[ASAP] Identification, Synthesis, and Comprehension of an Imidazole N ‑3 Regioisomeric Impurity of Olmesartan Medoxomil Key Intermediate
Organic Process Research& DevelopmentDOI: 10.1021/acs.oprd.2c00002 (Source: Organic Process Research and Development)
Source: Organic Process Research and Development - February 18, 2022 Category: Chemistry Authors: Jianwu Lu, Xiao Li, Shun Yuan, Yinquan Wang, Han Sun, Weizhao Weng, Yinfei Shi, Xiaoxu Wang, Kongcheng Huang, Xun Sun, and Taizhi Wu Source Type: research
The Clinical Efficacy of Clopidogrel Bisulfate Tablets Combined with Olmesartan Medoxomil for Ischemic Stroke with Hypertension and the Effect of Angiotensin II Type 1 Receptor Level on Prognosis
CONCLUSION: Clopidogrel bisulfate tablets combined with olmesartan medoxomil has prominent clinical effects in the treatment of ischemic stroke patients with hypertension, evidently improving the prognosis. In addition, the level of AT1R may be a vital factor affecting the prognosis.PMID:34745325 | PMC:PMC8566065 | DOI:10.1155/2021/4487393 (Source: Computational and Mathematical Methods in Medicine)
Source: Computational and Mathematical Methods in Medicine - November 8, 2021 Category: Statistics Authors: Jia Yu Wei Fang Xing Guo Haiyang Jiang Peng Sun Yufeng Liu Xin Jin Source Type: research
Comparison of pharmacodynamics and celiac effects of olmesartan medoxomil formulations by using olmesartan-induced celiac-rat-model
In this study, an artificial hypertension model was established with dose of 185 µmol /kg L-NAME (N ω-nitro-L-arginine methyl ester) twice in a day intraperitoneally in Wistar albino rats. To determine and compare side effects, the OM-Suspension and OM-SMEDDS were administered at 1.3 mg/kg therapeutic dose during one-month period to the rats. Tension of rats was recorded by measuring from their tails with non invasive blood pressure system. We observed celiac like enteropathy findings like villous atrophy and intraepithelial lymphocytosis and clinical changes like weight loss and severe diarrhea after the treatment with ...
Source: Current Drug Delivery - July 6, 2021 Category: Drugs & Pharmacology Authors: Yelda Komesli Bekir Ugur Ergur Ercument Karasulu Source Type: research
Comparison of pharmacodynamics and celiac effects of olmesartan medoxomil formulations by using olmesartan-induced celiac-rat-model
In this study, an artificial hypertension model was established with dose of 185 µmol /kg L-NAME (N ω-nitro-L-arginine methyl ester) twice in a day intraperitoneally in Wistar albino rats. To determine and compare side effects, the OM-Suspension and OM-SMEDDS were administered at 1.3 mg/kg therapeutic dose during one-month period to the rats. Tension of rats was recorded by measuring from their tails with non invasive blood pressure system. We observed celiac like enteropathy findings like villous atrophy and intraepithelial lymphocytosis and clinical changes like weight loss and severe diarrhea after the treatment with ...
Source: Current Drug Delivery - July 6, 2021 Category: Drugs & Pharmacology Authors: Yelda Komesli Bekir Ugur Ergur Ercument Karasulu Source Type: research
Comparison of pharmacodynamics and celiac effects of olmesartan medoxomil formulations by using olmesartan-induced celiac-rat-model
In this study, an artificial hypertension model was established with dose of 185 µmol /kg L-NAME (N ω-nitro-L-arginine methyl ester) twice in a day intraperitoneally in Wistar albino rats. To determine and compare side effects, the OM-Suspension and OM-SMEDDS were administered at 1.3 mg/kg therapeutic dose during one-month period to the rats. Tension of rats was recorded by measuring from their tails with non invasive blood pressure system. We observed celiac like enteropathy findings like villous atrophy and intraepithelial lymphocytosis and clinical changes like weight loss and severe diarrhea after the treatment with ...
