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[PMID]: 28271908 [Au] Autor: Nagaraj K; Narendar D; Kishan V [Ad] Endereço: a Department of Pharmaceutical Sciences , Laboratory of Nanotechnology, University College of Pharmaceutical Sciences, Kakatiya University , Warangal , India. [Ti] Título: Development of olmesartan medoxomil optimized nanosuspension using the Box-Behnken design to improve oral bioavailability. [So] Source: Drug Dev Ind Pharm;43(7):1186-1196, 2017 Jul. [Is] ISSN: 1520-5762 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: The aim of the present investigation was to enhance the oral bioavailability of olmesartan medoxomil by improving its solubility and dissolution rate by preparing nanosuspension (OM-NS), using the Box-Behnken design. In this, four factors were evaluated at three levels. Independent variables include: concentration of drug (X ), concentration of surfactant (X ), concentration of polymer (X ) and number of homogenization cycles (X ). Based on preliminary studies, the size (Y ), zeta potential (ZP) (Y ) and % drug release at 5 min (Y ) were chosen as dependent responses. OM-NS was prepared by high pressure homogenization method. The size, PDI, ZP, assay, in vitro release and morphology of OM-NS were characterized. Further, the pharmacokinetic (PK) behavior of OM-NS was evaluated in male wistar rats. Statistically optimized OM-NS formulation exhibited mean particle size of 492 nm, ZP of -27.9 mV and 99.29% release in 5 min. OM-NS showed more than four times increase in its solubility than pure OM. DSC and XRD analyses indicated that the drug incorporated into OM-NS was in amorphous form. The morphology of OM-NS was found to be nearly spherical with high dispersity by scanning electron microscopic studies. The PK results showed that OM lyophilized nanosuspension (NS) exhibited improved PK properties compared to coarse powder suspension and marketed tablet powder suspension (TS). Oral bioavailability of lyophilized NS was increased by 2.45 and 2.25 folds when compared to marketed TS and coarse powder suspension, respectively. Results of this study lead to conclusion that NS approach was effective in preparing OM formulations with enhanced dissolution and improved oral bioavailability. [Mh] Termos MeSH primário: Administração Oral Composição de Medicamentos/métodos Excipientes/química Liofilização/métodos Olmesartana Medoxomila/administração & dosagem Suspensões/administração & dosagem [Mh] Termos MeSH secundário: Animais Disponibilidade Biológica Química Farmacêutica Liberação Controlada de Fármacos Microscopia Eletrônica de Varredura Microscopia Eletrônica de Transmissão Olmesartana Medoxomila/química Tamanho da Partícula Ratos Ratos Wistar Solubilidade Tensoativos Suspensões/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Excipients); 0 (Surface-Active Agents); 0 (Suspensions); 6M97XTV3HD (Olmesartan Medoxomil) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170913 [Lr] Data última revisão: 170913 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170309 [St] Status: MEDLINE [do] DOI: 10.1080/03639045.2017.1304955

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[PMID]: 28116656 [Au] Autor: Jain S; Patel K; Arora S; Reddy VA; Dora CP [Ad] Endereço: Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S, Nagar, Punjab, 160062, India. sanyogjain@niper.ac.in. [Ti] Título: Formulation, optimization, and in vitro-in vivo evaluation of olmesartan medoxomil nanocrystals. [So] Source: Drug Deliv Transl Res;7(2):292-303, 2017 Apr. [Is] ISSN: 2190-3948 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: The aim of the present study is to increase the saturation solubility and oral bioavailability of olmesartan medoxomil (OLM) using nano-sized crystals produced using a combination of antisolvent precipitation and high-shear homogenization. A