Result of the test |
| Embodiment 1 | In 3min, all disintegrate is complete, and all by No. 2 sieves |
| Embodiment 2 | In 3min, all disintegrate is complete, and all by No. 2 sieves |
| Embodiment 3 | In 3min, all disintegrate is complete, and all by No. 2 sieves |
| Embodiment 4 | In 3min, all disintegrate is complete, and all by No. 2 sieves |
| Embodiment 5 | In 3min, all disintegrate is complete, and all by No. 2 sieves |
Result of the test shows, rutaecarpin dispersible tablet dispersing uniformity of the present invention meets the pharmacopeia requirement.
2, dissolution in vitro
Experimental condition: take 1% sodium lauryl sulphate 900ml by dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2010) is solvent, rotating speed 50rpm, and 37 ℃ ± 0.5 ℃ of temperature, operation, sample in 45min in accordance with the law.Measure content according to high performance liquid chromatography (two appendix VD of Chinese Pharmacopoeia version in 2010) in the 225nm place, and calculate dissolution, the results are shown in Table 2.
Table 2 dissolution in vitro result of the test
| Sample | Rutaecarpin dissolution (%) |
| Embodiment 1 | 66.91 |
| Embodiment 2 | 66.63 |
| Embodiment 3 | 65.53 |
| Embodiment 4 | 65.34 |
| Embodiment 5 | 66.19 |
By upper table, known, rutaecarpin dispersible tablet dissolution of the present invention can reach more than 60%.
From above-mentioned experiment, dispersion product prepared by the present invention meet the requirement of pharmacopeia to dispersing uniformity and dissolution in vitro, show dispersible tablet formulation success in the present invention.
The investigation of embodiment 7 rutaecarpin dispersible tablet of the present invention adjuvant
In the present embodiment, preparation rutaecarpin used, be all that rutaecarpin is crushed to particle diameter 1～10 μ m.
The preparation of 1 solid dispersion
Dispersible tablet is fast dissolving dosage form, and this dosage form mainly is applicable to insoluble drug and the medicine of bioavailability problem is arranged, and the medicine dispersity of slightly soluble oral medicine preparation is the principal element that affects stripping and absorption.Solid dispersion technology can by insoluble drug with molecule, colloid, crystallite or unformed state high degree of dispersion in the water-soluble solid carrier material, make medicine and there is very large dispersion, increased the wettability of medicine due to the existence of carrier material simultaneously, thereby with after gastro-intestinal Fluid contacts, can accelerate the dissolution rate of medicine, promote the absorption of medicine, thereby improve the bioavailability of medicine, reach efficient and quick-acting purposes.
1.1 the screening of solid dispersion carrier
Quick-releasing type solid dispersion carrier used mostly is water-soluble high-molecular compound, commonly uses Polyethylene Glycol (PEG) 4000 and 6000, polyvinylpyrrolidone (PVP), Poloxamer188 are arranged.The present invention selects these four kinds of adjuvants to carry out the preparation of solid dispersion, take dissolution as evaluation index.
1.1.1 the preparation of Polyethylene Glycol (PEG) 4000,6000 and Poloxamer188 sample
Get respectively each 9 parts of different carriers, in 80 ℃ of water bath with thermostatic control meltings, after adding respectively 1 part of rutaecarpin and stirring 30min, incline and rapidly, move to freezing solidifying under-20 ℃, taking-up dry, pulverize, sieving for standby.
1.1.2 the preparation of polyvinylpyrrolidone (PVP) sample
Take 1 part of rutaecarpin and add appropriate dehydrated alcohol, 60 ℃ are stirred to dissolve.Take again 9 parts of PVPk
30, add in above-mentioned ethanol, 60 ℃ are stirred to dissolve, and reclaim ethanol, dry, pulverize, sieve, standby.
1.1.3 the preparation of physical mixture:
Take by a certain percentage principal agent and carrier (rutaecarpin: carrier=1:9), pulverized 80 mesh sieves, mix homogeneously, kept dry, obtain.
1.1.4 the mensuration of dissolution, the results are shown in Table 3.
