INFLUENCE OF DOSE AND USP DISSOLUTION APPARATUS IN THE RELEASE PERFORMANCE OF REFERENCE TABLETS: PROPRANOLOL-HCl AND RANITIDINE-HCl CASES
Keywords:Flow-through cell method, Propranolol-HCl tablets, Ranitidine-HCl tablets, Reference drug products, USP basket apparatus, USP paddle apparatus
Objective: Due to quality of generic formulations depends on available information of reference drug products the aim of this work was to perform an in vitro dissolution study of two doses of propranolol-HCl and ranitidine-HCl reference tablets using USP basket or paddle apparatus and flow-through cell method.
Methods: Two doses of propranolol-HCl (10-mg and 80-mg) and ranitidine-HCl (150-mg and 300-mg) of Mexican reference products were used. Dissolution profiles of propranolol-HCl were obtained with USP basket apparatus at 100 rpm and 1000 ml of 1% hydrochloric acid. Profiles of ranitidine-HCl were determined with USP paddle apparatus at 50 rpm and 900 ml of distilled water. All formulations were also studied with the flow-through cell method using laminar flow at 16 ml/min. Dissolution profiles were compared by model-independent (f2 similarity factor, mean dissolution time and dissolution efficiency) and model-dependent methods (dissolution data adjusted to some mathematical equations). Time data, derived from these adjustments, as t50%, t63.25%, and t85% were used to compare dissolution profiles.
Results: With all approaches used and being high solubility drugs significant differences were found between low and high doses and between USP dissolution apparatuses (*P<0.05).
Conclusion: In vitro dissolution performance of two doses of propranolol-HCl and ranitidine-HCl was not expected. Considering the same USP dissolution apparatus, the reference tablets did not allow the simultaneous release of the used doses. The results could be of interest for pharmaceutical laboratories or health authorities that classify some drug products as a reference to be used in dissolution and bioequivalence studies.
Ashrafi S, Shapouri R, Shirkhani A, Mahdavi M. Anti-tumor effects of propranolol: adjuvant activity on a transplanted murine breast cancer model. Biomed Pharmacother 2018;104:45−51.
Porwal A, Swami G, Saraf SA. Preparation and evaluation of sustained release micro-balloons of propranolol. DARU 2011;19:193−201.
Maharjan R, Subedi G. Formulation and evaluation of floating in situ gel of ranitidine using natural polymers. Int J Pharm Pharm Sci 2014;6:205−9.
World Health Organization. Model List of Essential Medicines; 2017. Available from: https://apps.who.int/iris/bitstream/ handle/10665/273826/EML-20-eng.pdf?ua=1. [Last accessed on 30 Mar 2019].
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;58:265−78.
Vogelpoel H, Welink J, Amidon GL, Junginger HE, Midha KK, Möller H, et al. Biowaiver monographs for immediate release solid oral dosaje forms based on a biopharmaceutics classification system (BCS) literatura data: verapamil hydrochloride, propranolol hydrochloride, and atenolol. J Pharm Sci 2004;93:1945–56.
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.
Food and Drug Administration. Guidance for Industry: Waiver on in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a biopharmaceutics classification system; 2017. Available from: https://www.fda.gov/downloads/Drugs/./Guidances/UCM070246.pdf. [Last accessed on 30 Mar 2019].
United States Pharmacopeia and National Formulary USP 41-NF 36; The United States Pharmacopeial Convention, Inc: Rockville MD; 2018.
Farmacopea de los Estados Unidos Mexicanos. 11a. ed. México DF, Secretaría de Salud; 2014.
Sunesen VH, Pedersen BL, Kristensen HG, Müllertz A. In vitro in vivo correlations for a poorly soluble drug, danazol, using the flow-through dissolution method with biorelevant dissolution media. Eur J Pharm Sci 2005;24:305–13.
Szymanska E, Winnicka K. Comparison of flow-through cell and paddle methods for testing vaginal tablets containing a poorly water-soluble drug. Trop J Pharm Res 2013;12:39–44.
Emara LH, Emam MF, Taa NF, El-Ashmawy AA, Mursi NM. In vitro dissolution study of meloxicam immediate release products using flow-through cell (USP Apparatus 4) under different operational conditions. Int J Pharm Pharm Sci 2014;6:254−60.
Jinno J, Kamada N, Miyake M, Yamada K, Mukai T, Odomi M, et al. In vitro-in vivo correlation for the wet-milled tablet of poorly water-soluble cilostazol. J Controlled Release 2008;130:29−37.
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.
Medina JR, Ortiz HD, Hurtado M, Dominguez Ramirez AM. Influence of dose and the USP basket and flow-through cell dissolution apparatuses in the release kinetics of metronidazole immediate-release products. Int J Res Pharm Sci 2014;5:137−46.
