皮下埋植超长效氨氯地平制剂对自发性高血压大鼠血压及血药浓度的影响

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Abstract

Objective: To investigate the effects of super longacting subcutaneous implantable sustainedrelease amlodipine preparation on blood pressure and blood concentration of amlodipine in spontaneous hypertensive rats （SHR）. Methods: The carrier was synthesized with high molecular polymer polycaprolactone, and amlodipine raw material was added to make a slowrelease antihypertensive preparation that could be implanted subcutaneously. SHR was randomly divided into model control group, blank carrier group, drug gavage group, and sustainedrelease hypotension group, with 8 rats in each group. Another 8 male WKY rats were used as normal control group. The blank carrier and amlodipine sustainedrelease preparation were implanted under the skin of the neck and back of the blank carrier group and the sustainedrelease hypotension group, respectively. Amlodipine solution （0.45 mg/kg） was given to the SHR in the drug gavage group, and the rats in the normal control group and model control group were given the same volume of distilled water.During the intervention period，the rats′ tail arterial blood pressure was measured and venous blood was collected to detect the blood drug concentration regularly, and corresponding intervention lasted for 88 days. Results: From the 5th day after intervention, systolic blood pressure, diastolic blood pressure and mean arterial pressure of SHR in drug gavage group and sustainedrelease hypotension group were lower than those of the model control group （P<0.01）, and there was no statistical difference between the above groups and the normal control group （P>0.05）.Compared with drug gavage group, there was no significant difference in SHR systolic blood pressure, diastolic blood pressure and mean arterial pressure in sustainedrelease hypotension group （P>0.05）. Amlodipine concentration of SHR in sustainedrelease hypotension group reached a stable level on the 3rd day and remained until the 88th day after intervention. Conclusion: Subcutaneous implantation of super longacting subcutaneous implantable sustainedrelease amlodipine preparation, with one dose， could steadily reduce SHR blood pressure standards for 88 days and maintain a stable blood concentration.

Received: 29 September 2020

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	Articles by authors
	LU Lijuan1
	LUO Yumei2
	ZENG Guirong3
	WANG Wenfeng2

Cite this article:

LU Lijuan1,LUO Yumei2,ZENG Guirong3等.

Effect of super long-acting subcutaneous implantable sustained-release amlodipine preparation on blood pressure and drug concentration in spontaneously hypertensive rats

[J]. Journal of Jiangsu University(Medicine Edition), 2021, 31(02): 134-138.

URL:

http://zzs.ujs.edu.cn/xbyxb/EN/ OR http://zzs.ujs.edu.cn/xbyxb/EN/Y2021/V31/I02/134

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