Generic placeholder image

Current Drug Research Reviews

Editor-in-Chief

ISSN (Print): 2589-9775
ISSN (Online): 2589-9783

Research Article

The Evaluation of Valsartan Biopharmaceutics Properties

Author(s): Lara Maria Lopes de Castro*, Jacqueline de Souza, Tamires Guedes Caldeira, Bruna de Carvalho Mapa, Anna Flávia Matos Soares, Bruna Gomes Pegorelli, Carolina Carvalho Della Croce and Neila Márcia Silva Barcellos

Volume 12, Issue 1, 2020

Page: [52 - 62] Pages: 11

DOI: 10.2174/2589977511666191210151120

Abstract

Background: Solubility, intestinal permeability and dissolution are the main factors that govern the rate and extent of drugs absorption and are directly related to bioavailability. Biopharmaceutics Classification System (BCS) is an important tool which uses in vitro results for comparison with bioavailability in vivo (biowaiver). Valsartan is widely used in the treatment of hypertension and shows different BCS classification in the literature (BCS class II or III).

Objective: This work proposes the study of valsartan biopharmaceutics properties and its BCS classification.

Methods: High Performance Liquid Chromatography (HPLC) method was developed and validated to quantify the drug in buffers pH 1.2, 4.5 and 6.8 respectively. Valsartan solubility was determined in these three different media using shake flask method and intrinsic dissolution rate. Evaluation of dissolution profile from coated tablets was conducted.

Results: The low solubility (pH 1.2 and 4.5) and high solubility (pH 6.8) were observed for both solubility methods. Permeability data reported from the literature showed that valsartan is a low permeability drug. Valsartan presented the rapid release profile only in pH 6.8.

Conclusion: We defined that valsartan is a class IV drug, in disagreement with what has been published so far. It is important to emphasize that the conditions considered here are indicated to define the biopharmaceutics classification by regulatory agencies.

Keywords: Biopharmaceutics classification system, solubility, permeability, dissolution, biowaiver, valsartan.

