Formulation and Development Matrix Tablets Of Methimazole

V. BhambarKunal
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Abstract

Methimazole is active pharmaceutical ingredient effectively utilized in hyperthyroidism. Methimazole inhibits peroxidase as well as iodine interactions with thyroglobulin to produce triiodothyronine with thyroxine. Methimazole shows very low protein binding (1-10%) bounds to plasma proteins and easily metabolized by liver. In this investigation, efforts given to develop a sustained release matrix tablet of Methimazole. Sustained release drug delivery systems are for a maximum of 24 hours clinical effectiveness. Such systems are primarily for the drugs of short elimination half-life. However, drugs with long half-life also qualify if a reduction in steady state fluctuation is desired. Matrix tablets of methimazole were prepared by utilizing direct compression method. HPMC along with Sodium carboxy methyl cellulose used to retard drug release from the dosage form. Matrix tablets of methimazole were evaluated for different quality control test to improve quality of the product. In vitro release study of methimazole matrix tablets shows that polymer percentage used in the formula is enough to extend the release of the drug for at least 12 hr. In dissolution study of matrix of methimazole formulation F2 shows maximum drug release 97.93 % at the end of 6 hours while F1 shows least 83.64 %. Keywords: Matrix tablet, Methimazole, Sustained Release
甲巯咪唑基质片的研制与处方研究
甲巯咪唑是治疗甲亢的有效药物成分。甲巯咪唑抑制过氧化物酶以及碘与甲状腺球蛋白的相互作用,与甲状腺素产生三碘甲状腺原氨酸。甲巯咪唑与血浆蛋白的结合率很低(1-10%),容易被肝脏代谢。本研究旨在研制甲巯咪唑缓释基质片。缓释给药系统具有最长24小时的临床有效性。这种系统主要用于消除半衰期短的药物。但是,如果希望减少稳态波动,半衰期长的药物也符合条件。采用直接压缩法制备甲巯咪唑基质片。HPMC与羧甲基纤维素钠一起用于延缓药物从剂型中的释放。为提高产品质量,对甲巯咪唑基质片进行了不同的质量控制试验。甲巯咪唑基质片的体外释放研究表明,配方中所使用的聚合物百分比足以延长药物释放至少12小时。在甲巯咪唑制剂基质溶出度研究中,F2在6 h时释放度最大,为97.93%,F1最小,为83.64%。关键词:基质片;甲巯咪唑;缓释
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