口服固体制剂溶出方法建立和验证的技术探讨
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摘要
体外溶出检查通常被认为可反映药物的体内溶出行为和生物利用度情况,其在药物制剂研发和上市产品的质量控制中发挥着巨大的作用。一种溶出度实验方法的建立,需要综合考虑药物的物理化学性质和制剂学特征,确立合适的溶出条件以模拟药物的体内溶出行为。新建立的溶出方法不仅需要具有良好的准确性和耐用性,还要能区分不同质量属性的药物制剂。本文依据国内外药品监管机构关于建立和验证药物溶出方法的最新指导原则,通过查阅文献,综述了口服固体制剂溶出方法建立和溶出度标准制定的常见问题及研究进展,以期为药物溶出方法的建立和验证提供参考。
It is generally assumed that study of in vitro dissolution can reveal the in vivo behavior and bioavailability of a drug. The dissolution test indisputably plays a vital role in the research and development of pharmaceutical preparations as well as routine quality control of approved drugs. In order to develop an ideal dissolution method, the physicochemical properties of drug and the characteristics of its dosage form should be considered, and a proper dissolution condition be established to simulate the in vivo dissolution behavior of drugs. The new dissolution method should have the required characteristics of accuracy and durability, but also could distinguish pharmaceutic preparations with different quality. In recent years, there have been more and more reports on the establishment and verification of dissolution methods for oral solid dosage forms. However, there is very few review articles on the topic. According to the latest guidelines by domestic and foreign drug organizations, this review paper is prepared to summarize the most important skills and progress in the development of dissolution methods for oral solid preparations. The aim is to provide a reference for the development and validation of new dissolution methods.
It is generally assumed that study of in vitro dissolution can reveal the in vivo behavior and bioavailability of a drug. The dissolution test indisputably plays a vital role in the research and development of pharmaceutical preparations as well as routine quality control of approved drugs. In order to develop an ideal dissolution method, the physicochemical properties of drug and the characteristics of its dosage form should be considered, and a proper dissolution condition be established to simulate the in vivo dissolution behavior of drugs. The new dissolution method should have the required characteristics of accuracy and durability, but also could distinguish pharmaceutic preparations with different quality. In recent years, there have been more and more reports on the establishment and verification of dissolution methods for oral solid dosage forms. However, there is very few review articles on the topic. According to the latest guidelines by domestic and foreign drug organizations, this review paper is prepared to summarize the most important skills and progress in the development of dissolution methods for oral solid preparations. The aim is to provide a reference for the development and validation of new dissolution methods.
引文
[1]Tsume Y,Mudie DM,Langguth P,et al.The biopharmaceutics classification system:subclasses for in vivo predictive dissolution(IPD)methodology and IVIVC[J].Eur J Pharm Sci,2014,57:152-163.
[2]FDA.Guidance for industry:waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a Biopharmaceutics Classification System[S/OL].U.S.Department of Health and Human Services,Food and Drug Administration,Center for Evaluation and Research:2015[2017-11-13].https://www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation/guidances/ucm070246.pdf.
[3]Mc Carthy CA,Faisal W,O'shea JP,et al.In vitro dissolution models for the prediction of in vivo performance of an oral mesoporous silica formulation[J].J Control Release,2017,250:86-95.
[4]Marroum P.Role of in vitro-in vivo correlations in drug development[J].Dissolut Technol,2015,22:50-56.
[5]Reppas C,Vertzoni M.Biorelevant in-vitro performance testing of orally administered dosage forms[J].J Pharm Pharmacol,2012,64:919-930.
[6]Ashokraj Y,Daroi A,Gupta R,et al.Discriminatory dissolution method development and validation of etoricoxib tablets[J].Dissolut Technol,2016,23:30-34.
[7]United States Pharmacopeial Convention,Inc.The Dissolution Procedure:Development and Validation[S].Rockville:the United States Pharmacopeia,2016:1296-1316.
[8]Skwierczynski R,Curry P,Gray V,et al.Revision of the dissolution procedure:development and validation<1092[J].Dissolut Technol,2014,21:6-8.
[9]Vignaduzzo SE,Operto MA,Castellano PM.Development of a dissolution test for fenbendazole-praziquantel capsules using UV-PLS method[J].J Brazil Chem Soc,2017,28:1030-1037.