response surface design comprising 46 runs was used to optimize the OLM nanocrystal formulation. The optimized formulation was produced using a combination of D-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS) (0.7% w/v), Pluronic F-68® (0.5% w/v), and drug concentration (0.2% w/v) and subjected to 10 and 15 homogenization cycles at 1000 and 1700 bar, respectively. The particle size, polydispersity index (PDI), and zeta potential of optimized formulation were found to be 140 ± 10.34 nm, 0.07 ± 0.016, and -21.43 ± 2.33 mV, respectively. The optimized formulation exhibited irregular morphology as evaluated by scanning electron microscopy and was crystalline as determined by thermal analysis and powder X-ray diffraction studies. OLM nanocrystals showed a marked increase in the saturation solubility as well as rapid dissolution rate in comparison with the pure drug. No significant change in the particle size, PDI, and zeta potential was observed when optimized formulation was stored at room and refrigeration conditions for 3 months. Lastly, in vivo pharmacokinetic studies in Sprague-Dawley rats substantiate the ability of OLM nanocrystal formulation to significantly improve (∼4.6-fold) the oral bioavailability of OLM in comparison with the free drug. This study has established a potential and commercial viable OLM formulation with enhanced saturation solubility and in vivo oral bioavailability. [Mh] Termos MeSH primário: Anti-Hipertensivos Nanopartículas Olmesartana Medoxomila [Mh] Termos MeSH secundário: Animais Anti-Hipertensivos/administração & dosagem Anti-Hipertensivos/sangue Anti-Hipertensivos/química Anti-Hipertensivos/farmacocinética Disponibilidade Biológica Varredura Diferencial de Calorimetria Química Farmacêutica Liberação Controlada de Fármacos Feminino Microscopia Eletrônica de Varredura Nanopartículas/administração & dosagem Nanopartículas/química Olmesartana Medoxomila/administração & dosagem Olmesartana Medoxomila/sangue Olmesartana Medoxomila/química Olmesartana Medoxomila/farmacocinética Tamanho da Partícula Poloxâmero/química Difração de Pó Ratos Sprague-Dawley Tensoativos/química Difração de Raios X [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antihypertensive Agents); 0 (Surface-Active Agents); 106392-12-5 (Poloxamer); 6M97XTV3HD (Olmesartan Medoxomil) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171111 [Lr] Data última revisão: 171111 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170125 [St] Status: MEDLINE [do] DOI: 10.1007/s13346-016-0355-2

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[PMID]: 28005442 [Au] Autor: Nooli M; Chella N; Kulhari H; Shastri NR; Sistla R [Ad] Endereço: a Department of Pharmaceutics , National Institute of Pharmaceutical Education and Research (NIPER) - Hyderabad , Hyderabad , India. [Ti] Título: Solid lipid nanoparticles as vesicles for oral delivery of olmesartan medoxomil: formulation, optimization and in vivo evaluation. [So] Source: Drug Dev Ind Pharm;43(4):611-617, 2017 Apr. [Is] ISSN: 1520-5762 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: OBJECTIVE: Olmesartan medoxomil (OLM) is an antihypertensive drug with low oral bioavailability (28%) resulting from poor aqueous solubility, presystemic metabolism and P-glycoprotein mediated efflux. The present investigation studies the role of lipid nanocarriers in enhancing the OLM bioavailability through oral delivery. MATERIALS AND METHODS: Solid lipid nanoparticles (SLN) were prepared by solvent emulsion-evaporation method. Statistical tools like regression analysis and Pareto charts were used to detect the important factors effecting the formulations. Formulation and process parameters were then optimized using mean effect plot and contour plots. The formulations were characterized for particle size, size distribution, surface charge, percentage