Discriminatory in vitro dissolution tests of oral dosage forms containing poorly soluble drugs for a Quality by Design approach
Main Article Content
Abstract
The challenge of oral formulations, containing drugs that show pH-dependent solubility, is to increase the dissolution rate in different media that simulate the gastrointestinal conditions, to guarantee their availability for absorption. In this work, some dosage forms containing poorly soluble drugs (diclofenac sodium, ketoprofen and meloxicam) are evaluated in different media: pH 1.0 (simulating fasted state), pH 4.5 buffer (simulating fed state), deionised water and phosphate buffer pH 6.8 or pH 7.5. These last buffers are required by the U.S. Pharmacopoeia monographs. The results obtained in sink and non-sink conditions could show possible critical quality attributes of the drugs and these properties are highly significant for a Quality by Design (QbD) approach. Completely different performances were obtained in the four dissolution media by the products considered. This approach could be useful for the predictive analytics, for the critical risk assessment and control during production, for the design and the development of new drugs in QbD approach.
Keywords:
Quality by Design (QbD), Dissolution rate, solid dosage form(s), Solubility, US Pharmacopoeia (USP)
Article Details
How to Cite
MAGGI, Lauretta et al.
Discriminatory in vitro dissolution tests of oral dosage forms containing poorly soluble drugs for a Quality by Design approach.
Medical Research Archives, [S.l.], v. 6, n. 11, nov. 2018.
ISSN 2375-1924.
Available at: <https://esmed.org/MRA/mra/article/view/1855>. Date accessed: 27 dec. 2024.
doi: https://doi.org/10.18103/mra.v6i11.1855.
Section
Research Articles
The Medical Research Archives grants authors the right to publish and reproduce the unrevised contribution in whole or in part at any time and in any form for any scholarly non-commercial purpose with the condition that all publications of the contribution include a full citation to the journal as published by the Medical Research Archives.
References
1. ICH. The International Conference on Harmonization of Technical Requirements for Registration of Pharmaceuticals for Human Use, Quality Guideline Q8 (R2) Pharmaceutical Development. 2009.
2. FDA. Food and Drug Administration. Guidance for industry, Q8 (R1) Pharma-ceutical Development. 2009.
3. Pramod K, Tahir MA, Charoo NA, Ansa-ri SH, Ali J. Pharmaceutical product devel-opment: A quality by design approach. Int. J. Pharm. Investig. 2016; 6(3): 129.
4. Sangshetti JN, Deshpande M, Zaheer Z, Shinde DB, Arote R. Quality by design ap-proach: regulatory need. Arab. J. Chem. 2017; 10: 3412-3425.
5. Yu LX, Amidon G, Khan MA, Hoag SW, Polli J, Raju GK, Woodcock J. Under-standing Pharmaceutical Quality by Design. AAPS J. 2014; 16(4): 771-783.
6. Gabriel SE, Jaakkimainen L, Bombardier C. Risk for Serious Gastrointestinal Com-plications Related to Use of Nonsteroidal Anti-inflammatory Drugs: A Meta-analysis. Ann. Intern. Med. 1991; 115: 787-796.
7. Qureshi SA. Developing discriminatory drug dissolution tests and profiles: Some thoughts for consideration on the concept and its interpretation. Dissolut. Technol. 2006; 13: 18-23.
8. Siewert M. Perspectives of in vitro disso-lution tests in establishing in vivo/in vitro correlations. Eur. J Drug Metab. Pharmaco-kinet. 1993; 18(1): 7-18.
9. Hubert C, Lebrun P, Houari S, Ziemons E, Rozet E, Hubert P. Improvement of a stability-indicating method by Quality-by-Design versus Quality-by-Testing: A case of a learning process. J. Pharm. Biomed. Anal. 2014; 88: 401-409.
10. Shah V.P., Burbmg M, Noory A, Digbe S, Skelly JP. Influence of higher rates of agitation on release patterns of immediate-release drug products. J. Pharm. Sci. 1992; 81: 500-503.
11. Mudie DM, Amidon GL, Amidon GE. Physiological parameters for oral delivery and in vitro testing. Mol. Pharm. 2010; 7(5): 1388-1405.
