格列齐特生物黏附缓释片的研制及体外评价

Preparation and evaluation in vitra of the bio-adhesive gliclazide sustained-release tablets

目的 制备格列齐特生物黏附性缓释片, 考察其体外释药行为, 并测定其与家兔离体胃、小肠组织的黏附力。方法 以羟丙基甲基纤维素(HPMCK15M) 和卡波姆(carbopol, CP) 为生物黏附材料和骨架材料, 乳糖为稀释剂制备生物黏附性缓释片。以磷酸盐缓冲液(pH 8. 6) 400 mL为溶剂, 转篮法(转速150 r·min-1) 测定2、12、20 h时的释放度。以自制黏附力测定装置测定、比较格列齐特生物黏附性缓释片及格列齐特(Ⅱ) 片对家兔离体胃、肠组织的黏附力。结果 生物黏附性缓释片体外释放符合缓释制剂要求, 其与家兔离体胃、肠组织的黏附力明显大于普通片剂, 且与肠的黏附力大于与胃的黏附力。结论 格列齐特生物黏附缓释片的处方、工艺基本能够满足设计要求。

OBJECTIVE To prepare the sustained-release gliclazide tablets and to compare the adhesion of the bio-adhesive gliclazide sustained-release tablets and gliclazide tablets(Ⅱ)to the isolated stomach of the rabbit and the small intestine tissue.METHODS Hydroxypropyl Methl Cellulose(HPMC_ K15M)and Carbopol(CP_ 934P)were used as the bio-adhesive and binding materials in this research.Lactose was used as diluents in preparing the bio-adhesive gliclazide sustained-release tablets.The dissolution of bio-adhesive gliclazide sustained-release tablets and gliclazide tablets(Ⅱ)were determinated.We used self-made adhesion device to measure and compare the adhesion of the bio-adhesive gliclazide sustained-release tablets and gliclazide tablets(Ⅱ)to the isolated stomach of the rabbit and the small intestine tissues.RESULTS The dissolution of bio-adhesive sustained-release tablets at 2 h,12 h and 24 h were 18.9%～21.3%,72.6%～75.6%,and 88.8%～95.7% respectively,compared with those of gliclazide tablets(Ⅱ)were 38.3%,57.8% and 98.3% at 1 h,2 h and 8 h.The adhesion of bio-adhesive sustained-release tablets to isolated stomach and intestine tissues of the rabbit was obviously stronger than that of the common tablets,and the adhesion to the intestine was stronger than that to the stomach.CONCLUSIONS The bio-adhesive sustained-release tablets may meet the general requirements of the design.