Solid lipid nanoparticles as vesicles for oral delivery of Olmesartan Medoxomil: Formulation, optimization and in vivo evaluation.
CONCLUSION: In conclusion, SLN show promising approaches as a vehicle for oral delivery of drugs like OLM.
PMID: 28005442 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - December 24, 2016 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion
Publication date: December 2016 Source:Regulatory Toxicology and Pharmacology, Volume 82 Author(s): Bapi Gorain, Hira Choudhury, Rakesh Kumar Tekade, Saumen Karan, P. Jaisankar, Tapan Kumar Pal Poor aqueous solubility and unfavourable de-esterification of olmesartan medoxomil (a selective angiotensin II receptor blocker), results in low oral bioavailability of less than 26%. Improvement of oral bioavailability with prolonged pharmacodynamics activity of olmesartan in Wistar rats had been approached by nanoemulsification strategy in our previous article [Colloid Surface B, 115, 2014: 286]. In continuation to that wo...
Source: Regulatory Toxicology and Pharmacology - November 6, 2016 Category: Toxicology Source Type: research
Olmesartan Prevented Intra-articular Inflammation Induced by Zymosan in Rats.
The objective of this study was to study the effect of olmesartan medoxomil (OLM), an antihypertensive drug, on intra-articular inflammation induced by zymosan (Zy) in Wistar rats. Intra-articular inflammation was induced in the right knees of rats by 1 mg Zy dissolved in saline. The animals were divided into the following groups: saline only (oral saline and intra-articular saline); Zy only (intra-articular Zy and oral saline), and intra-articular Zy and oral OLM (5, 15, or 30 mg/kg) or diclofenac sodium (SD; 100 mg/kg). Twenty-four hours after Zy injection, synovial fluid was collected for total leukocyte counts, b...
Source: Biological and Pharmaceutical Bulletin - November 4, 2016 Category: Drugs & Pharmacology Authors: Guerra GC, de Menezes MS, de Araújo AA, de Araújo Júnior RF, de Medeiros CA Tags: Biol Pharm Bull Source Type: research
Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion.
Abstract
Poor aqueous solubility and unfavourable de-esterification of olmesartan medoxomil (a selective angiotensin II receptor blocker), results in low oral bioavailability of less than 26%. Improvement of oral bioavailability with prolonged pharmacodynamics activity of olmesartan in Wistar rats had been approached by nanoemulsification strategy in our previous article [Colloid Surface B, 115, 2014: 286]. In continuation to this work, we herewith report the biodistribution behaviour and 28-day repeated dose subchronic toxicity of olmesartan medoxomil nanoemulsion in Wistar rats following oral administrat...
Source: Regulatory Toxicology and Pharmacology : RTP - October 31, 2016 Category: Toxicology Authors: Gorain B, Choudhury H, Tekade RK, Karan S, Jaisankar P, Pal TK Tags: Regul Toxicol Pharmacol Source Type: research
Assessment of the Cardiovascular Risk of Olmesartan Medoxomil-Based Treatment: Meta-Analysis of Individual Patient Data
DiscussionThe results from this meta-analysis did not show a clinically meaningful or statistically significant difference in cardiovascular risk between OM and the placebo/active control groups, and thus did not corroborate the numerical imbalance observed in ROADMAP and ORIENT. (Source: American Journal of Cardiovascular Drugs)
Source: American Journal of Cardiovascular Drugs - August 25, 2016 Category: Cardiology Source Type: research
Byvalson - A Beta Blocker/ARB Combination for Hypertension
Date: September 12, 2016
Issue #:
1503Summary:
The FDA has approvedByvalson (Allergan), a fixed-dose
combination of the beta blocker nebivolol(Bystolic) and the angiotensin receptor blocker (ARB)
valsartan (Diovan, and generics), for treatment of
hypertension. It is the only combination product that
contains nebivolol, and the first to combine a beta
blocker with an ARB. (Source: The Medical Letter)
Source: The Medical Letter - August 24, 2016 Category: Drugs & Pharmacology Authors: admin Tags: ACE inhibitors Amlodipine Angiotensin receptor blockers Atacand Atenolol Avalide azilsartan Azor Bendroflumethiazide Benicar Beta blockers Bisoprolol Bystolic Byvalson Chlorthalidone Corzide Diovan Diuretics Edarbyclor Source Type: research
Population Pharmacokinetic Modeling of Olmesartan, the Active Metabolite of Olmesartan Medoxomil, in Patients with Hypertension
ConclusionThe final population pharmacokinetic model was demonstrated to be appropriate and effective and it can be used to assess the pharmacokinetic parameters of olmesartan in Indian patients with hypertension. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - August 16, 2016 Category: Drugs & Pharmacology Source Type: research
Olmesartan medoxomil: a guide to its use as monotherapy or in fixed-dose combinations with amlodipine and/or hydrochlorothiazide
AbstractOlmesartan medoxomil (OLM)-based antihypertensive treatment is a valuable option in the treatment of patients with mild to severe hypertension, including those with difficult-to-treat disease. Once-daily OLM, as monotherapy or in combination with hydrochlorothiazide (HCT) and/or amlopidine (AML), provides blood pressure (BP) control over the entire 24-h dosing interval, reduces systolic and diastolic BP, enables patients to achieve BP goals and is generally well tolerated. In patients who require treatment with two or more antihypertensives, treatment with fixed-dose combinations (FDC) of OLM (an angiotensin II rec...
Source: Drugs and Therapy Perspectives - August 11, 2016 Category: Drugs & Pharmacology Source Type: research
In vitro and in vivo effects of morin on the intestinal absorption and pharmacokinetics of olmesartan medoxomil solid dispersions.
