Abstract
Purpose
In this study, a new parameter, volume under response surface (VURS), based on the multiple integrals response surface (MIRS) was applied to establish in vitro-in vivo correlations (IVIVC) refer to in vitro dissolution data and in vivo pharmacokinetic data.
Materials and methods
The in vivo predictive capacity of f2 factor, dissolution efficiency (DE), and VURS were compared by investigating the multi-sourced diclofenac sodium extended-release tablets. In vitro dissolution tests were investigated under various conditions. Beagle dogs were used for in vivo pharmacokinetic study as a preliminary investigation of the new approach. In vivo pharmacokinetic experiments were conducted based on the crossed-over design principle, and the blood concentration was determined by LC-MS/MS method.
Results
Data indicated both DE value and f2 factor were unable to discriminate the significant difference in relative bioavailability among the test formulations, although they could suggest in vivo bio-inequivalent risk to some extent. VURS is successfully explored to establish an IVIVC in beagle dogs with diclofenac sodium extended-release formulations with similar release mechanism.
Conclusions
Compared with DE value and f2 factor, the advantage of VURS was demonstrated to predict in vivo parameters of test formulation with a similar or dissimilar release mechanism.
Similar content being viewed by others
References
Dokoumetzidis A, Macheras P. A century of dissolution research: from Noyes and Whitney to the biopharmaceutics classification system. Int J Pharm. 2006;321(1–2):1–11.
Lee SL, Raw AS, Yu L. Dissolution testing. In: Krishna R, Yu L, editors. Biopharmaceutics applications in drug development. USA: Springer Science + Business Media LLC; 2008. p. 47–74.
Demirtürk E, Öner L. Evaluation of in vitro dissolution profile comparison methods of immediate release gliclazide tablet formulations. J Fac Pharm. 2005;25:1–10.
Yuksel N, Kanik AE, Baykara T. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and -independent methods. Int J Pharm. 2000;209(1–2):57–67.
FDA. Guidance for industry: immediate release solid oral dosage forms— scale-up and postapproval changes: chemistry, manufacturing, and controls; in vitro dissolution testing, and in vivo bioequivalance documentation. Center for Drug Evaluation and Research, Rockville,MD November; 1995.
FDA. Guidance for industry: dissolution testing of immediate release solid oral dosage forms. Center for Drug Evaluation and Research, Rockville, MD August; 1997.
FDA. Guidance for industry: SUPAC-MR: modified release solid oral dosage forms—scale-up and postapproval changes: chemistry, manufacturing, and controls; in vitro dissolution testing, and in vivo bioequivalance documentation. Center for Drug Evaluation and Research, Rockville, MD September; 1997.
Khan KA, Rhodes CT. The concept of dissolution efficiency. J Pharm Pharmacol. 1975;27:48–9.
Wähling C, Schröter C, Hanefeld A. Flow-through cell method and IVIVR for poorly soluble drugs. Dissolution Techn. 2011;11:15–24.
Chuasuwan B, Binjesoh V, Polli JE, Zhang H, Amidon GL, Junginger HE, et al. Biowaiver monographs for immediate release solid oral dosage forms: diclofenac sodium and diclofenac potassium. J Pharm Sci. 2009;98(4):1206–19.
Bertocchi P, Antoniella E, Valvo L, Alimonti S, Memoli A. Diclofenac sodium multisource prolonged release tablets-a comparative study on the dissolution profiles. J Pharm Biomed Anal. 2005;37:679–85.
Jantratid E, De Maio V, Ronda E, Mattavelli V, Vertzoni M, Dressman JB. Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form. Eur J Pharm Sci. 2009;37:434–41.
Ministry of Health, P. R. China. Standard number: WS-133(X-105)-98; 1998.
Chinese Pharmacopoeia Commission. WS1-(X-036)-2006Z. In: Vol. 70 of Drug positive standard. People’s Medical Publishing House Co., LTD: Beijing, China; 2008. p. 134–5.
