Yasin Haya, Al-Taani Bashar, Salem Mutaz Sheikh
Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Ajman University, Ajman, UAE.
Res Pharm Sci. 2020 Dec 30;16(1):1-15. doi: 10.4103/1735-5362.305184. eCollection 2021 Feb.
Pregabalin is used in the treatment of epilepsy, chronic pain, and other psychological disorders. Preparation of pregabalin in the sustained-release formulation will enhance patient compliance and reduce the incidence of side effects. The aim of this study was to prepare sustained-release microspheres for pregabalin utilizing ethylcellulose and evaluate the processing factors that influence the fabrication and the performance of the prepared microspheres.
The microspheres were prepared using the water-oil-oil double emulsion solvent evaporation method. Microspheres were characterized for particle size, encapsulation efficiency, and drug release. The influence of the processing variables on the characteristics of the prepared microspheres was studied. Microspheres solid-state characterization performed using differential scanning calorimetry, Fourier transform infrared spectroscopy and scanning electron microscopy.
FINDINGS/RESULTS: The results described in the context of the current work illustrated the suitability of the water-oil-oil system in the preparation of sustained-release microspheres for pregabalin. The optimum formulation was prepared at a drug to polymer ratio of 1:3 w/w, stirring speed of 600 rpm, surfactant concentration of 1.5%, and external phase volume of 150 mL. This formula produced microspheres particle size in the range 600-1000 μm, with 87.6% yield, and 80.14 ± 0.53% encapsulation efficiency. Drug release from the microspheres was found to be diffusion controlled, with a pH-independent behavior.
The current work presented a successful attempt to fabricate a sustained-release microsphere comprising pregabalin. This will help overcome the frequent dosing problems with conventional pregabalin dosage forms and improve product performance.
普瑞巴林用于治疗癫痫、慢性疼痛及其他心理障碍。制备普瑞巴林缓释制剂可提高患者依从性并降低副作用发生率。本研究旨在利用乙基纤维素制备普瑞巴林缓释微球，并评估影响所制备微球的制备过程及性能的工艺因素。
采用水 - 油 - 油双乳液溶剂蒸发法制备微球。对微球的粒径、包封率和药物释放进行表征。研究工艺变量对所制备微球特性的影响。使用差示扫描量热法、傅里叶变换红外光谱法和扫描电子显微镜对微球进行固态表征。
当前工作所描述的结果表明水 - 油 - 油体系适用于制备普瑞巴林缓释微球。在药物与聚合物比例为1:3 w/w、搅拌速度为600 rpm、表面活性剂浓度为1.5%以及外相体积为150 mL的条件下制备出了最佳制剂。该配方制备的微球粒径在600 - 1000μm范围内，产率为87.6%，包封率为80.14 ± 0.53%。发现微球的药物释放受扩散控制，且与pH无关。
当前工作成功尝试制备了包含普瑞巴林的缓释微球。这将有助于克服传统普瑞巴林剂型频繁给药的问题并改善产品性能。
