Noor Rabia, Hasan S M Farid, Hassan Fouzia, Rehman Attique
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi, Pakistan.
Merck Pharmaceutical Industry (Pvt.) Ltd., S.I.T.E., Karachi, Pakistan.
Pak J Pharm Sci. 2017 Mar;30(2):407-414.
Meloxicam is a poor water soluble drug mostly prescribed in various rheumatic diseases. The present research study was design to formulate and increase the solubility of meloxicam in the tablet dosage form. A 3 full factorial design was employed to optimize meloxicam formulations. Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCL-PVA-PEG graft copolymer) and Povidone were taken as independent variables while cumulative drug release at 90 minutes was selected as dependent variable. All trial formulations complied with official standards. Multiple regression by Microsoft Excel on cumulative drug release of the selected formulations (F1, F2, F6- F9) showed the positive effect of PVCL-PVA-PEG graft copolymer (α = 0.05) and a negative effect of Povidone (α = 0.05). Formulation six (F6) (PVCL-PVA-PEG graft copolymer 3 mg and Povidone 22.5 mg / tablet) was considered as the optimal formulation based on its cumulative drug release. Dissolution kinetics by model dependent analysis predicted Weibull (R=0.99) as the best fit model in describing meloxicam dissolution kinetics. The role of PVCL-PVA-PEG graft copolymer should be explored with other solubilizers in future studies.
美洛昔康是一种水溶性较差的药物，主要用于治疗各种风湿性疾病。本研究旨在制备美洛昔康片剂并提高其溶解度。采用三因素全因子设计优化美洛昔康制剂。以聚乙烯己内酰胺-聚醋酸乙烯酯-聚乙二醇接枝共聚物（PVCL-PVA-PEG接枝共聚物）和聚维酮作为自变量，选取90分钟时的药物累积释放量作为因变量。所有试验制剂均符合官方标准。通过Microsoft Excel对所选制剂（F1、F2、F6 - F9）的药物累积释放量进行多元回归分析，结果显示PVCL-PVA-PEG接枝共聚物具有正向作用（α = 0.05），聚维酮具有负向作用（α = 0.05）。基于其药物累积释放量，制剂六（F6）（PVCL-PVA-PEG接枝共聚物3 mg，聚维酮22.5 mg/片）被认为是最佳制剂。通过模型依赖性分析的溶出动力学预测，威布尔模型（R = 0.99）是描述美洛昔康溶出动力学的最佳拟合模型。未来研究中应与其他增溶剂一起探索PVCL-PVA-PEG接枝共聚物的作用。