Graphical Abstract
[1]
World Health Organiozation Global status report on noncommunicable diseases 2014.Available at:. http://apps.who.int/iris/bitstream/handle/10665/148114/9789241564854_eng.pdf; jsessionid= B6D81E18B9AA15E3462A91388559C0A8?sequence=1
[2]
Corrêa TD, Namura JJ, Silva AP, Castro MG, Meneghini A, Ferreira C. Systemic arterial hypertension: News on its epidemiology, diagnosis and treatment. Arq Med ABC 2006; 31: 91-101.
[3]
Mancia G, Fagard R, Narkiewicz K, et al. 2013 ESH/ESC Guidelines for the management of arterial hypertension: The task force for the management of arterial hypertension of the European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). J Hypertens 2013; 31(7): 1281-357.
[http://dx.doi.org/10.1097/01.hjh.0000431740.32696.cc] [PMID: 23817082]
[4]
James PA, Oparil S, Carter BL, et al. 2014 evidence-based guideline for the management of high blood pressure in adults: Report from the panel members appointed to the Eighth Joint National Committee (JNC 8). JAMA 2014; 311(5): 507-20.
[http://dx.doi.org/10.1001/jama.2013.284427] [PMID: 24352797]
[5]
Flesch G, Müller P, Lloyd P. Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man. Eur J Clin Pharmacol 1997; 52(2): 115-20.
[http://dx.doi.org/10.1007/s002280050259] [PMID: 9174680]
[6]
Siddiqui N, Husain A, Chaudhry L, Alam MS, Mitra M, Bhasin PS. Pharmacological and pharmaceutical profile of valsartan: A review. J Appl Pharm Sci 2011; 1: 12-9.
[7]
Saydam M, Takka S. Bioavailability file: Valsartan. FABAD J Pharm Sci 2007; 32: 185-96.
[8]
Buxton ILO, Benet LZ. In: Goodman & Gilman: As bases farmacológicas da terapêutica. AMGH, Ed.. New York: McGraw-Hill 2012; p. 17.
[9]
Amidon GL, Lennernäs H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995; 12(3): 413-20.
[http://dx.doi.org/10.1023/A:1016212804288] [PMID: 7617530]
[10]
US Food and Drug Administration. Guidance for Industry 2017.https://www.fda.gov/downloads/Drugs/Guidances/ucm070246.pdf
[11]
European Medicines Agency. Committee for medicinal products for human use 2010.https://www.ema.europa.eu/documents/scientific-guideline/guideline-investigation-bioequivalence-rev1_en.pdf
[12]
Agência Nacional de Vigilância Sanitária. Resolução nº 37, de 3 de agosto de 2011. Diário Oficial da União 2011.
[13]
World Health Organization (WHO); Forty-ninth report of the WHO expert committee on specifications for pharmaceutical preparations 2015.Available at:. https://www.who.int/medicines/areas/quality_safety/quality_assurance/expert_committee/WHO_TRS_ 992_ web.pdf
[14]
Sreenivasa RB, Seshasayana A, Pardha SSV, Ravi KN, Narayan CPS, Ramana MKV. Correlation of “in vitro” release and “in vivo” absorption characteristics of rifampicin from ethylcellulose coated nonpareil beads. Int J Pharm 2001; 230(1-2): 1-9.
[http://dx.doi.org/10.1016/S0378-5173(01)00835-3] [PMID: 11672951]
[15]
Kaza R, Raju YP, Nagaraju R. Dissolution enhancement of valsartan using natural polymers by solid dispersion technique. Der Pharmacia Lettre 2013; 2: 126-34.
[16]
Chowdary KPR, Shankar KR, Sankar PR. Optimization of valsartan tablet formulation by 23 factorial design. JGTPS 2014; 1: 1374-9.
[17]
Govindaswamy R, Umasankar K. Formulation and evaluation of immediate release valsartan. Capsules by using croscarmellose sodium. IJRPNS 2014; 2: 147-52.
[18]
Kumar AA. kumara MS, Surekha K, Prasad C, Suresh S. Formulation and evaluation of sustained release valsartan matrix tablets by using natural polymers. Int J Pharma Bio Sci 2012; 2: 146-50.
[19]
United States Pharmacopeia. 37th ed. Rockville, MD: United States Pharmacopeial Convention 2014.
[20]
International Conference on Harmonization Validation of analytical procedures: Text and methodology proceedings of the international conference on harmonization. 2005.
[21]
Kumar N, Sangeetha D, Reddy OS, Reddy AM. Development and validation of a dissolution test for delayed release capsule formulation of duloxetine hydrochloride. Curr Pharm Anal 2012; 3: 236-46.
