Bhoyar Pk, Amgaonkar Ym
Department of Pharmaceutics, S.K.B. College of Pharmacy, New Kamptee, Dist: Nagpur, Maharashtra, India.
J Young Pharm. 2011 Apr;3(2):112-8. doi: 10.4103/0975-1483.80294.
Metformin hydrochloride is an oral antidiabetic biguinide agent, used in the management of non-insulin-dependent (type-2) diabetes mellitus. The purpose of present work was to formulate tasteless complexes of metformin hydrochloride with indion 234 and to evaluate molecular properties of drug complexes. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug to resin, and temperature. Drug resin complexes (DRC) were evaluated for taste masking and characterized by x-ray diffraction study and infrared spectroscopy. Metformin hydrochloride release from DRC is obtained at salivary and gastric pH and in the presence of electrolytes. The efficient drug loading was evident in batch process using activated indion 234 with a pH of 3.5 and drug-resin ratio of 1:1.2, while temperature enhances the complexation process. Infrared spectroscopy revealed complexation of -NH (drug) with indion 234. DRC are amorphous in nature. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Volunteers rated the complex as tasteless and agreeable. Complete drug release was observed at gastric pH in 3 h. The drug release was accelerated in the presence of electrolytes. Indion 234 is inexpensive, and the simple technique is effective for bitterness masking of metformin.
盐酸二甲双胍是一种口服抗糖尿病双胍类药物，用于治疗非胰岛素依赖型（2型）糖尿病。本研究的目的是制备盐酸二甲双胍与离子交换树脂Indion 234的无味复合物，并评估药物复合物的分子性质。对离子交换树脂上的药物负载进行了优化，考察了混合时间、活化、pH值影响、混合方式、药物与树脂比例以及温度等因素。对药物树脂复合物（DRC）进行了掩味评价，并通过X射线衍射研究和红外光谱进行了表征。在唾液和胃液pH值以及存在电解质的情况下，测定了DRC中盐酸二甲双胍的释放情况。在使用pH值为3.5的活化Indion 234且药物与树脂比例为1:1.2的分批过程中，有效药物负载明显，而温度可促进络合过程。红外光谱显示药物的-NH与Indion 234发生了络合。DRC本质上是无定形的。DRC在唾液pH值下的药物释放不足以产生苦味。志愿者将该复合物评为无味且口感良好。在胃液pH值下3小时观察到药物完全释放。在电解质存在下药物释放加速。Indion 234价格低廉，该简单技术对盐酸二甲双胍的苦味掩蔽有效。
