[1] Zhang Niping, Yu Shuqin, Wang Hui, Shen Yanyan, et al. Method for quantification of prazosin in dog plasmaand its application to pharmacokinetic study [J]. Journal of Southeast University (English Edition), 2011, 27 (2): 217-221. [doi:10.3969/j.issn.1003-7985.2011.02.022]

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Method for quantification of prazosin in dog plasmaand its application to pharmacokinetic study()

狗血浆中哌唑嗪的含量测定方法及其在药代动力学中的应用

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Journal of Southeast University (English Edition)[ISSN:1003-7985/CN:32-1325/N]

Volumn:

27

Issue:

2011 2

Page:

217-221

Research Field:

Chemistry and Chemical Engineering

Publishing date:

2011-06-30

Info

Title:

Method for quantification of prazosin in dog plasmaand its application to pharmacokinetic study

狗血浆中哌唑嗪的含量测定方法及其在药代动力学中的应用

Author(s):

Zhang Niping¹;  Yu Shuqin²;  Wang Hui²;  Shen Yanyan¹;  3;  Xu Shi¹;  Zhang Ling¹;  Xu Qian¹;  3

¹ Ministry of Education Key Laboratory of Environmental Medicine and Engineering, Southeast University, Nanjing 210009, China
² Jiangsu Key Laboratory for Medical Supermolecule Material and Application, Nanjing Normal University, Nanjing 210046, China
³ Suzhou Key Laboratory of Environment and Biosafety, Suzhou Institute, Southeast University, Suzhou 215123, China

张妮萍¹;  余书勤²;  王辉²;  申艳艳¹;  3;  徐师¹;  张玲¹;  许茜¹;  3

¹东南大学环境医学工程教育部重点实验室, 南京 210009; ²南京师范大学江苏省医药超分子及应用重点实验室, 南京 210046; ³东南大学苏州研究院苏州市环境与生物安全重点实验室, 苏州 215123

Keywords:

prazosin(PZS);  PZS-sulfobutyl ether beta-cyclodextrin(PZS-SBE-β-CD)inclusion complex tablets;  high performance liquid chromatography(HPLC);  pharmacokinetics

哌唑嗪;  PZS-SBE-β-CD包合物片剂;  高效液相色谱;  药物代谢动力学

PACS:

O657

DOI:

10.3969/j.issn.1003-7985.2011.02.022

Abstract:

A simple and sensitive high performance liquid chromatography method using fluorescence detection(HPLC-FLD)and a one-step single solvent extraction for the determination of prazosin(PZS)in dog plasma is developed and validated. After extraction with ether, the chromatographic separation of PZS is carried out using a reverse phase C18 column(150 mm×4.6 mm, 5 μm)with a mobile phase of 30% acetonitrile and 70% acetic acid-sodium acetate buffer solution(pH=3.6)and quantified by fluorescence detection operated with an excitation wavelength of 258 nm and an emission wavelength of 387 nm. The flow rate of the mobile phase is 1.0 mL/min and the retention time of PZS and the internal standard is found to be 4.4 and 5.8 min, respectively. The calibration curve is linear within a concentration range from 1.0 to 1 000.0 ng/mL(r²>0.998). The limit of detection is 0.4 ng/mL. The inter-day coefficient of variation(COV)of the calibration standards is below 5.0% and the mean accuracy is in the range from 92.7% to 104.2%. Moreover, by analyzing quality control plasma samples for three days, the results show that the method is precise and accurate, for the intra- and inter-day COV within 10% and the accuracy from 95.9% to 112.7%. The developed and validated method is successfully applied to pharmacokinetic study for the preclinical evaluation of a new peroral PZS-sulfobutyl ether beta-cyclodextrin(PZS-SBE-β-CD)inclusion complex tablets(test preparation), which demonstrates that the test preparation released PZS is conducted in a slow and controlled way, and the relative bioavailability of the test preparation is found to be 105.0%.

建立并评价了一种简单灵敏的方法测定狗血浆中PZS的含量.该方法利用HPLC-FLD结合乙醚萃取的前处理方法, 采用C18色谱柱(150 mm×4.6 mm, 5 μm), 流动相为30%乙腈和70%乙酸-乙酸钠缓冲液(pH=3.6), 荧光检测器的激发波长为258 nm, 发射波长为387 nm, 在流动相流速为1.0 mL/min 时, 其PZS和内标物的保留时间分别为4.4和5.8 min.标准曲线在1.0~1 000.0 ng/mL的浓度范围内呈线性相关(r²> 0.998), 检出限为0.4 ng/mL, 标准曲线的日间变异系数低于5.0%, 准确度在92.7%~104.2%范围内.在3 d的分析质量控制研究中, 日内和日间精密度均小于10%, 准确度为95.9%~112.7%.该方法成功应用于一种新的口服制剂(PZS-磺丁基醚-β-环糊精包合物)的临床前期药代动力学评价, 结果表明:该新型的包合药物具有缓释PZS的功效, 且其相对生物利用率为105.0%.