CONCLUSION: Our study demonstrated that increased solubilization through freeze-dried OLM loaded solid dispersion together with efflux inhibition improved intestinal permeability to one system that might lead to novel solubilization and efflux pump inhibition as a novel alternative potential to increase oral absorption and bioavailability of OLM.
PMID: 27487480 [PubMed - as supplied by publisher] (Source: Drug Development and Industrial Pharmacy)
Source: Drug Development and Industrial Pharmacy - August 4, 2016 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
The Impact of Azilsartan Medoxomil Treatment (Capsule Formulation) at Doses Ranging From 10 to 80 mg: Significant, Rapid Reductions in Clinic Diastolic and Systolic Blood Pressure
In this phase 2, multicenter, parallel‐group, double‐blind, dose‐ranging study, hypertensive adults (n=449) were randomized to receive one of five doses of a capsule formulation of azilsartan medoxomil (AZL‐M; 5, 10, 20, 40, 80 mg), olmesartan medoxomil (OLM) 20 mg, or placebo once daily. The primary endpoint was change in trough clinic diastolic blood pressure (DBP) at week 8. AZL‐M provided rapid statistically and clinically significant reductions in DBP and systolic blood pressure (SBP) vs placebo at all doses except 5 mg. Placebo‐subtracted changes were greatest with the 40 mg dose (DBP, −5.7 mm Hg;...
Source: The Journal of Clinical Hypertension - July 31, 2016 Category: Cardiology Authors: Alfonso Perez, Charlie Cao Tags: Original Paper Source Type: research
Azilsartan in Patients With Mild to Moderate Hypertension Using Clinic and Ambulatory Blood Pressure Measurements
This was a phase 2, multicenter, randomized, parallel‐group, double‐blind dose‐ranging study. Hypertensive adults (n=555) received one of five doses of azilsartan (AZL; 2.5, 5, 10, 20, 40 mg), olmesartan medoxomil (OLM) 20 mg, or placebo once daily. The primary endpoint was change in trough clinic diastolic blood pressure (DBP) at week 8. Compared with placebo, all AZL doses (except 2.5 mg) provided statistically and clinically significant reductions in DBP and systolic blood pressure (SBP) based on both clinic blood pressure (BP) and 24‐hour ambulatory BP monitoring (ABPM). AZL 40 mg was statistically superior vs ...
Source: The Journal of Clinical Hypertension - June 30, 2016 Category: Cardiology Authors: Alfonso Perez, Charlie Cao Tags: Original Paper Source Type: research
Persistent olmesartan-based blood pressure–lowering effects on morning hypertension in Asians: the HONEST study
Persistent olmesartan-based blood pressure–lowering effects on morning hypertension in Asians: the HONEST study
Hypertension Research 39,
334 (May 2016). doi:10.1038/hr.2015.148
Authors: Kazuomi Kario, Ikuo Saito, Toshio Kushiro, Satoshi Teramukai, Mai Yaginuma, Yoshihiro Mori, Yasuyuki Okuda, Fumiaki Kobayashi & Kazuyuki Shimada (Source: Hypertension Research)
Source: Hypertension Research - May 5, 2016 Category: Cardiology Authors: Kazuomi KarioIkuo SaitoToshio KushiroSatoshi TeramukaiMai YaginumaYoshihiro MoriYasuyuki OkudaFumiaki KobayashiKazuyuki Shimada Tags: angiotensin receptor antagonists Asia blood pressure monitoring olmesartan medoxomil Source Type: research
Augmented circadian rhythm of the intrarenal renin–angiotensin systems in anti-thymocyte serum nephritis rats
Augmented circadian rhythm of the intrarenal renin–angiotensin systems in anti-thymocyte serum nephritis rats
Hypertension Research 39,
312 (May 2016). doi:10.1038/hr.2015.151
Authors: Shinsuke Isobe, Naro Ohashi, Sayaka Ishigaki, Takayuki Tsuji, Yukitoshi Sakao, Akihiko Kato, Hiroaki Miyajima, Yoshihide Fujigaki, Akira Nishiyama & Hideo Yasuda (Source: Hypertension Research)
Source: Hypertension Research - May 5, 2016 Category: Cardiology Authors: Shinsuke IsobeNaro OhashiSayaka IshigakiTakayuki TsujiYukitoshi SakaoAkihiko KatoHiroaki MiyajimaYoshihide FujigakiAkira NishiyamaHideo Yasuda Tags: anti-thymocyte serum nephritis circadian rhythm Intrarenal RAS olmesartan medoxomil Source Type: research
Design, formulation and optimization of novel soft nano-carriers for transdermal olmesartan medoxomil delivery: In vitro characterization and in vivo pharmacokinetic assessment
The objective of the work was to formulate, optimize and evaluate the transdermal potential of novel vesicular nano-invasomes, containing above anti-hypertensive agent. To achieve the above purpose, soft carriers (viz. nano-invasomes) of olmesartan with β-citronellene as potential permeation enhancer were developed and optimized using Box-Behnken design. The physicochemical characteristics e.g., vesicle size, shape, entrapment efficiency and skin permeability of the nano-invasomes formulations were evaluated. The optimized formulation was further evaluated for in vitro drug release, confocal microscopy and in vivo pharmac...
Source: International Journal of Pharmaceutics - April 8, 2016 Category: Drugs & Pharmacology Source Type: research
Erratum to: Efficacy and Safety Study of Olmesartan Medoxomil, Amlodipine, and Hydrochlorothiazide Combination Therapy in Patients with Hypertension Not Controlled with Olmesartan Medoxomil and Hydrochlorothiazide Combination Therapy: Results of a Randomized, Double-Blind, Multicenter Trial
(Source: American Journal of Cardiovascular Drugs)
Source: American Journal of Cardiovascular Drugs - March 18, 2016 Category: Cardiology Source Type: research