of drug entrapped in nanoparticles, drug-excipients interactions, powder X-ray diffraction analysis and drug release in vitro. RESULTS AND DISCUSSION: The optimized formulation comprised glyceryl monostearate, soya phosphatidylcholine and Tween 80 as lipid, co-emulsifier and surfactant, respectively, with an average particle size of 100 nm, PDI 0.291, zeta potential of -23.4 mV and 78% entrapment efficiency. Pharmacokinetic evaluation in male Sprague Dawley rats revealed 2.32-fold enhancement in relative bioavailability of drug from SLN when compared to that of OLM plain drug on oral administration. CONCLUSION: In conclusion, SLN show promising approaches as a vehicle for oral delivery of drugs like OLM. [Mh] Termos MeSH primário: Lipídeos/química Nanopartículas/química Olmesartana Medoxomila/administração & dosagem Olmesartana Medoxomila/química [Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/química Administração Oral Animais Anti-Hipertensivos/administração & dosagem Anti-Hipertensivos/química Anti-Hipertensivos/farmacocinética Disponibilidade Biológica Química Farmacêutica/métodos Portadores de Fármacos/química Estabilidade de Medicamentos Emulsões/química Emulsões/farmacocinética Excipientes/química Masculino Olmesartana Medoxomila/farmacocinética Tamanho da Partícula Ratos Ratos Sprague-Dawley Solubilidade Tensoativos/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Antihypertensive Agents); 0 (Drug Carriers); 0 (Emulsions); 0 (Excipients); 0 (Lipids); 0 (Surface-Active Agents); 6M97XTV3HD (Olmesartan Medoxomil) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161223 [St] Status: MEDLINE [do] DOI: 10.1080/03639045.2016.1275666

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[PMID]: 27487480 [Au] Autor: Surampalli G; Satla M; Nanjwade BK; Patil PA [Ad] Endereço: a Department of Pharmacology and Toxicology , Vaagdevi Institute of Pharma Sciences , Telangana, Warangal , India. [Ti] Título: In vitro and in vivo effects of morin on the intestinal absorption and pharmacokinetics of olmesartan medoxomil solid dispersions. [So] Source: Drug Dev Ind Pharm;43(5):812-829, 2017 May. [Is] ISSN: 1520-5762 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: PURPOSE: In-situ evaluation to corroborate morin effects on the intestinal absorption and pharmacokinetic behavior of freeze-dried OLM-loaded solid dispersions with Caco-2 and in-vivo studies Methods: Intestinal transport and absorption studies were examined by Caco-2 permeability, in-situ single pass perfusion and closed-loop models along with in-vivo pharmacokinetic studies to evaluate and confirm the effect of P-gp-mediated activity of morin. We evaluated the intestinal membrane damage in the presence of morin by measuring the release of protein and lactate dehydrogenase (LDH) followed by using qualitative and quantitative morphometric analysis to describe the surface characteristics of intestinal epithelium. RESULTS: Morin showed the highest P value 13.8 ± 0.34 × 10 cm/s in jejunum than ileum (p < .01) at 100 µM with absorption enhancement of 1.31-fold together with enhanced (p < .01) secretory transport of 6.27 ± 0.27 × 10 cm/s in Caco-2 monolayer cells. Our findings noticed 2.37 (in-situ); 2.39 (in-vivo) and 1.43 (in-situ); 1.36 (in-vivo) fold increase in AUC with elevated C and shortened T for freeze-dried solid dispersion in the presence of morin as compared to pure OLM and freeze-dried solid dispersions without morin, respectively. CONCLUSIONS: 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. [Mh] Termos MeSH primário: Flavonoides/farmacologia Íleo/metabolismo Absorção Intestinal/efeitos dos fármacos Jejuno/metabolismo Olmesartana Medoxomila/farmacologia Olmesartana Medoxomila/farmacocinética [Mh] Termos MeSH secundário: Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo Disponibilidade Biológica Células CACO-2 Linhagem Celular Tumoral Liofilização/métodos Seres Humanos Mucosa Intestinal/metabolismo Permeabilidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Flavonoids); 6M97XTV3HD (Olmesartan Medoxomil); 8NFQ3F76WR (morin) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160804 [St] Status: MEDLINE [do] DOI: 10.1080/03639045.2016.1220569

