Razzaq Sobia, Hanif Sana, Syed Muhammad Ali, Iqbal Javed, Hassan Syed Saeedul, Raza Syed Atif, Riaz Humayun, Abid Farah
Department of Pharmacy, The University of Lahore, Lahore, Pakistan.
University College of Pharmacy, University of The Punjab, Lahore, Pakistan.
Pak J Pharm Sci. 2018 Sep;31(5):1903-1910.
The current study was designed to evaluate mucoadhesive buccal tablet containing metronidazole (MTZ) for local action aided by Hydroxypropylmethylcellulose K4M (HPMC) and Carbopol 940® (CP) as mucoadhesive polymers with other ingredients like sodium starch glycolate (SSG), polyvinyl pyrollidone K30 (PVP) as disintegrant and binders respectively. Formulations (F1-F8) were prepared by direct compression method and characterized for different physicochemical parameters. Results showed that the average weight and friability were within USP limits. Maximum mucoadhesive time was observed for F2 (14 hr) containing moderate amount of HPMC and CP used in the study. Up most mucoadhesive strength value was observed with F3 containing highest amount of HPMC used. Results indicated that high amount of HPMC was linked with the moderate to higher mucoadhesive strength and time. Maximum swelling index was observed in F7 (191.3%). Only F1-F3 showed complete in vitro MTZ release within 3 hr. Formulations containing PVP released MTZ incompletely over time while SSG released earlier. Formulation F1 was considered best in terms of MTZ release (100.5%) with diffusion based Korsmeyer-Peppas release kinetics. Therefore, MTZ exhibiting best physicochemical characters in mucoadhesive buccal tablet was found in F1 containing HPMC and CP in amounts of 37.5 mg and 25 mg, respectively, for local action.
本研究旨在评估含甲硝唑(MTZ)的粘膜粘附口腔片,该片剂借助羟丙基甲基纤维素K4M(HPMC)和卡波姆940®(CP)作为粘膜粘附聚合物,并添加其他成分,如分别用作崩解剂和粘合剂的淀粉乙醇酸钠(SSG)、聚乙烯吡咯烷酮K30(PVP)。采用直接压片法制备了制剂(F1 - F8),并对其不同的理化参数进行了表征。结果表明,平均重量和脆碎度均在USP规定的限度内。在本研究中,含适量HPMC和CP的F2制剂的粘膜粘附时间最长(14小时)。含最高量HPMC的F3制剂的粘膜粘附强度值最高。结果表明,高含量的HPMC与中等至高的粘膜粘附强度和时间相关。F7制剂的溶胀指数最高(191.3%)。只有F1 - F3在3小时内显示出MTZ的完全体外释放。含PVP的制剂随时间推移MTZ释放不完全,而SSG释放较早。就MTZ释放而言(100.5%),基于扩散的Korsmeyer - Peppas释放动力学表明F1制剂最佳。因此,对于局部作用,在分别含有37.5 mg和25 mg HPMC和CP的F1粘膜粘附口腔片中发现MTZ具有最佳的理化特性。