BIOWAIVER STUDY OF IMMEDIATE RELEASE GLIMEPIRIDE TABLETS
Objective: Demonstrating therapeutic equivalency regarding the efficacy and safety among originator products and generics is a key step in permitting the marketing of generic products. The study aimed to evaluate the bioequivalence of five different generic brands of Glimepiride tablets under biowaiver conditions.
Methods: The quality of the tablet products, including uniformity of weight, friability, and disintegration test, was assessed using the United State Pharmacopeia (USP) general monograph for the tablet dosage form. The content of glimepiride in the tablets was measured using UV spectrophotometer at the wavelength 229 nm. The release of Glimepiride from the tested and originator tablet products was evaluated using the dissolution profiles conducted in HCI buffer pH 1.2, and phosphate buffer pH 6.4 and 7.8 by USP dissolution apparatus II. The bioequivalence of test products was assessed using the similarity and difference factors.
Results:The tested products complied to USP requirements for quality standards; all the products show rapid disintegration, D1 show higher time (Three minutes) while D3 show lower time (28 seconds). The content of test products was (104.68, 93.75, 97.21, 97.03, and 102.10) for D1, D2, D3, D4, and D5 , respectively, compare to 103.70 for OB. Dissolution profiles revealed that the highest similarity to the originator was showed in pH 6.4; f2 ranged (74.5-68.4) for all the tested products and low similarity in pH 7.8; f2 ranged (45.2-64.7).
Conclusion: The study showed that the generic products has noticeable similarity with the originator brand and it can be interchangeable.
2. Kalantzi L, Reppas C, Dressman JB, Amidon G, Junginger HE, Midha KK, et al.Biowaiver monographs for immediate release solid oral dosage forms: acetaminophen [paracetamol]. J Pharm Sci 2006;95:4–14.
3. Verbeeck RK, Junginger HE, Midha KK, Shah VP, Barends, DM. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: chloroquine phosphate, chloroquinesulfate and chloroquine hydrochloride. J Pharm Sci 2005;94:1389–95.
4. Potthast H, Dressman JB, Junginger HE, Midha KK, Oeser H.Biowaiver monographs for immediate release solid oral dosage forms: Ibuprofen. J Pharm Sci 2005;94:2121–31.
5. Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennerna H, Hussain AS, et al. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharm 2004;1:85–96.
6. Kortejarvi H, Yliperttula M, Dressman JB, Junginger HE, Midha KK, Shah VP, et al.Biowaiver monographs for immediate release solid oral dosage forms: ranitidine hydrochloride. J Pharm Sci 2005;94:1617–25.
7. 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. US Food and Drug Administration, Center for Drug Evaluation and Research. USA; 2000. Available from:http://www.fda.gov/cder/guidance/3618fnl.pdf. [Last accessed on 10 Jul 2020]
8. The Biopharmaceutics Classification System (BCS) Guidance. Available from:http://www.fda.gov/aboutfda/centersoffices/officeofmedicalproductsandtobacco/cder/ucm128219.htm. [Last accessed on 10 Jul 2020]
9. WHO. Multisource (generic) pharmaceutical products: Guidelines on registration requirements to establish interchangeability. Working document AS/04.093/Rev.4. World Health Organization; 2005.Available from: http://www.who.int/medicines/services/expertcommittees/pharm prep/QAS04_093Rev4_final.pdf [Last accessed on 10 Jul 2020].
10. Yu LX, Amidon GL, Polli JE, Zhao H, Mehta MU, Conner DP, et al.Biopharmaceuticsclassification system: the scientific basis for biowaiver extensions. Pharm Res 2002;19:921–5.
11. Bergstrom CA, Luthman K, Artursson P. Accuracy of calculated pH-dependent aqueous drug solubility. Eur J Pharm Sci 2004;22:387–98.
12. Lindenberg M, Kopp S, Dressman JB. Classification of orally administered drugs on the World Health Organization model list of essential medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm 2004;58:265–8.
13. Wu CY, Benet LZ. Predicting drug disposition via application of BCS: Transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 2005;22:11–23.
