【摘要】：目的研究溴新斯的明多囊脂質(zhì)體(neostigmine bromide multivesicular liposomes,NB-MVLs)與溴新斯的明(neostigmine bromide,NB)注射劑在大鼠體內(nèi)的藥物代謝動力學(xué)。方法12只健康大鼠,雌雄各半,隨機(jī)分為2組,分別單次皮下注射給予SD大鼠NB-MVLs或NB注射劑(0.15 mg/kg)。采用反相高效液相色譜法測定不同時間點大鼠血漿中NB的濃度,計算藥動學(xué)參數(shù)并進(jìn)行生物等效性分析。結(jié)果 NB-MVLs與NB注射劑給藥后,測得藥時曲線下面積分別為(35.56±4.62)mg·h·L-1和(15.97±5.22)mg·h·L-1,峰濃度(Cmax)分別為(2.49±0.31)mg/L和(4.61±0.91)mg/L,達(dá)峰時間(Tmax)分別為(2.40±0.89)h和(0.45±0.11)h,半衰期分別為(15.14±6.81)h和(1.79±0.27)h,AUC0-t、AUC0-∞及Cmax采用DAS 2.1.1軟件進(jìn)行雙單側(cè)t檢驗和[1-2α]90%可信區(qū)間考察,Tmax采用Wilcoxon非參數(shù)檢驗,生物等效性分析結(jié)果表明NB-MVLs與NB具有生物不等效性。結(jié)論將NB制成多囊脂質(zhì)體后,生物利用度明顯提高,釋放藥物平穩(wěn)緩慢,NB-MVLs與NB具有生物不等效性。
[Abstract]:Objective to study the pharmacokinetics of (neostigmine bromide multivesicular liposomes,NB-MVLs and neostigmine bromide,NB injection in rats. Methods Twelve healthy rats, half male and half female, were randomly divided into two groups. SD rats were given NB-MVLs or NB injection (0.15 mg/kg). The concentration of NB in plasma of rats at different time points was determined by reversed-phase high performance liquid chromatography (RP-HPLC). The pharmacokinetics parameters were calculated and the bioequivalence was analyzed. Results after administration of NB-MVLs and NB injection, the area under the curve was (35.56 鹵4.62) mg 路h 路L-1 and (15.97 鹵5.22) mg 路h 路L-1, respectively. The peak concentration (Cmax) was (2.49 鹵0.31) mg/L and (4.61 鹵0.91) mg/L, respectively. The (Tmax) was (2.40 鹵0.89) h and (0.45 鹵0.11) h, respectively. The half-lives were (15.14 鹵6.81) h and (1.79 鹵0.27) h, respectively. AUC _ 0 and Cmax were tested by DAS 2.1.1 software for double unilateral t test and [1 鈮，

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