In Vitro Evaluation of Mucoadhesive Vaginal Tablets of Antifungal Drugs Prepared with Thiolated Polymer and Development of a New Dissolution Technique for Vaginal Formulations

スポンサーリンク

概要

• 論文の詳細を見る

• The main objective of this work was to develop antifungal matrix tablet for vaginal applications using mucoadhesive thiolated polymer. Econazole nitrate (EN) and miconazole nitrate (MN) were used as antifungal drugs to prepare the vaginal tablet formulations. Thiolated poly(acrylic acid)–cysteine (PAA-Cys) conjugate was synthesized by the covalent attachment of L-cysteine to PAA with the formation of amide bonds between the primary amino group of L-cysteine and the carboxylic acid group of the polymer. Vaginal mucoadhesive matrix tablets were prepared by direct compression technique. The investigation focused on the influence of modified polymer on water uptake behavior, mucoadhesive property and release rate of drug. Thiolated polymer increased the water uptake ratio and mucoadhesive property of the formulations. A new simple dissolution technique was developed to simulate the vaginal environment for the evaluation of release behavior of vaginal tablets. In this technique, daily production amount and rate of the vaginal fluid was used without any rotational movement. The drug release was found to be slower from PAA-Cys compared to that from PAA formulations. The similarity study results confirmed that the difference in particle size of EN and MN did not affect their release profile. The release process was described by plotting the fraction released drug versus time and n fitting data to the simple exponential model: Mt/M∞=ktn. The release kinetics were determined as Super Case II for all the formulations prepared with PAA or PAA-Cys. According to these results the mucoadhesive vaginal tablet formulations prepared with PAA-Cys represent good example for delivery systems which prolong the residence time of drugs at the vaginal mucosal surface.

著者

• Metin Dilek

  Department Of Microbiology And Clinical Microbiology Ege University Medical Faculty

• Hilmioglu Polat

  Department of Microbiology and Clinical Microbiology, Faculty of Medicine, Ege University

• Vetter Anja

  Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck

• Bernkop-Schnurch Andreas

  Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck

• Ay Senyıgıt

  Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University

• Baloglu Esra

  Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University

• Karavana Sinem

  Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University

• Guneri Tamer

  Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University

関連論文

• The efficacy of two different lipid-based amphotericin B in neonatal Candida septicemia
• In Vitro Evaluation of Mucoadhesive Vaginal Tablets of Antifungal Drugs Prepared with Thiolated Polymer and Development of a New Dissolution Technique for Vaginal Formulations

スポンサーリンク