[http://dx.doi.org/10.2174/157341212801619360]
[22]
United States Pharmacopeia. 40th ed. Rockville, MD: United States Pharmacopeial Convention 2017.
[25]
National Health Surveillance Agency. Exchangeable similar medicationsis http://portal.anvisa.gov.br/medicamentos-similares2018.
[26]
United States Pharmacopeia. 39th ed. Rockville, MD: United States Pharmacopeial Convention 2016.
[27]
Khan KA, Rhodes CT. The concept of dissolution efficiency. J Pharm Pharmacol 1975; 27(1): 48-9.
[http://dx.doi.org/10.1111/j.2042-7158.1975.tb09378.x] [PMID: 235616]
[28]
Yu LX, Carlin AS, Amidon GL, Hussain AS. Feasibility studies of utilizing disk intrinsic dissolution rate to classify drugs. Int J Pharm 2004; 270(1-2): 221-7.
[http://dx.doi.org/10.1016/j.ijpharm.2003.10.016] [PMID: 14726137]
[29]
Kerns EH, Di L. Drug-like properties: Concepts, structure design and methods: From ADME to toxicity optimization. 1st ed. Burlington, Massachusetts: Elsevier 2008.
[30]
Kassim NA, Whitehouse M, Ramachandran C, et al. Molecular Properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharmaceutics 2003; 1: 85-96.
[31]
Storpirtis S, Oliveira PG, Rodrigues D, Maranho D. Relevant biopharmacotechnical considerations in the manufacture of generic drugs: Factors affecting the dissolution and absorption of drugs. Braz J Pharm Sci 1999; 1: 1-16.
[32]
Issa MG, Ferraz HG. Intrinsic dissolution as a tool for evaluating drug solubility in accordance with the biopharmaceutics classification system. Dissolut Technol 2011; 18: 6-13.
[http://dx.doi.org/10.14227/DT180311P6]
[33]
Dezani AB, Pereira TM, Caffar AM, Reis JM, Serra CHR. Equilibrium solubility versus intrinsic dissolution: Characterization of lamivudine, stavudine and zidovudine for BCS classification. Braz J Pharm Sci 2013; 49: 853-63.
[http://dx.doi.org/10.1590/S1984-82502013000400026]
[34]
Martinez MN, Amidon GL. A mechanistic approach to understanding the factors affecting drug absorption: A review of fundamentals. J Clin Pharmacol 2002; 42(6): 620-43.
[http://dx.doi.org/10.1177/00970002042006005] [PMID: 12043951]
[35]
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(2): 265-78.
[http://dx.doi.org/10.1016/j.ejpb.2004.03.001] [PMID: 15296954]
[38]
Dressman JB, Fleisher D. Mixing-tank model for predicting dissolution rate control or oral absorption. J Pharm Sci 1986; 75(2): 109-16.
[http://dx.doi.org/10.1002/jps.2600750202] [PMID: 3958917]
[39]
National Health Surveillance Agency. Resolution No 31, of August 11, 2010. Official Diary of the Union 2010.
[40]
Zakeri-Milani P, Barzegar-Jalali M, Azimi M, Valizadeh H. Biopharmaceutical classification of drugs using Intrinsic Dissolution Rate (IDR) and rat intestinal permeability. Eur J Pharm Biopharm 2009; 73(1): 102-6.
[http://dx.doi.org/10.1016/j.ejpb.2009.04.015] [PMID: 19442726]
[41]
D’Arcy DM, Corrigan OI, Healy AM. Evaluation of hydrodynamics in the basket dissolution apparatus using computational fluid dynamics- Dissolution rate implications. Eur J Pharm Sci 2006; 27(2-3): 259-67.
[http://dx.doi.org/10.1016/j.ejps.2005.10.007] [PMID: 16314078]
[42]
Nalluri BN, Krishna MR, Rao TP, Crooks PA. Effect of recrystallization on the pharmaceutical properties of valsartan for improved therapeutic efficacy. J Appl Pharm Sci 2012; 10: 126-32.
[http://dx.doi.org/10.7324/JAPS.2012.21025]
[43]
Souza JB, Souza J, Castro LML, Siqueira MF, Savedra RML, Silva-Barcellos NM. Evaluation of the losartan solubility in the biowaiver context by shake-flask method and intrinsic dissolution. Pharm Dev Technol 2019; 24(3): 283-92.
[http://dx.doi.org/10.1080/10837450.2018.1472610] [PMID: 29723078]
[44]
Oliveira ME, Manzo RH. Rio de. 2009; p. 192.
[45]
Souza J, Freitas ZMF, Storpirtis S. In vitro models for determining drug absorption and predicting the dissolution/absorption ratio. Braz J Pharm Sci 2007; 43: 515-27.
[46]
Marques MRC. Rio de. 2009; p. 96.
[47]
