降压尼索地平缓释片的处方、研制与优化

K. Kumar, K. Sunand, N. Mounika, M. Samad, A. M. Babu, K. M. Chinnala
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引用次数: 0

摘要

药物分子必须是水溶性的,才能轻易地传递到细胞膜上。许多药物是不溶于水的,这在剂型的开发中造成了许多问题。控制给药配方以控制动力学释放药物数天或数月,减少给药频率,最大限度地减少副作用,提高患者依从性。尼索地平是一种钙通道拮抗剂,用于治疗水溶性非常差的高血压。因此,有必要提高药物释放率。因此,本研究对尼索地平缓释片配方进行设计、配制和评价。采用滚压法制备尼索地平控释基质片。制剂前研究证实了药物与制剂中所用辅料的纯度和相容性。预压缩研究证实了配方共混物的压缩稳定性。对所有制备的制剂进行了各种物理和压缩参数的评估,如体积和密度、硬度、脆性和体外药物释放研究。制备的压缩尼索地平缓释片的释药结果均在预期范围内。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation, Development, and Optimization of Anti- Hypertensive Nisoldipine Extended-Release Tablet Formulation
A drug molecule has to be water-soluble to be readily delivered to the cellular membrane. Many drugs are waterinsoluble, which creates numerous problems in the development of dosage forms. Controlled drug delivery formulation releases the drug with controlled kinetics for days and months, reducing the frequency of dosing, minimizing side effects, and improving patient compliance. Nisoldipine is a calcium channel antagonist that is indicated for the treatment of hypertension with very poor aqueous solubility. Thus, there is a need to improve the rate of drug release. Hence, the study was carried out to design, formulate and evaluate sustained-release tablet formulation of nisoldipine. Nisoldipine controlled release matrix tablets were prepared by roll compaction method. Preformulation studies have confirmed the purity and compatibility of drug with excipients used in the formulation. Pre-compression studies have confirmed the stability of formulation blends for compression. All the prepared formulations were evaluated for various physical and compression parameters such as bulk and tapped density, hardness, friability, and in vitro drug release studies. The results of drug release from prepared compressed nisoldipine extended-release tablets were found to be within the desired range.
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