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Phospholipid-bile salts-mixed micelles incorporated in oral ...

Phospholipid-bile salts-mixed micelles incorporated in oral fast dissolving films for improving the oral bioavailability of poorly water soluble drugs

作     者:Qingyuan Lv Minggui Lin Chao Yu Baode Shen He Xu Chengying Shen Ling Dai Hailong Yuan Jin Han 

作者单位:Department of Pharmacy302 Military Hospital Institute of Tuberculosis309 Military Hospital 

会议名称:《“好医生杯”中药制剂创新与发展论坛》

会议日期:2013年

学科分类:1006[医学-中西医结合] 10[医学] 100602[医学-中西医结合临床] 

基  金:supported by the National Key New Drugs Innovation Foundation(No.2013ZX09J13109-06C) the Natural Science Found of Beijing city of China(No.7122176) the Scientific Research Foundation for the Returned Overseas Chinese Scholars,State Education Ministry(No.20101561) 

关 键 词:Cucurbitacin B phospholipid-bile salts-mixed micelles fast dissolving oral films oral bioavailability poorly water soluble drugs 

摘      要:The phospholipid-bile salts-mixed micelles(PL-BS-MMs)are potent carriers used for oral absorption of drugs that are poorly soluble in water;however,there are many limitations associated with liquid formulations.In the current study,the feasibility of preparing a solid PL-BS-MMs by incorporating liquid PL/SDC-MMs with solid fast dissolving oral films(FDOFs)carriers was examined.FDOFs incorporated with Cucurbitacin B(Cu B)loaded PL-BS-MMs have been developed and characterised.FDOFs were produced by solvent casting method.The formulation presenting the best characteristics before solidifying and after reconstitution.FDOFs containing Cu B loaded PL/SDC-MMs was easily reconstituted in a transparent and clear solution giving back a colloidal system with spherical micelles in the submicron range.The pharmacokinetics study showed that the FDOFs containing PL/SDC-MMs not only kept the absorption properties as same as liquid PL/SDC-MMs,but also significantly increased the oral bioavailability of Cu B compared to the Cu B solution(p0.05).This study showed that the solid PL/SDC-MMs based on FDOFs could represent a novel platform for the delivery of poorly water soluble drugs via oral administration.Furthermore,the integration with the FDOFs could also provide a simple and cost-effective manner for the solidification of PL/SDC-MMs.

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