提高卡维地洛的治疗效果:提高疗效的固体分散胶囊研究

Pavan Kumar, Subhash Pg, Hindustan Abdul Ahad, Pawan Dhamala, Suprith D
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摘要

本研究的主要目的是通过采用以β-环糊精为载体的固体分散技术来改善和评估卡维地洛的溶解速率。我们采用了三种不同的方法来制造含卡维地洛的固体分散体:揉捏法、物理混合法和溶剂蒸发法。这些方法以不同的药物-载体比例(1:1、1:2 和 1:3)加入了 β-环糊精。初始阶段包括制剂前评估,包括建立校准曲线、确定最大λ值、确定熔点、研究在不同溶剂中的溶解度,以及通过傅立叶变换红外分析评估卡维地洛与聚合物的相容性。随后的制剂后分析包括重量变化、卡维地洛含量、锁定长度、水分渗透、崩解时间、体内溶解和稳定性测试。制剂前测试的结果与既定参考一致。傅立叶变换红外分析表明,卡维地洛与载体之间没有相互作用。卡维地洛含量、重量变化和崩解时间测试均符合 IP 标准规定的允许限度。然而,由于卡维地洛的溶解度有限,溶解度不够。在体外溶解度曲线中,以β-环糊精为载体、卡维地洛与载体的比例为 1:3 的捏和法制备的 "KN3 "制剂显示出 94.671% 的良好释放度,优于其他制备方法。
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Advancing Carvedilol's Therapeutic Impact: A Study On Solid Dispersion Capsules for Improved Efficacy
This study aimed primarily to improve and evaluate the dissolution rate of Carvedilol by employing a solid dispersiontechnique with β-Cyclodextrin as the carrier. Three distinct methods were utilized to create Carvedilol-containing soliddispersions: The Kneading method, Physical mixture, and Solvent evaporation method. These methods incorporated β-Cyclodextrin at varying drug-carrier ratios (1:1, 1:2, and 1:3). The initial phase encompassed pre-formulation assessments, includingthe establishment of a calibration curve, determination of lambda maximum, melting point determination, investigation of solubilityin different solvents, and evaluation of Carvedilol-polymer compatibility through FTIR analysis. Subsequent post-formulationanalyses included tests for weight variation, Carvedilol content, lock length, moisture permeation, disintegration time, in-vitrodissolution, and stability. The results of the pre-formulation tests were consistent with established references. FTIR analysisrevealed no interactions between the Carvedilol and the carrier. Carvedilol content, weight variation, and disintegration time testsmet the permissible limits outlined in IP standards. Both lock length and moisture permeation tests conformed to the criteria.However, due to Carvedilol's limited solubility, dissolution was inadequate. Among the in-vitro dissolution profiles, the "KN3"formulation, prepared using the Kneading method with a 1:3 ratio of Carvedilol to Carrier, employing β-Cyclodextrin as thecarrier, exhibited superior discharge at 94.671%, outperforming other preparation methods.
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