The screening of table 3 water-solubility carrier
By upper table, drawn, under carrier and principal agent same ratio condition, Poloxamer188 improves maximum to the dissolution of rutaecarpin, therefore selects Poloxamer188 to prepare the carrier of solid dispersion as rutaecarpin.
1.2 the screening of solid dispersion carrier ratio
The proportioning of design rutaecarpin and tetra-ratios of Poloxamer188, rutaecarpin and Poloxamer188 ratio are respectively 1:2,1:4,1:6 and 1:9, and the dissolution of take is investigated as index, to determine best ratio of adjuvant.The results are shown in Table 4.
The screening of table 4 solid dispersion adjuvant ratio
Result shows, the dissolution that rutaecarpin and Poloxamer188 ratio are 1:4 and the dissolution difference of 1:9 are little, and a little higher than 1:9 ratio, therefore for reducing supplementary product consumption, determine rutaecarpin and the Poloxamer188 ratio in 1:4, adopt fusion method to prepare solid dispersion.
The selection of 2 filleies
Filler commonly used has microcrystalline Cellulose, mannitol, lactose, dextrin and starch etc., and the alone investigation of filler is first carried out in this experiment, then carries out the coupling investigation of filler.Take mobility, tabletting difficulty or ease, disintegration, dispersing uniformity and tablet weight variation is screened as index.
2.1 the alone screening of filler
Take microcrystalline Cellulose, mannitol, lactose, dextrin and starch respectively as filler, mix in proportion tabletting with rutaecarpin solid dispersion powder.The results are shown in Table 5.
The alone investigation of table 5 filler
In single choice, mannitol, the equal tabletting of dextrin are unsuccessful, and mouldability is poor; Lactose tabletting difficulty; The starch disintegration time is long; Take microcrystalline Cellulose as filler, the effect optimum.But microcrystalline Cellulose fine powder in preparation process is more, and mobility is poor, therefore considers to mix and use filler.
2.2 the coupling of filler screening
Select lactose, mannitol, dextrin, starch to be prepared in the mode of 1:1 ratio combination respectively with microcrystalline Cellulose respectively.Result of the test is in Table 6.
The coupling screening of table 6 filler
Result is all better with lactose and microcrystalline Cellulose coupling compressibility, mobility, meets dispersing uniformity and disintegration the pharmacopeia requirement, and therefore selecting lactose and microcrystalline Cellulose coupling is filler.
The selection of 3 disintegrating agents
Disintegrating agent is most important in dispersible tablet, and the kind of disintegrating agent, consumption, ratio are the keys of dispersible tablet molding.
At present, in dispersible tablet, disintegrating agent commonly used has crosslinked methylcellulose (CCMC-Na), carboxymethyl starch sodium (CMS-Na), low light propyl cellulose (L-HPc), polyvinylpyrrolidone (PVP), crospolyvinylpyrrolidone (PVPP), the microcrystalline Cellulose (MCC) etc. of replacing, wherein to hang down, replace that light propyl cellulose (L-HPC), crosslinked polyethylene adjoin pyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na) is comparatively outstanding, better performances, be widely used.It is evaluation index that disintegration and the dispersing uniformity of dispersible tablet take in the present invention, investigates respectively the situation of the alone and coupling of disintegrating agent, the results are shown in Table 7.
The screening of table 7 disintegrating agent kind
Result shows, take CMS-Na+PVPP and L-HPC+PVPP disintegration as better, and both differences are not remarkable, all within 1min, and tablet appearance and dispersing uniformity better.L-HPC+PVPP take disintegration as optimum, and CMS-Na is than the L-HPC price, therefore selection L-HPC+PVPP is disintegrating agent in addition.
The selection of 4 lubricants
Because of the solid dispersion of preparation, through pulverizing 80 mesh sieves, after filler and disintegrating agent are mixed homogeneously, be 38.61 ° angle of repose, good fluidity, and the solid dispersion powder is water solublity, should not be granulated with aqueous binders, prevents the inhomogeneities of content.Therefore adopt direct powder compression, have advantages of that time-saving energy-saving, simple process, operation are few.
