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经鼻腔给予昂丹司琼的新型微球传递系统给药:离体和在体研究。

Nasal administration of ondansetron using a novel microspheres delivery system Part II: ex vivo and in vivo studies.

机构信息

Department of Pharmaceutics, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, India.

出版信息

Pharm Dev Technol. 2010 Dec;15(6):653-7. doi: 10.3109/10837450903479970. Epub 2009 Dec 18.

Abstract

Gellan gum-based mucoadhesive microspheres of ondansetron hydrochloride for intranasal systemic delivery were prepared to avoid first pass effect, an alternative route of administration to injection and to enhance systemic bioavailability of ondansetron hydrochloride. The microspheres were prepared using spray method. The evaluation results of microspheres were reported in our previous study. The aim of this work was to study the in vivo performance of mucoadhesive microspheres in comparison with oral and intravenous preparations of ondansetron hydrochloride. The nasal delivery system gave increased AUC(0-240) and C(max) as compared to those of oral delivery. In conclusion, the gellan gum-based microsphere formulation of ondansetron hydrochloride with mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption.

摘要

盐酸昂丹司琼的基于胶凝多糖的粘膜粘附微球用于经鼻全身递药,以避免首过效应,提供一种替代注射的给药途径,并提高盐酸昂丹司琼的全身生物利用度。微球是通过喷雾方法制备的。微球的评价结果在我们之前的研究中已有报道。本工作的目的是研究与盐酸昂丹司琼的口服和静脉制剂相比,粘膜粘附微球的体内性能。与口服制剂相比,鼻腔给药剂型使 AUC(0-240)和 C(max)增加。总之,具有增加的渗透速率的胶凝多糖基盐酸昂丹司琼微球制剂具有粘膜粘附特性,有望延长鼻内停留时间,从而增加鼻内吸收。

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