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托吡酯经皮给药制剂的研制与评价

Formulation and evaluation of transdermal drug delivery of topiramate.

作者信息

Cherukuri Suneetha, Batchu Uma Rajeswari, Mandava Kiranmai, Cherukuri Vidhyullatha, Ganapuram Koteswara Rao

机构信息

Department of Pharmaceutics, Bomma Institute of Pharmacy, Khammam, Telangana, India.

Department of Pharmaceutical Chemistry, Bharat Institute of Technology, JNTUH, Hyderabad, India.

出版信息

Int J Pharm Investig. 2017 Jan-Mar;7(1):10-17. doi: 10.4103/jphi.JPHI_35_16.

DOI:10.4103/jphi.JPHI_35_16
PMID:28405574
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5370344/
Abstract

BACKGROUND

Transdermal drug delivery system (TDDS) was designed to sustain the release and improve the bioavailability of drug and patient compliance. Among the various types of transdermal patches, matrix dispersion type systems disperse the drug in the solvent along with the polymers and solvent is allowed to evaporate forming a homogeneous drug-polymer matrix. The objective of the present study was to design and formulate TDDS of topiramate (TPM) and to evaluate their extended release and .

MATERIALS AND METHODS

In the present study, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising TPM with different ratios of hydrophilic and hydrophobic polymeric combinations using solvent casting technique.

RESULTS

The physicochemical compatibility of the drug and the polymers was studied by Fourier transform infrared spectroscopy. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. The patches were further subjected to various physical evaluations along with the permeation studies using pig ear skin.

CONCLUSIONS

On the basis of results obtained from the physical evaluation and studies the patches containing the polymers, that is, Eudragit L 100 and polyvinylpyrrolidone, with oleic acid as the penetration enhancer were considered as the best formulations for the transdermal delivery of TPM.

摘要

背景

经皮给药系统（TDDS）旨在实现药物的持续释放，提高药物的生物利用度以及患者的顺应性。在各类透皮贴剂中，基质分散型系统将药物与聚合物一同分散于溶剂中，随后使溶剂蒸发，形成均匀的药物 - 聚合物基质。本研究的目的是设计并制备托吡酯（TPM）的经皮给药系统，并评估其缓释性能。

材料与方法

在本研究中，尝试采用溶剂浇铸技术开发一种包含TPM的基质型透皮治疗系统，该系统采用不同比例的亲水和疏水聚合物组合。

结果

通过傅里叶变换红外光谱研究了药物与聚合物的物理化学相容性。所得结果表明药物与聚合物之间不存在物理化学不相容性。这些贴剂进一步进行了各种物理评价，并使用猪耳皮肤进行了渗透研究。

结论

基于物理评价和研究结果，含有聚合物（即Eudragit L 100和聚乙烯吡咯烷酮）且以油酸作为渗透促进剂的贴剂被认为是TPM经皮给药的最佳制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/a06320d75c0e/IJPI-7-10-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/97c15be70394/IJPI-7-10-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/c4f1d0f32996/IJPI-7-10-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/1849f76896f3/IJPI-7-10-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/d7406e9f41f1/IJPI-7-10-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/99666917b9e3/IJPI-7-10-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/2226af01067a/IJPI-7-10-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/a06320d75c0e/IJPI-7-10-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/97c15be70394/IJPI-7-10-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/c4f1d0f32996/IJPI-7-10-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/1849f76896f3/IJPI-7-10-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/d7406e9f41f1/IJPI-7-10-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/99666917b9e3/IJPI-7-10-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/2226af01067a/IJPI-7-10-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0004/5370344/a06320d75c0e/IJPI-7-10-g012.jpg

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