[10]de Souza Anselmo C,de Carvalho Mendes T,da Silva Honorio T,et al.Development and validation of a dissolution test for lutein tablets and evaluation of intestinal permeability[J].Food Chem,2016,210:63-69.
[11]Machado JC,Lange AD,Todeschini V,et al.Development and validation of a discriminative dissolution method for atorvastatin calcium tablets using in vivo data by LC and UV methods[J].AAPS Pharm Sci Tech,2014,15:189-197.
[12]Marques M.Dissolution media simulating fasted and fed states[J].Dissolut Technol,2004,11:16.
[13]Jantratid E,Dressman J.Biorelevant dissolution media simulating the proximal human gastrointestinal tract:an update[J].Dissolut Technol,2009,16:21-25.
[14]Dressman J.Evolution of dissolution media over the last twenty years[J].Dissolut Technol,2014,21:6-10.
[15]Lakshmi CS,Badarinath AV.An updated review of dissolution apparatus for conventional and novel dosage forms[J].Int J Pharm Res Rev,2013,2:42-53.
[16]Simon A,Amaro MI,Healy AM,et al.Development of a discriminative in vitro release test for rivastigmine transdermal patches using pharmacopeial apparatuses:USP 5 and USP 6[J].AAPS Pharm Sci Tech,2017,18:2561-2569.
[17]Li ZQ,He X,Liu CX.Recent advances in drug dissolution/permeation synchronous evaluation technologies based on physiological characteristics of gastrointestinal tract[J].Acta Pharm Sin(药学学报),2016,51:1540-1550.
[18]Pestieau A,Evrard B.In vitro biphasic dissolution tests and their suitability for establishing in vitro-in vivo correlations:a historical review[J].Eur J Pharm Sci,2017,102:203-219.
[19]Cascone S,Lamberti G,Marra F,et al.Gastrointestinal behavior and ADME phenomena:I.in vitro simulation[J].J Drug Deliv Sci Technol,2016,35:272-283.
[20]Schnorr SL,Crittenden AN,Venema K,et al.Assessing digestibility of hadza tubers using a dynamic in-vitro model[J].Am J Phys Anthropol,2015,158:371-385.
[21]Hasan M,Rahman M,Islam R,et al.A key approach on dissolution of pharmaceutical dosage forms[J].Pharm Innov J,2017,6:168-180.
[22]Zishan M,Amir M,Ahmad Z,et al.Review on application and factor affecting and official monographs in dissolution process[J].J Drug Deliv Therapeut,2017,7:19-27.
[23]Kakhi M.Classification of the flow regimes in the flowthrough cell[J].Eur J Pharm Sci,2009,37:531-544.
[24]United States Pharmacopeial Convention,Inc.Dissolution[S].Rockville:the United States Pharmacopeia,2016:588-598.
[25]Vignaduzzo SE,Operto MA,Castellano PM.Development and validation of a dissolution test method for albendazole and praziquantel in their combined dosage form[J].J Brazil Chem Soc,2015,26:729-735.
[26]United States Pharmacopeial Convention,Inc.Validation of Compendial Procedures[S].Rockville:the United States Pharmacopeia,2014:1445-1450.
[27]Abualhasan M,Qutob T,Obedat S,et al.Dissolution method development and validation of rutin tablet[J].Palest Med Pharm J,2017,2:55-62.
[28]Hermans A,Abend AM,Kesisoglou F,et al.Approaches for establishing clinically relevant dissolution specifications for immediate release solid oral dosage forms[J].AAPS J,2017,19:1-13.
[29]Sautel M,Krstulovi?AM.Pharmaceutical analysis beyond compendial requirements[J].J Sep Sci,2005,28:1529-1538.
[30]Skelly JP,Amidon GL,Barr WH,et al.In vitro and in vivo testing and correlation for oral controlled/modified-release dosage forms[J].Pharm Res,1990,7:975-982.
[31]El-Shenawy AA,Ahmed MM,Mansour HF,et al.Torsemide fast dissolving tablets:development,optimization using BoxBhenken design and response surface methodology,in vitrocharacterization,and pharmacokinetic assessment[J].AAPS Pharm Sci Tech,2017,18:2168-2179.
[32]Chinese Pharmacopoeia Commission.Pharmacopeia of the People’s Republic of China(中华人民共和国药典)[S].Vol2.Beijing:China Medical Science Press,2015:319-320.
