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Studies On Preparation Of The Compound Asiaticoside Cataplasm

Posted on:2014-02-01Degree:MasterType:Thesis
Country:ChinaCandidate:X HuFull Text:PDF
GTID:2231330398454119Subject:Pharmacy
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Hypertrophic scars (hypertrophic scars, HS) is the abnormal proliferationof tissue in the wound healing process.For a long time,the treatment ofhypertrophic scars plagued the majority of medical researchers. In the the scargrowing season, drug therapy play an important role,commonly usedhormones, silicon agents, anticancer drugs, immunosuppressants andcytokines, hormone drugs commonly used in the local injection of the scar,obvious side effects and poor patient compliance; silicon preparations due toits poor permeability, in the hot weather skin is easy to produce small pimplesor even ulceration; cytotoxicity of anticancer drugs, effective doses close tothe toxic dose, the dose is difficult to control, it is difficult for clinicalapplications; of immunosupp-ressive agents and cytokines have side effectsand expensive, not much used to clinical application. This article aims toselect the efficacy of the drug and a suitable dosage form to provide newproducts and preparations which are safe and effective clinical treatment ofHS.Asiaticosides is triterpenoid saponin compound which is extracted fromthe the Umbelliferae Centella asiatica (L.)Urb. Experiments show thatasiaticosides could inhibit the growth of fibroblasts, used clinicallyasiaticoside cream ointment, combined with FuYuan tablet (asiaticoside)treating hypertrophic scars. Triamcinolone acetonide is a treatment for scarefficacy of steroid hormones, can effectively inhibit the scar collagensynthesis, increase the activity of collagenase and promote collagen breakdown, commonly used in the local injection of the treatment of hypertr-ophic scars. Vitamin E is often used to moisture and protect dr-y,delicate skinof scar. But,clothing friction will cause the loss of cream drugs, and oralmedications play a systemic role, the eff-ect of lowering long-term use ofhormone drugs can cause significant side effects, and local injection have asense of pain, compliance of patient poor. In order to bring its effect into fullplay, reduce adverse effect, prolong its effect time, the study develop cross-linking gel paste of combining with asiaticoside, triamcinolone acetonideand vitamin E. The research of prescription process scr-eening, qualitystandards, pharmacodynamics and acute toxicity and irritation studies weresupplied for clinical safe and effective treatment of hypertrophic scarsproducts.With selection of the gel cream matrix material, ultimately choosingpartially neutralized sodium polyacrylate NP700as the gel ointments matrixskeleton material, aluminum glycinate as cross linker, PVP-K90and CMC-Naas a tackifier, glycerol humectants and kaolin as filler.The single factor test and orthogonal test were used to design formulationswith tacking strength and holding strength as indi cators and investigate thedosage level of sodium polyacrylate NP700(A), the Gan hydroxyl aluminum(B), CMC-Na (C) and the glycerin (D) which have gel paste matrix propertiesaffect, orthogonal design method was used to optimize the amount of thesefour factors, to arrange four factors and three levels of L9(34) test, the finaloptimization get the NP700: Gan hydroxyl Aluminum: CMC-Na: glycerol=4.0:0.4:1.0:40. Optimized formulation was prepared matrix uniformappearance, soft and moderate skin conformability, good patching.A modified Franz diffusion cell device and mouse skin in vitro astransdermal barrier were used to study the effect of1%azone,0.5%menthol,1%1,2-di-hydroxypropane and1%azone combine with1%1,2-di-hydrox- ypropane on the in vitro percutaneous permeability of the compound asiatico-side gel paste.The impact eventually filter out the1%azone combine with1%1,2-di-hydroxypropane as penetration enhancers of compound asiaticosidegel paste.The experiment studied the paste content, shaped, tacking strength andweight differences of compound asiaticoside gel paste,established the metho-ds determinnation of asiaticoside, made-cassoside and triamcinoloneacetonide, the results showed that the compound asiaticoside gel pastecomplies with the requirements of the pharmacopoeia.In this study, through mouse skin experiments in vitro and the scar invivo, studied the penetrating effect of triamcinolone acetonide andasiaticosides on gel paste and creams, the results showed that the amount ofdrug stranded per area in the gel paste is higher than cream.The experiment established rabbit ear hypertrophic scar model and usedContractubex and Asiaticosides cream as reference, studied scarmorphological changes in each groups through visual observa-tion, MDAdetermination,HE staining and VG staining.The results show that thecompound asiaticoside gel paste could make scar soft, the color fades, inhibitthe growth of scar, and its effect better than asiaticoside cream.The experiment used a method of self-control to investigate the skinirritation of compound asiaticoside gel paste for Japanese white rabbits, theresults show that the the compound asiaticoside gel paste have non-irritating tothe skin.This experiment used asiaticoside cream as a positive control, andinvestigated the acute toxicity test of high,medium and low three dose groupsin the compound asiaticoside gel paste for SD rats.The results showed that thecompound asiaticoside gel paste have high security and low toxicity, and aresafe to use in the usual dose. Conclusion: This study developed compound asiaticoside gel paste,prescription process is reasonably practicable, could use industrial production;preparations of established could control quality, meet the requirements of thepharmacopoeia; obviously inhibit the growth of scar, better than commerciallyasiaticoside cream; preparations are safe, stimulating small and have goodapplication prospects.
Keywords/Search Tags:asiaticoside, madecassoside, triamcinolone acetonide gelpaste, hypertrophic scars
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