| 姜黄素纳米乳的制备和药动学及药效学研究 |
| 投稿时间：2022-09-30 修订日期：2023-05-05 点此下载全文 |
| 引用本文：骆锦前,王婷,尤本明,陈方剑.姜黄素纳米乳的制备和药动学及药效学研究[J].药学实践杂志,2023,41(7):416~421,436 |
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| 基金项目:上海市科委生物医药领域科技支撑项目（16401901900） |
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| 中文摘要:目的 探究姜黄素纳米乳在大鼠体内的药动学特性和对大鼠高脂血症的药效作用。方法 建立大鼠血浆中姜黄素的高效液相色谱-质谱联用（HPLC-MS）含量测定方法，考察纳米乳的体内药动学过程。建立SD大鼠高脂血症动物模型，初步考察姜黄素纳米乳对高脂饮食诱导的大鼠高脂血症的药效作用。结果 体内药动学研究结果表明，以姜黄素原料药为参比制剂，姜黄素纳米乳的相对生物利用度为313.47 %；以市售片剂为参比制剂，姜黄素纳米乳的相对生物利用度为279.52 %。纳米乳组的Cmax为原料药组的201.48 %，为片剂组的193.02 %，且比原料药组及片剂组具有更高的MRT值（为原料药组的183.52 %，是片剂组的154.21 %）。药效学研究结果表明姜黄素纳米乳口服给药系统能显著降低模型大鼠的血清总胆固醇（TC）、低密度脂蛋白（LDLc），缓解高脂饮食给模型大鼠造成的肝脏脂质沉积及肝损伤。结论 姜黄素纳米乳口服给药系统能够有效改善姜黄素的生物利用度，具有良好的降血脂作用，并能够控制高脂血症大鼠体重增长和改善由脂质代谢紊乱造成的肝脏系数变化。 |
| 中文关键词:姜黄素 纳米乳 高脂血症 药代动力学 药效学 |
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| Preparation, pharmacokinetics and pharmacodynamics of curcumin nano emulsion |
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| Abstract:Objective To explore the pharmacokinetic properties of curcumin nano emulsion and its pharmacodynamic effects on hyperlipidemia in rats. Methods The method for determination of curcumin was established by HPLC-MS. The pharmacokinetics characteristics of curcumin nano emulsion oral administration system were investigated. SD rats were used as model animals to establish hyperlipidemia animal models, and the pharmacodynamic effects of curcumin nano emulsion on hyperlipidemia induced by high fat diet was preliminarily investigated. Results The results of pharmacokinetic studies in vivo showed that the relative bioavailability of curcumin nano emulsion was 313.47% with bulk drug group as the reference preparation. The relative bioavailability of curcumin nano emulsion was 279.52 % with tablets as reference preparation. Cmax of curcumin nano emulsion group was 201.48 % of that of bulk drug group and 193.02 % of that of tablet group, and had higher MRT value (183.52 % of that of bulk drug group and 154.21 % of that of tablet group) than bulk drug group and tablet group. Pharmacodynamics research results showed that curcumin nano emulsion oral administration system could significantly reduce the levels of triglyceride and LDL-c in serum of model rats, and relieve liver lipid deposition and liver injury caused by high-fat diet in model animals. Conclusion The oral administration system of curcumin nano emulsion could effectively improve the bioavailability of curcumin, which has a good hypolipidemic effect. It also could control the weight gain of hyperlipidemia rats and improve the changes of liver coefficient caused by lipid metabolism disorder. |
| keywords:Curcumin Nano emulsion Hyperlipidemia Pharmacokinetics Pharmacodynamics |
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