Department of Pharmaceutics, AISSMS College of Pharmacy, Kennedy Road, Near R.T.O., Pune, 411001, India.
AAPS PharmSciTech. 2022 May 9;23(5):133. doi: 10.1208/s12249-022-02285-x.
Sediment delivery model (SeDeM) system is innovative tool to correlate micromeritic properties of powders with compressibility. It involves computation of indices which facilitate direct compressibility of solids and enable corrective measures through particle engineering. Study had multiple objectives, viz, (i) to enhance solubility of BCS class II, nevirapine using solid dispersions; (ii) SeDeM analyses of excipients and solid dispersions to analyze direct compressibility; and (iii) prepare orodispersible tablets (ODT). Solid dispersions were prepared by solvent evaporation. Superdisintegrants and solid dispersions were analyzed for primary indices of dimension, compressibility, flowability, stability, and disgregability derived from micromeritic properties. Radar diagrams were constructed to provide visual clues to deficient properties for direct compressibility. ODTs were prepared using excipients which passed criteria for direct compressibility and evaluated for tablet properties. Solid dispersions with Eudragit S100 revealed 6 to 10 fold increase in solubility in various dissolution media including biorelevant media in comparison with plain drug. Solubility was found to be pH dependent. SeDeM analyses facilitated identification of superdisintegrants and excipients with unfavorable compressibility. Radar diagrams provided a clear pictorial evidence of lacunae in powder properties. Based on SeDeM results, tablets were formulated by direct compression using crosspovidone, croscarmellose sodium, and mannitol. All batches showed 40% release in first minute in simulated salivary fluid.
沉降输送模型 (SeDeM) 系统是一种创新的工具，可将粉末的微观性质与可压缩性相关联。它涉及到计算指数的过程，这些指数有助于固体的直接可压缩性，并通过颗粒工程实现纠正措施。该研究有多个目标，即：(i) 使用固体分散体提高 BCS 类 II 药物奈韦拉平的溶解度；(ii) 通过 SeDeM 分析赋形剂和固体分散体来分析直接可压缩性；(iii) 制备口腔崩解片 (ODT)。固体分散体通过溶剂蒸发法制备。超级崩解剂和固体分散体用于分析来自微观性质的主要尺寸、可压缩性、流动性、稳定性和崩解性指数。雷达图用于提供直接可压缩性缺陷属性的直观线索。使用通过直接可压缩性标准的赋形剂制备 ODT，并对片剂性质进行评估。与普通药物相比，Eudragit S100 固体分散体显示出 6 至 10 倍的溶解度增加，在各种溶解介质中，包括生物相关介质。溶解度依赖于 pH 值。SeDeM 分析有助于识别具有不利可压缩性的超级崩解剂和赋形剂。雷达图提供了粉末性质空白的清晰图像证据。根据 SeDeM 结果，使用交聚维酮、交联羧甲纤维素钠和甘露醇通过直接压片法制备片剂。所有批次在模拟唾液中均在第一分钟内释放 40%。
