CN100512807C - Pharmaceutical for preventing and curing acute gout, tumor and hepatic/pulmonary fibrosis and preparation method thereof - Google Patents
Pharmaceutical for preventing and curing acute gout, tumor and hepatic/pulmonary fibrosis and preparation method thereof Download PDFInfo
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- CN100512807C CN100512807C CNB2004100224102A CN200410022410A CN100512807C CN 100512807 C CN100512807 C CN 100512807C CN B2004100224102 A CNB2004100224102 A CN B2004100224102A CN 200410022410 A CN200410022410 A CN 200410022410A CN 100512807 C CN100512807 C CN 100512807C
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- cataplasma
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- colchicine
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Abstract
The invention discloses a colchicines medicament and its preparing method, which is prepared from colchicines or its derivative and right base material and findings. The medicament is mainly for treating acute gout, tumor and liver pulmonary fibrosis.
Description
Technical field
The present invention relates to the transdermal administration dosage form that a kind of prevention and treatment can be used for the medicine of acute gout, the pulmonary fibrosis of tumor regulating liver-QI, specifically the colchicine sheet changes cataplasma into by tablet, the invention particularly relates to the preparation method and the substrate of this medicine cataplasma.
Background technology
Prescription of the present invention derives from the colchicine sheet in the Pharmacopoeia of the People's Republic of China (version was second in 2000).Former dosage form is a tablet.Colchicine is the class high-activity biological alkali with strong toxic and side effects.Existing clinical existing tablet and injection, but clinical reflection has more toxicity after using: bone marrow depression, nausea,vomiting,diarrhea are arranged, just secrete, peripheral neuritis, nephrotoxicity, inhibition breathing etc. and can cause agranulocytosis and aplastic anemia etc.Because of the safety of this product oral preparations lower.And medicine as the treatment human body diseases the high activity material, its safety is primary all the time.And external preparation is better than oral preparations aspect safety, and colchicine untoward reaction under long-term low dose is slight.The present invention just is being based on this point and is adopting transdermal administration technology (TTS) to change cataplasma into Tripterygium Hypoglaucum Hutch Tablet.To reach inner disease outer treat, slow release and rake purpose to administration.Compare with other dosage form, have than high-tech content.
Transdermal administration technology (TTS) is the forward position direction in current pharmaceutics field.Cataplasma system is with medicine dissolution or be mixed in natural and the synthesizing water-solubility macromolecular material substrate and the stand is applied to and mounts on the backing material, for the external preparation that sticks in skin.It also belongs to the transdermal administration technology, and its original shape is " poultice ".Polymer-based material in the cataplasma can absorb better and carrying comprises water solublity and fat-soluble composition, and gives " gelation " molding.Owing to contain the moisture up to 40%～60% in the drug matrices, such structure is just as one " Drug Storage ", can be fast, contained active ingredient in the transdermal release substrate enduringly.Be that cataplasma has big, moisture many, the easily absorption of medicine of drug loading, good permeability, the advantage little to skin irritation.Cataplasma is compared the cataplasma poisonous side effect of medicine with oral formulations little, and safety improves greatly.Liver first-pass effect does not take place in medicine in addition, is not subjected to gastric emptying and liver function influence, the bioavailability height, approximate slow release " drug administration by injection ", it is also very convenient to stop medication, and cataplasma has been exempted the worries that the patient takes medicine simultaneously, because take medicine offending thing always.To compare cataplasma safe with injection, belongs to painless, no wound administration, convenient drug administration.
The composition of catablasm base material generally contains following a few class:
● the preferred gelatin of the sticker (being adhesive agent again) of a skeleton function, methylcellulose, carboxymethyl cellulose and sodium salt, polyacrylic acid and sodium salt thereof (PANA), polyvinyl alcohol, polyvinylpyrrolidone series (PVP), carbomer etc.
● filler mainly contains: clay, Pulvis Talci, micropowder silica gel, calcium carbonate, Kaolin, kieselguhr, zinc oxide, kaolin, titanium dioxide, lithopone etc.
