Enhancement of solubility and dissolution of ibuprofen microparticle prepared by ultrasonic spray drying

Revika Rachmaniar, C. Panatarani, I. Joni, Marline Abdasah, T. Rusdiana
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引用次数: 3

Abstract

Ibuprofen (IBU) is one of the most commonly used nonsteroidal anti-inflammatory drugs with high permeability and low solubility. The aims of this research is to improve the solubility and dissolution of the IBU by reducing particle size using ultrasonic spray drying method and utilizing watersoluble polymer (polyvinyl alcohol (PVA)) and surfactant (sodium lauryl sulphate (SLS)) for particles formulation. The results showed that increasing amount of PVA, smaller particle size of as-prepared IBU-PVA-SLS was obtained, 6.3-fold smaller than untreated IBU. The in vitro drug release study for simulated gastric fluid without enzymes (0.1 N HCl or Buffer pH 1.2) shows the dissolution of prepared IBU-PVA-SLS significantly increase 2.4-fold higher than untreated IBU for dissolution time of 30 minutes. While the solubility of the IBU-PVA-SLS was increased 4.7-fold compare to untreated IBU. In general, IBU possessing relatively high dissolution in intestinal fluid. In contrast, the finding of recent investigation on dissolution of IBU-PVA-SLS is significantly increase in gastric fluid, either due to smaller particles size or PVA-SLS. Thus, despite the PVA and SLS determine the particles formation during polymerization yielding smaller particle size, they also responsible for effective drug delivery system. It was concluded that PVA and SLS in ultrasonic spray drying technique for IBU preparation successfully reduces the particle size and effectively enhances the solubility and dissolution rate of poorly water-soluble IBU in 0.1 N HCl.
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超声喷雾干燥法提高布洛芬微粒的溶解度和溶出度
布洛芬(Ibuprofen, IBU)是最常用的高通透性、低溶解度的非甾体类抗炎药之一。本研究的目的是通过超声波喷雾干燥法减小颗粒尺寸,利用水溶性聚合物(聚乙烯醇(PVA))和表面活性剂(十二烷基硫酸钠(SLS))进行颗粒配方,提高IBU的溶解度和溶解度。结果表明,随着PVA添加量的增加,制备的IBU-PVA- sls的粒径变小,比未处理的IBU小6.3倍。无酶模拟胃液(0.1 N HCl或缓冲液pH 1.2)体外药物释放研究表明,在溶出时间为30分钟时,制备的IBU- pva - sls的溶出度比未处理的IBU显著提高2.4倍。与未治疗的IBU相比,IBU- pva - sls的溶解度提高了4.7倍。一般来说,IBU在肠液中具有较高的溶出度。相比之下,最近对IBU-PVA-SLS溶出的研究发现,胃液中IBU-PVA-SLS的溶出明显增加,这可能是由于颗粒尺寸较小或PVA-SLS所致。因此,尽管PVA和SLS在聚合过程中决定了颗粒的形成,产生更小的颗粒尺寸,但它们也负责有效的药物输送系统。综上所述,PVA和SLS在制备IBU的超声波喷雾干燥技术中成功地减小了IBU的粒径,有效地提高了难水溶性IBU在0.1 N HCl中的溶解度和溶解速率。
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