14. The Merck Index. Version 12.1 on CD-ROM. Merck and Co., Whitehouse Station, NJ, USA; 1996. p. 1151-63.
15. Nair A, Abrahamsson B, Barends DM, Groot DW, Kopp S, Polli JE, et al.Biowaiver monographs for immediate-release solid oral dosage forms: primaquine phosphate. J Pharm Sci 2012;101:936-45.
16. Hassan HA, Charoo NA, Ali AA, Alkhatem SS. Establishment of bioequivalence indicating dissolution specification for candesartan cilexetil tablets using a convolution model. Dissolution Technol 2015;22:36-45.
17. Qureshi SA. In vitro-in vivocorrelation (IVIVC) and determining drug concentrations in blood from dissolution testing–a simple and practical approach. Open Drug Delivery J 2010;4:38-47.
18. Blume EJ, Schug BS. The biopharmaceutical classification system (BCS): class III drugs better candidates for BA/BE waiver? Eur J Pharm Sci 1999;9:117–21.
19. Blonde L. Current antihyperglycemic treatment guidelines and algorithms for patients with type 2 diabetes mellitus. Am JMed 2010;123:S12-8.
20. Basit A, Riaz M, Fawwad A. Glimepiride: evidence-based facts, trends, and observations.Vasc Health Risk Manag 2012;8:463-72.
21. Drug Approval Package. Amaryl® (Glimepiride) NDA# 20-496S-002. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/nda/99/020496S002.cfm [Last accessed on 10 Jul 2020]
22. MassiBenedetti M. Glimepiride in type 2 diabetes mellitus: a review of the worldwide therapeutic experience. ClinTher 2003;25:799-816.
23. Sola D, Rossi L, Schianca GP, Maffioli P, Bigliocca M, Mella R, et al. Sulfonylureas and their use in clinical practice. Arch Med Sci 2015;11:840-8.
24. Das IJ, Deepthi R, Rajashekar Y, Samal HB. Design and characterization of glimepiride fast-dissolving tablets. Int J PharmTech Res 2015;8:1-1.
25. WHO Expert Committee on Specifications for Pharmaceutical Preparations. WHO Technical Report Series, No. 937, Annex 8. Proposal to waive in vivo bioequivalence requirements for WHO Model List of Essential Medicines immediate-release, solid oral dosage forms. World Health Organization: Geneva; 2006.
26. Vidyadhara S, Babu JR, Sasidhar RL, Ramu A, Prasad SS, Tejasree M. Formulation and evaluation of glimepiride solid dispersions and their tablet formulations for enhanced bioavailability. Pharmanest 2011;4:15-20.
27. Pharmacopeia, U. S. "35/National Formulary 30." Rockville, MD: US Pharmacopeial Convention, Inc; 2012.
28. Rowe R, Sheske P, Weller P. Handbook of pharmaceutical excipients. In: Rockvilled MD. Asian edition; 2000. p. 843-65.
29. World Health Organization. Guidance on waiver of in vivo bioequivalence requirements. Available from:http://apps.who.int/medicine docs’/documents/s23056en/s23056en.pdf. [Last accessed on 08 Sep 2019]
30. Costa P. An alternative method to the evaluation of similarity factor in dissolution testing. Int J Pharm 2001;220:77–83.
31. Yoshida I, Sakai Y. The applications of the content uniformity test and the weight variation test on process validation tests of multiple ingredient preparations. Chem Pharm Bull 1999;47:678-83.
32. Nishat N, Muhammad A, Rumana M, Farhana R, Ashiqul A. A comparative study of physical parameters of selected ketorolac tromethamine tablets available in the pharma market of Bangladesh. J Appl Pharm 2011;8:101-3.
33. Aulton ME, Taylor K. Aulton’s pharmaceutics: the design and manufacture of medicines. 4thed. New York: Churchill Livingstone Elsevier; 2013.
34. Niazi SK. Handbook of bioequivalence testing. 1sted. New York: Informa Healthcare; 2007.
35. Reddy NH, Patnala S, Kanfer I. Investigation of biowaivers for immediate release formulations containing BCS III drugs, acyclovir, atenolol, and ciprofloxacin hydrochloride, using dissolution testing. AAPS PharmSciTech 2017;18:424-31.
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