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[PMID]: 27421242 [Au] Autor: Perez A; Cao C [Ad] Endereço: Takeda Development Center Americas, Inc., Deerfield, IL. [Ti] Título: Azilsartan in Patients With Mild to Moderate Hypertension Using Clinic and Ambulatory Blood Pressure Measurements. [So] Source: J Clin Hypertens (Greenwich);19(1):82-89, 2017 Jan. [Is] ISSN: 1751-7176 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: 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 OLM. Clinic BP was associated with a pronounced placebo effect (-6 mm Hg), whereas this was negligible with ABPM (±0.5 mm Hg). Adverse event frequency was similar in the AZL and placebo groups. Based on these and other findings, subsequent trials investigated the commercial AZL medoxomil tablet at doses 20 to 80 mg/d using 24-hour ABPM. [Mh] Termos MeSH primário: Anti-Hipertensivos/administração & dosagem Benzimidazóis/administração & dosagem Hipertensão/tratamento farmacológico Olmesartana Medoxomila/administração & dosagem Oxidiazóis/administração & dosagem [Mh] Termos MeSH secundário: Adulto Idoso Anti-Hipertensivos/uso terapêutico Benzimidazóis/uso terapêutico Determinação da Pressão Arterial Monitorização Ambulatorial da Pressão Arterial Interação do Duplo Vínculo Método Duplo-Cego Feminino Seres Humanos Masculino Meia-Idade Olmesartana Medoxomila/uso terapêutico Oxidiazóis/uso terapêutico Resultado do Tratamento [Pt] Tipo de publicação: CLINICAL TRIAL, PHASE II; COMPARATIVE STUDY; JOURNAL ARTICLE; MULTICENTER STUDY [Nm] Nome de substância: 0 (Antihypertensive Agents); 0 (Benzimidazoles); 0 (Oxadiazoles); 6M97XTV3HD (Olmesartan Medoxomil); F9NUX55P23 (azilsartan) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170922 [Lr] Data última revisão: 170922 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160717 [St] Status: MEDLINE [do] DOI: 10.1111/jch.12873

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[PMID]: 27815174 [Au] Autor: Gorain B; Choudhury H; Tekade RK; Karan S; Jaisankar P; Pal TK [Ad] Endereço: Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India; Faculty of Pharmacy, Lincoln University College, Kuala Lumpur, Malaysia. Electronic address: bapi@lincoln.edu.my. [Ti] Título: Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion. [So] Source: Regul Toxicol Pharmacol;82:20-31, 2016 Dec. [Is] ISSN: 1096-0295 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: 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 work, we herewith report the biodistribution behaviour and 28-day repeated dose sub-chronic toxicity of olmesartan medoxomil nanoemulsion in Wistar rats following oral administration. The levels of olmesartan in collected biological samples were estimated using our validated LC-MS/MS technique. Our biodistribution study showed significantly higher brain concentrations of olmesartan (0.290 ± 0.089 µg/mL, 0.333 ± 0.071 µg/mL and 0.217 ± 0.062 µg/mL at 0.5, 2.0 and 8.0 h post dosing, respectively) when administered orally as nanoemulsion formulation as compared to the aqueous suspension. In addition, the olmesartan nanoemulsion was found to be safe and non-toxic, as it neither produced any lethality nor remarkable haematological, biochemical and structural adverse effects as observed during the 28-days sub-chronic toxicity studies in experimental Wistar rats. It is herewith envisaged that the developed nanoemulsion formulation approach for the delivery of olmesartan medoxomil via oral route can further be explored in memory