大蒜素衍生物烯丙基半胱氨酸缓释制剂的制备及其体内药物动力学考察

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Abstract Objective To prepare sustained-release granules of S-allylcysteine(SAC)of a kind of water-soluble allicin derivatives to improve its bioavailability in rats.Methods In this experiment,the formulation was selected from the types of excipients,the ratio of main drugs and excipients and the dosage of release regulator.The preparation method was screened from the preparation temperature,heating time and the particle size of solid dispersion.Eudragit ® RS 30D was selected as blocking agent and solvent evaporation method was used to prepare the solid dispersion.The formulation and process were optimized by orthogonal design and characterized by differential scanning calorimetry(DSC)and X-ray diffraction(XRD).Blood samples were collected at 0.1,0.5,1,2,3,4,5,6,8,10,12,24 and 48 h after oral administration(35 mg/kg).The plasma concentration of SAC was determined by high performance liquid chromatography(HPLC)and the pharmacokinetic parameters were calculated.Results Eudragit ® RS 30D was used as carrier,SAC to carrier mass ratio of 1∶8,using solvent evaporation at 60℃heating for 24 h,the prepared SAC solid dispersion has good sustained release effect and good stability(RSD was 3.1%).XRD showed that no new peak appeared and phase characterization showed that SAC was highly dispersed in the carrier in amorphous or molecular state.The Cmax and Tmax of SAC solid dispersion were(5.46±1.31)μg/ml and(5.23±1.18)h and the relative bioavailability was 140.42%.Conclusion The method screened out in this study can be used for the preparation of water-soluble drug sustained-release preparations.SAC solid dispersions can significantly improve the bioavailability of SAC and prolong the effective time of drugs.

Key words： S-allylcysteine Solid dispersion Sustained-release preparation Pharmacokinetics

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LIU Xu. Preparation and pharmacokinetic study in vivo of allicin derivative S-allylcysteine sustained-release preparation[J]. 中国当代医药, 2021, 28(27): 17-18.

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http://dangdaiyiyao.com/EN/ OR http://dangdaiyiyao.com/EN/Y2021/V28/I27/17

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