Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
J Pharm Pharmacol. 2011 Feb;63(2):169-78. doi: 10.1111/j.2042-7158.2010.01214.x.
The objective of this study was to prepare gliclazide-chitosan microparticles with tripolyphosphate by ionic crosslinking.
Chitosan microparticles were produced by emulsification and ionotropic gelation. The effects of process variables including chitosan concentration, pH of tripolyphosphate solution, glutaraldehyde volume and release modifier agent such as pectin added to the tripolyphosphate crosslinking solution were evaluated. The microparticles were examined with scanning electron microscopy, infrared spectroscopy and differential scanning colorimetry. The serum glucose lowering effect of gliclazide microparticles was studied in streptozotocin-diabetic rabbits compared with the effect of pure gliclazide powder and gliclazide commercial tablets.
The particle sizes of tripolyphosphate-chitosan microparticles were over the range 675-887 µm and the loading efficiency of drug was greater than 94.0%. In-vivo testing of the gliclazide-chitosan microparticles in diabetic rabbits demonstrated a significant antidiabetic effect of gliclazide-chitosan microparticles after 8 h that lasted for 18 h compared with gliclazide powder, which produced a maximum hypoglycaemic effect after 4 h.
The results suggests that gliclazide-chitosan microparticles are a valuable system for the sustained delivery of gliclazide.
本研究旨在通过离子交联法制备载格列齐特的壳聚糖微球。
采用乳化-离子凝胶化法制备壳聚糖微球。考察了壳聚糖浓度、三聚磷酸溶液 pH 值、戊二醛体积以及在三聚磷酸交联溶液中添加释放调节剂（如果胶）等工艺变量对微球的影响。采用扫描电子显微镜、红外光谱和差示扫描量热法对微球进行了研究。将格列齐特微球的降血糖效果与纯格列齐特粉末和格列齐特商业片剂在链脲佐菌素诱导的糖尿病兔中的效果进行了比较。
三聚磷酸-壳聚糖微球的粒径在 675-887 µm 之间，药物载药量大于 94.0%。在糖尿病兔体内试验中，格列齐特-壳聚糖微球在 8 小时后表现出显著的抗糖尿病作用，持续 18 小时，而格列齐特粉末在 4 小时后产生最大的降血糖作用。
结果表明，格列齐特-壳聚糖微球是一种有价值的格列齐特持续释放系统。
