摘要
目的:研究紫苏醇(POH)溶液(POH-SL)、POH亚微乳(POH-SE)与POH壳聚糖亚微乳(POH-CSSE)在大鼠体内的药动学特征。方法:将大鼠随机分为POH-SL组、POH-SE组及PH-CSSE组,每组6只,尾静脉注射相应药物65 mg/kg,采用高效液相色谱法检测给药后5、10、15、30、45、60、120、240、360、480、600 min的血药浓度,Kinetica 4.4.1软件计算药动学参数。色谱条件:色谱柱为Agilent Zorbax XDB C18,流动相为乙腈-水(40∶60),流速为1.0 ml/min,检测波长为210 nm,柱温为30℃,进样量为20μl。结果:POH检测质量浓度的线性范围为0.05~25μg/m(lr=0.999 6),平均方法回收率为(95.64±0.03)%^(98.65±0.09)%,RSD≤8.62%(n=5)。POH-SL、POH-SE、POH-CSSE的药动学参数分别为t1/2β(81.65±0.107)、(121.58±0.021)、(130.69±0.031)min,AUC0-∞(4 944.19±0.024)、(6 716.22±0.044)、(7 008.46±0.035)mg·min/L,K10(0.005 397±0.012)、(0.004 216±0.012)、(0.004 186±0.013)min-1;其中与POH-SL比较,POH-SE和POH-CSSE的t1/2β、AUC0-∞明显增加(P<0.05)。结论:POH-CSSE在体内有较好的长循环作用,有助于延长POH的吸收。
OBJECTIVE： To study the pharmacokinetics characteristics of Perillyl alcohol （POH） solution （POH-SL）, Perillyl alcohol submicron emulsions （POH-SE） and Perillyl alcohol chitosan submicron emulsions （POH-CSSE） in rats. METHODS： Rats were randomly divided into POH-SL group, POH-SE group and POH-CSSE group with 6 rats in each group. They were given rele- vant medicines 65 mg/kg intravenously via tail vein. The lzlasma concentrations of POH were determined by HPLC 5, 10, 15, 30, 45, 60, 120, 240, 360, 480 and 600 min after medication. The pharmacokinetic parameters of POH were calculated by Kinetica 4.4.1 software. The determination was performed on Agilent Zorbax XDB Ct8 column with mobile phase consisted of acetonitrile-wa- ter （40 ： 60） at the flow rate of 1.0 ml/min. The detection wavelength was set at 210 nm and column temperature was 30 C. The sample size was 20 ul. RESULTS： The linear range of POH were 0.05-25 μg/ml （r=0.999 6） with average recovery of （95.64 ＋ 0.03）%-（98.65 ＋ 0.09）% （RSD〈8.62%, n=5）. The pharmacokinetic parameters of POH-SL, POH-SE and POH-CSSE were as follows： t~/2~ （81.65 ＋ 0.107） min, （121.58 ＋ 0.021） min and （130.69 ＋ 0.031） min; AUC0-~ ： （4 944.19 ＋ 0.024） mg-min/L, （6 716.22 ＋ 0.044） mg.min/L and （7 008.46 ＋ 0.035） mg.min/L; /（10：（0.005 397 ＋ 0.021） min-t, （0.004 216 ＋ 0.012） min-1 and （0.004 186 ＋ 0.013） mill-1. Compared with POH-SL and AUC0- of POH-SE and POH-CSSE were increased significantly （P〈 0.05）. CONCLUSIONS： POH-CSSE has a better long-circulating effect in rats, which can extend absorption of POH.
出处
《中国药房》
CAS
CSCD
2013年第45期4255-4257,共3页
China Pharmacy
关键词
紫苏醇
壳聚糖
亚微乳
大鼠
药动学
Perillyl alcohol
Chitosan
Submicron er~ ulsion
Rats
Pharmacokinetics