References:

[1] Solomon H M, Wier P J, Ippolito D L, et al. Effect of prazosin on sperm transport in male rats[J]. Reproductive Toxicology, 1997, 11(4): 627-631.
[2] de Mey C, Michel M C, McEwen J, et al. A double-blind comparison of terazosin and tamsulosin on their differential effects on ambulatory blood pressure and nocturnal orthostatic stress testing [J]. European Urology, 1998, 33(5): 481-488.
[3] Stella V J, Rao V M, Zannou E A, et al. Mechanisms of drug release from cyclodextrin complexes[J]. Advanced Drug Delivery Reviews, 1999, 369(1): 3-16.
[4] Fernandes C M, Veiga F J B. Stability evaluation of cyclodextrin inclusion complexes used in a new sustained-release formulation of nicardipine hydrochloride[J]. STP Pharma Sciences, 2003, 13(2): 119-124.
[5] Domingues Z R, Cortés M E, Gomes T A, et al. Bioactive glass as a drug delivery system of tetracycline and tetracycline associated with beta-cyclodextrin[J]. Biomaterials, 2004, 25(2): 327-333.
[6] Frézard F, Martins P S, Bahia A P C O, et al. Enhanced oral delivery of antimony from meglumine antimoniate/beta-cyclodextrin nanoassemblies[J]. International Journal of Pharmaceutics, 2008, 347(1/2): 102-108.
[7] Thatiparti T R, Shoffstall A J, von Recum H A. Cyclodextrin-based device coatings for affinity-based release of antibiotics[J]. Biomaterials, 2010, 31(8): 2335-2347.
[8] Thatiparti T R, von Recum H A. Cyclodextrin complexation for affinity-based antibiotic delivery[J]. Macromolecular Bioscience, 2010, 10(1): 82-90.
[9] Nagase Y, Hirata M, Wada K, et al. Improvement of some pharmaceutical properties of DY-9760e by sulfobutyl ether β-cyclodextrin[J]. International Journal of Pharmaceutics, 2001, 229(1/2): 163-172.
[10] Sripalakit P, Nermhom P, Saraphanchotiwitthaya A. Validation and pharmacokinetic application of a method for determination of doxazosin in human plasma by high-performance liquid chromatography[J]. Biomedical Chromatography, 2006, 20(8): 729-735.
[11] Cheah P Y, Yuen K H, Liong M L. Improved high-performance liquid chromatographic analysis of terazosin in human plasma[J]. Journal of Chromatography B, 2000, 745(2): 439-443.
[12] Zavitsanos A P, Alebic-Kolbah T. Enantioselective determination of terazosin in human plasma by normal phase high-performance liquid chromatography electrospray mass spectrometry[J]. Journal of Chromatography A, 1998, 794(1/2): 45-56.
[13] Rathinavelu A, Malave A. High-performance liquid-chromatography using electrochemical detection for the determination of prazosin in biological samples[J]. Journal of Chromatography B, 1995, 670(1):177-182.
[14] Wei X Y, Yin J F, Yang G L, et al. On-line solid-phase extraction with a monolithic weak cation-exchange column and simultaneous screening of α₁-adrenergin receptor antagonists in human plasma[J]. Journal of Separation Science, 2007, 30(17): 2851-2857.
[15] The Pharmacopoeia Commission of PRC. The pharmacopoeia of the People’s Republic of China [S]. Beijing: Beijing Chemical Industry Press, 2005.

Memo

Memo:

Biographies: Zhang Niping(1987—), female, graduate; Xu Qian(corresponding author), female, doctor, associate professor, q_xu@163.com.
Foundation items: Pre-Research Foundation for the National Natural Science Foundation of Southeast University(No. 9225000007), Suzhou Science and Technology Development Projects(No.YJS0948).
Citation: Zhang Niping, Yu Shuqin, Wang Hui, et al. Method for quantification of prazosin in dog plasma and its application to pharmacokinetic study[J].Journal of Southeast University(English Edition), 2011, 27(2):217-221.[doi:10.3969/j.issn.1003-7985.2011.02.022]

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