Effects of subcutaneously implanted sustained-release valsartan preparation on systolic pressure and its plasma concentration
in spontaneously hypertensive rats
LUO Yu-mei 1, JIANG De-qian 2, BAI Yang 3 , LI Chun-ping 3, ZHONG Yan-xia 1,GUO Hong-bo 1, LUO Yu-chan 1, LUO Yu-jun 1
(1. Department of Cardiology, Longgang People′s Hospital,Shenzhen Guangdong 518172; 2. Department of Cardiology, the Second Xiangya Hospital of Central South University, Changsha Hunan 410011; 3. Graduate School of Guangdong Medical University, Zhanjiang Guangdong 524023， China)
Abstract：[Abstract\]Objective: To examine the effectiveness of subcutaneously implanted sustainedrelease 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 sustainedrelease preparation for subcutaneous implantation. SHR were randomly divided into blank control 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 valsartan preparation(100 mg/s) respectively, and SHR in group C were administered with valsartan solutions［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 pressure 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 valsartan 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 twentyfourth 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 smoothly, and achieve a stable target blood pressure as well as oral drugs once day for 2 weeks, and maintain more stable plasma concentration.
［Key words］longacting antihypertention; subcutaneous implantation; sustainedrelease antihypertensive agents; spontaneously hypertensive rat; plasma drug concentration
收稿日期: 2018-03-15
基金资助:
深圳市龙岗区科技计划项目(201505153001018)
作者简介: 罗玉梅（1970—），女，湖南郴州人，主任医师，博士，主要研究方向为高血压
引用本文:
罗玉梅1, 姜德谦2, 白杨3, 李春萍3, 钟艳霞1, 郭洪波1, 罗玉婵1, 罗玉君1. 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, 2008, 28(03): 217-221.
LUO Yu-Mei-1, Jiang-De-Qian-2, Bai-Yang-3, Li-Chun-Ping-3, Zhong-Yan-Xia-1, Guo-Hong-Bo-1, Luo-Yu-Chan-1, Luo-Yu-Jun-1. Effects of subcutaneously implanted sustained-release valsartan preparation on systolic pressure and its plasma concentration
in spontaneously hypertensive rats. Journal of Jiangsu University(Medicine Edition), 2008, 28(03): 217-221.
2008, Vol. 28 
