Pharmacokinetic Characteristics of Gualou-Xiebai Intragastric Floating Pellets in Rats by LC-MS / MS

doi:10. 3969/j. issn. 2096-2266. 2021. 10. 001

Abstract

Abstract:

Objective： To study the plasma concentration and pharmacokinetics of 3，29-dibenzoyl-karounitriol （3，29-DK） in Gualou-Xiebai intragastric floating pellets （hereinafter referred to as "Gualou-Xiebai pellets"） at different time points in rats by liquid chromatography tandem mass spectrometry（LC-MS/MS）. Methods： 12 SPF SD male rats were randomly divided into Gualou- Xiebai pellets group（2.0 g/kg） and Gualou-Xiebai extracts group（1.4 g/ kg）， the blood samples were taken from the orbit 0 h before administration and 0.5， 1， 2， 3， 4， 6， 8， 10， 12， 24， 36， 48 h after administration in Gualou-Xiebai pellets group， the blood samples were taken from the orbit 0 h before administration and 5，10，30 min， 1， 1.5， 2， 3， 4， 6 and 8 h after administration in the Gualou-Xiebai extracts group， and the pharmacokinetic parameters were calculated. Results： Compared with the Gualou-Xiebai extracts group， the 3，29-DK peak time， AUC and t1/2 in the Gualou-Xiebai pellet group were significantly prolonged （P<0.05）， and MRT was significantly increased （P<0.05）， CLz/F， Cmax was significantly reduced （P<0.05）. Conclusion： The release rate of 3，29-DK in Gualou-Xiebai pellets was stable in rats， without sudden release and rapid release， and the metabolic time was prolonged. Gualou-Xiebai pellets have sustained-release effect.

Key words: LC-MS/MS； Gualou-Xiebai intragastric floating pellets； 3, 29-dibenzoyl-karounitriol； pharmacokinetics

CLC Number:

R965

Yan Haiyan, Sun Dekao, Zou Chuncai.

Pharmacokinetic Characteristics of Gualou-Xiebai Intragastric Floating Pellets in Rats by LC-MS / MS [J]. Journal of Dali University, 2021, 6(10): 1-.

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References

〔1〕鄢海燕，孙德考，邹纯才，等.引药米酒对瓜蒌薤白中3，29-DK的药代动力学的影响〔J〕.大理大学学报，2018，3（8）：1-5.

〔2〕游晓勇，郭义然，李金生.瓜蒌薤白半夏汤加减配合地奥心血康治疗冠心病42例疗效观察〔J〕.中国民族民间医药，2016，25（7）：78.

〔3〕孙德考，邹纯才，鄢海燕，等.瓜蒌薤白胃内漂浮微丸的制备及体外释放度测定〔J〕.国际药学研究杂志，2019，46（5）：398-404.

〔4〕邹纯才，徐启祥，鄢海燕，等.不同配伍比例的瓜蒌皮-瓜蒌子与瓜蒌的化学指纹特征相似性研究〔J〕.国际药学研究杂志，2017，44（3）：278-281.

〔5〕冯果，吴增光，何新，等.UPLC-MS/MS分析瓜蒌子中3，29-二苯甲酰基栝楼仁三醇在大鼠体内的组织分布情况〔J〕.中国实验方剂学杂志，2017，23（21）：86-92.

〔6〕 ZHAO C， ZHANG N， CHEN B， et al. A Rapid and Sensitive LC-MS/MS Method for Quantification of 3，29-Dibenzoyl Rarounitriol in Rat Plasma： Application to a Pharmacokinetic Study〔J〕. Biomed Chromatogr，2015，29（8）：1229-1234.

〔7〕薛钧升，姚庆宇，李健，等.液相色谱-质谱串联定量测定裸鼠血浆中的来曲唑：方法学建立、验证以及药物动力学研究应用〔J〕.中国药学杂志，2018，27（10）：665-674.

〔8〕宋妍.HPLC-MS/MS法测定大鼠血浆中紫杉醇含量及其脂质体药代动力学研究〔J〕.天津医科大学学报，2019，25（3）：292-295.

〔9〕燕晓晶，王佳，杜光光，等.HPLC-MS/MS法研究奥克梯隆型皂苷元在比格犬血浆中的药代动力学特征〔J〕.中药新药与临床药理，2019，30（1）：66-71.

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[2]	Wang Yanquan, Zhang Honghan, Lü Hong, Li Cailin, Najib Mohammerd, Peng Fang, Wu Dingyu. Study on Reversal of Multidrug Resistance of Drug-Resistant Cell Lines by Polypeptide PAE2 from Periplaneta americana [J]. Journal of Dali University, 2021, 6(8): 1-6.
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[6]	Li Yan, Shao Mingyuan, Guo Chao, Yang Qiangli, Cao Chang'e, Lai Yong. Therapeutic Effects of Ganlong Capsule on Liver Fibrosis in Rats Induced by Pig Serum [J]. , 2018, 3(10): 13-17.
[7]	Zhang Handan, Wu Daoxun, Zhang Haizhu, Li Yang. Effects of Ethanol Extracts of Blaps rynchopetera Fairmaire on Proliferation of Human Embryonic Lung Diploid Fibroblast [J]. , 2018, 3(10): 18-21.
[8]	YAN Hai-Yan, SUN De-Kao, JU Chun-Cai, ZHANG Min-Jie. Effect of Rice Wine as Cites Drug on Pharmacokinetics of 3,29-DK in Gualou-Xiebai [J]. , 2018, 3(8): 1-5.
[9]	Li-Chun-Yan, CHEN Jin-Ru, DONG Shou-Tang, LIU Xi, HAO Fang-Fang, LI Dong-Mei, LI Dan-Dan. A Study of Anti-hepatic Fibrosis Activities of Extracts from Walnut Shell of Juglans sigillata D. in Vitro [J]. , 2018, 3(4): 5-11.
[10]	Liu-Xi, XU Dong-Mei, CHEN Jin-Ru, GAO Bei, LI Dong-Mei, LI Chun-Yan. A Study of the Anti-lung Cancer Activities of the Extracts from Pineconeof Pinus yunnanensis Franch. in Vitro [J]. , 2018, 3(4): 17-23.
[11]	Xia Mengkai, Zeng Jing, Niu Chunli, Peng Fang. Effect of Ganlong Capsule and Periplaneta americana Skimmed Cream on Bile Secretion of Normal Rats [J]. J4, 2015, 14(2): 4-7.
[12]	Zhou Shubo, Zhang Bensi. A Study of Effects and Mechanism of Pitavastatin on Monocrotaline-induced Pulmonary Arterial Hypertension in Rats [J]. J4, 2015, 14(2): 16-20.