Rediguieri CF, Porta V, Nunes DSG, Nunes TM, Junginger HE, Kopp S, et al. Biowaiver monographs for immediate release solid oral dosage forms: metronidazole. J Pharm Sci 2011;100:1618−27.
Daousani C, Macheras P. Scientific considerations concerning the EMA change in the definition of “dose” of the BCS-based biowaiver guideline and implications for bioequivalence. Int J Pharm 2015;478:606−9.
COFEPRIS. Listado actualizado de medicamentos de referencia 2017/08, Mexico. Available from: https://www.gob.mx/ cms/uploads/attachment/file/197452/lMR_2017-08_V006.pdf. [Last accessed on 30 Mar 2019]
Moore JW, Flanner HH. Mathematical comparison of dissolution profiles. Pharm Technol 1996;20:64−75.
Podczeck F. Comparison of in vitro dissolution profiles by calculating mean dissolution time (MDT) or mean residence time (MRT). Int J Pharm 1993;97:93−100.
Anderson NH, Bauer M, Boussac N, Khan-Malek R, Munden P, Sardaro M. An evaluation of fit factors and dissolution efficiency for the comparison of in vitro dissolution profiles. J Pharm Biomed Anal 1998;17:811−22.
Demirturk E, Oner L. In vitro-in vivo correlations. FABAD J Pharm Sci 2003;28:215−24.
Zhang Y, Huo M, Zhou J, Zou A, Li W, Yao C, et al. DD Solver: an add-in program for modeling and comparison of dissolution profiles. AAPS J 2010;12:263−71.
Yuksel N, Kanik AE, Baykara T. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and independent methods. Int J Pharm 2000;209:57−67.
Kortejarvi H, Shawahna R, Koski A, Malkki J, Ojala K, Yliperttula M. Very rapid dissolution is not needed to guarantee bioequivalence for biopharmaceutics classification system (BCS) I drugs. J Pharm Sci 2010;99:621−5.
Shokhin IE, Ramenskaya GV, Vasilenko GF, Malalshenko EA. Assessment of the possibility of using comparative in vitro dissolution kinetics (biowaiver) instead of in vivo bioequivalence evaluation for establishing the interchangeability of generic drugs. Pharm Chem J 2011;45:107−9.
Langenbucher F, Benz D, Kurth W, Moller H, Otz M. Standardized flow-cell method as an alternative to existing pharmacopoeial dissolution testing. Pharm Ind 1989;51:1276−81.
Steffansen B, Brodin B, Und Nielsen C. editors. Molecular Biopharmaceutics. ULLA Pharmacy Series. Pharmaceutical Press; 2010.
Adams E, Coomans D, Smeyers Verbeke J, Massart DL. Non-linear mixed effects models for the evaluation of dissolution profiles. Int J Pharm 2002;240:37−53.
Food and Drug Administration. Guidance for Industry: Dissolution testing of immediate release solid dosage forms; 1997. Available from: https://www.fda.gov/downloads/drugs/guidances/ucm070237.pdf. [Last accessed on 30 Mar 2019]
Medina JR, Cortes M, Romo E. Comparison of the USP apparatus 2 and 4 for testing the in vitro release performance of ibuprofen generic suspensions. Int J Appl Pharm 2017;9:90−5.
Medina JR, Aguilar E, Hurtado M. Dissolution behavior of carbamazepine suspensions using the USP dissolution apparatus 2 and the flow-through cell method with simulated GI fluids. Int J Pharm Pharm Sci 2017;9:111−6.
Shah VP, Gurbarg M, Noory A, Dighe S, Skelly JP. Influence of high rates of agitation on release patters of immediate-release drug products. J Pharm Sci 1992;81:500−3.
Emara LH, El-Menshawi BS, Estefan MY. In vitro-in vivo correlation and comparative bioavailability of vicamine in prolonged-release preparations. Drug Dev Ind Pharm 2000;26:243−51.
Hurtado M, Vargas Y, Dominguez Ramirez AM, Cortes AR. Comparison of dissolution profiles for albendazole tablets using USP apparatus 2 and 4. Drug Dev Ind Pharm 2003;29:777−84.
Medina JR, Salazar DK, Hurtado M, Cortes AR, Dominguez Ramirez AM. Comparative in vitro dissolution study of carbamazepine immediate-release products using the USP paddles method and the flow-through cell system. Saudi Pharm J 2014;22:141−7.
Cales P. Optimal use of propranolol in portal hypertension. Gastroenterol Clin Biol 2005;29:207−8.
Polli JE. In vitro-in vivo relationships of several “immediate” release tablets containing a low permeability drug. In: Young D, Devane JG, Butler J. editors. In vitro-in vivo correlations. 1st ed. Boston: Springer; 1997. p. 191−8.