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通过新型自纳米乳化粉末(SNEP)制剂增强利培酮的口服给药:体外和离体评估

Enhanced oral delivery of risperidone through a novel self-nanoemulsifying powder (SNEP) formulations: in-vitro and ex-vivo assessment.

作者信息

Bandi Srikanth, Sanka Krishna, Bakshi Vasudha

机构信息

a Department of Pharmaceutics, School of Pharmacy (Formerly Lalitha College of Pharmacy) , Anurag Group of Institutions , Hyderabad , Telangana , India.

出版信息

J Microencapsul. 2016 Sep;33(6):544-553. doi: 10.1080/02652048.2016.1223200. Epub 2016 Aug 28.

Abstract

CONTEXT

The oral delivery of risperidone encounters a number of problems, such as pH dependent solubility and low bioavailability, due to its lipophilicity and aqueous insolubility.

OBJECTIVE

To improve the solubility, dissolution and intestinal permeation thereby bioavailability of risperidone through a novel self-nanoemulsifying powder (SNEP) formulations.

MATERIALS AND METHODS

Oleic acid, Tween 20, PEG 600 and Aerosil 200 were chosen as oil, surfactant, co-surfactant and carrier, respectively from solubility and emulsification studies. Ternary phase diagram was constructed to determine emulsifying region.

RESULTS AND DISCUSSION

The Z-average and polydispersity Index of developed formulation was 83.1 nm and 0.306, respectively. Ex vivo permeation studies on isolated rat intestine indicated that the amount of risperidone permeated from SNEP formulation was increased around 4- and 1.8-fold than that of pure drug and marketed formulation, respectively.

CONCLUSION

This developed SNEP formulations can be regarded as novel and commercially feasible alternative to the current risperidone formulations.

摘要

背景

由于利培酮具有亲脂性且在水中不溶,其口服给药存在诸多问题,如pH依赖性溶解度和低生物利用度。

目的

通过新型自纳米乳化粉末(SNEP)制剂提高利培酮的溶解度、溶出度和肠道渗透性,从而提高其生物利用度。

材料与方法

通过溶解度和乳化研究,分别选择油酸、吐温20、聚乙二醇600和气相二氧化硅20(Aerosil 200)作为油相、表面活性剂、助表面活性剂和载体。构建三元相图以确定乳化区域。

结果与讨论

所开发制剂的Z-平均粒径和多分散指数分别为83.1nm和0.306。对离体大鼠肠道进行的体外渗透研究表明,利培酮从SNEP制剂中的渗透量分别比纯药物和市售制剂增加了约4倍和1.8倍。

结论

所开发的SNEP制剂可被视为当前利培酮制剂新颖且具有商业可行性的替代方案。

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