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盐酸莫西沙星微水凝胶的制剂与评价

Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.

作者信息

Nanjwade Basavaraj K, Deshmukh Rucha V, Gaikwad Kishori R, Parikh Kemy A, Manvi F V

机构信息

Department of Pharmaceutics, KLE University College of Pharmacy, JN Medical College Campus, Belgaum, 590010, Karnataka, India.

出版信息

Eur J Drug Metab Pharmacokinet. 2012 Jun;37(2):117-23. doi: 10.1007/s13318-011-0070-9. Epub 2011 Oct 21.

Abstract

The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.

摘要

眼部药物递送领域是制药科学家面临的有趣且具有挑战性的工作之一。需要建立新的眼科药物递送方法,以克服传统剂型的固有缺点,从而提高眼部生物利用度。原位水凝胶以滴剂形式滴入眼内,并在盲管中发生溶胶-凝胶转变,通过增加与角膜组织的接触时间来提高眼部生物利用度,从而减少给药频率。本研究的目的是开发一种眼科药物递送系统,该系统使用三种具有不同原位凝胶化机制的胶凝剂来制备盐酸莫西沙星(一种氟喹诺酮类抗生素)的原位水凝胶。聚氧乙烯(一种pH敏感胶凝剂)、海藻酸钠(一种离子敏感胶凝剂)和泊洛沙姆(一种温度敏感胶凝剂)与羟丙甲纤维素K4M(作为增稠剂,可增加药物在眼腔内的停留时间)一起用于形成原位水凝胶。对有前景的制剂MF(4)、MF(5)和MF(9)进行了pH值、药物含量、体外凝胶化、体外药物释放、体内药物释放、眼部刺激性和稳定性评估。制剂MF(4)、MF(5)和MF(9)的药物含量百分比分别为98.2%、98.76%和99.43%;在20 rpm时的粘度分别为15.724×100、16.108×100和15.213×100 cP,累积释放百分比分别为75.364%、74.081%和71.752%,C(max)分别为1164.16、1187.09和1220.58 ng/ml。所开发的制剂具有治疗效果、稳定性且无刺激性,并能在8小时内持续释放药物。

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