Sarfraz Rai Muhammad, Ahmad Mahmood, Mahmood Asif, Akram Muhammad Rouf, Abrar Asad
Faculty of Pharmacy, University of Sargodha, Sargodha.
Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur.
Drug Des Devel Ther. 2017 Oct 24;11:3083-3096. doi: 10.2147/DDDT.S143712. eCollection 2017.
The aim of this study was to enhance the solubility of rosuvastatin (RST) calcium by developing β-cyclodextrin--poly(2-acrylamido-2-methylpropane sulfonic acid [AMPS]) hydrogel microparticles through aqueous free-radical polymerization technique. Prepared hydrogel microparticles were characterized for percent entrapment efficiency, solubility studies, Fourier transform infrared spectroscopy, differential scanning calorimetry, thermal gravimetric analysis, powder X-ray diffraction, scanning electron microscopy, zeta size and potential, swelling and release studies. Formulations (HS1-HS9) have shown entrapment efficiency between 83.50%±0.30% and 88.50%±0.25%, and optimum release was offered by formulation HS7 at both pH levels, ie, 1.2 (89%) and 7.4 (92%). The majority of microparticles had a particle size of less than 500 µm and zeta potential of -37 mV. Similarly, optimum solubility, ie, 10.66-fold, was determined at pH 6.8 as compared to pure RST calcium, ie, 7.30-fold. In vivo studies on fabricated hydrogel microparticulate system in comparison to pure drug were carried out, and better results regarding pharmacokinetic parameters were seen in the case of hydrogel microparticles. A potential approach for solubility enhancement of RST calcium and other hydrophobic moieties was successfully developed.
本研究的目的是通过水溶液自由基聚合技术制备β-环糊精-聚（2-丙烯酰胺基-2-甲基丙烷磺酸[AMPS]）水凝胶微粒，以提高瑞舒伐他汀（RST）钙的溶解度。对制备的水凝胶微粒进行包封率、溶解度研究、傅里叶变换红外光谱、差示扫描量热法、热重分析、粉末X射线衍射、扫描电子显微镜、zeta尺寸和电位、溶胀和释放研究等表征。制剂（HS1-HS9）的包封率在83.50%±0.30%至88.50%±0.25%之间，HS7制剂在pH值为1.2（89%）和7.4（92%）时均表现出最佳释放。大多数微粒的粒径小于500 µm，zeta电位为-37 mV。同样，与纯RST钙相比，在pH 6.8时测定的最佳溶解度为10.66倍，而纯RST钙为7.30倍。对制备的水凝胶微粒系统与纯药物进行了体内研究，水凝胶微粒在药代动力学参数方面表现出更好的结果。成功开发了一种提高RST钙和其他疏水部分溶解度的潜在方法。