Source: Current Drug Delivery - July 6, 2021 Category: Drugs & Pharmacology Authors: Yelda Komesli Bekir Ugur Ergur Ercument Karasulu Source Type: research
Development and validation of a stability-indicating UPLC method for the determination of Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide degradation impurities in their triple-combination dosage form using factorial design of experiments
Biomed Chromatogr. 2021 Jun 10:e5194. doi: 10.1002/bmc.5194. Online ahead of print.ABSTRACTThe current work describes development and validation of a stability-indicating UPLC method for the determination of Olmesaratan Medoxomil (OLM), Amlodipine Besylate (AMB), Hydrochlorothiazide (HCT) and their degradation products in the triple-combination tablet dosage form. The separation was achieved using Zorbax Eclipse plus C8 RRHD (100mm x 3.0 mm), 1.8μm column with gradient elution of mobile phase-A containing 0.02M of sodium phosphate buffer (pH 3.35) and mobile phase B as acetonitrile and water (90:10, v/v). The detector sig...
Source: Biomedical Chromatography : BMC - June 10, 2021 Category: Biomedical Science Authors: Vishnu Murthy Marisetti Prakash Katakam Vijaya Krishna Siddhani Naresh Kumar Katari Source Type: research
Development and validation of a stability-indicating UPLC method for the determination of Olmesartan Medoxomil, Amlodipine and Hydrochlorothiazide degradation impurities in their triple-combination dosage form using factorial design of experiments
Biomed Chromatogr. 2021 Jun 10:e5194. doi: 10.1002/bmc.5194. Online ahead of print.ABSTRACTThe current work describes development and validation of a stability-indicating UPLC method for the determination of Olmesaratan Medoxomil (OLM), Amlodipine Besylate (AMB), Hydrochlorothiazide (HCT) and their degradation products in the triple-combination tablet dosage form. The separation was achieved using Zorbax Eclipse plus C8 RRHD (100mm x 3.0 mm), 1.8μm column with gradient elution of mobile phase-A containing 0.02M of sodium phosphate buffer (pH 3.35) and mobile phase B as acetonitrile and water (90:10, v/v). The detector sig...
Source: Biomedical Chromatography : BMC - June 10, 2021 Category: Biomedical Science Authors: Vishnu Murthy Marisetti Prakash Katakam Vijaya Krishna Siddhani Naresh Kumar Katari Source Type: research
[ASAP] Understanding and Controlling the Formation of an < italic toggle="yes" > N < /italic > -Alkyl Impurity in Olmesartan Medoxomil: A Derivative via Michael-Type Addition between Tetrazole and Mesityl Oxide In Situ Generated from Acetone
Organic Process Research& DevelopmentDOI: 10.1021/acs.oprd.0c00506 (Source: Organic Process Research and Development)
Source: Organic Process Research and Development - May 6, 2021 Category: Chemistry Authors: Jianwu Lu, Yinfei Shi, Xiao Li, Xiaomin Liang, Yinquan Wang, Shun Yuan, and Taizhi Wu Source Type: research
Convergent Synthesis of Angiotensin II Receptor Blockers through C –H Arylation of 1-Benzyl-5-phenyl-1H-tetrazole with Functionalized Aryl Bromides
Synthesis DOI: 10.1055/a-1472-0925 Highly convergent synthesis of angiotensin II receptor blockers has been accomplished by means of late-stage C–H arylation using functionalized aryl bromides. C–H arylation of 1-benzyl-5-phenyl-1H-tetrazole with aryl bromides carrying methyl 2-ethoxybenzimidazole-7-carboxylate unexpectedly provided coupling products where ethyl group was migrated from oxygen to nitrogen atom. The O-to-N ethyl migration was completely suppressed by the use of N-pivaloyl-l-valine rather than the combined use of triphenylphosphine and sodium mesitylenesulfonate to result in the preferential formation of ...
