直接压片法制备格列美脲黏合剂及其体外评价

Anum Akram, A. Kiran, Saddiqa Naeem
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引用次数: 2

摘要

目的:研究含降糖药格列美脲黏附含片的处方及评价,以避免首次通过效应,提高其生物利用度,减少给药频率和剂量相关副作用。方法:采用直接加压法制备。测定片剂的重量变化、硬度、表面pH、药物含量均匀度、百分比溶胀指数、生物黏附强度、体外停留时间、体外药物溶出度、体外药物释放动力学、体外渗透及稳定性。结果:FTIR研究显示药物、聚合物和赋形剂之间没有相互作用的证据。制剂的表面pH值为6.80±0.02,生物黏附强度为36.3±0.04g,离体停留时间为325min,溶胀指数为289.8±0.52%。含4mg格列美脲的制剂在理想治疗浓度下具有6 h的缓释率(93.98±0.8%)。格列美脲通过羊颊膜的速率为3.56 mg,通量为0.27 mg / h -1 cm-2。体外释放动力学研究表明,各制剂均符合零级动力学,并遵循非菲克扩散机制。结论:最佳制剂符合各项评价参数,并能通过口腔黏膜渗透。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation of glimepiride mucoadhesive tablets by direct compression method and their in-vitro evaluation
Objectives: The present investigation is concerned with formulation and evaluation of mucoadhesive buccal tablets containing antidiabetic drug, glimepiride, to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. Methods: The tablets were prepared by direct compression method. The tablets were tested for weight variation, hardness, surface pH, drug content uniformity, percentage swelling index, bio adhesive strength, exvivo residence time in-vitro drug dissolution study, in-vitro drug release kinetic study, ex-vivo permeation study and stability study. Results: FTIR studies showed no evidence on interactions between drug, polymers, and excipients. The surface pH, bio adhesive strength, ex-vivo residence timeand swelling index of formulation was found to be 6.80±0.02, 36.3±0.04g, 325min and 289.8±0.52%, respectively. The formulation containing 4 mg of glimepiride exhibited 6 h sustained drug release i.e. 93.98±0.8% with desired therapeutic concentration. The drug permeation from the formulation was slow and steady and 3.56 mg of glimepiride could permeate through sheep buccal membrane with a flux of 0.27 mg hr-1 cm-2 . The in-vitro release kinetics studies reveal that all formulations fits well with zero order kinetics and followed non-Fickian diffusion mechanism. Conclusion: Hence, it was concluded that the best formulation was suitable for all the evaluation parameters and can be permeated through human buccal mucosa.
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