Chinese Pharmacopoeia Commission. WS1-(X-046)-2006Z. In: Vol. 70 of Drug positive standard. People’s Medical Publishing House Co., LTD: Beijing, China; 2008. p. 160–1.
SFDA. Standard number: YBH09102009; 2009.
Chinese Pharmacopoeia Commission. (2002). Drug positive standards. In: Pharmacopoeia supplement 2002ed. People’s Medical Publishing House Co., LTD: Beijing, China; 2009. p. 34.
Sun C, Shen Y, Sun D, Hang T, Tu J. Method development and validation for the determination of indiquinoline tartrate, a novel kappa opioid agonist, and its related substances by high-performance liquid chromatography. J Chromatogr Sci. 2012;50(4):343–8.
Fu JJ, Wang XL, Xu LS, Meng J, Weng Y, Li GF, et al. Preparation and in vitro–in vivo evaluation of double layer coated and matrix sustained release pellet formulations of diclofenac potassium. Int J Pharm. 2011;406(1–2):84–90.
Abdel-Hamid ME et al. High-performance liquid chromatography–mass spectrometric analysis of furosemide in plasma and its use in pharmacokinetic studies. Il Farmaco. 2000;55(6–7):448–54.
Abdel-Hamid ME, Ladislav N, Hoda H. Determination of diclofenac sodium, flufenamic acid, indomethacin and ketoprofen by LC-APCI-MS. J Pharm Biomed Anal. 2001;24(4):587–94.
Sparidans RW, Lagas JS, Schinkel AH, Schellensa JHM, Beijnena JH. Liquid chromatography–tandem mass spectrometric assay for diclofenac and three primary metabolites in mouse plasma. J Chromatogr B. 2008;872(1–2):77–82.
Lau HSH, Chan K, Shum L, Adair S, Ross H, Eyring H, Gause D and John V. Dose-proportionality of diclofenac sodium (Voltaren) in man. (Conference abstract). Pharmaceutical Res. 1989; 6: S194.
Garbacz G, Wedemeyer RS, Nagel S, Giessmann T, Monnikes H, Wilson CG, et al. Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses. Eur J Pharm Biopharm. 2008;70(2):421–8.
Davit BM, Nwakama PE, Buehler GJ, Conner DP, Haidar SH, Patel DT, et al. Comparing generic and innovator drugs: a review of 12 years of bioequivalence data from the United States Food and Drug Administration. Ann Pharmacother. 2009;43(10):1583–97.
Wen Y, Kolonich HR, Kruszewski KM, Giannoukakis N, Gawalt ES, Meng WS. Retaining antibodies in tumors with a self-assembling injectable system. Mol Pharm. 2013;10(3):1035–44.
Wen Y, Liu W, Bagia C, Zhang S, Bai M, Janjic JM, et al. Antibody-functionalized peptidic membranes for neutralization of allogeneic skin antigen-presenting cells. Acta Biomater. 2014;10(11):4759–67.
Cleland JL, Daugherty A, Mrsny R. Emerging protein delivery methods. Curr Opin Biotechnol. 2001;12(2):212–9.
Wen Y, Meng WS. Recent in vivo evidences of particle-based delivery of small-interfering rna (sirna) into solid tumors. J Pharm Innov. 2014;9(2):158–73.
Author information
Authors and Affiliations
Corresponding authors
Additional information
Baoming Ning and Xi Liu contributed equally to this work.
Rights and permissions
About this article
Cite this article
Ning, B., Liu, X., Luan, H. et al. Characterization of Multi-Sourced Diclofenac Sodium Extended-Release Tablet Dissolution Profiles: A New Approach to Establish an In vitro-In vivo Correlation Based on Multiple Integral Response Surface. J Pharm Innov 10, 302–312 (2015). https://doi.org/10.1007/s12247-015-9227-4
Published:
Issue Date:
DOI: https://doi.org/10.1007/s12247-015-9227-4