[33]United States Pharmacopeial Convention,Inc.Carbamazepine Tablets[S].Rockville:the United States Pharmacopeia,2015:2917-2920.
[34]FDA.Guidance for industry:extended release oral dosage forms:development,evaluation,and application of in vitro/in vivo correlations[S/OL].U.S.Department of Health and Human Services,Food and Drug Administration,Center for Evaluation and Research,1997[2017-11-13].https://www.fda.gov/downloads/drugs/guid Ancecomplianceregulatoryinfor mation/guidances/ucm070239.pdf.
[35]United States Pharmacopeial Convention,Inc.Oxycodone Hydrochloride Extended-Release Tablets[S].Rockville:the United States Pharmacopeia,2012:4642-4644.
[36]United States Pharmacopeial Convention,Inc.Levothyroxine Sodium Tablets[S].Rockville:the United States Pharmacopeia,2012:4109-4110.
[37]United States Pharmacopeial Convention,Inc.Pantoprazole Sodium Delayed-release Tablets[S].Rockville:the United States Pharmacopeia,2012:4682-4686.
[38]Hassan HA,Charoo NA,Ali AA,et al.Establishment of a bioequivalence-indicating dissolution specification for candesartan cilexetil tablets using a convolution model[J].Dissolut Technol,2015,22:36-43.
[39]United States Pharmacopeial Convention,Inc.In Vitro In Vivo Evaluation of Dosage Forms[S].Rockville:the United States Pharmacopeia,2011:1277-1288.
[40]Roudier B,Davit BM,Beyssac E,et al.In vitro-in vivo correlation’s dissolution limits setting[J].Pharm Res,2014,31:2529-2538.
[41]Van Buskirk GA,Shah V,Yacobi A,et al.PQRI workshop report:application of IVIVC in formulation development[J].Dissolut Technol,2014,21:51-58.
[42]Deshmukh S,Avachat A,Garkal A,et al.Optimization of a dissolution method in early development based on IVIVC using small animals:application to a BCS class II drug[J].Dissolut Technol,2016,23:34-41.
[43]Lai HQ,Hu Y,Li XD.The in vitro dissolution of total composition of the tablet of rhizomes of ligusticum chuanxiong components and in vitro-in vivo correlation by the method of area under the absorbance-wavelength curve[J].Acta Pharm Sin(药学学报),2015,50:788-792.
[44]Chinese Pharmacopoeia Commission.Pharmacopeia of the People’s Republic of China(中华人民共和国药典)[S].Vol4.Beijing:China Medical Science Press,2015:118,368.
[45]Pan RX,Gao Y,Chen WL,et al.Dissolution testing combined with computer simulation technology to evaluate the bioequivalence of domestic amoxicillin capsule[J].Acta Pharm Sin(药学学报),2014,49:1155-1161.
[46]Suarez-Sharp S,Li M,Duan J,et al.Regulatory experience with in vivo in vitro correlations(IVIVC)in new drug applications[J].AAPS J,2016,18:1379-1390.
[47]Zhang X,Duan J,Kesisoglou F,et al.Mechanistic oral absorption modeling and simulation for formulation development and bioequivalence evaluation:report of an FDA public workshop[J].CPT:Pharmacometrics Syst Pharmacol,2017,6:492-495.
[48]Fotaki N,Biswas D,D’Souza S,et al.Dissolution highlights from the 2016 AAPS annual meeting in Denver[J].Dissolut Technol,2017,24:68-72.
[2]FDA.Guidance for industry:waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a Biopharmaceutics Classification System[S/OL].U.S.Department of Health and Human Services,Food and Drug Administration,Center for Evaluation and Research:2015[2017-11-13].https://www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation/guidances/ucm070246.pdf.
[3]Mc Carthy CA,Faisal W,O'shea JP,et al.In vitro dissolution models for the prediction of in vivo performance of an oral mesoporous silica formulation[J].J Control Release,2017,250:86-95.
[4]Marroum P.Role of in vitro-in vivo correlations in drug development[J].Dissolut Technol,2015,22:50-56.
[5]Reppas C,Vertzoni M.Biorelevant in-vitro performance testing of orally administered dosage forms[J].J Pharm Pharmacol,2012,64:919-930.
