普那霉素纳米粒肠溶胶囊的制备及药动学评价  

Preparation and Pharmacokinetic Evaluation of Enteric-coated Capsules Filled with Pristinamycin Nanoparticles

作　　者：赵欣 孙立昂[2] 戈梅 沈琦[2] ZHAO Xin;SUN Li’ang;GE Mei;SHEN Qi(College of Pharmacy,Dali University,Dali 671000;School of Pharmacy,Shanghai Jiao Tong University,Shanghai 200240;Shanghai Laiyi Center for Biopharmaceutical R&D,Shanghai 200240)

机构地区：[1]大理大学药学院,云南大理671000 [2]上海交通大学药学院,上海200240 [3]上海来益生物药物研究开发中心有限责任公司,上海200240

出　　处：《中国医药工业杂志》2021年第5期661-668,共8页Chinese Journal of Pharmaceuticals

摘　　要：使用高压均质法分别制备普那霉素Ⅰ_(A)和Ⅱ_(A)纳米混悬剂,冻干所得的纳米粒按比例混合后填入胶囊,经浸蘸肠溶包衣液制成纳米粒肠溶胶囊,并考察该胶囊的体外释放行为及在大鼠体内的药动学特征。动态光散射(DLS)法测得普那霉素Ⅰ_(A)和Ⅱ_(A)纳米混悬剂的粒径分别为(354.42±80.26)与(370.35±74.92)nm,且多分散系数(PDI)均小于0.3,透射电镜(TEM)下均呈类球形。体外释放试验表明,60 min内普那霉素纳米粒肠溶胶囊中2种成分的累积释放率分别可达90.77%与78.22%。大鼠药动学试验表明,与普通胶囊相比,该纳米粒肠溶胶囊中2种成分的相对生物利用度分别为158.27%与132.58%。因而将普那霉素制备成纳米粒肠溶胶囊后可显著提高其生物利用度,进而为其肠溶剂型的改进提供参考。The nanosuspensions of pristinamycinsⅠ_(A) andⅡ_(A) were prepared by high pressure homogenization method,then their nanoparticles were obtained by lyophilization.The enteric-coated capsules filled with above freeze-dried nanoparticles proportionally were prepared during a dipping process.The in vitro release and pharmacokinetic characteristics of the product in rats were evaluated.The mean particle sizes of pristinamycinsⅠ_(A) andⅡ_(A) nanosuspensions measured by dynamic light scattering(DLS)were(354.42±80.26)and(370.35±74.92)nm with polydispersion index(PDI)less than 0.3.Under the transmission electron microscope(TEM),both nanoparticles were spherical in shape.The results of in vitro release test showed that the release of pristinamycinsⅠ_(A) andⅡ_(A) at 60 min from the enteric-coated capsules were 90.77%and 78.22%,respectively.And their relative bioavailabilities in rats were 158.27%and 132.58%,showing a significant increase as compared to the ordinary capsules.In conclusion,the bioavailability of enteric-coated capsules of pristinamycin nanoparticles was significantly improved,which could provide some references for formulation improvement of pristinamycin enteric-coated preparations.

关 键 词：普那霉素 纳米混悬剂 纳米粒 肠溶胶囊 体外释放 生物利用度 

分 类 号：R944.5[医药卫生—药剂学]