dysfunction and brain ischemia, for better brain penetration and improved clinical application in stroke patients. [Mh] Termos MeSH primário: Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacocinética Anti-Hipertensivos/farmacocinética Portadores de Fármacos Nanopartículas Óleos/química Olmesartana Medoxomila/farmacocinética Água/química [Mh] Termos MeSH secundário: Administração Oral Bloqueadores do Receptor Tipo 1 de Angiotensina II/administração & dosagem Bloqueadores do Receptor Tipo 1 de Angiotensina II/química Bloqueadores do Receptor Tipo 1 de Angiotensina II/toxicidade Animais Anti-Hipertensivos/administração & dosagem Anti-Hipertensivos/química Anti-Hipertensivos/toxicidade Biomarcadores/sangue Peso Corporal/efeitos dos fármacos Encéfalo/metabolismo Cromatografia Líquida Ingestão de Líquidos/efeitos dos fármacos Composição de Medicamentos Ingestão de Alimentos/efeitos dos fármacos Emulsões Masculino Nanomedicina/métodos Olmesartana Medoxomila/administração & dosagem Olmesartana Medoxomila/química Olmesartana Medoxomila/toxicidade Tamanho do Órgão/efeitos dos fármacos Permeabilidade Ratos Wistar Reprodutibilidade dos Testes Medição de Risco Espectrometria de Massas em Tandem Distribuição Tecidual Testes de Toxicidade Subcrônica [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE [Nm] Nome de substância: 0 (Angiotensin II Type 1 Receptor Blockers); 0 (Antihypertensive Agents); 0 (Biomarkers); 0 (Drug Carriers); 0 (Emulsions); 0 (Oils); 059QF0KO0R (Water); 6M97XTV3HD (Olmesartan Medoxomil) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170316 [Lr] Data última revisão: 170316 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161106 [St] Status: MEDLINE

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[PMID]: 27574399 [Au] Autor: Park JS; Shin JH; Hong TJ; Seo HS; Shim WJ; Baek SH; Jeong JO; Ahn Y; Kang WC; Kim YH; Kim SH; Hyon MS; Choi DH; Nam CW; Park TH; Lee SC; Kim HS [Ad] Endereço: Department of Cardiology, Ajou University School of Medicine, Suwon. [Ti] Título: Efficacy and safety of fixed-dose combination therapy with olmesartan medoxomil and rosuvastatin in Korean patients with mild to moderate hypertension and dyslipidemia: an 8-week, multicenter, randomized, double-blind, factorial-design study (OLSTA-D RCT: OLmesartan rosuvaSTAtin from Daewoong). [So] Source: Drug Des Devel Ther;10:2599-609, 2016. [Is] ISSN: 1177-8881 [Cp] País de publicação: New Zealand [La] Idioma: eng [Ab] Resumo: The pill burden of patients with hypertension and dyslipidemia can result in poor medication compliance. This study aimed to evaluate the efficacy and safety of fixed-dose combination (FDC) therapy with olmesartan medoxomil (40 mg) and rosuvastatin (20 mg) in Korean patients with mild to moderate hypertension and dyslipidemia. This multicenter, randomized, double-blind, factorial-design study included patients aged ≥20 years with mild to moderate essential hypertension and dyslipidemia. Patients were randomly assigned to receive FDC therapy (40 mg olmesartan medoxomil, 20 mg rosuvastatin), 40 mg olmesartan medoxomil, 20 mg rosuvastatin, or a placebo. The percentage change from baseline in low-density lipoprotein cholesterol levels was compared between FDC therapy and olmesartan medoxomil, and the change from baseline in diastolic blood pressure was compared between FDC therapy and rosuvastatin 8 weeks after treatment. A total of 162 patients were included. The least square mean percentage change (standard error) from baseline in low-density lipoprotein cholesterol levels 8 weeks after treatment was significantly greater in the FDC than in the olmesartan medoxomil group (-52.3% [2.8%] vs -0.6% [3.5%], P<0.0001), and the difference was -51.7% (4.1%) (95% confidence interval: -59.8% to -43.6%). The least square mean change (standard error) from baseline in diastolic blood pressure 