Direct powder compression requires powder to have mobility preferably, therefore selects micropowder silica gel commonly used and magnesium stearate and both couplings to be investigated.Take angle of repose, tablet weight variation as investigating index, determine proper lubrication agent kind.The results are shown in 8.
The investigation of table 8 lubricant kind
As seen from the above table, magnesium stearate and micropowder silica gel are significantly improved to powder flowbility, and tablet weight variation is little, therefore adopt magnesium stearate and the micropowder silica gel lubricant as this product.
The screening of 5 adjuvant ratios
Filler has MCC, lactose, disintegrating agent L-HPC and PVPP, magnesium stearate lubricant and micropowder silica gel, wherein filler and disintegrating agent account for principal element to the impact of dispersible tablet, therefore select MCC(A), lactose (B), L-HPC (C), PVPP (D) be the investigation factor, each factor is got 3 levels, in Table 9.Wherein, the rutaecarpin solid dispersion accounts for 33% of total weight of formulation; The total consumption of adjuvant accounts for 67%, wherein, and the constant consumption 1.67% of magnesium stearate, the constant consumption 1.67% of micropowder silica gel, the constant consumption 1.3% of Aspartane.
Table 9 factor level
5.1 orthogonal experiments and analysis
In the situation that stator is heavy and medicine, operation repetitive, press L9 (34) orthogonal test.Investigate two indexs in this test, for objectively responding relation between each factor and factor level to the impact of rutaecarpin dispersible tablet quality, intend adopting the aggregative weighted point system.Use disintegration (X) and hardness (Y) for deliberated index, optimize and obtain the less and larger prescription of hardness disintegration.Comprehensive grading OD=Yi/YMAX * 30+ (1-Xi/XMAX) * 70.Orthogonal experiments is in Table 10, and result is carried out to statistical procedures, the results are shown in Table 11.
Table 10 Orthogonal Experiment and Design table and result
Table 11 analysis of variance table
F0.05(2,2)=19
By orthogonal experiments intuitive analysis and range analysis, drawn, the influence factor is sequentially: D>B>C>A, optimum combination is A
2b
3c
1d
1.And above 9 prescriptions all can reach the requirement of 2010 editions Pharmacopoeias of the People's Republic of China to the dispersible tablet dispersing uniformity.
Analysis of variance draws, factor D has appreciable impact, and factor A, B, C do not make significant difference.Therefore with A
2b
3c
1d
1for best moulding process.
6 conclusions
Known by above-mentioned experiment, rutaecarpin of the present invention is prepared into and disperses best prescription, the technique of sheet as follows:
Preparation method:
(1) take supplementary material by the prescription proportioning;
(2) get rutaecarpin and be crushed to particle diameter 1～10 μ m, then mix with PLURONICS F87, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, pulverized after 80 mesh sieves with microcrystalline Cellulose, lactose, L-HPc, PVPP, magnesium stearate and micropowder silica gel, mix evenly after direct compression.
Below illustrate beneficial effect of the present invention by test example.
The dissolution of test example 1 rutaecarpin dispersible tablet of the present invention and general formulation relatively
Rutaecarpin conventional tablet A: get rutaecarpin 10g, in situation about not pulverizing, after mixing with PLURONICS F87 40g, microcrystalline Cellulose 41g, lactose 41g, L-HPc5.5g, PVPP5.5g, magnesium stearate 2.5g, micropowder silica gel 2.5g, Aspartane 2g, direct compression.
Rutaecarpin conventional tablet B: get rutaecarpin 10g, after being crushed to particle diameter 1-10 μ m, after mixing with PLURONICS F87 40g, microcrystalline Cellulose 41g, lactose 41g, L-HPc5.5g, PVPP5.5g, magnesium stearate 2.5g, micropowder silica gel 2.5g, Aspartane 2g, direct compression.
The rutaecarpin dispersible tablet of above-mentioned rutaecarpin conventional tablet A, B and the embodiment of the present invention 1 preparation is carried out to the contrast of 45min dissolution, and result sees table.
