厄贝沙坦自微乳化释药系统及其颗粒剂研究  

Study on irbesartan self-microemulsifying drug delivery system and its granules

作　　者：龚麟凤 张琪 汪洋 GONG Linfeng;ZHANG Qi;WANG Yang(Department of Pharmacy,the Red Cross Hospital of Wuhan,Wuhan 430015,China)

机构地区：[1]武汉市红十字会医院药剂科,武汉430015

出　　处：《西北药学杂志》2021年第6期956-961,共6页Northwest Pharmaceutical Journal

摘　　要：目的研制厄贝沙坦自微乳化释药系统(IRB-SMEDDSs)及其颗粒剂,并对其性质进行评价。方法测定厄贝沙坦(IRB)在不同油相、乳化剂和助乳化剂中的溶解度,并根据各辅料的相容性实验确定了IRB-SMEDDSs的处方组成,并通过伪三元相图确定各辅料用量;以硅酸镁铝作为载体将IRB-SMEDDSs固化成颗粒剂;评价IRB-SMEDDSs的理化性质,比较IRB市售片剂、IRB-SMEDDSs及其颗粒剂的体外溶出度;考察IRB-SMEDDSs及其颗粒剂在加速条件下的稳定性。结果IRB-SMEDDSs的处方组成为:丙二醇单辛酸酯(Capryol 90)为油相,聚氧乙烯蓖麻油(Cremophor EL)为乳化剂,二乙二醇单乙基醚(Transcutol P)为助乳化剂,配比为6∶3∶1。IRB-SMEDDSs形成的微乳稀释稳定性良好,浊点较高,在透射电镜下可观察到微乳呈球状,分散性良好;IRB-SMEDDSs及其颗粒剂中的药物溶出速率均显著快于市售IRB片;在加速条件下放置3个月,IRB-SMEDDSs及其颗粒剂稳定性均良好。结论将IRB制备成自微乳化释药系统及其颗粒剂,均显著提高了药物的溶出速率,有望提高药物的生物利用度。Objective To develop irbesartan self-microemulsifying drug delivery systems(IRB-SMEDDSs)and granules,and to evaluate their properties.Methods The solubility of irbesartan(IRB)in different oil phases,emulsifiers and co-emulsifiers was determined,and the formulation composition of IRB-SMEDDSs was determined according to the compatibility experiment of each excipient,and the dosage of each excipient was determined by pseudo-ternary phase diagram.Magnesium aluminometasilicate was used as a carrier to solidify IRB-SMEDDSs into granules.The physical and chemical properties of IRB-SMEDDSs were evaluated,and the in vitro dissolution rates of IRB commercial tablets,IRB-SMEDDSs and its granules were compared.The stability of IRB-SMEDDSs and granules under accelerated conditions was investigated.Results The formulation composition of IRB-SMEDDSs was as follows:Capryol 90 as the oil phase,Cremophor EL as the emulsifier,and Transcutol P as the co-emulsifier.The optimal ratio of the formulation was 6∶3∶1.The microemulsion formed by IRB-SMEDDSs showed good dilution stability and high cloud point.Under transmission electron microscope,the microemulsion was spherical and had good dispersibility.The drug dissolution rate of IRB-SMEDDSs and its granules was significantly higher than IRB Tablets.IRB-SMEDDSs and its granules had good stability after 3 months under accelerated conditions.Conclusion IRB was prepared into IRB-SMEDDSs and its granules,which significantly increased the dissolution rate and was expected to improve the bioavailability of irbesartan.

关 键 词：厄贝沙坦(IRB) 自微乳化释药系统(SMEDDSs) 固体化 溶出度 稳定性 生物利用度 

分 类 号：R94[医药卫生—药剂学]