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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摘要目的: 探讨皮下埋植超长效缓释氨氯地平制剂对自发性高血压大鼠（spontaneously hypertensive rats，SHR）血压及血液中药物浓度的影响。方法: 用高分子聚合物聚己内酯合成载体，加入氨氯地平原料药制成可皮下埋植的缓释降压制剂。将雄性SHR随机分成模型对照组、空白载体组、药物灌胃组、缓释降压组，每组8只；另取8只雄性WKY大鼠作为正常对照组。将空白载体、氨氯地平缓释制剂分别植入空白载体组及缓释降压组SHR的颈背部皮下，药物灌胃组SHR予以氨氯地平溶液（0.45 mg/kg）灌胃，正常对照组、模型对照组大鼠给予同体积蒸馏水灌胃。干预期间，定期测定各组大鼠尾动脉血压，采静脉血检测血浆药物浓度，共干预88 d。结果：从干预后第5天开始，氨氯地平药物灌胃组及缓释降压组SHR收缩压、舒张压及平均动脉压均低于模型对照组（P<0.01），与正常对照组WKY大鼠差异无统计学意义（P>0.05）；与药物灌胃组比较，缓释降压组SHR收缩压、舒张压及平均动脉压差异无统计学意义（P>0.05）。缓释降压组SHR氨氯地平血药浓度于第3天开始达到稳定水平，一直维持到干预后第88天。结论：皮下埋植超长效氨氯地平缓释制剂，用药1次，即可平稳降低SHR血压达标维持88 d，且能维持稳定的血药浓度。

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	卢丽娟 1
	罗玉梅2
	曾贵荣3
	王文峰2

关键词 ：皮下埋植, 超长效缓释降压制剂, 自发性高血压大鼠, 血药浓度

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.

收稿日期: 2020-09-29

基金资助:深圳市龙岗区科技计划（医疗卫生类）项目（LGKCYLWS2018000067）

作者简介: 卢丽娟（1992—），女，硕士研究生

引用本文:

卢丽娟 1，罗玉梅2，曾贵荣3，王文峰2. 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[J]. 江苏大学学报:医学版, 2021, 31(02): 134-138. LU Lijuan1， LUO Yumei2， ZENG Guirong3， WANG Wenfeng2.

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

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

链接本文:

http://zzs.ujs.edu.cn/xbyxb/CN/ 或 http://zzs.ujs.edu.cn/xbyxb/CN/Y2021/V31/I02/134

［1］胡盛寿, 高润霖, 刘力生, 等.《中国心血管病报告2018》概要\[J\].中国循环杂志, 2019, 34（3）:209-220.

［2］罗玉梅, 姜德谦, 白杨, 等.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.

［3］Pohlmann AR, Fonseca FN, Paese K, et al. Poly（εcaprolactone） microcapsules and nanocapsules in drug delivery\[J\].Expert Opin Drug Deliv, 2013, 10（5）:623-638.

［4］李佳璞. 聚己内酯基质型给药系统制备及释药性能研究\[D\].西安：西安科技大学,2020.

［5］王诺，田武，王成伟. 一种戈舍瑞林缓释植入剂的制备方法\[P\]. 中国专利：CN 102755627A , 2012-10-31.

［6］张超,王海,庞丽云,等.聚己内酯埋植剂的制备及药物通透性研究\[J\].国际生物医学工程杂志,2014,37（5）:279-282.

［7］吴莹,张彩萍,濮娜.缓释药用材料的发展及缓释型降血压药物应用特点\[J\].中国组织工程研究与临床康复,2010,14（21）:3895-3898.

［8］孔华．尼莫地平渗透泵控释片\[D\].武汉：武汉工程大学，2013.

［9］邱凯锋，姚少毅，邓丽华．高效液相色谱法测定乌拉地尔缓释胶囊的含量及有关物质\[J\]．中国医院药学杂志，2011，31（23）：1983-1984.

［10］梁爽,王立,宋春晓,等.缓控释技术在药物防治心血管疾病中的应用\[J\].中国医院药学杂志,2017,37（11）:1112-1115.

［11］Yang Z, Yu J, Yang T, et al. A method for the preparation of sustained releasecoated Metoprolol Succinate pelletcontaining tablets\[J\]. Pharm Dev Technol， 2016，21（8）:943-950.

［12］Kumaravelrajan R, Narayanan N, Suba V. Development and evaluation of controlled porosity osmotic pump for nifedipine and metoprolol combination\[J\]. Lipids Health Dis， 2011，10:51.

［13］Jonat W. Overview of luteinizing hormonereleasing hormone agonists in early breast cancerbenefits of reversible ovarian ablation\[J\]. Breast Cancer Res Treat, 2002, 75（Suppl 1）:23-26.

［14］钱翠凤,黄紫蓉.皮下埋植避孕剂的研究进展\[J\].国际生殖健康/计划生育杂志,2013,32（2）:107-110.

［15］Shephard CJ, Drovandi AD. Sustainedrelease subdermal buprenorphine implants: the future of opioid use disorder management\[J\].J Pharm Pract Res，2019, 49（1）:41-49.

［16］宋云，钟霞.促性腺激素释放激素激动剂类药物缓控释制剂研究进展\[J\]. 中国新药杂志,2017,26（3）:300-303.

［17］王文雯.卡莫司汀植入剂治疗脑胶质瘤的研究进展\[J\]. 中国肿瘤临床与康复,2015,22（2）:254-256.

［18］白杨,万新红,罗玉梅,等.皮下埋植缓释剂临床应用的研究进展\[J\].医学理论实践,2017,30（7）:975-977.

［19］吴建明, 高小平, 柯潇, 等. 氨氯地平联用松龄血脉康胶囊对大鼠的血药浓度及降压作用的影响\[J\].华西药学杂志, 2012, 27（6）: 646-649.