| 摘要: |
| 目的 研究溴新斯的明多囊脂质体(neostigmine bromide multivesicular liposomes,NB-MVLs)与溴新斯的明(neostigmine bromide,NB)注射剂在大鼠体内的药物代谢动力学。方法 12只健康大鼠,雌雄各半,随机分为2组,分别单次皮下注射给予SD大鼠NB-MVLs或NB注射剂(0.15 mg/kg)。采用反相高效液相色谱法测定不同时间点大鼠血浆中NB的浓度,计算药动学参数并进行生物等效性分析。结果 NB-MVLs与NB注射剂给药后,测得药时曲线下面积分别为(35.56±4.62) mg·h·L-1和(15.97±5.22) mg·h·L-1,峰浓度(Cmax)分别为(2.49±0.31) mg/L和(4.61±0.91) mg/L,达峰时间(Tmax)分别为(2.40±0.89) h和(0.45±0.11) h,半衰期分别为(15.14±6.81) h和(1.79±0.27) h,AUC0-t、AUC0-∞及Cmax采用DAS 2.1.1软件进行双单侧t检验和[1-2α] 90%可信区间考察,Tmax采用Wilcoxon非参数检验,生物等效性分析结果表明NB-MVLs与NB具有生物不等效性。结论 将NB制成多囊脂质体后,生物利用度明显提高,释放药物平稳缓慢,NB-MVLs与NB具有生物不等效性。 |
| 关键词: 溴新斯的明 多囊脂质体 药代动力学 生物利用度 |
| DOI：10.3724/SP.J.1008.2015.00459 |
| 投稿时间：2014-09-29修订日期：2014-12-09 |
| 基金项目: |
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| Pharmacokinetics of neostigmine bromide multivesicular liposomes in rats |
| LEI Ting-ting1,LUO Wen2,ZHAO Hua1,HE Dan1,ZHANG Jing-qing1* |
(1. Medicine Engineering Research Center in University, Chongqing Medical University, Chongqing 400016, China;
2. Department of Pharmacy, Second Affiliated Hospital of Chongqing Medical University, Chongqing 400010, China
*Corresponding author) |
| Abstract: |
| Objective To study the pharmacokinetics of neostigmine bromide multivesicular liposomes (NB-MVLs) and conventional neostigmine bromide (NB) injection in rats. Methods Twelve healthy rats, half male and half female, were randomly divided into two groups. One group was injected with NB-MVLs and the other with reference NB (0.15 mg/kg). RP-HPLC was used to examine neostigmine concentrations in rat plasma at different time points, and the pharmacokinetic parameters and relative bio-availability were calculated. Results Pharmacokinetic parameters of NB-MVLs and NB were as follows: AUC0-t (35.56±4.62) mg·h·L-1 vs (15.97±5.22) mg·h·L-1;Tmax(2.40±0.89) h vs (0.45±0.11) h; Cmax (2.49±0.31) mg/L vs (4.61±0.91) mg/L; and t1/2 (15.14± 6.81) h vs (1.79±0.27) h, respectively. AUC0-t, AUC0-∞ and Cmax were studied by DAS 2.1.1 software for double unilateral t test and [1-2α] 90% confidence interval, and Tmax was precessed by Wilcoxon nonparametric test to evaluate the bioequivalence of NB-MVLs and NB. The result showed that NB-MVLs and NB were not bioequivalent. Conclusion Neostigmine in the form of multivesicular liposomes has improved bioavailability and stable drug release; NB-MVLs and NB are not bioequivalent. |
| Key words: neostigmine bromide multivesicular liposomes pharmacokinetics biological availability |
