SBA-15与SBA-16作为药物载体的性能研究

Comparative Study on Improvement of Diabetic Model Rats between SBA-15/GLZ and SBA-16/GLZ

目的：通过建立SD大鼠2型糖尿病模型的方法,研究不同的介孔材料SAB-15与SAB-16分别载药格列齐特（GLZ）,释放速率的作用,以筛选出最佳的载药系统,为临床制剂提供参考。方法：考察SAB-15/GLZ、SAB-16/GLZ的载药、释药性能,建立大鼠糖尿病模型,分别检测灌胃给药前（0h）和给药后各时间点（3 h,6 h,9 h,12 h,24 h,27 h,30 h,48 h）各组大鼠血糖浓度的变化。结果：1载药系统的热重分析,SBA-15/GLZ、SBA-16/GLZ在200-700℃均有显著的失重,分别是14.3%和15.4%,且SBA-16/GLZ失重高于SBA-15/GLZ;2FTIR分析中,在红外光谱中500 cm^-1-2000 cm^-1波数范围内两种材料载药均出现了4个吸收强度较大的特征峰,二者波数范围相同,波峰相似,且与GLZ的分布趋势大致一致,且SBA-16/GLZ的吸收强度略高于SBA-15/GLZ;3载药系统的结构性质,与SBA-15比较,SBA-15/GLZ在比表面积、孔隙容积上均减小（P〈0.01）,与SBA-16比较,SBA-16/GLZ比表面积、孔隙容积上均减小,且SBA-16/GLZ的比表面积、孔隙容积均显著小于SBA-15/GLZ（P〈0.01）;4释放速率：SBA-15/GLZ内格列齐特有一个迅速的释放过程,12 h即达90%以上,24 h后缓释量逐渐趋于平缓,48 h释放量即达到95%以上,最终缓释量约在97%水平;而SBA-16/GLZ内格列齐特的缓释相对平缓,12 h之内释放了80%左右,显著低于同等时间点SBA-15对格列齐特释放（P〈0.05）,48 h最终缓释量约在90%的水平;5血糖变化,在0 h测得的血糖结果中,模型组及各给药组的血糖均显著升高,且≥13.8 mmo L/L,说明造模成功;12 h的血糖值最低,随着时间的推移,GLZ组的血糖变化梯度最大,SBA-15/GLZ次之,SBA-16/GLZ血糖值的变化曲线较平坦,说明介孔材料能有效载药、平稳缓释、在动物模型体内平稳持续释药并发挥作用,避免血糖浓度忽高忽低,SBA-16/GLZ缓释效果显著优于SBA-15/GLZ。结论：SAB-16介孔材料的载药量高于SAB-15,缓释持续时间长。

Objective： This paper was to research on different mesoporous materials SAB-15 and SAB-16 respectively, the drug loaded Zig Leo Te （GLZ） release rate effect by the method of establishing model of SD rats with type 2 diabetes, and to screen out the best drug carrier-system for clinical use. Methods： Diabetic rat model was established, then to investigate the effect of SAB-15 / GLZ, SBA-16/GLZ and detect the blood glucose, plasma insulin at the point of 0 h, 3 h, 6 h, 9 h, 12 h, 24 h, 27 h, 30 h, 48 h. Results： ①The weight analysis system loaded with heat showed that, SBA-15/GLZ and SBA-16/GLZ in 200 -700 ℃ showed a significant weight loss, respectively 14. 3% and 15.4%, and SBA-16/G LZ weight loss was higher than that of SBA-15/GLZ; ②The FTIR analysis, in the IR spectra of 500 cm^-1- 2000 cm^-1 , wave number range material drug carrier appeared 4 absorption intensity of characteristic peak, and the two peak wave number range is similar, and generally consistent with the distribution of GLZ and SBA- 16/GLZ, the absorption intensity is slightly higher than that of SBA-15/GLZ; ③The structure properties of the drug carrier system, compared with SBA-15, SBA-15/GLZ specific surface area, pore volume were reduced （P 〈 0. 01 ） ; that compared with SBA-16, SBA-16/GLZ surface area and porevolume decreased, and the SBA-16/GLZ specific surface area and pore volume were significantly less than SBA-15/GLZ （P 〈0. 01 ） ; ④Release rate： SBA -15 to GLZ procedure of a quick release and he quantity achieved above 90% at the 12 th h, the rate slowed down after 24 h, at the 48th h the quantity achieced above 95%, eventually slow release quantity was about 97%. The SBA-16/GLZ sustained-release relatively flat, within 12 h released by about 80%, Significantly lower than SBA -15 at the same point in time （P 〈0. 05 ）, eventually slow release quantity was about 90%. ⑤The changes of blood glucose showed that, measured at 0＇h h blood glucose results in the model group and the drug group blood sugar were significantly increased, and was higher than 13.8mmoL/L, indicating a successful model; The glucose concentration of each group at 12＇h h was the lowest, and blood glucose in GLZ group change gradient was the biggest, SBA-15/GLZ group change gradient was less than GLZ group, the curve of change with SBA -16 / GLZ group curve was flat as time went by. Which indicated that be effective, sustained release drug carrier, and played a role in the animal model in vivo sustained drug release and smooth, prevent blood glucose concentration fluctuat, SBA-16 sustained release effect was superior to that of SBA-15. Conclusion： The description of the drug loading of SBA-16 mesoporous materi- al is better than SBA-15 which with releasing of long duration.