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Research of Sustained-Release Pellets of Loxoprofen Soudium

Author: TangLinZuo
Tutor: WangJing；WangZhongYan
School: Shenyang Pharmaceutical University
Course: Pharmacy
Keywords: Loxoprofen sodium Sustained-release pellets Intestinal absorption Extrusion spheronization Pharmacokinetics
CLC: R94
Type: Master's thesis
Year: 2006
Downloads: 80
Quote: 1
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Abstract

Sodium loxoprofen (Loxoprofen sodium, Loxo) benzenepropanoic acid non-steroidal anti-inflammatory drugs (NSAID), is a prodrug . Its pharmacologically active metabolites Trans - OH , having excellent anti-inflammatory analgesic effect , clinically used for the treatment of chronic rheumatoid arthritis, osteoarthritis , periarthritis and other inflammatory . The This paper sodium sustained-release pellets prepared loxoprofen to achieve reduced toxicity to maintain a steady blood concentration , improve patient compliance purpose of The preformulation studies have shown that : loxoprofen sodium in different pH solutions solubility differences ; within the scope of the study , the oil / water partition coefficient decreases with increasing pH value . In rat intestine absorption test results show that : the sodium absorption in the bowel loxoprofen good , non-specific absorption mechanism of drug absorption in the intestine by passive diffusion . Extrusion - spheronization , indicators such as yield , roundness , through the prescription process factors visits and orthogonal test , prepared loxoprofen sodium pellets . Uses of Eudragit ( ? ) NE 30D aqueous dispersion as a coating material , loxoprofen sodium pellets using a fluidized bed suspension coating method , the sustained-release coated . Release as an indicator single factor established coating process . Vitro release profile of sustained-release pellets of the drug release mechanism meets a kinetic equation . The test results show that the influencing factors , sustained-release pellets of light, heat stable . Preliminary stability test results show that the formulation is stable . To the sodium ordinary loxoprofen piece reference preparation , homemade sustained-release pellets Beagle dogs single dose pharmacokinetic study . Preparation of reference substance of the active metabolite of Trans-OH , simultaneous determination of the plasma concentration of Loxo and Trans-OH . The pharmacokinetic parameters calculated results show that the absorption process of loxoprofen sodium sustained-release pellets Beagle dogs with sustained release characteristics . Loxo and Trans-OH relative bioavailability of 96.43% and 101.91% , respectively . Statistical analysis method in the AUC _{- ∞ < / sub > ( Loxo ) and the AUC _{, , 0 - ∞ ( Trans - OH) to evaluate the extent of absorption of the two formulations are bioequivalent . Deconvolution method of sustained release pellets in vivo results show good correlation .}}

Research of Sustained-Release Pellets of Loxoprofen Soudium

Abstract

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