[6]Ashokraj Y,Daroi A,Gupta R,et al.Discriminatory dissolution method development and validation of etoricoxib tablets[J].Dissolut Technol,2016,23:30-34.
[7]United States Pharmacopeial Convention,Inc.The Dissolution Procedure:Development and Validation[S].Rockville:the United States Pharmacopeia,2016:1296-1316.
[8]Skwierczynski R,Curry P,Gray V,et al.Revision of the dissolution procedure:development and validation<1092[J].Dissolut Technol,2014,21:6-8.
[9]Vignaduzzo SE,Operto MA,Castellano PM.Development of a dissolution test for fenbendazole-praziquantel capsules using UV-PLS method[J].J Brazil Chem Soc,2017,28:1030-1037.
[10]de Souza Anselmo C,de Carvalho Mendes T,da Silva Honorio T,et al.Development and validation of a dissolution test for lutein tablets and evaluation of intestinal permeability[J].Food Chem,2016,210:63-69.
[11]Machado JC,Lange AD,Todeschini V,et al.Development and validation of a discriminative dissolution method for atorvastatin calcium tablets using in vivo data by LC and UV methods[J].AAPS Pharm Sci Tech,2014,15:189-197.
[12]Marques M.Dissolution media simulating fasted and fed states[J].Dissolut Technol,2004,11:16.
[13]Jantratid E,Dressman J.Biorelevant dissolution media simulating the proximal human gastrointestinal tract:an update[J].Dissolut Technol,2009,16:21-25.
[14]Dressman J.Evolution of dissolution media over the last twenty years[J].Dissolut Technol,2014,21:6-10.
[15]Lakshmi CS,Badarinath AV.An updated review of dissolution apparatus for conventional and novel dosage forms[J].Int J Pharm Res Rev,2013,2:42-53.
[16]Simon A,Amaro MI,Healy AM,et al.Development of a discriminative in vitro release test for rivastigmine transdermal patches using pharmacopeial apparatuses:USP 5 and USP 6[J].AAPS Pharm Sci Tech,2017,18:2561-2569.
[17]Li ZQ,He X,Liu CX.Recent advances in drug dissolution/permeation synchronous evaluation technologies based on physiological characteristics of gastrointestinal tract[J].Acta Pharm Sin(药学学报),2016,51:1540-1550.
[18]Pestieau A,Evrard B.In vitro biphasic dissolution tests and their suitability for establishing in vitro-in vivo correlations:a historical review[J].Eur J Pharm Sci,2017,102:203-219.
[19]Cascone S,Lamberti G,Marra F,et al.Gastrointestinal behavior and ADME phenomena:I.in vitro simulation[J].J Drug Deliv Sci Technol,2016,35:272-283.
[20]Schnorr SL,Crittenden AN,Venema K,et al.Assessing digestibility of hadza tubers using a dynamic in-vitro model[J].Am J Phys Anthropol,2015,158:371-385.
[21]Hasan M,Rahman M,Islam R,et al.A key approach on dissolution of pharmaceutical dosage forms[J].Pharm Innov J,2017,6:168-180.
[22]Zishan M,Amir M,Ahmad Z,et al.Review on application and factor affecting and official monographs in dissolution process[J].J Drug Deliv Therapeut,2017,7:19-27.
[23]Kakhi M.Classification of the flow regimes in the flowthrough cell[J].Eur J Pharm Sci,2009,37:531-544.
[24]United States Pharmacopeial Convention,Inc.Dissolution[S].Rockville:the United States Pharmacopeia,2016:588-598.
[25]Vignaduzzo SE,Operto MA,Castellano PM.Development and validation of a dissolution test method for albendazole and praziquantel in their combined dosage form[J].J Brazil Chem Soc,2015,26:729-735.
[26]United States Pharmacopeial Convention,Inc.Validation of Compendial Procedures[S].Rockville:the United States Pharmacopeia,2014:1445-1450.
[27]Abualhasan M,Qutob T,Obedat S,et al.Dissolution method development and validation of rutin tablet[J].Palest Med Pharm J,2017,2:55-62.
[28]Hermans A,Abend AM,Kesisoglou F,et al.Approaches for establishing clinically relevant dissolution specifications for immediate release solid oral dosage forms[J].AAPS J,2017,19:1-13.
