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双氯芬酸钠口腔黏附片的研制与评价

Formulation and evaluation of diclofenac sodium buccoadhesive discs.

作者信息

El-Samaligy M S, Yahia S A, Basalious E B

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Kasr El-aini Street, Cairo, Egypt.

出版信息

Int J Pharm. 2004 Nov 22;286(1-2):27-39. doi: 10.1016/j.ijpharm.2004.07.033.

DOI:10.1016/j.ijpharm.2004.07.033
PMID:15501000
Abstract

Twenty diclofenac sodium buccoadhesive discs containing Cp974p, polycarbophil, PEO, SCMC-medium viscosity (SCMC-MV), SCMC-ultrahigh viscosity (SCMC-UHV) or their combinations were prepared. These buccoadhesive discs were evaluated for release pattern, swelling capacity, surface pH, mucoadhesion performance, and in vitro permeation of diclofenac sodium through buccal membranes. In vivo testing of mucoadhesion time, strength of adhesion, irritation, bitterness due to drug swallowing and disc disintegration in the buccal cavity were also performed. Drug bioavailability of a selected diclofenac sodium buccoadhesive product was then compared with that of Voltarin 100 SR tablet. The percentage relative bioavailability of diclofenac sodium from the selected buccoadhesive disc 50 mg was found to be 141.31%.

摘要

制备了20个含Cp974p、聚卡波非、聚氧化乙烯、中粘度羧甲基纤维素钠(SCMC-MV)、超高粘度羧甲基纤维素钠(SCMC-UHV)或其组合的双氯芬酸钠口腔粘附片。对这些口腔粘附片进行了释放模式、溶胀能力、表面pH值、粘膜粘附性能以及双氯芬酸钠透过颊粘膜的体外渗透评估。还进行了粘膜粘附时间、粘附强度、刺激性、因药物吞咽引起的苦味以及口腔内片剂崩解的体内测试。然后将所选双氯芬酸钠口腔粘附产品的药物生物利用度与扶他林100 SR片进行比较。发现所选50 mg口腔粘附片中双氯芬酸钠的相对生物利用度百分比为141.31%。

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