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奈韦拉平自乳化药物递送系统的处方设计、优化及评价

Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine.

作者信息

Chintalapudi Ramprasad, Murthy T E G K, Lakshmi K Rajya, Manohar G Ganesh

机构信息

Department of Pharmaceutics, Bapatla College of Pharmacy, Bapatla, Guntur, Andhra Pradesh, India.

Department of Pharmaceutical Analysis, Nirmala College of Pharmacy, Mangalagiri, Guntur, Andhra Pradesh, India.

出版信息

Int J Pharm Investig. 2015 Oct-Dec;5(4):205-13. doi: 10.4103/2230-973X.167676.

DOI:10.4103/2230-973X.167676
PMID:26682191
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4675002/
Abstract

BACKGROUND

The aim of the present study was to formulate and optimize the self-emulsifying drug delivery systems (SEDDS) of nevirapine (NVP) by use of 2(2) factorial designs to enhance the oral absorption of NVP by improving its solubility, dissolution rate, and diffusion profile. SEDDS are the isotropic mixtures of oil, surfactant, co-surfactant and drug that form oil in water microemulsion when introduced into the aqueous phase under gentle agitation.

MATERIALS AND METHODS

Solubility of NVP in different oils, surfactants, and co-surfactants was determined for the screening of excipients. Pseudo-ternary phase diagrams were constructed by the aqueous titration method, and formulations were developed based on the optimum excipient combinations with the help of data obtained through the maximum micro emulsion region containing combinations of oil, surfactant, and co-surfactant. The formulations of SEDDS were optimized by 2(2) factorial designs.

RESULTS

The optimum formulation of SEDDS contains 32.5% oleic acid, 44.16% tween 20, and 11.9% polyethylene glycol 600 as oil, surfactant, and co-surfactant respectively. The SEDDS was evaluated for the following drug content, self-emulsification time, rheological properties, zeta potential, in vitro diffusion studies, thermodynamic stability studies, and in vitro dissolution studies. An increase in dissolution was achieved by SEDDS compared to pure form of NVP.

CONCLUSION

Overall, this study suggests that the dissolution and oral bioavailability of NVP could be improved by SEDDS technology.

摘要

背景

本研究的目的是通过使用二因素析因设计来制备和优化奈韦拉平（NVP）的自乳化药物递送系统（SEDDS），通过改善其溶解度、溶解速率和扩散特性来提高NVP的口服吸收。SEDDS是油、表面活性剂、助表面活性剂和药物的各向同性混合物，在温和搅拌下引入水相时会形成水包油微乳液。

材料与方法

测定NVP在不同油、表面活性剂和助表面活性剂中的溶解度以筛选辅料。采用水相滴定法构建伪三元相图，并借助通过包含油、表面活性剂和助表面活性剂组合的最大微乳液区域获得的数据，基于最佳辅料组合开发制剂。通过二因素析因设计对SEDDS制剂进行优化。

结果

SEDDS的最佳制剂分别含有32.5%的油酸、44.16%的吐温20和11.9%的聚乙二醇600作为油、表面活性剂和助表面活性剂。对SEDDS进行了以下药物含量、自乳化时间、流变学性质、ζ电位、体外扩散研究、热力学稳定性研究和体外溶出度研究。与纯形式的NVP相比，SEDDS实现了溶出度的增加。

结论

总体而言，本研究表明SEDDS技术可提高NVP的溶出度和口服生物利用度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b025/4675002/b983c8f49d8e/IJPI-5-205-g025.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b025/4675002/6a1b41fffcce/IJPI-5-205-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b025/4675002/e9c1e861e3ad/IJPI-5-205-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b025/4675002/fc729422d342/IJPI-5-205-g014.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b025/4675002/cfce47c67f2d/IJPI-5-205-g015.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b025/4675002/99e46759a1a1/IJPI-5-205-g017.jpg
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