12. Lionberger RA, Lee SL, Lee L, Raw A, Yu LX. Quality by Design: Concepts for ANDAs. AAPS J. 2008; 10(2): 268–276.
13. Lee SL, O’Connor TF, Yang X, Cruz CN, Chatterjee S, Madurawe RD, Moore CMV, Yu LX, Woodcock J. Modernizing Pharmaceutical Manufacturing: from Batch to Continuous Production. J. Pharm. Innov. 2015; 10(3): 191-199.
14. Yu LX. Pharmaceutical quality by de-sign: product and process development, un-derstanding, and control. Pharm. Res. 2008; 25(4): 781-791.
15. Charoo NA, Shamsher AA, Zidan AS, Rahman Z. Quality by design approach for formulation development: a case study of dispersible tablets. Int. J. Pharm. 2012; 423(2): 167-178.
16. Anand O, Lawrence XY, Conner DP, Davit BM. Dissolution testing for generic drugs: an FDA perspective. AAPS J. 2011; 13(3): 328.
17. Petralito S, Zanardi I, Memoli A, Anne-sini MC, Millucci V, Travagli V. Apparent solubility and dissolution profile at non-sink conditions as quality improvement tools. In: Basnet P, ed. Promising Pharma-ceuticals. Vol. 5. Rijeka, Croatia: InTech; 2012. pp. 83-100.
18. Liu P, De Wulf O, Laru J, Heikkilä T, van Veen B, Kiesvaara J, Hirvonen J, Pel-tonen L, Laaksonen T. Dissolution studies of poorly soluble drug nanosuspensions in non-sink conditions. AAPS PharmSciTech 2013; 14(2): 748-756.
19. Siewert M, Dressman J, Brown C, Shah V, Williams R. FIP/AAPS guidelines for dissolution/in vitro release testing of nov-el/special dosage forms. Dissolut. Technol. 2003; 10: 10-13.
20. Dickinson PA, Lee WW, Stott PW, Townsend AI, Smart JP, Ghahramani P, Hammett T, Billett L, Behn S, Gibb RC, Abrahamsson B. Clinical relevance of dis-solution testing in quality by design. AAPS J. 2008; 10(2): 380-390.
21. Chuasuwan B, Binjesoh V, Polli JE, Zhang H, Amidon GL, Junginger HE, Mid-ha KK, Shah VP, Stavchansky S, Dressman JB, Barends DM. Biowaiver monographs for immediate release solid oral dosage forms: Diclofenac sodium and diclofenac potassium. J. Pharm. Sci. 2009; 98: 1206-1219.
22. Fini A, Fazio G, Feroci G. Solubility and solubilitation proprierties of non-steroidal anti infiammatory drugs. Int. J. Pharm. 1995; 126 (1–2): 95-102.
23. Shohin IE, Kulinich JI, Ramenskaya GV, Abrahamsson B, Kopp S, Langguth P, Polli JE, Shah VP, Groot DW, Barends DM, Dressman JB. Biowaiver monographs for immediate-release solid oral dosage forms: Ketoprofen. J. Pharm. Sci. 2012; 101: 3593–3603.
24. Thorsteinn L, Dagný H. Determination of aqueous solubility by heating and equili-bration: A technical note. AAPS PharmSci-Tech. 2006; 7(1): 29-32.
25. Luger P, Daneck K, Engel W, Trum-mlitz G, Wagner K. Structure and physico-chemical properties of meloxicam, a new NSAID. Eur. J. Pharm. Sci. 1996; 4(3): 175-187.
26. Ambrus R, Kocbek P, Kristl J, Šibanc R, Rajkó R, Szabó-Révész P. Investigation of preparation parameters to improve the dissolution of poorly water-soluble melox-icam. Int. J. Pharm. 2009; 381(2): 153-159.
27. Reagents. Solutions/Buffer solutions. The United States Pharmacopeia (USP40 - NF35). United States Pharmacopeial Con-vention, Inc., Rockville, MD; 2017. pp. 2409-2411.
28. Diclofenac Sodium/Official Mono-graphs. The United States Pharmacopeia (USP40 - NF35). United States Pharma-copeial Convention, Inc., Rockville, MD; 2017. pp. 3731-36.
29. Ketoprofen/Official Monographs. The United States Pharmacopeia (USP40 - NF35). United States Pharmacopeial Con-vention, Inc., Rockville, MD; 2017. pp. 4749-53.
