Dipartimento di Scienze per la promozione della Salute e Materno Infantile "Giuseppe D'Alessandro", Palermo, Italy.
Advanced Technologies Network Center (ATeN Center), University of Palermo, Viale Delle Scienze - Edificio, 18 - 90128, Palermo, Italy.
Pharm Res. 2020 Feb 19;37(3):57. doi: 10.1007/s11095-020-2778-1.
Solid dispersions (SDs) represent the most common formulation technique used to increase the dissolution rate of a drug. In this work, the three most common methods used to prepare SDs, namely spray-drying, solvent-casting and freeze-drying, have been compared in order to investigate their effect on increasing drug dissolution rate.
Three formulation strategies were used to prepare a polymer mixture of polyvinyl-alcohol (PVA) and maltodextrin (MDX) as SDs loaded with the following three model drugs, all of which possess a poor solubility: Olanzapine, Dexamethasone, and Triamcinolone acetonide. The SDs obtained were analysed and compared in terms of drug particle size, drug-loading capacity, surface homogeneity, and dissolution profile enhancement. Physical-chemical characterisation was conducted on pure drugs, as well as the formulations made, by way of thermal analysis and infrared spectroscopy.
The polymers used were able to increase drug saturation solubility. The formulation strategies affected the drug particle size, with the solvent-casting method resulting in more homogenous particle size and distribution when compared to the other methods. The greatest enhancement in the drug dissolution rate was seen for all the samples prepared using the solvent-casting method.
All of the methods used were able to increase the dissolution rate of the pure drugs alone, however, the solvent-casting method produced SDs with a higher surface homogeneity, drug incorporation capability, and faster dissolution profile than the other techniques.
固体分散体(SDs)是提高药物溶解速率最常用的制剂技术之一。在这项工作中,比较了三种最常用的制备 SDs 的方法,即喷雾干燥、溶剂浇铸和冷冻干燥,以研究它们对提高药物溶解速率的影响。
使用三种配方策略制备了聚乙烯醇(PVA)和麦芽糊精(MDX)的聚合物混合物作为 SDs,负载以下三种模型药物,这些药物的溶解度都较差:奥氮平、地塞米松和曲安奈德。对获得的 SDs 进行了分析和比较,包括药物粒径、载药量、表面均一性和溶解性能的提高。通过热分析和红外光谱对纯药物和制剂进行了物理化学特性分析。
所使用的聚合物能够提高药物的饱和溶解度。制剂策略影响药物粒径,与其他方法相比,溶剂浇铸法得到的粒径更均匀、分布更均匀。所有使用溶剂浇铸法制备的样品的药物溶解速率均有显著提高。
所有使用的方法都能够单独提高纯药物的溶解速率,然而,溶剂浇铸法制备的 SDs 具有更高的表面均一性、药物包封能力和更快的溶解性能,优于其他技术。