Delving into the Latest Updates on Olmesartan Medoxomil/Azelnidipine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Azelnidipine/olmesartan medoxomil, Rezaltas

+ [1]

Target

AT1R x L-type calcium channel

Action

antagonists, blockers

Mechanism

AT1R antagonists(Angiotensin II Receptor Type 1 antagonists), L-type calcium channel blockers(Voltage-gated L-type calcium channel blockers)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Daiichi Sankyo Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (20 Jan 2010),

Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC33H34N4O6

InChIKeyZKFQEACEUNWPMT-UHFFFAOYSA-N

CAS Registry123524-52-7

View All Structures (2)

The purpose of this study is to investigate which combination therapy is more effective in reducing the incidence of cardiovascular events in Japanese elderly high-risk hypertensive patients: AT1 subtype angiotensin II receptor antagonist/calcium channel blocker or AT1 subtype angiotensin II receptor antagonist/low dose diuretic.

Start Date01 Apr 2007

Sponsor / Collaborator

Japan Heart Foundation

100 Clinical Results associated with Olmesartan Medoxomil/Azelnidipine

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100 Translational Medicine associated with Olmesartan Medoxomil/Azelnidipine

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100 Patents (Medical) associated with Olmesartan Medoxomil/Azelnidipine

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1

Literatures (Medical) associated with Olmesartan Medoxomil/Azelnidipine

01 Jan 2020·AAPS PharmSciTech

Chronological Delivery of Antihypertensive Drugs in Bilayered Core-in-Cup Buccoadhesive Tablets: In Vitro and In Vivo Evaluation

Article

Author: Nageeb El-Helaly, Sara ; Rashad, Amira A ; El-Gazayerly, Omaima N ; Abd El Rehim, Randa T

Hypertension shows circadian blood pressure rhythms (day-night pattern) that urge the delivery of antihypertensive drugs at the right time in the desired levels. Thus, a bilayered core-in-cup buccoadhesive tablet was formulated that immediately releases olmesartan, to give a burst effect, and controls azelnidipine release, to prolong its therapeutic effect. The main challenge was the poor bioavailability of azelnidipine due to its poor aqueous solubility and first-pass effect. Hence, liquisolid compact buccoadhesive tablets were prepared to enhance solubility, dissolution profiles, and bypass the oral route. Two factorial designs were conducted to study the type and concentration effect of the mucoadhesive polymers on the dissolution and mucoadhesion of olmesartan and azelnidipine. Characterization studies were conducted regarding drug content, surface pH, water uptake, mucoadhesive strength, in vitro release, and ex vivo permeability. The core-in-cup olmesartan/azelnidipine buccoadhesive tablet showed similar release profile to the statistically optimized formulae of each drug. In vitro dissolution study showed enhanced release of azelnidipine than the directly compressed tablets, to comply with the regulatory standards of controlled release systems. In vivo pharmacokinetic study of olmesartan and azelnidipine conducted on human volunteers against Rezaltas® 10/8 mg tablet showed percentage relative bioavailability of 106.12 and 470.82%, respectively. Graphical Abstract.

100 Deals associated with Olmesartan Medoxomil/Azelnidipine

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	C09D	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	Japan	Daiichi Sankyo Co., Ltd.	20 Jan 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ISC2020	Not Applicable	Post-stroke Fatigue	36	Olmesartan/Azelnidipine combination	(ocvrdonlkr) = wvlhbgvfdd rnjvttpulk (pwjspfhlzy )	-	01 Feb 2020
				High-dose olmesartan	(ocvrdonlkr) = xcdkczmgvf rnjvttpulk (pwjspfhlzy )