Pharmacokinetic and pharmacodynamic evaluation of nano-fixed dose combination for hypertension.
Amlodipine
/ pharmacokinetics
Animals
Antihypertensive Agents
/ pharmacokinetics
Benzimidazoles
/ pharmacokinetics
Biphenyl Compounds
/ pharmacokinetics
Disease Models, Animal
Drug Combinations
Hydrochlorothiazide
/ pharmacokinetics
Hypertension
Male
Nanoparticles
Rats
Rats, Wistar
Tetrazoles
/ pharmacokinetics
Journal
Journal of hypertension
ISSN: 1473-5598
Titre abrégé: J Hypertens
Pays: Netherlands
ID NLM: 8306882
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
pubmed:
7
5
2020
medline:
27
5
2021
entrez:
7
5
2020
Statut:
ppublish
Résumé
The current study was planned to formulate, characterize and evaluate the pharmacokinetics, and pharmacodynamics of a novel 'NanoFDC' comprising hydrochlorothiazide, candesartan (CNDT) and amlodipine. The candidate drugs were loaded in poly(DL-lactide-co-glycolide) by emulsion-diffusion-evaporation method. The formulations were evaluated for their size, morphology, drug loading and in-vitro release individually. Repeat dose pharmacokinetic and pharmacodynamic study of the nano-fixed dose combination (FDC) was done in dexamethasone-induced animal model. The entrapment efficiencies ranged from 44 ± 2.1, 32.2 ± 4 and 40.5 ± 2.6% for amlodipine, hydrochlorothiazide and CNDT, respectively. The nanoparticles ranged in size from 164 to 215 nm. In-vitro release profile of the nanoformulation showed unto 90% release by day 7 in simulated gastric fluid and simulated intestinal fluid, respectively. In pharmacokinetic analysis a sustained-release for 7 days was observed in nano-FDC group. Once weekly oral dosing of nano-FDC of amlodipine, CNDT and hydrochlorothiazide provided adequate antihypertensive effect which was not statistically different from daily dosing of free drugs in dexamethasone-induced animal model. Once weekly oral dosing of nano-FDC of amlodipine, CNDT and hydrochlorothiazide provided adequate antihypertensive effect and was not statistically different from daily dosing of free drugs in dexamethasone-induced animal model. This study provides proof of concept of feasibility of once weekly dosing of a nano-FDC comprising three antihypertensive drugs, which can lead to significant improvement in patient adherence to therapy.
Identifiants
pubmed: 32371763
doi: 10.1097/HJH.0000000000002429
pii: 00004872-202008000-00027
doi:
Substances chimiques
Antihypertensive Agents
0
Benzimidazoles
0
Biphenyl Compounds
0
Drug Combinations
0
Tetrazoles
0
Hydrochlorothiazide
0J48LPH2TH
Amlodipine
1J444QC288
candesartan
S8Q36MD2XX
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1593-1602Références
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