柳氮磺吡啶肠溶片人体生物等效性研究

梁燕; 王凌; 王蕊; 常臻; 钟延强; 邹豪

doi:10.3969/j.issn.1006-0111.2013.06.007

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柳氮磺吡啶肠溶片人体生物等效性研究

梁燕, 王凌, 王蕊, 常臻, 钟延强, 邹豪

文章导航 > 药学实践与服务 > 2013 > 31(6): 424-427,466

梁燕, 王凌, 王蕊, 常臻, 钟延强, 邹豪. 柳氮磺吡啶肠溶片人体生物等效性研究[J]. 药学实践与服务, 2013, 31(6): 424-427,466. doi: 10.3969/j.issn.1006-0111.2013.06.007

引用本文:

梁燕, 王凌, 王蕊, 常臻, 钟延强, 邹豪. 柳氮磺吡啶肠溶片人体生物等效性研究[J]. 药学实践与服务, 2013, 31(6): 424-427,466. doi: 10.3969/j.issn.1006-0111.2013.06.007

LIANG Yan, WANG Ling, WANG Rui, CHANG Zhen, ZHONG Yan-qiang, ZOU Hao. Study on bioequivalence of sulfasalazine enteric-coated tablet in healthy volunteers[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(6): 424-427,466. doi: 10.3969/j.issn.1006-0111.2013.06.007

Citation:

LIANG Yan, WANG Ling, WANG Rui, CHANG Zhen, ZHONG Yan-qiang, ZOU Hao. Study on bioequivalence of sulfasalazine enteric-coated tablet in healthy volunteers[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(6): 424-427,466. doi: 10.3969/j.issn.1006-0111.2013.06.007

柳氮磺吡啶肠溶片人体生物等效性研究

doi: 10.3969/j.issn.1006-0111.2013.06.007

梁燕¹,
王凌²,
王蕊³,
常臻³,
钟延强¹,
邹豪^1,

1.
第二军医大学药学院药剂学教研室, 上海 200433
2.
四川大学华西药学院, 成都 610041
3.
上海信谊药厂有限公司药物研究所, 上海 201206

Study on bioequivalence of sulfasalazine enteric-coated tablet in healthy volunteers

1.
Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
2.
Huaxi School of Pharmacy, Sichuan University, Chengdu 610041, China
3.
Institute of Drug Research, Shanghai Xinyi Pharmaceutical Co., Ltd. Shanghai 201206, China

摘要: 目的柳氮磺吡啶肠溶片(sulfasalazine enteric-coated tablet,SECT)属于口服不易吸收的药物,其人体药动学和相对生物利用度研究存在一定难度。本研究通过评价不同厂家生产的两种制剂的生物等效性,建立SECT的研究方法。方法对24名健康男性志愿者按随机交叉自身对照的方法,给予单剂量口服500 mg SECT受试制剂和参比制剂,两次试验间隔为1周,分别测定血浆柳氮磺吡啶(sulfasalazine,SS)、磺胺吡啶(sulfapyridine,SP)、5-氨基水杨酸(5-aminosalicylic acid,5-ASA)浓度。结果血浆中SS、SP、5-ASA的药动学参数如下:以AUC_0→t计算,受试制剂SECT中SS相对生物利用度为(108.8±24.1)%;SP相对生物利用度为(105.0±25.0)%;5-ASA相对生物利用度为(94.1±22.0)%。以AUC_0→∞计算,受试制剂SECT中SS相对生物利用度为(106.9±23.4)%;SP相对生物利用度为(104.1±25.0)%;5-ASA相对生物利用度为(93.6±22.2)%。受试制剂与参比制剂的血药浓度-时间曲线基本一致,受试制剂与参比制剂主要药动学参数无显著性差异(P>0.05)。结论两家厂家生产的SECT,受试制剂与参比制剂在健康中国人体内具有生物等效性。
- 柳氮磺吡啶 /
- 磺胺吡啶 /
- 5-氨基水杨酸 /
- 生物等效性
Abstract: Objective To evaluate the pharmacokinetics and relative bioavailability of sulfasalazine enteric-coated tablets from two different factories in healthy volunteers. Methods 24 healthy male volunteers were enrolled in the study.A single oral dose(500 mg) of test and reference Sulfasalazine Enteric-coated tablet preparations were given respectively to the volunteers according to randomized two way cross over study design.The washout period was l week.The plasma concentrations of Sulfasalazine(SASP)and sulfapyridine(SP)were determined by HPLC-UV method, the plasma concentrations of 5-aminosalicylic acid(5-ASA) were determined by HPLC-FLU method. Results The pharmacokinetic parameters of SASP, SP and 5-ASA in plasma were as follows:according to AUC_0→t, the relative bioavailability of SASP、SP and 5-ASA was (108.8±24.1)%, (105.0±25.0)% and (94.1±22.0)% in the test preparations; while according to AUC_0→∞, the relative bioavailability of SASP、SP and 5-ASA was (106.9±23.4)%, (104.1±25.0)% and (93.6±22.2)% in the test preparations. Mean plasma concentration-time curve of the test product was highly close to that of the reference product.There was no significant difference in pharmacokinetic parameters between the test and reference preparations of sulfasalazine enteric-coated tablets (P>0.05). Conclusion The results of statistical analysis showed that the two sulfasalazine enteric-coated tablets from different factories in healthy volunteers were bioequivalent.
- sulfasalazine(SASP) /
- sulfapyridine(SP) /
- 5-aminosalicylic acid(5-ASA) /
- pharmacokinetics and relative bioavailability

