| DOI: https://doi.org/10.14456/mujps.2017.3 | Pharm Sci Asia 2017; 44(1), 32-39 |
Bioequivalence study of diacerein 50 mg capsules in healthy Vietnamese volunteersG.T.H. Nguyen*, N.T.A. Le, H.T.T. Tran, V.N. Nguyen
- Institute of Drug Quality Control - Ho Chi Minh City, 200 Cobac Street, District 1, Ho ChiMinh City, Vietnam
Diacerein is chemically 4, 5-diacetyloxy-9, 10-dioxo-anthracene-2-carboxylic acid and is a disease modifying antirheumatoid drug used in the treatment of Osteoarthritis and chronic inflammatory arthritis. Diacerein is entirely converted into its active metabolite rhein (4,5-dihydroxy - 9,10-dioxoan thracene-2-carboxylic acid) before reaching the systemic circulation. This drug is administered orally as 50 mg twice daily and the the therapeutic concentration of rhein in blood plasma changes in a wide range of 1-10000 ng/mL, so a highly sensitive and accurate HPLC method was developed to quantify rhein in human plasma. This method successfully applied to the bioequivalence study of two formulations of diacerein 50 mg in healthy Vietnamese populations. After dosing, serial blood samples were collected for a period of 24 hrs. The power of all primary pharmacokinetic parameters were greater than 80 % indicating that the number of subjects was enough to confirm the bioequivalence of two formulations. No subject withdrew from our study, and no adverse events were found on analysis of vital signs or laboratory test results during the study. No abnormalities were found in clinical or biochemical parameters when comparing baseline versus end-of-study assessments. The 90% confidence intervals for the ratios of Cmax (93.43 % - 102.80%), AUC0-t (90.17 % - 113.76%) and AUC0-∞ (90.48 % - 113.32%) suggested that a single dose of the test and reference formulations of diacerein met the FDA regulatory requirements of bioequivalence.
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