Suppr超能文献

使用药物黏附透皮贴剂实现吡格列酮的有效治疗递送及生物利用度提高

Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch.

作者信息

Nair Anroop B, Gupta Sumeet, Al-Dhubiab Bandar E, Jacob Shery, Shinu Pottathil, Shah Jigar, Morsy Mohamed Aly, SreeHarsha Nagaraja, Attimarad Mahesh, Venugopala Katharigatta N, Akrawi Sabah H

机构信息

Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.

Department of Pharmacology, M. M. College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana 133203, India.

出版信息

Pharmaceutics. 2019 Jul 23;11(7):359. doi: 10.3390/pharmaceutics11070359.

Abstract

The administration of pioglitazone as an oral therapy is restricted due to various challenges. The aim of the current investigation was to evaluate the suitability of pioglitazone in adhesive transdermal patch as an alternative delivery system, in order to improve therapeutic delivery. Drug in adhesive pioglitazone (2% /) transdermal patch were optimized for drug release, suitable adhesive, and skin permeation enhancer. The selected patch was examined for drug-loading capacity and the patch with greater pioglitazone (6% /) was evaluated in rat models. The release of pioglitazone was influenced by the tested adhesive and was shown to be significantly higher ( < 0.001) with patch, prepared using Duro-Tak 87-2516. The ex vivo permeation results substantiate the release data as a greater transdermal flux (15.67 ± 2.35 µg/cm/h) was demonstrated in patch fabricated with Duro-Tak 87-2516. Skin penetration enhancers promoted the ex vivo transdermal delivery of pioglitazone, and was ~2 folds ( < 0.0001) higher with propylene glycol, as compared to patch without enhancer. The maximum solubility of pioglitazone in Duro-Tak 87-2516 was found to be 6% /. Increasing the drug content in patch enhanced the transdermal flux and was highest when the pioglitazone level was 6% / (72.68 ± 5.76 µg/cm/h). In vivo pharmacokinetic data demonstrate that the AUC in transdermal application (13,506.51 ± 1649.92 ng·h/mL) was ~2 times higher ( < 0.0001) as compared to oral dosage form. In conclusion, the promising results observed here signifies that developed patch could be a viable alternative for oral therapy of pioglitazone.

摘要

由于各种挑战,吡格列酮口服治疗的应用受到限制。当前研究的目的是评估吡格列酮在黏附性透皮贴剂中作为一种替代给药系统的适用性,以改善治疗药物递送。对黏附性吡格列酮(2%/)透皮贴剂中的药物进行了药物释放、合适的黏合剂和皮肤渗透促进剂方面的优化。对所选贴剂的载药量进行了检测,并在大鼠模型中对含更高吡格列酮(6%/)的贴剂进行了评估。吡格列酮的释放受所测试黏合剂的影响,使用Duro-Tak 87-2516制备的贴剂显示其释放量显著更高(<0.001)。体外渗透结果证实了释放数据,因为在使用Duro-Tak 87-2516制备的贴剂中显示出更高的透皮通量(15.67±2.35μg/cm/h)。皮肤渗透促进剂促进了吡格列酮的体外透皮递送,与不含促进剂的贴剂相比,使用丙二醇时其透皮递送量高出约2倍(<0.0001)。发现吡格列酮在Duro-Tak 87-2516中的最大溶解度为6%/。增加贴剂中的药物含量可提高透皮通量,当吡格列酮水平为6%/时透皮通量最高(72.68±5.76μg/cm/h)。体内药代动力学数据表明,透皮给药的AUC(13506.51±1649.92 ng·h/mL)与口服剂型相比高出约2倍(<0.0001)。总之,此处观察到的有希望的结果表明,所开发的贴剂可能是吡格列酮口服治疗的一种可行替代方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a56/6681070/1548f1f84aac/pharmaceutics-11-00359-g001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验