[1]	CDER/FDA. Guidance for Industry, Bioavailability and Bioequivalence Studies for Orally Administered Drug Products-General Considerations, March 2003.http://www.fda.gov/downloads/Drugs/Guidance Compliance Regulatory Information/Guidances/UCM070124.pdf.
[2]	FDA. Draft Guidance on Sulfasalazine,Feb 2010.http://www.fda.gov/downloads/Drugs/Guidance_Compliance_Regulatory_Information/Guidances/UCM199673.pdf.
[3]	李金恒,刘存刚,姚旋,等.HPLC梯度洗脱法测定血浆中柳氮磺吡啶及其代谢物[J].医学研究生学报, 2008, 7(21):682.
[4]	白小红,胡爽,李进霞,等.高效液相色谱法测定人血浆中柳氮磺胺吡啶及其代谢物[J].中国医院药学杂志,2004,24(4):208.
[5]	Ma JJ,Liu CG,Li JH,et al. Effects of NAT2 polymorphism on SASP pharmacokinetics in Chinese population[J].Clin Chem Acta,2009,407:30.
[6]	Gu GZ,Xia HM,Pang ZQ,et al.Determination of sulphasalazine and its main metabolite sulphapyridine and 5-aminosalicylic acid in human plasma by liquid chromategraphy/tandem mass spectrometry and its application to a pharmacokinetic study[J].J Chromtog B,2011,879:449.

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柳氮磺吡啶肠溶片人体生物等效性研究

doi: 10.3969/j.issn.1006-0111.2013.06.007

1. 第二军医大学药学院药剂学教研室, 上海 200433

2. 四川大学华西药学院, 成都 610041

3. 上海信谊药厂有限公司药物研究所, 上海 201206

收稿日期: 2013-03-25
修回日期: 2013-05-15

关键词:

摘要: 目的柳氮磺吡啶肠溶片(sulfasalazine enteric-coated tablet,SECT)属于口服不易吸收的药物,其人体药动学和相对生物利用度研究存在一定难度。本研究通过评价不同厂家生产的两种制剂的生物等效性,建立SECT的研究方法。方法对24名健康男性志愿者按随机交叉自身对照的方法,给予单剂量口服500 mg SECT受试制剂和参比制剂,两次试验间隔为1周,分别测定血浆柳氮磺吡啶(sulfasalazine,SS)、磺胺吡啶(sulfapyridine,SP)、5-氨基水杨酸(5-aminosalicylic acid,5-ASA)浓度。结果血浆中SS、SP、5-ASA的药动学参数如下:以AUC_0→t计算,受试制剂SECT中SS相对生物利用度为(108.8±24.1)%;SP相对生物利用度为(105.0±25.0)%;5-ASA相对生物利用度为(94.1±22.0)%。以AUC_0→∞计算,受试制剂SECT中SS相对生物利用度为(106.9±23.4)%;SP相对生物利用度为(104.1±25.0)%;5-ASA相对生物利用度为(93.6±22.2)%。受试制剂与参比制剂的血药浓度-时间曲线基本一致,受试制剂与参比制剂主要药动学参数无显著性差异(P>0.05)。结论两家厂家生产的SECT,受试制剂与参比制剂在健康中国人体内具有生物等效性。

