Gannu Ramesh, Palem Chinna Reddy, Rao Y Madhusudan
Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506 009 (A.P.), India.
PDA J Pharm Sci Technol. 2009 Sep-Oct;63(5):401-8.
The aim of the investigation was to develop and evaluate buccoadhesive tablets of diltiazem hydrochloride (DZH) using hydroxypropyl methyl cellulose (HPMC) K4M and Carbopol 934 as mucoadhesive polymers. Formulations A1, A2, A3, A4, and B1, B2, and B3, were composed of HPMC K4M and Carbopol 934 at ratios of 1:2, 1:3, 1:4, 1:5, and 1:1, 1:2, 1:3, respectively. The developed formulations were evaluated for physicochemical, in vitro drug release, in vitro adhesion and in vivo studies in healthy human volunteers. The buccal absorption study in healthy volunteers revealed that about 36.86% of the drug was absorbed. Formulation A3 showed maximum release in 8 h. As the concentration of polymer in the formulation increased, the drug release decreased. The bioavailability of diltiazem from buccoadhesive tablets was 1.57-fold higher than oral tablets. The basic pharmacokinetic parameters, C(Max), T(Max), and the area under the curve, were calculated and showed statistically significant difference (P < 0.05) when the drug was given by the buccal route compared to that of oral tablet. The results indicate that suitable bioadhesive buccal tablets with improved bioavailability could be prepared.
本研究的目的是使用羟丙基甲基纤维素（HPMC）K4M和卡波姆934作为粘膜粘附聚合物来研制和评估盐酸地尔硫卓（DZH）口腔粘附片。制剂A1、A2、A3、A4以及B1、B2和B3分别由比例为1:2、1:3、1:4、1:5以及1:1、1:2、1:3的HPMC K4M和卡波姆934组成。对所研制的制剂进行了理化性质、体外药物释放、体外粘附以及在健康人体志愿者中的体内研究评估。在健康志愿者中进行的口腔吸收研究显示，约36.86%的药物被吸收。制剂A3在8小时内显示出最大释放量。随着制剂中聚合物浓度的增加，药物释放量减少。地尔硫卓口腔粘附片的生物利用度比口服片高1.57倍。计算了基本药代动力学参数C（Max）、T（Max）以及曲线下面积，结果显示，与口服片相比，经口腔给药时这些参数具有统计学显著差异（P < 0.05）。结果表明，可以制备出具有改善生物利用度的合适的生物粘附口腔片。