● wetting agent mainly contains: glycerol, Polyethylene Glycol (PEG), sorbitol, propylene glycol, glycerol etc.
● the preferred azone of Percutaneous absorption enhancer, propylene glycol, menthol (or Mentholum), Borneolum Syntheticum, Camphora, eucalyptus oil, oleic acid, dimethyl sulfoxide etc.
● play the oils and fats of emollescence; T-80 (medicine peptizaiton), liquid paraffin, Oleum Ricini, methyl salicylate etc.
● gelatinizing agent: zinc oxide, the contour valent metal oxide of titanium oxide.
● the interlinkage regulator: metal-chelator actually as EDTA, with the speed of control interlinkage reaction, forms colloid and is delayed to after the coating.
● other is also just like citric acid, phosphorous acid, Fructus Capsici extract etc.
Cataplasma adding menthol (or Mentholum), Borneolum Syntheticum, Camphora are cold mould; The adding Fructus Capsici extract is a pattern of fever.
Summary of the invention
Colchicine is to belong to a kind of alkaloid that extracts the plants such as light mushroom, Gloriosa saperba L. genus from Liliaceae Europe plant colchicine people bulb, Liliaceae Yunnan Province of China Lijing Pseudobulbus Cremastrae Seu Pleiones.Colchicine treatment gout starts from 1820, is become the classical medicine and the specific medicament for the treatment of acute gouty arthritis after the purification in 1940.Main pharmacological: this product is to the selective antiinflammation of acute gouty arthritis, its mechanism may be to move by suppressing the neutrophilic granulocyte chemotactic, suppress its infiltration and engulf, stop its secretion chemokines, thereby reduce the inflammatory reaction that uric acid crystal causes, stop acute attack and prevent outbreak.After the general medication first a few hours posterior joint red, swollen, heat and disappear at once bitterly.This product pair cell mitosis has obvious inhibitory action simultaneously, can make cell stop metaphase of cell division, chromosome can not be moved to the two poles of the earth, thereby cause cell death, so certain antitumor action is arranged.But because the excessive (LD of its toxicity
50=1.6mg/kg), often producing more serious toxicity, excessive injection also can cause animal dead.Therefore this has limited its application to a certain extent.For reducing the side effect of colchicine to human body, so that be human service better, the present invention makes cataplasma with colchicine (or derivatives thereof) and suitable substrate and other adjuvant.
The present invention is implemented by following scheme:
Colchicine cataplasma of the present invention, the principal agent in its prescription is colchicine (or derivatives thereof), the more described cataplasma made from suitable substrate and adjuvant of any pharmaceutics;
Colchicine of the present invention (or derivatives thereof) cataplasma, its described colchicine (C
22H
25NO
6) derivant is meant any to 2. described colchicine (C
22H
25NO
6) chemical constitution carry out the derivant of chemical modification gained;
Employed adjuvant of the preparation method of colchicine cataplasma of the present invention and substrate can be the above any adjuvant and the substrate of preparation cataplasma of pharmaceutics.
The preparation method of colchicine of the present invention (or derivatives thereof) cataplasma, mainly be: colchicine is dissolved with an amount of purified water, add plaster such as oils and fats and Percutaneous absorption enhancer material commonly used again, get medicinal liquid, press the mixed of 1:1～1000 again with substrate, stirred 15～40 minutes, coating, the film section is closed in cutting, and packing promptly gets cataplasma.
The preparation method of colchicine of the present invention (or derivatives thereof) cataplasma, concrete steps are as follows:
1. colchicine is dissolved with an amount of purified water, add plaster such as oils and fats and Percutaneous absorption enhancer material commonly used again, get medicinal liquid;
2. the gained medicinal liquid is pressed the mixed of 1:1～1000 again with substrate, stirred 15～40 minutes, and coating, the film section is closed in cutting, and packing promptly gets cataplasma.