English Abstract

Study on bioequivalence of sulfasalazine enteric-coated tablet in healthy volunteers

1. Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

2. Huaxi School of Pharmacy, Sichuan University, Chengdu 610041, China

3. Institute of Drug Research, Shanghai Xinyi Pharmaceutical Co., Ltd. Shanghai 201206, China

Received Date: 2013-03-25
Rev Recd Date: 2013-05-15

Keywords:

sulfasalazine(SASP) /
sulfapyridine(SP) /
5-aminosalicylic acid(5-ASA) /
pharmacokinetics and relative bioavailability

Abstract: Objective To evaluate the pharmacokinetics and relative bioavailability of sulfasalazine enteric-coated tablets from two different factories in healthy volunteers. Methods 24 healthy male volunteers were enrolled in the study.A single oral dose(500 mg) of test and reference Sulfasalazine Enteric-coated tablet preparations were given respectively to the volunteers according to randomized two way cross over study design.The washout period was l week.The plasma concentrations of Sulfasalazine(SASP)and sulfapyridine(SP)were determined by HPLC-UV method, the plasma concentrations of 5-aminosalicylic acid(5-ASA) were determined by HPLC-FLU method. Results The pharmacokinetic parameters of SASP, SP and 5-ASA in plasma were as follows:according to AUC_0→t, the relative bioavailability of SASP、SP and 5-ASA was (108.8±24.1)%, (105.0±25.0)% and (94.1±22.0)% in the test preparations; while according to AUC_0→∞, the relative bioavailability of SASP、SP and 5-ASA was (106.9±23.4)%, (104.1±25.0)% and (93.6±22.2)% in the test preparations. Mean plasma concentration-time curve of the test product was highly close to that of the reference product.There was no significant difference in pharmacokinetic parameters between the test and reference preparations of sulfasalazine enteric-coated tablets (P>0.05). Conclusion The results of statistical analysis showed that the two sulfasalazine enteric-coated tablets from different factories in healthy volunteers were bioequivalent.

梁燕, 王凌, 王蕊, 常臻, 钟延强, 邹豪. 柳氮磺吡啶肠溶片人体生物等效性研究[J]. 药学实践与服务, 2013, 31(6): 424-427,466. doi: 10.3969/j.issn.1006-0111.2013.06.007

引用本文:

梁燕, 王凌, 王蕊, 常臻, 钟延强, 邹豪. 柳氮磺吡啶肠溶片人体生物等效性研究[J]. 药学实践与服务, 2013, 31(6): 424-427,466. doi: 10.3969/j.issn.1006-0111.2013.06.007

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柳氮磺吡啶肠溶片人体生物等效性研究

doi: 10.3969/j.issn.1006-0111.2013.06.007

Study on bioequivalence of sulfasalazine enteric-coated tablet in healthy volunteers

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柳氮磺吡啶肠溶片人体生物等效性研究

doi: 10.3969/j.issn.1006-0111.2013.06.007

1. 第二军医大学药学院药剂学教研室, 上海 200433 2. 四川大学华西药学院, 成都 610041 3. 上海信谊药厂有限公司药物研究所, 上海 201206

English Abstract

Study on bioequivalence of sulfasalazine enteric-coated tablet in healthy volunteers

1. Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China 2. Huaxi School of Pharmacy, Sichuan University, Chengdu 610041, China 3. Institute of Drug Research, Shanghai Xinyi Pharmaceutical Co., Ltd. Shanghai 201206, China

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1. 第二军医大学药学院药剂学教研室, 上海 200433

2. 四川大学华西药学院, 成都 610041

3. 上海信谊药厂有限公司药物研究所, 上海 201206

1. Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

2. Huaxi School of Pharmacy, Sichuan University, Chengdu 610041, China

3. Institute of Drug Research, Shanghai Xinyi Pharmaceutical Co., Ltd. Shanghai 201206, China