US Food and Drug Administration. Guidance for Industry 2018.https://www.fda.gov/downloads/Drugs/Guidances/UCM456594.pdf
[48]
Shah VP, Konecny JJ, Everett RL, McCullough B, Noorizadeh AC, Skelly JP. In vitro dissolution profile of water-insoluble drug dosage forms in the presence of surfactants. Pharm Res 1989; 6(7): 612-8.
[http://dx.doi.org/10.1023/A:1015909716312] [PMID: 2798311]
[49]
Löbenberg R, Krämer J, Shah VP, Amidon GL, Dressman JB. Dissolution testing as a prognostic tool for oral drug absorption: Dissolution behavior of glibenclamide. Pharm Res 2000; 17(4): 439-44.
[http://dx.doi.org/10.1023/A:1007529020774] [PMID: 10870988]
[50]
He Z, Zhong D, Chen X, Liu X, Tang X, Zhao L. Development of a dissolution medium for nimodipine tablets based on bioavailability evaluation. Eur J Pharm Sci 2004; 21(4): 487-91.
[http://dx.doi.org/10.1016/j.ejps.2003.11.009] [PMID: 14998579]
[51]
Prista LN, Alves AC, Morgado R. Pharmaceutical technology. 5th ed. Lisbon: Calouste Gulbenkian Foundation 1995.
[52]
Sivla RL, Volpato NM. Means for dissolving nimesulide tablets: Action of surfactants. Braz J Pharm Sci 2002; 2: 163-72.
[53]
Balimane PV, Chong S, Morrison RA. Current methodologies used for evaluation of intestinal permeability and absorption. J Pharmacol Toxicol Methods 2000; 44(1): 301-12.
[http://dx.doi.org/10.1016/S1056-8719(00)00113-1] [PMID: 11274897]
[54]
Refsgaard HHF, Jensen BF, Brockhoff PB, Padkjaer SB, Guldbrandt M, Christensen MS. In silico prediction of membrane permeability from calculated molecular parameters. J Med Chem 2005; 48(3): 805-11.
[http://dx.doi.org/10.1021/jm049661n] [PMID: 15689164]
[55]
Sugano K, Takata N, Machida M, Saitoh K, Terada K. Prediction of passive intestinal absorption using bio-mimetic artificial membrane permeation assay and the paracellular pathway model. Int J Pharm 2002; 241(2): 241-51.
[http://dx.doi.org/10.1016/S0378-5173(02)00240-5] [PMID: 12100852]
[56]
Poirier A, Cascais AC, Funk C, Lavé T. Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn 2009; 36(6): 585-611.
[http://dx.doi.org/10.1007/s10928-009-9139-3] [PMID: 19936896]
[57]
Skolnik S, Lin X, Wang J, Chen XH, He T, Zhang B. Towards prediction of in vivo intestinal absorption using a 96-well Caco-2 assay. J Pharm Sci 2010; 99(7): 3246-65.
[http://dx.doi.org/10.1002/jps.22080] [PMID: 20166204]
[58]
Nekkanti V, Venkatesan N, Wang Z, Betageri GV. Improved oral bioavailability of valsartan using proliposomes: Design, characterization and in vivo pharmacokinetics. Drug Dev Ind Pharm 2015; 41(12): 2077-88.
[http://dx.doi.org/10.3109/03639045.2015.1075026] [PMID: 26289004]
[59]
Lozoya-Agullo I, Zur M, Wolk O, et al. In-situ intestinal rat perfusions for human Fabs prediction and BCS permeability class determination: Investigation of the single-pass vs. the Doluisio experimental approaches. Int J Pharm 2015; 480(1-2): 1-7.
[http://dx.doi.org/10.1016/j.ijpharm.2015.01.014] [PMID: 25595387]
[60]
Lozoya-Agullo I, González-Álvarez I, González-Álvarez M, Merino-Sanjuán M, Bermejo M. In Situ perfusion model in rat colon for drug absorption studies: Comparison with small intestine and Caco-2 cell model. J Pharm Sci 2015; 104(9): 3136-45.
[http://dx.doi.org/10.1002/jps.24447] [PMID: 25891783]
[61]
Pérez M, Cárdenas W, Ramírez G, Pérez M, Restrepo P. A comparative, cross-over, double blind, randomized study for bioequivalence assessment between two formulations of valsartan capsules vs. tablets. Colomb Med 2006; 2: 114-20.
[62]
Hedaya MA, Helmy SA. Pharmacokinetic interactions of valsartan and hydrochlorothiazide: An open-label, randomized, 4-period crossover study in healthy Egyptian male volunteers. Clin Ther 2013; 35(6): 846-61.
[http://dx.doi.org/10.1016/j.clinthera.2013.04.014] [PMID: 23795576]
[63]
van de Waterbeemd H, Gifford E. ADMET in silico modelling: Towards prediction paradise? Nat Rev Drug Discov 2003; 2(3): 192-204.
[http://dx.doi.org/10.1038/nrd1032] [PMID: 12612645]

© 2024 Bentham Science Publishers | Privacy Policy