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布洛芬从喷雾干燥颗粒和喷雾冷冻颗粒中的溶出度。

Dissolution of ibuprofen from spray dried and spray chilled particles.

作者信息

Elkordy Amal A, Essa Ebtessam A

机构信息

University of Sunderland, Department of Pharmacy, Health and Well-being, Sunderland SR13SD, UK.

出版信息

Pak J Pharm Sci. 2010 Jul;23(3):284-90.

Abstract

The formulation of hydrophobic drugs for oral drug delivery is challenging due to poor solubility, poor dissolution and poor wetting of these drugs. Consequently, the aim of this study was to improve the dissolution of a model poorly water soluble drug, ibuprofen. Microparticles containing ibuprofen were produced by spray drying and spray chilling technology in the absence/presence of a hydrophilic surfactant. Poloxamer 127, tri-block copolymer, was chosen as the hydrophilic surfactant to improve drug particle wettability and hence the dissolution rate. The prepared formulations were evaluated for in vitro dissolution and intrinsic solubility. In addition, the produced drug particles were characterised by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier transform infrared spectroscopy (FT-IR). SEM revealed changes in the surface morphology of processed ibuprofen, suggesting the effective formation of the drug particles. DSC data showed shifting of the melting peak of the drug towards lower melting temperature in the prepared particles, indicating the possibility of drug /polymer interaction. The results of the dissolution studies of spray dried ibuprofen and spray dried ibuprofen/Poloxamer 127 particles showed significantly (P<0.05) increased percentage drug release compared to control (ibuprofen raw material). For spray chilling, the prepared particles did not improve the dissolution of the drug, the dissolution was even less than that of the control. DSC and FT-IR results demonstrated that spray drying reduced drug crystallinity, but for spray chilled particles there was evidence of polymorphic changes in the drug with and without the surfactant. Consequently, it is believed that spray drying of ibuprofen is a useful tool to improve wettability, solubility and hence the dissolution behaviour of poorly water soluble drugs, in contrast to spray chilling technique.

摘要

由于疏水性药物的溶解度差、溶出度低和润湿性差,其口服给药制剂的制备具有挑战性。因此,本研究的目的是提高一种典型的难溶性药物布洛芬的溶出度。在有无亲水性表面活性剂的情况下,通过喷雾干燥和喷雾冷冻技术制备了含布洛芬的微粒。选择三嵌段共聚物泊洛沙姆127作为亲水性表面活性剂,以改善药物颗粒的润湿性,从而提高溶出速率。对所制备的制剂进行体外溶出度和固有溶解度评估。此外,通过扫描电子显微镜(SEM)、差示扫描量热仪(DSC)和傅里叶变换红外光谱(FT-IR)对所制备的药物颗粒进行表征。SEM显示加工后的布洛芬表面形态发生变化,表明药物颗粒有效形成。DSC数据显示所制备颗粒中药物的熔点峰向较低熔点温度偏移,表明存在药物/聚合物相互作用的可能性。喷雾干燥的布洛芬和喷雾干燥的布洛芬/泊洛沙姆127颗粒的溶出度研究结果表明,与对照(布洛芬原料药)相比,药物释放百分比显著(P<0.05)增加。对于喷雾冷冻,所制备的颗粒并未改善药物的溶出度,其溶出度甚至低于对照。DSC和FT-IR结果表明,喷雾干燥降低了药物的结晶度,但对于喷雾冷冻颗粒,无论有无表面活性剂,药物均存在多晶型变化的证据。因此,与喷雾冷冻技术相比,布洛芬的喷雾干燥是改善难溶性药物润湿性、溶解度及溶出行为的有效手段。

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