Table 12
| Sample | 45min dissolution (%) |
| Rutaecarpin conventional tablet A | 0 |
| Rutaecarpin conventional tablet B | 11.60 |
| Rutaecarpin dispersible tablet of the present invention | 66.44 |
The rutaecarpin dispersible tablet has obviously improved the dissolution of insoluble medicine rutaecarpin, is conducive to rutaecarpin absorption in vivo.
In sum, rutaecarpin dispersible tablet provided by the invention, disintegration time is short, dispersing uniformity is high, can significantly improve the dissolution of rutaecarpin in solid preparation, be conducive to rutaecarpin absorption in vivo, and then improved the bioavailability of medicine, for the clinical application for the treatment of hyperuricemia, gout provides new selection.
Claims (1)
1. a rutaecarpin dispersible tablet, it is characterized in that: it is the preparation be prepared from by the supplementary material that comprises following weight proportion:
Rutaecarpin 7-13 part, solid dispersion water-solubility carrier material 30-50 part, filler 70-90 part, disintegrating agent 8-14 part;
Wherein, described solid dispersion water-solubility carrier material is PLURONICS F87; Filler is microcrystalline Cellulose: lactose=(1-3): (1-3) w/w; Disintegrating agent is crospolyvinylpyrrolidone: carboxymethyl starch sodium=(1-3): (1-3) w/w or crospolyvinylpyrrolidone: low-substituted hydroxypropyl cellulose=(1-3): (1-3) w/w.
2. rutaecarpin dispersible tablet according to claim 1, it is characterized in that: it is the preparation be prepared from by the supplementary material that comprises following weight proportion:
10 parts of rutaecarpins, 40 parts of PLURONICS F87s, 82 parts of filleies, 11 parts of disintegrating agents;
Wherein, filler is microcrystalline Cellulose: lactose=1:1w/w; Disintegrating agent is crospolyvinylpyrrolidone: carboxymethyl starch sodium=1:1 w/w or crospolyvinylpyrrolidone: low-substituted hydroxypropyl cellulose=1:1 w/w.
3. rutaecarpin dispersible tablet according to claim 1 and 2, it is characterized in that: it also contains following adjuvant: 5 parts of lubricants, 2 parts of correctivess.
4. rutaecarpin dispersible tablet according to claim 3 is characterized in that: described lubricant is selected from one or more the combination in micropowder silica gel, magnesium stearate, Pulvis Talci, Polyethylene Glycol, corn starch; Described correctives is selected from one or more the combination in mannitol, steviosin, aspartame.
5. rutaecarpin dispersible tablet according to claim 4, it is characterized in that: it is the preparation be prepared from by the supplementary material that comprises following weight proportion:
10 parts of rutaecarpins, 40 parts of PLURONICS F87s, 41 parts of microcrystalline Cellulose, 41 parts of lactose,
5.5 parts of L-HPc, 5.5 parts of PVPP, 2.5 parts of magnesium stearate, 2.5 parts of micropowder silica gels, 2 parts of Aspartane.
6. the preparation method of rutaecarpin dispersible tablet claimed in claim 1, it is characterized in that: it comprises following operating procedure:
(1) take supplementary material by the prescription proportioning;
(2), after getting rutaecarpin and being crushed to particle diameter 1 ~ 10 μ m, with solid dispersion water-solubility carrier material mixing, adopt fusion method to prepare solid dispersion;
(3) get the solid dispersion that step (2) prepares, after mixing with filler, disintegrating agent, tabletting or granulate after tabletting again.
7. preparation method according to claim 6, it is characterized in that: described fusion method concrete operations are as follows: solid dispersion water-solubility carrier material is heated to molten condition, after rutaecarpin is mixed homogeneously, be cooled to curing, after drying, pulverize, obtain solid dispersion.
8. preparation method according to claim 7, is characterized in that: be cooled to-10 ~ 30 ℃ and solidify.
9. the purposes of the described rutaecarpin dispersible tablet of claim 1-5 any one in the medicine of preparation treatment hyperuricemia, gout.
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| CN105709236B (en) * | 2016-01-26 | 2019-02-22 | 西南民族大学 | A kind of composition and cataplasm promoting rutaecarpin Transdermal absorption |
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