8 weeks after treatment was significantly greater in the FDC group than in the rosuvastatin group (-10.4 [1.2] mmHg vs 0.1 [1.6] mmHg, P<0.0001), and the difference was -10.5 (1.8) mmHg (95% confidence interval: -14.1 to -6.9 mmHg). There were 50 adverse events in 41 patients (22.7%) and eight adverse drug reactions in five patients (2.8%). The study found that FDC therapy with olmesartan medoxomil and rosuvastatin is an effective, safe treatment for patients with hypertension and dyslipidemia. This combination may improve medication compliance in patients with a large pill burden. [Mh] Termos MeSH primário: Anti-Hipertensivos/uso terapêutico Dislipidemias/tratamento farmacológico Hipertensão/tratamento farmacológico Olmesartana Medoxomila/uso terapêutico Rosuvastatina Cálcica/uso terapêutico [Mh] Termos MeSH secundário: Anti-Hipertensivos/administração & dosagem Anti-Hipertensivos/efeitos adversos Método Duplo-Cego Combinação de Medicamentos Feminino Seres Humanos Masculino Meia-Idade Olmesartana Medoxomila/administração & dosagem Olmesartana Medoxomila/efeitos adversos República da Coreia Rosuvastatina Cálcica/administração & dosagem Rosuvastatina Cálcica/efeitos adversos [Pt] Tipo de publicação: JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL [Nm] Nome de substância: 0 (Antihypertensive Agents); 0 (Drug Combinations); 6M97XTV3HD (Olmesartan Medoxomil); 83MVU38M7Q (Rosuvastatin Calcium) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170403 [Lr] Data última revisão: 170403 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160831 [St] Status: MEDLINE [do] DOI: 10.2147/DDDT.S112873

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[PMID]: 27565974 [Au] Autor: Wang AC; Stellmacher U; Schumi J; Tu N; Reimitz PE [Ad] Endereço: Biostatistics, Daiichi Sankyo Pharma Development, 399 Thornall Street, Edison, NJ, 08837, USA. awang@dsi.com. [Ti] Título: Assessment of the Cardiovascular Risk of Olmesartan Medoxomil-Based Treatment: Meta-Analysis of Individual Patient Data. [So] Source: Am J Cardiovasc Drugs;16(6):427-437, 2016 Dec. [Is] ISSN: 1179-187X [Cp] País de publicação: New Zealand [La] Idioma: eng [Ab] Resumo: INTRODUCTION: Results from two long-term studies (ROADMAP and ORIENT) indicated a numerical imbalance in the number of cardiovascular deaths between the olmesartan medoxomil (OM) and placebo groups. OBJECTIVE: Our objective was to conduct an individual patient data meta-analysis to provide more complete information regarding OM-associated cardiovascular risks and/or benefits. METHODS: We created an integrated database based on 191 clinical trials from the OM development program. Events were identified and adjudicated by an independent, blinded clinical events committee. The incidence of major cardiovascular events and total mortality for OM versus placebo/active control were evaluated, and the effect of OM on cardiovascular mortality (main endpoint of interest) and morbidity was calculated using a two-stage approach (Tian method). RESULTS: A total of 46 studies (~27,000 patients) met the US FDA-specified inclusion criteria (phase II-IV randomized, double-blind, placebo- or active-controlled studies [OM-based monotherapy or combination, double-blind period ≥28 days] and adult patients). The incidence of known adjudicated endpoints in the analysis of all studies combined was low among OM (0.11-0.53 %) and placebo/active control (0.08-0.76 %) groups. For cardiovascular mortality, the estimated risk difference (OM vs. control) was 0.00070 (95 % confidence interval [CI] -0.0011 to 0.0024; p = 0.60); the risk difference for each endpoint was <1/1000, with no statistically significant difference between groups. Results were similar with and without ROADMAP and ORIENT. DISCUSSION: The 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. [Mh] Termos MeSH primário: