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氟康唑口腔崩解片的制备及处方工艺对其性质的影响

Preparation of fluconazole buccal tablet and influence of formulation expedients on its properties.

作者信息

Mohamed Saifulla P, Muzzammil Shariff, Pramod Kumar T M

机构信息

Department of Pharmaceutics, College of Pharmacy, JSS University, Sri Shivarathreeshwara Nagar, Mysore-570 015, Karnataka, India.

出版信息

Yao Xue Xue Bao. 2011 Apr;46(4):460-5.

PMID:21748974
Abstract

The aim of present study was to prepare buccal tablets of fluconazole for oral candidiasis. The dosage forms were designed to release the drug above the minimum inhibitory concentration for prolonged period of time so as to reduce the frequency of administration and to overcome the side effects of systemic treatment. The buccal tablets were prepared by using Carbopol 71G and Noveon AA-1 by direct compression method. Microcrystalline cellulose was used as the filler and its effect was also studied. The prepared dosage forms were evaluated for physicochemical properties, in vitro release studies and mucoadhesive properties using sheep buccal mucosa as a model tissue. Tablets containing 50% of polymers (Carbopol & Noveon) were found to be the best with moderate swelling along with favorable bioadhesion force, residence time and in vitro drug release. The in vitro drug release studies revealed that drug released for 8 h, which in turn may reduce dosing frequency and improved patient compliance in oral candidiasis patients.

摘要

本研究的目的是制备用于治疗口腔念珠菌病的氟康唑口腔片。这些剂型的设计旨在使药物在最低抑菌浓度以上长时间释放,从而减少给药频率并克服全身治疗的副作用。采用卡波姆71G和诺维隆AA - 1通过直接压片法制备口腔片。微晶纤维素用作填充剂,并对其效果进行了研究。以绵羊颊黏膜为模型组织,对制备的剂型进行了理化性质、体外释放研究和黏膜粘附性质评价。发现含有50%聚合物(卡波姆和诺维隆)的片剂效果最佳,具有适度的溶胀以及良好的生物粘附力、滞留时间和体外药物释放性能。体外药物释放研究表明,药物释放长达8小时,这反过来可能会减少口腔念珠菌病患者的给药频率并提高患者依从性。

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