HPMC修饰的氟苯尼考微晶体的制备及表征  

Preparation and characterization of Florfenicol microcrystal modified by HPMC

作　　者：曹航[1] 符华林[1] 何燕飞[1] 张伟[1] 卢朝成[1] 刘梦娇[1] 张艳丽[1] 

机构地区：[1]四川农业大学动物医学院,四川雅安625014

出　　处：《华西药学杂志》2015年第2期152-154,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的制备氟苯尼考微晶体,提高氟苯尼考的溶解度,以促进吸收并增加其生物利用度。方法使用改良溶剂反溶剂法制备羟丙甲纤维素(HPMC)修饰的氟苯尼考微晶体,通过正交优化得到最佳制备工艺。考察其形态学、体外溶解性质、稳定性,并通过差示扫描量热法(DSC)和X射线衍射法研究其晶型变化。结果反溶剂为水、溶剂为丙酮、温度为4℃、HPMC为4 mg·m L-1时,制备的微晶体最大饱和溶解度为3.13 mg·m L-1,溶解速度明显增加;原药和微晶体在形态学上差异较大且微晶体粒的径明显小于原药,二者对高温、高湿、强光均稳定;DSC和X射线衍射实验表明药物晶型从两种转变成了一种。结论该制备工艺简单,HPMC修饰的氟苯尼考微晶体明显增加了氟苯尼考的溶解度和溶解速度,性质稳定,有较好的应用前景。OBJECTIVE To prepare hydroxy propyl methyl cellulose（HPMC） modified florfenicol microcrystal and study its physical properties and characterization. METHODS Modified solvent - antisolvent recrystallization was used to prepare florfenicol microcrystal and best preparation method was obtained by orthogonal optimization. Morphology, properties of in vitro dissolution and stability were studied. Moreover its changes of crystal form was studied by differential scanning calorimetry（DSC） and X -ray diffraction. RESULTS While the condition of water as anti - solvent, acetone as solvent, concentration of HPMC as 4 mg·m L^-1 and at the temperature of 4~C, the saturated solubility of florfenicol microcrystal was 3.13 mg·m L^-1, and its dissolution was significantly increased. For the mor- phology, there were significant differences between original drug and microcrystal, and the particle size of microcrystal was smaller than original drug. Both of the microcrystal and original drug were very stable to the high temperature, high humidity and intense light. DSC and X - ray diffraction showed original drug had two crystal forms, and turned into one after preparation of the microcrystal. CONCLU- SION This preparation method is very simple and florfenicol microcrystal modified by HPMC.

关 键 词：氟苯尼考 羟丙甲纤维素 微晶体 重结晶 溶解度 表征 正交实验 制备工艺 差示扫描量热法 X射线衍射法 

分 类 号：R94[医药卫生—药剂学]