[29]Sautel M,Krstulovi?AM.Pharmaceutical analysis beyond compendial requirements[J].J Sep Sci,2005,28:1529-1538.
[30]Skelly JP,Amidon GL,Barr WH,et al.In vitro and in vivo testing and correlation for oral controlled/modified-release dosage forms[J].Pharm Res,1990,7:975-982.
[31]El-Shenawy AA,Ahmed MM,Mansour HF,et al.Torsemide fast dissolving tablets:development,optimization using BoxBhenken design and response surface methodology,in vitrocharacterization,and pharmacokinetic assessment[J].AAPS Pharm Sci Tech,2017,18:2168-2179.
[32]Chinese Pharmacopoeia Commission.Pharmacopeia of the People’s Republic of China(中华人民共和国药典)[S].Vol2.Beijing:China Medical Science Press,2015:319-320.
[33]United States Pharmacopeial Convention,Inc.Carbamazepine Tablets[S].Rockville:the United States Pharmacopeia,2015:2917-2920.
[34]FDA.Guidance for industry:extended release oral dosage forms:development,evaluation,and application of in vitro/in vivo correlations[S/OL].U.S.Department of Health and Human Services,Food and Drug Administration,Center for Evaluation and Research,1997[2017-11-13].https://www.fda.gov/downloads/drugs/guid Ancecomplianceregulatoryinfor mation/guidances/ucm070239.pdf.
[35]United States Pharmacopeial Convention,Inc.Oxycodone Hydrochloride Extended-Release Tablets[S].Rockville:the United States Pharmacopeia,2012:4642-4644.
[36]United States Pharmacopeial Convention,Inc.Levothyroxine Sodium Tablets[S].Rockville:the United States Pharmacopeia,2012:4109-4110.
[37]United States Pharmacopeial Convention,Inc.Pantoprazole Sodium Delayed-release Tablets[S].Rockville:the United States Pharmacopeia,2012:4682-4686.
[38]Hassan HA,Charoo NA,Ali AA,et al.Establishment of a bioequivalence-indicating dissolution specification for candesartan cilexetil tablets using a convolution model[J].Dissolut Technol,2015,22:36-43.
[39]United States Pharmacopeial Convention,Inc.In Vitro In Vivo Evaluation of Dosage Forms[S].Rockville:the United States Pharmacopeia,2011:1277-1288.
[40]Roudier B,Davit BM,Beyssac E,et al.In vitro-in vivo correlation’s dissolution limits setting[J].Pharm Res,2014,31:2529-2538.
[41]Van Buskirk GA,Shah V,Yacobi A,et al.PQRI workshop report:application of IVIVC in formulation development[J].Dissolut Technol,2014,21:51-58.
[42]Deshmukh S,Avachat A,Garkal A,et al.Optimization of a dissolution method in early development based on IVIVC using small animals:application to a BCS class II drug[J].Dissolut Technol,2016,23:34-41.
[43]Lai HQ,Hu Y,Li XD.The in vitro dissolution of total composition of the tablet of rhizomes of ligusticum chuanxiong components and in vitro-in vivo correlation by the method of area under the absorbance-wavelength curve[J].Acta Pharm Sin(药学学报),2015,50:788-792.
[44]Chinese Pharmacopoeia Commission.Pharmacopeia of the People’s Republic of China(中华人民共和国药典)[S].Vol4.Beijing:China Medical Science Press,2015:118,368.
[45]Pan RX,Gao Y,Chen WL,et al.Dissolution testing combined with computer simulation technology to evaluate the bioequivalence of domestic amoxicillin capsule[J].Acta Pharm Sin(药学学报),2014,49:1155-1161.
[46]Suarez-Sharp S,Li M,Duan J,et al.Regulatory experience with in vivo in vitro correlations(IVIVC)in new drug applications[J].AAPS J,2016,18:1379-1390.
[47]Zhang X,Duan J,Kesisoglou F,et al.Mechanistic oral absorption modeling and simulation for formulation development and bioequivalence evaluation:report of an FDA public workshop[J].CPT:Pharmacometrics Syst Pharmacol,2017,6:492-495.
[48]Fotaki N,Biswas D,D’Souza S,et al.Dissolution highlights from the 2016 AAPS annual meeting in Denver[J].Dissolut Technol,2017,24:68-72.