Anti-Hipertensivos/efeitos adversos Anti-Hipertensivos/uso terapêutico Doenças Cardiovasculares/induzido quimicamente Sistema Cardiovascular/efeitos dos fármacos Olmesartana Medoxomila/efeitos adversos Olmesartana Medoxomila/uso terapêutico [Mh] Termos MeSH secundário: Ensaios Clínicos como Assunto Método Duplo-Cego Quimioterapia Combinada/efeitos adversos Quimioterapia Combinada/métodos Seres Humanos Ensaios Clínicos Controlados Aleatórios como Assunto Fatores de Risco [Pt] Tipo de publicação: JOURNAL ARTICLE; META-ANALYSIS [Nm] Nome de substância: 0 (Antihypertensive Agents); 6M97XTV3HD (Olmesartan Medoxomil) [Em] Mês de entrada: 1701 [Cu] Atualização por classe: 170117 [Lr] Data última revisão: 170117 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160828 [St] Status: MEDLINE

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[PMID]: 27562051 [Au] Autor: Li H; Shi LY; Chen L; Lu YZ; Yu B; Qi GX [Ad] Endereço: Department of Cardiology, the First Affiliated Hospital of China Medical University, Shenyang 110001, China. [Ti] Título: [Impact of olmesartan medoxomil on atherosclerosis lesions in apolipoprotein E knockout mice]. [So] Source: Zhonghua Yi Xue Za Zhi;96(31):2502-6, 2016 Aug 16. [Is] ISSN: 0376-2491 [Cp] País de publicação: China [La] Idioma: chi [Ab] Resumo: OBJECTIVE: To investigate the effect and possible mechanisms of olmesartan medoxomil on atherosclerosis of apolipoprotein E knockout (ApoE(-/-)) mice. METHODS: Sixteen 6-week-old male ApoE(-/-) mice were randomly divided into atherosclerosis model group fed with high fat diet, and olmesartan medoxomil intervention group fed with high fat diet and olmesartan medoxomil (10 mg·kg(-1)·day(-1,) per gavage). Eight C57BL/6 mice were fed with normal diet, and treated for 12 weeks.The blood pressure and the serum level of lipid were detected; the aorta were removed, oil red staining for plaque area, Hematoxylin and eosin (HE) staining for plaque morphology, Elastica van Gieson (EVG) staining for elastin, and picrosirius red (PSR) for collagen respectively; and the expression of cathepsin S (Cat S), smooth action protein (ASMA) and macrophage surface molecule-3 (Mac-3) were detected by immunohistochemisty analysis. RESULTS: Serum cholesterol and low density lipoprotein levels were significantly higher in atherosclerosis model group than in control group[(15.08±1.64) vs (2.06±0.15) mmol/L, (15.60±1.05) vs (0.00±0.00) mmol/L] (all P<0.01), while triglyceride level was similar between the two group.In contrast to model group, the mice in intervention group showed no statistical difference in blood pressure and plasma lipid levels, while the plaque areas in the aorta were significantly decreased (P<0.05) as well as the expression of Cat S and Mac-3[(2.4±1.2) vs (8.8±3.2)%, (2.2±1.2) vs (7.2±2.8)%] (all P<0.01). In addition, the elastin levels, collagen contents, and the expression of ASMA remained significantly higher compared with model group (P<0.05). CONCLUSION: Olmesartan medoxomil could slow down the atherosclerosis process, the possible mechanism was implicated with the suppression of Cat S and decreased inflammatory responses alongside the increased elastin and collagen contents. [Mh] Termos MeSH primário: Aterosclerose [Mh] Termos MeSH secundário: Animais Aorta Apolipoproteínas E Catepsinas Dieta Hiperlipídica Lipídeos Macrófagos Masculino Camundongos Camundongos Endogâmicos C57BL Camundongos Knockout Olmesartana Medoxomila Placa Aterosclerótica [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Apolipoproteins E); 0 (Lipids); 6M97XTV3HD (Olmesartan Medoxomil); EC 3.4.- (Cathepsins); EC 3.4.22.27 (cathepsin S) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170320 [Lr] Data última revisão: 170320 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160827 [St] Status: MEDLINE [do] DOI: 10.3760/cma.j.issn.0376-2491.2016.31.013