Source: Synthesis - March 31, 2021 Category: Chemistry Authors: Seki, Masahiko Takahashi, Yusuke Tags: paper Source Type: research
ARB-Based Combination Therapy for the Clinical Management of Hypertension and Hypertension-Related Comorbidities: A Spotlight on Their Use in COVID-19 Patients
AbstractEssential hypertension is the most common cardiovascular (CV) risk factor, being primarily involved in the pathogenesis of CV disease and mortality worldwide. Given the high prevalence and growing incidence of this clinical condition in the general population in both high and low-income countries, antihypertensive drug therapies are frequently prescribed in different hypertension-related CV diseases and comorbidities. Among these conditions, evidence are available demonstrating the clinical benefits of lowering blood pressure (BP) levels, particularly in those hypertensive patients at high or very high CV risk prof...
Source: High Blood Pressure and Cardiovascular Prevention - March 12, 2021 Category: Cardiology Source Type: research
Visualisation of real-time oral biodistribution of fluorescent labeled self-microemulsifying drug delivery system of olmesartan medoxomil using optical imaging method.
This study showed that OM-SMEDDS can be succesfully labeled with fluorescent dye and tracked with optical imaging method for the visualisation of biodistribution of drugs and is also useful for enhanced bioavailability.
PMID: 33191089 [PubMed - as supplied by publisher] (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - November 17, 2020 Category: Drugs & Pharmacology Tags: Drug Metab Pharmacokinet Source Type: research
Solubility determination and solution thermodynamics of olmesartan medoxomil in (PEG-400 + water) cosolvent mixtures.
Authors: Al-Shdefat R
Abstract
The solubility and solution thermodynamic properties of a weakly water-soluble compound olmesartan medoxomil (OLM) in binary "polyethylene glycol (PEG-400) + water" cosolvent compositions were determined. The "mole fraction solubility (x e)" of OLM in binary "PEG-400 + water" cosolvent compositions and pure solvents (PEG-400 and water) was determined at "T = 295.15-330.15 K" and "p = 0.1 MPa". The Hansen solubility parameter (HSP) of OLM, pure PEG-400, pure water and binary "PEG-400 + water" cosolvent compositions free of OLM were also predicted. The obtained x e va...
Source: Drug Development and Industrial Pharmacy - November 6, 2020 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research
Correction to: Bioavailability Enhancement of Olmesartan Medoxomil Using Hot-Melt Extrusion: In-Silico, In-Vitro, and In-Vivo Evaluation.
Abstract
During production, the supplemental file "Trajectory analysis of 5ns MD simulation of VA-64 and OLM.mpeg", as well as the "RunNo and Serial numbers", for Table III and Table VII respectively, were inadvertently omitted from the published article.
PMID: 33006687 [PubMed - as supplied by publisher] (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - October 1, 2020 Category: Drugs & Pharmacology Authors: Jadhav P, Gokarna V, Deshpande V, Vavia P Tags: AAPS PharmSciTech Source Type: research
Bioavailability Enhancement of Olmesartan Medoxomil Using Hot-Melt Extrusion: In-Silico, In-Vitro, and In-Vivo Evaluation.
Abstract
Olmesartan medoxomil (OLM) an antihypertensive molecule with poor solubility and poor bioavailability (26% when taken orally) was selected as a model drug. Herein, rationale development of amorphous solid dispersion with hot-melt extrusion of poorly bioavailable OLM was carried out with the aid of quality by design (QbD), in-silico, in-vitro, and in-vivo evaluations. Polymer selection commenced with the selection of thermoplastic water-soluble polymers with the compatible processing temperature window as per the thermal behavior of OLM. Molecular dynamics (MD) simulations as well assisted in the s...
Source: AAPS PharmSciTech - September 3, 2020 Category: Drugs & Pharmacology Authors: Jadhav P, Gokarna V, Deshpande V, Vavia P Tags: AAPS PharmSciTech Source Type: research