Plaster such as said oils and fats and Percutaneous absorption enhancer material commonly used is meant in the preparation method of colchicine of the present invention (or derivatives thereof) cataplasma: one or more materials in menthol, Mentholum, Borneolum Syntheticum, Camphora, azone, oleic acid, eucalyptus oil, DMSO, T-80, Oleum Ricini, white mineral oil, methyl salicylate, the Fructus Capsici extract.With the flexibility, the tolerance to cold that improve cataplasma or play the Percutaneous absorption enhancer effect;
Substrate of the present invention can mix by weight by containing following natural and synthetic high molecular polymer: sodium polyacrylate: 1～5 part, polyvinylpyrrolidone K-30:10～35 part, sodium carboxymethyl cellulose: 10～20 parts, gelatin: 1～10 part, Kaolin: 10～25 parts, propylene glycol: 5～20 parts, PEG400: 20～60 parts, glycerol: 50～100 parts.
Substrate optimum organization of the present invention is (mixing by weight): sodium polyacrylate: 2 parts, polyvinylpyrrolidone K-30:28 part, sodium carboxymethyl cellulose: 16 parts, gelatin: 2 parts, Kaolin: 16 parts, propylene glycol: 14 parts, PEG400: 40 parts, glycerol: 80 parts.
The preparation technology of substrate of the present invention is:
Step 1: it is an amount of that gelatin, sodium carboxymethyl cellulose and the polyvinylpyrrolidone K-30 of aforementioned proportion added water respectively, and swelling under 40 ℃～60 ℃ water-baths is scattered in the glycerol under 40 ℃～60 ℃ water-baths.
Step 2: sodium polyacrylate is scattered in the propylene glycol, adds Kaolin then, add 11～22 parts in water then, stir, make and be dissolved into transparent colloid.
Step 3: under 40 ℃～60 ℃ water-baths step 2 gained mixture is added in the step 1, stir, add PEG400 again, stirring promptly gets catablasm base material.
The present invention is through pharmacodynamics test research-usefulness rat carrageenan foot swelling test, the result show cause scorching before and after creme group paw swelling of the present invention and negative control group significant difference is relatively arranged; With the mice ear test, the result shows that the present invention has antiinflammatory action; Carry out analgesic test research with mice hot plate method and writhing method, the result shows that creme of the present invention has analgesic activity preferably.
The embodiment of preparation aspect further specifies the present invention for example below, and this embodiment only is used to the present invention is described and the present invention is not had any restriction.
The specific embodiment
Embodiment:
Prepare the colchicine medicinal liquid as follows:
Colchicine is dissolved with an amount of purified water, add 2% azone again, 0.6 times of material that amount is made up of Mentholum, Borneolum Syntheticum, Camphora and Oleum Ricini stirs, and gets medicinal liquid.
Prepare substrate more as follows:
Step 1: it is an amount of that gelatin, sodium carboxymethyl cellulose and the polyvinylpyrrolidone K-30 of aforementioned proportion added water respectively, and swelling under 40 ℃～60 ℃ water-baths is scattered in the glycerol under 40 ℃～60 ℃ water-baths.
Step 2: sodium polyacrylate is scattered in the propylene glycol, adds Kaolin then, add 11～22 parts in water then, stir, make and be dissolved into transparent colloid.
Step 3: under 40 ℃～60 ℃ water-baths step 2 gained mixture is added in the step 1, stir, add PEG400 again, stirring promptly gets catablasm base material.
Prepare the colchicine cataplasma more as follows:
Get 1 part of above-mentioned medicinal liquid.Stir.Again this medicinal liquid is added in 10 parts of substrate that prepare as stated above and mix, stirred 20 minutes, coating, the film section is closed in cutting, and packing promptly gets cataplasma.
