Exploring the potential of porous silicas as a carrier system for dissolution rate enhancement of artemether

作     者：Jaywant N.Pawar Harita R.Desai Kailas K.Moravkar Deepak K.Khanna Purnima D.Amin 

作者机构：Department of Pharmaceutical Sciences and TechnologyInstitute of Chemical Technology(Elite Status)N.P.MargMatunga(E)Mumbai 400019India Applied TechnologyInorganic MaterialsEvonik Degussa India Pvt.Ltd.Krislon HouseSakivihar RoadSakinakaAndheri(East)Mumbai 400069India 

出 版 物：《Asian Journal of Pharmaceutical Sciences》 (亚洲药物制剂科学（英文）)

年 卷 期：2016年第11卷第6期

页      面：760-770页

核心收录：

学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1002[医学-临床医学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：University Grants Commission  UGC  (UGC-SAP/ICT-DPST/2012-13/1115) 

主　　题：Artemether Solubility Solid dispersion Porous silica Aeropearl 300 

摘      要：Malaria is a parasitic and vector determined blood-conceived infectious disease transmitted through infected mosquitoes. Anti-malarial drug resistance is a major health problem, which hinders the control of malaria. A Results of a survey of drug-resistant malaria demonstrated safe proclivity to nearby all anti-malarial regimes accessible except from artemisinin and its derivatives. Artemether is a BCS class IV drug effective against acute and severe falciparum malaria;hence there is a strong need to improve its solubility. Silica is one of the most widely studied excipients. Silica can be used in solubility enhancement by preparing its solid solution/dispersion with the drug. The objective of this research was to improve dissolution rate of Artemether using non-precipitated porous silica(Aeroperl 300 Pharma) and precipitated silica like EXP. 9555, EXP. 9560, and EXP. 9565. Specific surface area calculated from BET method of porous silicas viz. APL 300(A), Exp. 9555(B), Exp. 9560(C), Exp. 9565(D) was found to be 294.13 m^2/g(A), 256.02 m^2/g(B), 213.62 m^2/g(C) and 207.22 m^2/g(D) *** drug release from the developed formulation was found to be significantly higher as compared to neat ARM. This improved solubility and release kinetics of ARM may be attributed to high surface area, improved wettability and decreased crystallinity. Solid-state characterization of the developed optimized formulation F3 was carried out with respect to FTIR chemical imaging, XRD,SEM, and DSC. All the porous silicas which we have explored in the present context showed a significant capability as a carrier for solubility enhancement of ARM.