本文關(guān)鍵詞：甲磺酸達比加群酯膠囊處方篩選　出處：《北京理工大學(xué)》2015年碩士論文　論文類型：學(xué)位論文

  更多相關(guān)文章： 甲磺酸達比加群酯 膠囊 處方

【摘要】：甲磺酸達比加群酯是國內(nèi)未上市的新藥,在臨床上具有廣泛的用途,目前用于膝關(guān)節(jié)置換術(shù)或髖關(guān)節(jié)置換手術(shù)的靜脈血栓預(yù)防。然而,達比加群酯膠囊的制劑處方為丸芯比較特殊的酒石酸的多顆粒制劑,且輔料酒石酸對原料的穩(wěn)定性有較大的影響,但因在體內(nèi)形成酸性環(huán)境,該輔料的使用是有必要的,需要采用多顆粒技術(shù)將酒石酸與原料通過隔離層的包裹分離開,制備難度較大。本文通過對國外專利處方工藝分析及對原研產(chǎn)品的檢驗和剖析,建立了以酒石酸、阿拉伯膠、羥丙甲纖維素、羥丙纖維素(SSL)、滑石粉(1250目),羥丙甲纖維素膠囊殼等為輔料,乙醇(95%)和異丙醇為溶劑,采用離心造粒機,粉末層積法制備酒石酸丸芯,用流化床包隔離層,最后用流化床上載甲磺酸達比加群酯的制粒工藝,制備了符合質(zhì)量要求的甲磺酸達比加群酯膠囊,批量為3萬。與原研產(chǎn)品對比測定結(jié)果表明,試制品在四種介質(zhì)中的溶出曲線與原研制劑相似,干燥失重及膠囊殼干燥失重等質(zhì)量指標與原研產(chǎn)品接近,體外溶出行為、雜質(zhì)譜與原研一致。符合國家藥品審評中心的對甲磺酸達比加群酯膠囊的品質(zhì)要求。
[Abstract]:Dabigatran etexilate mesylate is not listed on the domestic drug, is widely used in clinic, currently used for venous thrombosis of knee arthroplasty or hip replacement surgery and prevention. However, dabigatran capsule prescription for special pill core tartaric acid multi particle preparation, stability and accessories tartaric acid for raw materials have great influence, but due to the formation of acidic environment in the body, the use of the materials is necessary, need to adopt the multi particle technology will tartaric acid and raw material through the isolation layer package from preparation difficult. Based on the analysis of patent prescription abroad and in the inspection and analysis of the original research products, established by Arabia gum, tartaric acid, hydroxypropyl methyl cellulose, hydroxypropyl cellulose (SSL), talcum powder (1250 mesh), hypromellose capsule shell and other accessories (95%), ethanol and isopropanol as solvent, made by centrifugal Machine, powder laminated preparation of tartaric acid pellets, using fluidized bed granulation process package isolation layer, finally by fluidized bed on dabigatran etexilate mesylate and preparation to meet the quality requirements of dabigatran etexilate mesylate capsules, batch is 30 thousand. And the original product comparison test results show that the prototype in four a medium dissolution curve and the original formulation is similar to that of dry weight and dry weight loss capsule shell quality indicators and the original product close to the in vitro dissolution behavior, consistent with the original research. The impurity profiling conforms to the National Center for drug evaluation of dabigatran mesylate group quality ester capsule requirements.

【學(xué)位授予單位】：北京理工大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2015
【分類號】：R927.1

【參考文獻】

相關(guān)期刊論文 前1條

1 孫藝紅,胡大一;華法林對中國人心房顫動患者抗栓的安全性和有效性研究[J];中華內(nèi)科雜志;2004年04期

，

本文編號：1365984