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Preparation and evaluation of fast dissolving ibuprofen-polyethylene glycol 6000 solid dispersions.

机译:快速溶解的布洛芬-聚乙二醇6000固体分散体的制备和评估。

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摘要

To improve its oral absorption, rapidly dissolving ibuprofen solid dispersions (SD) were prepared in a relatively easy, simple, quick, inexpensive, and reproducible manner, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). They were evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and resolidification as revealed by SEM indicated the formation of effective SDs. Absence or shifting toward the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. However, no such interactions in the solid state were confirmed by FTIR spectra that showed the presence of drug crystalline in SDs. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C(max), and a significant decrease in T(max) over pureibuprofen. Preliminary results from this study suggested that the preparation of fast-dissolving ibuprofen SDs by low temperature melting method using PEG 6000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution, and absorption rate of ibuprofen.
机译:为了提高其口服吸收性,以相对容易,简单,快速,廉价且可重现的方式制备了快速溶解的布洛芬固体分散体(SD),其特征在于扫描电子显微镜(SEM),差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)。对它们在大鼠中的布洛芬的溶解度,体外释放和口服生物利用度进行了评估。 SEM显示,熔融和再凝固过程中单个表面性能的损失表明形成了有效的SD。在SD和DSC研究中,药物混合物和物理混合物中药物峰的熔融温度不存在或朝较低熔点方向移动表明药物-聚合物相互作用的可能性。但是,FTIR光谱未显示固态中的此类相互作用,FTIR光谱显示SD中存在药物晶体。大鼠肠中布洛芬从SD释放的更快导致AUC和C(max)显着增加,而T(max)显着低于pureibuprofen。这项研究的初步结果表明,采用PEG 6000作为可熔融亲水聚合物载体的低温熔融方法制备快速溶解的布洛芬SD可能是提高布洛芬的溶解度,溶解度和吸收率的一种有前途的方法。

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