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吡罗昔康在固体分散体系统中的溶出度和生物利用度的提高。

Enhancement of dissolution and bioavailability of piroxicam in solid dispersion systems.

作者信息

Pan R N, Chen J H, Chen R R

机构信息

School of Pharmacy, College of Medicine, National Taiwan University, Republic of China.

出版信息

Drug Dev Ind Pharm. 2000 Sep;26(9):989-94. doi: 10.1081/ddc-100101327.

Abstract

Solid dispersion systems of water-insoluble piroxicam in polyethylene glycol (PEG) 4000 and in urea were prepared by fusion and solvent methods and were characterized in this study. The in vitro dissolution studies showed that the dispersion systems containing piroxicam and PEG4000 or urea gave faster dissolution than the corresponding simple mixtures. The differential scanning calorimetry (DSC) study indicated that the piroxicam-PEG system prepared by the fusion method is a solid dispersion, while the piroxicam-urea system prepared by the solvent method is likely to be a solid solution of piroxicam in urea. The storage testings showed that all dispersions were stable, except that uptake of water during storage may occur in the PEG system. A single-dose study with rabbits showed that the dispersion systems provided statistically significant to a higher extent and rate of bioavailability than the corresponding physical mixture (p < 0.05).

摘要

采用熔融法和溶剂法制备了水不溶性吡罗昔康在聚乙二醇(PEG)4000和尿素中的固体分散体系统,并在本研究中对其进行了表征。体外溶出度研究表明,含有吡罗昔康和PEG4000或尿素的分散体系统比相应的简单混合物具有更快的溶出度。差示扫描量热法(DSC)研究表明,通过熔融法制备的吡罗昔康-PEG系统是一种固体分散体,而通过溶剂法制备的吡罗昔康-尿素系统可能是吡罗昔康在尿素中的固溶体。储存试验表明,所有分散体均稳定,但PEG系统在储存期间可能会吸水。对兔子进行的单剂量研究表明,与相应的物理混合物相比,分散体系统在生物利用度的程度和速率上具有统计学意义上的显著提高(p < 0.05)。

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