Claims (2)
1, the medicine of a kind of prevention and treatment acute gout, the pulmonary fibrosis of tumor regulating liver-QI is characterized in that it is by containing colchicine C
22H
25NO
6Medicine and the cataplasma made of suitable substrate and adjuvant:
Described cataplasma it take following steps to make:
Step 1: colchicine is dissolved with an amount of purified water, add oils and fats and Percutaneous absorption enhancer plaster material commonly used again, get medicinal liquid;
Step 2: step 1 gained medicinal liquid is pressed the mixed of 1:1～1000 again with substrate, stirred 15～40 minutes, coating, the film section is closed in cutting, and packing promptly gets cataplasma;
The preparation technology of described substrate is:
Step 1: it is an amount of that the polyvinylpyrrolidone K-30 of the sodium carboxymethyl cellulose of the gelatin of 1～10 weight portion, 10～20 weight portions and 10～35 weight portions is added water respectively, swelling under 40～60 ℃ of water-baths is scattered in the glycerol of 50～100 weight portions under 40～60 ℃ of water-baths;
Step 2: the sodium polyacrylate of 1～5 weight portion is scattered in the propylene glycol of 5～20 weight portions, adds the Kaolin of 10～25 weight portions then, add 11～22 parts in water again, stir, make and be dissolved into transparent colloid;
Step 3: in the material that under 40～60 ℃ of water-baths step 2 gained transparent colloid adding step 1 is made, stir, add the PEG400 of 20～60 weight portions again, stirring promptly gets catablasm base material.
2, the medicine of a kind of prevention according to claim 1 and treatment acute gout, the pulmonary fibrosis of tumor regulating liver-QI is characterized in that the weight part ratio of following material among the preparation technology of described substrate is:
2 weight portion sodium polyacrylate, 28 weight account polyethylene ketopyrrolidine K-30,16 weight portion sodium carboxymethyl cellulose, 2 weight portion gelatin, 16 weight portion Kaolin, 14 weight portion propylene glycol, 40 weight portion PEG400s, 80 weight portion glycerol.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100224102A CN100512807C (en) | 2004-04-27 | 2004-04-27 | Pharmaceutical for preventing and curing acute gout, tumor and hepatic/pulmonary fibrosis and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CNB2004100224102A CN100512807C (en) | 2004-04-27 | 2004-04-27 | Pharmaceutical for preventing and curing acute gout, tumor and hepatic/pulmonary fibrosis and preparation method thereof |
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| CN1568951A CN1568951A (en) | 2005-01-26 |
| CN100512807C true CN100512807C (en) | 2009-07-15 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106038064A (en) * | 2016-04-28 | 2016-10-26 | 邱清泉 | Medicine patch for treating postoperative wound edema and preparation method of medicine patch |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101991858B (en) * | 2009-08-18 | 2012-06-27 | 天津京英透皮材料科技开发有限公司 | Novel externally applied auxiliary material and preparation method thereof |
| CN103251550B (en) * | 2012-02-20 | 2016-04-20 | 上海市计划生育科学研究所 | Transdermal administration unguentum containing colchicine and preparation method thereof |
| CN104586856A (en) * | 2014-12-30 | 2015-05-06 | 新昌县大成生物科技有限公司 | Drug composition containing Criofolinine and application thereof |
| CN113041210B (en) * | 2016-11-08 | 2023-06-02 | 北京天衡军威医药技术开发有限公司 | Colchicine external composition |
-
2004
- 2004-04-27 CN CNB2004100224102A patent/CN100512807C/en not_active Expired - Fee Related
Non-Patent Citations (2)
| Title |
|---|
| 巴布剂——一个既新又古老的剂型. 易军等.江西中医学院学报，第10卷第1期. 1998 |
| 巴布剂——一个既新又古老的剂型. 易军等.江西中医学院学报，第10卷第1期. 1998 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106038064A (en) * | 2016-04-28 | 2016-10-26 | 邱清泉 | Medicine patch for treating postoperative wound edema and preparation method of medicine patch |
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| CN1568951A (en) | 2005-01-26 |
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Granted publication date: 20090715 Termination date: 20100427 |