Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
College of Pharmacy, University of Sargodha, Sargodha, Pakistan.
PLoS One. 2021 Apr 30;16(4):e0250876. doi: 10.1371/journal.pone.0250876. eCollection 2021.
Pentazocine (PTZ) is a narcotic analgesic used to manage moderate to severe, acute and chronic pains. In this study, PTZ loaded Ethyl cellulose microsphere has been formulated for sustained release and improved bioavailability of PTZ. These microspheres were fabricated by oil in water emulsion solvent evaporation technique. A three factorial, three levels Box-Behnken design was applied to investigate the influence of different formulation components and process variables on the formulation response using the numeric approach through the design expert® software. All the formulations were characterized for the morphology, different physicochemical properties and the results were supported with the ANOVA analysis, three dimensional contour graphs and regression equations. The maximum percentage yield was 98.67% with 98% entrapment of PTZ. The mean particle size of the formulations ranges from 50-148μm, which directly relates to the concentration of polymer and inversely proportional to the stirring speed. SEM revealed the spherical shape of PTZ microspheres with porous structures. These are physically, chemically and thermally stable as confirmed through Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD) and thermal gravimetric (TG) analysis respectively. The microspheres provided a sustained release of the PTZ for more than 12 hours, following zero order with fickian and non fickian diffusion. The results indicate that prepared microspheres can be a potential drug delivery system (DDS) for the delivery of PTZ in the management of pains.
戊唑辛（PTZ）是一种麻醉性镇痛药，用于治疗中重度、急性和慢性疼痛。在这项研究中，PTZ 负载乙基纤维素微球被制成了缓释制剂，以提高 PTZ 的生物利用度。这些微球是通过油包水乳液溶剂蒸发技术制备的。采用三因素、三水平 Box-Behnken 设计，通过数值方法应用设计专家®软件，考察不同配方成分和工艺变量对制剂响应的影响。所有制剂均进行了形态学、不同理化性质的表征，并通过方差分析、三维等高线图和回归方程进行了支持。最大收率为 98.67%，PTZ 的包封率为 98%。制剂的平均粒径范围为 50-148μm，这与聚合物的浓度直接相关，与搅拌速度成反比。扫描电子显微镜（SEM）显示了 PTZ 微球具有多孔结构的球形。通过傅里叶变换红外光谱（FTIR）、粉末 X 射线衍射（PXRD）和热重（TG）分析分别证实了它们在物理、化学和热方面的稳定性。微球提供了超过 12 小时的 PTZ 持续释放，遵循零级和菲克扩散。结果表明，所制备的微球可作为 PTZ 的潜在药物传递系统（DDS），用于疼痛管理。
