PDF(Pubmed)
Abstract：
Microparticles as a multicompartment drug delivery system are beneficial for poorly soluble drugs. Mucoadhesive polymers applied in microparticle technology prolong the contact of the drug with the mucosa surface enhancing drug bioavailability and extending drug activity. Sodium alginate (ALG) and hydroxypropyl methylcellulose (hypromellose, HPMC) are polymers of a natural or semi-synthetic origin, respectively. They are characterized by mucoadhesive properties and are applied in microparticle technology. Spray drying is a technology employed in microparticle preparation, consisting of the atomization of liquid in a stream of gas. In this study, the pharmaceutical properties of spray-dried ALG/HPMC microparticles with posaconazole were compared with the properties of physical mixtures of powders with equal qualitative and quantitative compositions. Posaconazole (POS) as a relatively novel antifungal was utilized as a model poorly water-soluble drug, and hard gelatin capsules were applied as a reservoir for designed formulations. A release study in 0.1 M HCl showed significantly prolonged POS release from microparticles compared to a mixture of powders. Such a relationship was not followed in simulated vaginal fluid (SVF). Microparticles were also characterized by stronger mucoadhesive properties, an increased swelling ratio, and prolonged residence time compared to physical mixtures of powders. The obtained results indicated that the pharmaceutical properties of hard gelatin capsules filled with microparticles were significantly different from hard gelatin capsules with mixtures of powders.
摘要：
微粒作为多室药物递送系统对于难溶性药物是有益的。在微粒技术中应用的粘膜粘附聚合物延长了药物与粘膜表面的接触,增强了药物的生物利用度并延长了药物活性。海藻酸钠（ALG）和羟丙基甲基纤维素（羟丙甲纤维素，HPMC）是天然或半合成来源的聚合物，分别。它们的特征在于粘膜粘附特性,并应用于微粒技术。喷雾干燥是一种用于微粒制备的技术，由液体在气流中的雾化组成。在这项研究中,将具有泊沙康唑的喷雾干燥的ALG/HPMC微粒的药物特性与具有相同定性和定量组成的粉末的物理混合物的特性进行了比较。泊沙康唑（POS）作为一种相对新颖的抗真菌药被用作水溶性差的模型药物，和硬明胶胶囊作为设计制剂的储库。在0.1MHCl中的释放研究显示,与粉末混合物相比,从微粒的POS释放显著延长。在模拟阴道液（SVF）中没有遵循这种关系。微粒的特征还在于更强的粘膜粘附特性，增加的溶胀率，与粉末的物理混合物相比，停留时间延长。获得的结果表明，填充有微粒的硬明胶胶囊的药物性能与具有粉末混合物的硬明胶胶囊明显不同。