30. Meloxicam/Official Monographs. The United States Pharmacopeia (USP40 - NF35). United States Pharmacopeial Con-vention, Inc., Rockville, MD; 2017. pp. 4991-95.
31. Dajun DS, Wen H, Taylor LS. Non-Sink Dissolution Conditions for Predicting Product Quality and In Vivo Performance of Supersaturating Drug Delivery Systems. J. Pharm. Sci. 2016; 105(9): 2477-2488.
32. Friuli V, Maggi L, Bruni G, Musitelli G, Conte U. Influence of dissolution media and presence of alcohol on the in vitro per-formance of pharmaceutical products con-taining an insoluble drug. J. Pharm. Sci. 2018; 107 (1): 507-511.
33. Hermans A, Abend AM, Kesisoglou F, Flanagan T, Cohen MJ, Diaz DA, Mao Y, Zhang L, Webster G K, Lin Y, Hahn DA, Coutant CA, Grady H. Approaches for Es-tablishing Clinically Relevant Dissolution Specifications for Immediate Release Solid Oral Dosage Forms. AAPS J. 2017; 19(6): 1537-1549.
2. FDA. Food and Drug Administration. Guidance for industry, Q8 (R1) Pharma-ceutical Development. 2009.
3. Pramod K, Tahir MA, Charoo NA, Ansa-ri SH, Ali J. Pharmaceutical product devel-opment: A quality by design approach. Int. J. Pharm. Investig. 2016; 6(3): 129.
4. Sangshetti JN, Deshpande M, Zaheer Z, Shinde DB, Arote R. Quality by design ap-proach: regulatory need. Arab. J. Chem. 2017; 10: 3412-3425.
5. Yu LX, Amidon G, Khan MA, Hoag SW, Polli J, Raju GK, Woodcock J. Under-standing Pharmaceutical Quality by Design. AAPS J. 2014; 16(4): 771-783.
6. Gabriel SE, Jaakkimainen L, Bombardier C. Risk for Serious Gastrointestinal Com-plications Related to Use of Nonsteroidal Anti-inflammatory Drugs: A Meta-analysis. Ann. Intern. Med. 1991; 115: 787-796.
7. Qureshi SA. Developing discriminatory drug dissolution tests and profiles: Some thoughts for consideration on the concept and its interpretation. Dissolut. Technol. 2006; 13: 18-23.
8. Siewert M. Perspectives of in vitro disso-lution tests in establishing in vivo/in vitro correlations. Eur. J Drug Metab. Pharmaco-kinet. 1993; 18(1): 7-18.
9. Hubert C, Lebrun P, Houari S, Ziemons E, Rozet E, Hubert P. Improvement of a stability-indicating method by Quality-by-Design versus Quality-by-Testing: A case of a learning process. J. Pharm. Biomed. Anal. 2014; 88: 401-409.
10. Shah V.P., Burbmg M, Noory A, Digbe S, Skelly JP. Influence of higher rates of agitation on release patterns of immediate-release drug products. J. Pharm. Sci. 1992; 81: 500-503.
11. Mudie DM, Amidon GL, Amidon GE. Physiological parameters for oral delivery and in vitro testing. Mol. Pharm. 2010; 7(5): 1388-1405.
12. Lionberger RA, Lee SL, Lee L, Raw A, Yu LX. Quality by Design: Concepts for ANDAs. AAPS J. 2008; 10(2): 268–276.
13. Lee SL, O’Connor TF, Yang X, Cruz CN, Chatterjee S, Madurawe RD, Moore CMV, Yu LX, Woodcock J. Modernizing Pharmaceutical Manufacturing: from Batch to Continuous Production. J. Pharm. Innov. 2015; 10(3): 191-199.
14. Yu LX. Pharmaceutical quality by de-sign: product and process development, un-derstanding, and control. Pharm. Res. 2008; 25(4): 781-791.
15. Charoo NA, Shamsher AA, Zidan AS, Rahman Z. Quality by design approach for formulation development: a case study of dispersible tablets. Int. J. Pharm. 2012; 423(2): 167-178.
16. Anand O, Lawrence XY, Conner DP, Davit BM. Dissolution testing for generic drugs: an FDA perspective. AAPS J. 2011; 13(3): 328.
17. Petralito S, Zanardi I, Memoli A, Anne-sini MC, Millucci V, Travagli V. Apparent solubility and dissolution profile at non-sink conditions as quality improvement tools. In: Basnet P, ed. Promising Pharma-ceuticals. Vol. 5. Rijeka, Croatia: InTech; 2012. pp. 83-100.
