Department of Pharmaceutics, Faculty of Pharmacy, El-Minia University, El-Minia Governate 61732, Egypt.
J Pharm Sci. 2010 Oct;99(10):4285-94. doi: 10.1002/jps.22153.
The objective of the present study was to evaluate the potential of ternary system (comprised of famotidine, beta-cyclodextrin (beta-CyD) or its derivatives and a hydrophilic polymer) as an approach for enhancing the aqueous solubility and masking the bitter taste of famotidine. The aqueous solubility of famotidine increased in the presence of beta-CyDs, particularly sulfobutyl ether beta-CyD (SBE-beta-CyD), and it was further enhanced by the combination of SBE-beta-CyD and polyvinyl pyrrolidone (Povidone) K30. The solid binary (drug-beta-CyDs) and ternary (drug-beta-CyDs-Povidone K30) systems were prepared by the kneading and freeze-drying methods. The dissolution rates of these solid systems were much faster than that of the drug alone. A taste perception study was carried out, initially using a taste sensory machine and subsequently on human volunteers to evaluate the taste masking ability of the ternary complexation. Our results indicated that the combination of SBE-beta-CyD and Povidone K30 is effective not only in the enhancement of the solubility and dissolution rate of famotidine, but also in masking of the bitter taste of the drug. This technique may be of value for the pharmaceutical industries, especially in preparation of rapidly disintegrating tablets dealing with bitter drugs to improve patient compliance and thus effective pharmacotherapy.
本研究的目的是评估三元体系（由法莫替丁、β-环糊精（β-CyD）或其衍生物和亲水性聚合物组成）作为一种提高法莫替丁水溶性和掩盖其苦味的方法的潜力。β-CyD 的存在可增加法莫替丁的水溶性，特别是磺丁基醚-β-环糊精（SBE-β-CyD），并且 SBE-β-CyD 与聚乙烯吡咯烷酮（Povidone）K30 的组合可进一步增强其水溶性。通过捏合和冷冻干燥方法制备了固体二元（药物-β-CyD）和三元（药物-β-CyD-Povidone K30）系统。这些固体系统的溶解速率比单独的药物快得多。进行了味觉感知研究，最初使用味觉感知机，然后在人体志愿者上进行，以评估三元络合的掩味能力。我们的结果表明，SBE-β-CyD 和 Povidone K30 的组合不仅有效提高了法莫替丁的溶解度和溶解速率，而且掩盖了药物的苦味。该技术可能对制药行业具有价值，特别是在制备用于改善患者顺应性和有效药物治疗的快速崩解片时，处理苦味药物。
