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自微乳药物传递系统提高齐墩果酸口服生物利用度的设计与评价。

Self-microemulsifying drug delivery system for improved oral bioavailability of oleanolic acid: design and evaluation.

机构信息

Pharmacy Department, Shandong Provincial Qianfoshan Hospital, Shandong University, Jinan, People's Republic of China.

出版信息

Int J Nanomedicine. 2013;8:2917-26. doi: 10.2147/IJN.S47510. Epub 2013 Aug 8.

DOI:10.2147/IJN.S47510
PMID:23966781
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3743642/
Abstract

Oleanolic acid is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance the solubility and oral bioavailability of oleanolic acid. The formulation design was optimized by solubility assay, compatibility tests, and pseudoternary phase diagrams. The morphology, droplet size distribution, zeta potential, viscosity, electrical conductivity, and refractive index of a SMEDDS loaded with oleanolic acid were studied in detail. Compared with oleanolic acid solution, the in vitro release of oleanolic acid from SMEDDS showed that the drug could be released in a sustained manner. A highly selective and sensitive high-performance liquid chromatographymass spectrometry method was developed for determination of oleanolic acid in rat plasma. This method was used for a pharmacokinetic study of an oleanolic acid-loaded SMEDDS compared with the conventional tablet in rats. Promisingly, a 5.07-fold increase in oral bioavailability of oleanolic acid was achieved for the SMEDDS compared with the marketed product in tablet form. Our studies illustrate the potential use of a SMEDDS for delivery of oleanolic acid via the oral route.

摘要

齐墩果酸是一种水溶性差、口服生物利用度低的药物。已经开发出自微乳药物传递系统（SMEDDS）来提高齐墩果酸的溶解度和口服生物利用度。通过溶解度测定、相容性试验和伪三元相图优化了制剂设计。详细研究了载齐墩果酸的 SMEDDS 的形态、粒径分布、Zeta 电位、粘度、电导率和折射率。与齐墩果酸溶液相比，SMEDDS 中齐墩果酸的体外释放表明药物可以持续释放。建立了一种高选择性和高灵敏度的高效液相色谱-质谱法测定大鼠血浆中齐墩果酸的含量。该方法用于比较齐墩果酸载 SMEDDS 与大鼠普通片剂的药代动力学研究。令人鼓舞的是，与市售片剂相比，SMEDDS 使齐墩果酸的口服生物利用度提高了 5.07 倍。我们的研究说明了 SMEDDS 作为通过口服途径传递齐墩果酸的潜在用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/aac85a63df22/ijn-8-2917Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/d62b46653ab2/ijn-8-2917Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/9f21ffc97ca8/ijn-8-2917Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/08ef1c998003/ijn-8-2917Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/5f1485b7f4be/ijn-8-2917Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/ae943ccfe3b4/ijn-8-2917Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/fd3f763920fd/ijn-8-2917Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/aac85a63df22/ijn-8-2917Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/d62b46653ab2/ijn-8-2917Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/9f21ffc97ca8/ijn-8-2917Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/08ef1c998003/ijn-8-2917Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/5f1485b7f4be/ijn-8-2917Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/ae943ccfe3b4/ijn-8-2917Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/fd3f763920fd/ijn-8-2917Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6dbb/3743642/aac85a63df22/ijn-8-2917Fig7.jpg

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