江苏大学学报（医学版）2018，Vol.28Issue(3)：217-221,5.DOI:10.13312/j.issn.1671-7783.y180071
皮下埋植缬沙坦缓释制剂对自发性高血压大鼠血压及血药浓度的影响
Effects of subcutaneously implanted sustained-release valsartan preparation on systolic pressure and its plasma concentration in spontaneously hypertensive rats
摘要
Abstract
Objective:To examine the effectiveness of subcutaneously implanted sustained-release valsartan preparation on systolic pressure and plasma drug concentration in spontaneously hypertensive rat (SHR). Methods: The valsartan original medicine was loaded into a silicone tube and sealed to be a sustained-release preparation for subcutaneous implantation. SHR were randomly divided into blank con-trol group(group A),valsartan implant group(group B),valsartan gavage group(group C),and SHR in group A and group B were implanted subcutaneously with blank silicone tube and sustained-release val-sartan preparation(100 mg/s) respectively,and SHR in group C were administered with valsartan solu-tions[16 mg/(kg·d)] by gavage. Healthy Wistar rats were used as the normal control group (group D),and the sham operation was performed. All groups were administered for fifteen days. Mean blood pressure of the rat tail artery and plasma concentration were monitored regularly. Results:Systolic pres-sure of SHR in group B and group C were lower than that of SHR in group A(P<0.05) after seven days of intervention,but there was no statistical difference found between group C and group B. This trend has been maintained until the end of the experiment. After two hours of treatment,the plasma level of valsar-tan of SHR in group B reached a stable level. However,the plasma level of valsartan of SHR reached the peak at 2 hours after first gavaged with valsartan in goup C,which was 4.8 times as high as that of SHR in group B. Then,plasma level of valsartan of SHR in group C decreased gradually,and was lower than that of SHR in group B(P<0.05) at twenty-fourth hours(the next day,before gaving medicine). With gavaging by valsartan once a day,the lowest plasma level of valsartan of SHR in group C was increased gradually,and reached the level that of SHR in group B(P>0.05) after intervention of 48 hours, and remained this trend at the end of the experiment. Conclusion: Subcutaneous implantation of valsartan sustained-release preparation,only single treatment,can reduce SHR systolic pressure long and smooth-ly,and achieve a stable target blood pressure as well as oral drugs once day for 2 weeks, and maintain more stable plasma concentration.关键词
长效降压/皮下埋植/缓释降压制剂/自发性高血压大鼠/血药浓度Key words
long-acting antihypertention/subcutaneous implantation/sustained-release antihyperten-sive agents/spontaneously hypertensive rat/plasma drug concentration分类
医药卫生引用本文复制引用
罗玉梅,姜德谦,白杨,李春萍,钟艳霞,郭洪波,罗玉婵,罗玉君..皮下埋植缬沙坦缓释制剂对自发性高血压大鼠血压及血药浓度的影响[J].江苏大学学报（医学版）,2018,28(3):217-221,5.基金项目
深圳市龙岗区科技计划项目(201505153001018) （201505153001018）