18. Liu P, De Wulf O, Laru J, Heikkilä T, van Veen B, Kiesvaara J, Hirvonen J, Pel-tonen L, Laaksonen T. Dissolution studies of poorly soluble drug nanosuspensions in non-sink conditions. AAPS PharmSciTech 2013; 14(2): 748-756.
19. Siewert M, Dressman J, Brown C, Shah V, Williams R. FIP/AAPS guidelines for dissolution/in vitro release testing of nov-el/special dosage forms. Dissolut. Technol. 2003; 10: 10-13.
20. Dickinson PA, Lee WW, Stott PW, Townsend AI, Smart JP, Ghahramani P, Hammett T, Billett L, Behn S, Gibb RC, Abrahamsson B. Clinical relevance of dis-solution testing in quality by design. AAPS J. 2008; 10(2): 380-390.
21. Chuasuwan B, Binjesoh V, Polli JE, Zhang H, Amidon GL, Junginger HE, Mid-ha KK, Shah VP, Stavchansky S, Dressman JB, Barends DM. Biowaiver monographs for immediate release solid oral dosage forms: Diclofenac sodium and diclofenac potassium. J. Pharm. Sci. 2009; 98: 1206-1219.
22. Fini A, Fazio G, Feroci G. Solubility and solubilitation proprierties of non-steroidal anti infiammatory drugs. Int. J. Pharm. 1995; 126 (1–2): 95-102.
23. Shohin IE, Kulinich JI, Ramenskaya GV, Abrahamsson B, Kopp S, Langguth P, Polli JE, Shah VP, Groot DW, Barends DM, Dressman JB. Biowaiver monographs for immediate-release solid oral dosage forms: Ketoprofen. J. Pharm. Sci. 2012; 101: 3593–3603.
24. Thorsteinn L, Dagný H. Determination of aqueous solubility by heating and equili-bration: A technical note. AAPS PharmSci-Tech. 2006; 7(1): 29-32.
25. Luger P, Daneck K, Engel W, Trum-mlitz G, Wagner K. Structure and physico-chemical properties of meloxicam, a new NSAID. Eur. J. Pharm. Sci. 1996; 4(3): 175-187.
26. Ambrus R, Kocbek P, Kristl J, Šibanc R, Rajkó R, Szabó-Révész P. Investigation of preparation parameters to improve the dissolution of poorly water-soluble melox-icam. Int. J. Pharm. 2009; 381(2): 153-159.
27. Reagents. Solutions/Buffer solutions. The United States Pharmacopeia (USP40 - NF35). United States Pharmacopeial Con-vention, Inc., Rockville, MD; 2017. pp. 2409-2411.
28. Diclofenac Sodium/Official Mono-graphs. The United States Pharmacopeia (USP40 - NF35). United States Pharma-copeial Convention, Inc., Rockville, MD; 2017. pp. 3731-36.
29. Ketoprofen/Official Monographs. The United States Pharmacopeia (USP40 - NF35). United States Pharmacopeial Con-vention, Inc., Rockville, MD; 2017. pp. 4749-53.
30. Meloxicam/Official Monographs. The United States Pharmacopeia (USP40 - NF35). United States Pharmacopeial Con-vention, Inc., Rockville, MD; 2017. pp. 4991-95.
31. Dajun DS, Wen H, Taylor LS. Non-Sink Dissolution Conditions for Predicting Product Quality and In Vivo Performance of Supersaturating Drug Delivery Systems. J. Pharm. Sci. 2016; 105(9): 2477-2488.
32. Friuli V, Maggi L, Bruni G, Musitelli G, Conte U. Influence of dissolution media and presence of alcohol on the in vitro per-formance of pharmaceutical products con-taining an insoluble drug. J. Pharm. Sci. 2018; 107 (1): 507-511.
33. Hermans A, Abend AM, Kesisoglou F, Flanagan T, Cohen MJ, Diaz DA, Mao Y, Zhang L, Webster G K, Lin Y, Hahn DA, Coutant CA, Grady H. Approaches for Es-tablishing Clinically Relevant Dissolution Specifications for Immediate Release Solid Oral Dosage Forms. AAPS J. 2017; 19(6): 1537-1549.