The Bioequivalence Between Valsartan Oral Solution and Suspension Formulations Developed for Pediatric Use.
bioequivalence
hypertension
pharmacodynamics
pharmacokinetics
valsartan
Journal
Clinical pharmacology in drug development
ISSN: 2160-7648
Titre abrégé: Clin Pharmacol Drug Dev
Pays: United States
ID NLM: 101572899
Informations de publication
Date de publication:
07 2022
07 2022
Historique:
received:
25
10
2021
accepted:
12
12
2021
pubmed:
21
1
2022
medline:
6
7
2022
entrez:
20
1
2022
Statut:
ppublish
Résumé
The bioequivalence of valsartan 160 mg oral solution compared to suspension was assessed in a single-dose, open-label, randomized, 2-period, 2-way crossover study in 82 healthy adults. The participants were randomly assigned (1:1) to receive a single dose of the solution or suspension formulation in each of the two treatment periods. Serial blood samples for pharmacokinetic evaluation were collected up to 48 hours post-dose. The pharmacokinetic parameters were estimated by noncompartmental methods and analyzed as per bioequivalence criteria of statistical analysis. The peak plasma concentration of valsartan was reached with median time of 1 and 3 hours with solution and suspension formulation, respectively. Compared to suspension formulation, the mean peak plasma concentration with solution formulation was higher by 32% (90%CI, 1.27-1.38) while the geometric mean ratios (1.09) and the associated 90%CIs (1.05-1.13) of both the areas under the concentration time-curves (from time zero to the last quantifiable concentration and from time zero to infinity) were contained in the required range of 0.80 to 1.25. No new safety signals were observed with either of the formulations.
Substances chimiques
Suspensions
0
Tablets
0
Valsartan
80M03YXJ7I
Types de publication
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
843-848Informations de copyright
© 2022, The American College of Clinical Pharmacology.
Références
Song P, Zhang Y, Yu J, et al. Global prevalence of hypertension in children: a systematic review and meta-analysis. JAMA Pediatr. 2019;173(12):1154-1163.
Dionne JM, Abitbol CL, Flynn JT. Hypertension in infancy: diagnosis, management and outcome. Pediatr Nephrol. 2012;27(1):17-32.
Kraut EJ, Boohaker LJ, Askenazi DJ, Fletcher J, Kent AL; Neonatal Kidney Collaborative. Incidence of neonatal hypertension from a large multicenter study [Assessment of Worldwide Acute Kidney Injury Epidemiology in Neonates-AWAKEN]. Pediatr Res. 2018;84(2):279-289.
Ashraf M, Irshad M, Parry NA. Pediatric hypertension: an updated review. Clin Hypertens. 2020;26(1):22.
Cheah WL, Edmund Shin CV, Ayu Akida AR. Blood pressure profile for children aged 5 to 6 years and its associated factors - a cross-sectional study in Kuching district, Sarawak. Malays Fam Physician. 2019;14(1):2-9.
Ghazi L, Drawz P. Advances in understanding the renin-angiotensin-aldosterone system (RAAS) in blood pressure control and recent pivotal trials of RAAS blockade in heart failure and diabetic nephropathy. F1000Res. 2017;6 (F1000 Faculty Rev):297.
Siddiqi N, Shatat IF. Antihypertensive agents: a long way to safe drug prescribing in children. Pediatr Nephrol. 2020;35(11):2049-2065.
Vega IL. ACE inhibitors vs ARBs for primary hypertension. Am Fam Physician. 2015;91(8):522-523.
Jankauskiene A, Drozdz D, Wasilewska A, De Paula Bernardes R, Glazer R, Valentine M, Tan M, Chaiang Y, Bapatla K. Efficacy and safety of valsartan in children aged 1-5 years with hypertension, with or without chronic kidney disease: a randomized, double-blind study followed by open-label phase. Curr Med Res Opin. 2021;1-23.
Blumer J, Batisky DL, Wells T, Shi V, Solar-Yohay S, Sunkara G. Pharmacokinetics of valsartan in pediatric and adolescent subjects with hypertension. J Clin Pharmacol. 2009;49(2):235-241.
Flynn JT, Meyers KE, Neto JP, et al. Efficacy and safety of the Angiotensin receptor blocker valsartan in children with hypertension aged 1 to 5 years. Hypertension. 2008;52(2):222-228.
Schaefer F, van de Walle J, Zurowska A, et al. Efficacy, safety and pharmacokinetics of candesartan cilexetil in hypertensive children from 1 to less than 6 years of age. J Hypertens. 2010;28(5):1083-1090.
Sunkara G, Bende G, Mendonza AE, et al. Bioavailability of valsartan oral dosage forms. Clin Pharmacol Drug Dev. 2014;3(2):132-138.
Nahata MC. Lack of pediatric drug formulations. Pediatrics. 1999;104(3 Pt 2):607-609.
Habtemariam B, Sallas W, Sunkara G, Kern S, Jarugula V, Pillai G. Population pharmacokinetics of valsartan in pediatrics. Drug Metab Pharmacokinet. 2009;24(2):145-152.
Parati G, Asmar R, Bilo G, Kandra A, Di Giovanni R, Mengden T. Effectiveness and safety of high-dose valsartan monotherapy in hypertension treatment: the ValTop study. Hypertens Res. 2010;33(10):986-994.
Chow SC. Bioavailability and bioequivalence in drug development. Wiley Interdiscip Rev Comput Stat. 2014;6(4):304-312.
Prasad PP, Yeh CM, Gurrieri P, Glazer R, McLeod J. Pharmacokinetics of multiple doses of valsartan in patients with heart failure. J Cardiovasc Pharmacol. 2002;40(5):801-807.
Wellington K, Faulds DM. Valsartan/hydrochlorothiazide: a review of its pharmacology, therapeutic efficacy and place in the management of hypertension. Drugs. 2002;62(13):1983-2005.
Fogari R, Zoppi A. A drug safety evaluation of valsartan. Expert Opin Drug Saf. 2011;10(2):295303.