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[PMID]: 27180444 [Au] Autor: Zheng R; Hwang HM; Kim BH [Ti] Título: COMPARATIVE BIOAVAILABILITY OF A FIXED-DOSE COMBINATION TABLET OF OLMESARTAN MEDOXOMIL/HYDROCHLOROTHIAZIDE IN HEALTHY KOREAN VOLUNTEERS. [So] Source: Acta Pol Pharm;73(2):509-16, 2016 Mar-Apr. [Is] ISSN: 0001-6837 [Cp] País de publicação: Poland [La] Idioma: eng [Ab] Resumo: Combination therapy with diuretics and angiotensin II type 1 (AT1) receptor antagonist is frequently recommended for the control of blood pressure in hypertensive patients. This study was targeted to compare pharmacokinetic profiles of a new generic fixed-dose combination (FDC) tablet of olmesartan medoxomil/hydrochlorothiazide 20/12.5 mg and a reference formulation of Olmetec Plus 20/12.5 mg tablets in healthy volunteers. The study design was a randomized sequence and two-way crossover study in healthy subjects. They were to be randomly assigned to either one of the two sequence groups; each subject sequentially received a single oral dose of reference and test tablet with 7-day washout period. Blood sample was collected at pre-dose and at 0.33, 0.67, 1, 1.33, 1.67, 2, 2.5, 3, 4, 6, 8, 12, 24, 36 and 48 h post-dose. The blood concentrations were analyzed by LC-MS/MS. Both of the 90% CI for the treatment ratios (test/reference) of C(max) and AUC(last) were to be in the range of 0.800-1.250 with regards to olmesartan medoxomil and hydrochlorothiazide; the geometric mean ratios (test/reference) for olmesartan C(max) and AUC(last) were 0.979 (90% CI, 0.934-1.027) and 0.992 (0.946-1.041), respectively, and those for hydrochlorothiazide C(max) and AUC(last) were 0.966 (0.975-1.110) and 0.999 (0.963-1.038), respectively. No serious adverse events were reported during the study. The generic formulation of olmesartan medoxomil/hydrochlorothiazide 20/12.5 mg tablet was bioequivalent with the reference formulation of Olmetec Plus 20/12.5 mg tablet in regards to the pharmacokinetic parameters of olmesartan medoxomil and hydrochlorothiazide. Clinical Research Information Service (CRIS) Registration Number: KCT0001025. (https://cris.nih.go.kr/ Mar 18, 2014) [Mh] Termos MeSH primário: Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacocinética Anti-Hipertensivos/farmacocinética Grupo com Ancestrais do Continente Asiático Medicamentos Genéricos/farmacocinética Hidroclorotiazida/farmacocinética Olmesartana Medoxomila/farmacocinética Inibidores de Simportadores de Cloreto de Sódio/farmacocinética [Mh] Termos MeSH secundário: Administração Oral Adulto Bloqueadores do Receptor Tipo 1 de Angiotensina II/administração & dosagem Bloqueadores do Receptor Tipo 1 de Angiotensina II/sangue Anti-Hipertensivos/administração & dosagem Anti-Hipertensivos/sangue Disponibilidade Biológica Cromatografia Líquida Estudos Cross-Over Combinação de Medicamentos Medicamentos Genéricos/administração & dosagem Voluntários Saudáveis Seres Humanos Hidroclorotiazida/administração & dosagem Hidroclorotiazida/sangue Meia-Idade Olmesartana Medoxomila/administração & dosagem Olmesartana Medoxomila/sangue República da Coreia Inibidores de Simportadores de Cloreto de Sódio/administração & dosagem Inibidores de Simportadores de Cloreto de Sódio/sangue Comprimidos Espectrometria de Massas em Tandem Equivalência Terapêutica Adulto Jovem [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Angiotensin II Type 1 Receptor Blockers); 0 (Antihypertensive Agents); 0 (Drug Combinations); 0 (Drugs, Generic); 0 (Sodium Chloride Symporter Inhibitors); 0 (Tablets); 0J48LPH2TH (Hydrochlorothiazide); 6M97XTV3HD (Olmesartan Medoxomil) [Em] Mês de entrada: 1606 [Cu] Atualização por classe: 160516 [Lr] Data última revisão: 160516 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160517 [St] Status: MEDLINE

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