固体分散和中药片剂法提高抗原虫剂溶解度,提高其溶出率

Dr. Sourabh Jain, Ms. Ragini Bundela, Dr. Karunakar Shukla, Limhan Sachin Sadu
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引用次数: 0

摘要

药物溶出度是水溶性差药物生物利用度的限速步骤,影响药物的体内吸收。本研究成功研制了基于固体分散体的阿托伐酮片剂给药体系,通过与PEG 4000形成固体分散体,改善了阿托伐酮的溶出特性。对于阿托伐醌制剂,选择F1,因为其在180 min内释放率约为46%。药物与其他赋形剂的FTIR光谱未显示任何相互作用,并且经稳定性研究选择的制剂是稳定的。体外溶出研究表明,与纯药物相比,阿托伐醌固体分散体的溶出率有相当大的提高。从FTIR光谱分析可知,固体分散体中阿托伐醌与PEG 4000之间没有明确的化学相互作用,没有观察到重要的新峰。阿托伐酮固体分散体片(F1)的前20 min释药率为30.33%,180 min释药率为46.45%。由此可见,溶剂蒸发技术可有效地在PEG-4000和PVP-K - 30亲水性聚合物中制备水溶性差的阿托伐酮固体分散体。因此,可以给出这样的陈述,即通过溶剂蒸发技术使用水溶性载体进行固体分散,可以明显提高水溶性差的阿托伐康的溶解速率和溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Solubility enhancement of antiprotozoal agent by solid dispersion and herbal tablet method to improve its rate of dissolution
Drug dissolution is the rate limiting step for bioavailability of poor aqueous soluble drug that consequently affects the in vivo drug absorption. In the present study solid dispersion based drug delivery system of Atovaquone were successfully developed in the form of tablets with improved dissolution characteristic by forming solid dispersion with PEG 4000. For the Atovaquone formulation, F1 was chosen as it has % drug release about 46 % in 180 min. FTIR spectra of drug with other excipients have not shown any interaction and also selected formulation was stable after stability studies. The in-vitro dissolution studies revealed a considerable boost in dissolution rate of Solid dispersions of Atovaquone in contrast to pure drug. From FTIR spectroscopy, it was concluded that there was no well-defined chemical interaction between Atovaquone and PEG 4000 in Solid dispersions, as no important new peaks could be observed. The Atovaquone solid dispersion based tablet (F1) showed 30.33% drug release within first 20 min. and 46.45% drug release within 180 min.Thus from studies, it could be concluded that solid dispersion of poor aqueous soluble Atovaquone by solvent evaporation technique were effectively formulate during PEG-4000 and PVP-K 30 hydrophilic polymers. Thus, the statement can be given that the rate of dissolution and solubility of poor aqueous soluble Atovaquon can be appreciably improved by solid dispersion by use of water soluble carriers by solvent evaporation technique.
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