Month: November 2022

Hamada, Teruki published the artcileMicrominipig: A suitable animal model to estimate oral absorption of sustained-release formulation in humans, Computed Properties of 21829-25-4, the main research area is pharmaceutical oral sustained release formulation gastrointestinal absorption simulation microminipig; Deconvolution analysis; Gastrointestinal absorption; Microminipig; Non-compartmental analysis; Sustained-release formulation.

We investigated the gastrointestinal absorption characteristics of oral sustained-release formulations in microminipigs, dogs, and monkeys in order to clarify the similarities in absorption properties between these animals and humans. Time profiles of oral absorption of nifedipine and valproic acid were calculated from the plasma concentration-time profiles of the drugs by a deconvolution method. The curves for both drugs in microminipigs were close to or slightly higher than those in humans, whereas those in monkeys were lower. Furthermore, the plasma concentration-time profiles of the drugs were subjected to non-compartmental anal. The fractions of a dose absorbed into the portal vein (FaFg) in microminipigs ranged from 50 to 100% of the human values, whereas those in monkeys were less than half the human values. In addition, the other absorption-related parameters for the sustained-release formulation in microminipigs, as well as monkeys, were comparable to those in humans. In conclusion, the oral absorption properties of microminipigs and humans were similar regarding the sustained-release formulations. Therefore, microminipig is a suitable animal model to estimate the oral absorption of sustained-release formulations in humans.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Biological uptake. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Computed Properties of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Doris, Ursula published the artcileA sexy approach to pacemaking: differences in function and molecular make up of the sinoatrial node, Application In Synthesis of 21829-25-4, the main research area is pacemaking sinoatrial node human.

Functional properties of the sinoatrial node (SAN) are known to differ between sexes. Women have higher resting and intrinsic heart rates. Sex determines the risk of developing certain arrhythmias such as sick sinus syndrome, which occur more often in women. We believe that a major contributor to these differences is in gender specific ion channel expression. QPCR was used to compare ion channel gene expression in the SAN and right atrium (RA) between male and female rats. Histol., immunohistochem. and signal intensity anal. were used to locate the SAN and determine abundance of ion channels. The effect of nifedipine on extracellular potential recording was used to determine differences in beating rate between sexes. MRNAs for Cav1.3, Kir3.1, and Nkx2-5, as well as expression of the L-Type Ca2+ channel protein, were higher in the female SAN. Females had significantly higher intrinsic heart rates and the effect of nifedipine on isolated SAN preparations was significantly greater in male SAN. Computer modeling using a SAN cell model demonstrated a higher propensity of pacemaker-related arrhythmias in females. This study has identified key differences in the expression of Cav1.3, Kir3.1 and Nkx2-5 at mRNA and/or protein levels between male and female SAN. Cav1.3 plays an important role in the pacemaker function of the SAN, therefore the higher intrinsic heart rate of the female SAN could be caused by the higher expression of Cav1.3. The differences identified in this study advance our understanding of sex differences in cardiac electrophysiol. and arrhythmias.

Histology and Histopathology published new progress about Atrial arrhythmia. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Application In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pyka-Pajak, Alina published the artcileComparison of the utility of RP-TLC technique and different computational methods to assess the lipophilicity of selected antiparasitic, antihypertensive, and anti-inflammatory drugs, Computed Properties of 72509-76-3, the main research area is antiparasitic anti inflammatory drug lipophilicity RP TLC technique; Ościk’s equation; Soczewiński–Wachtmeister’s equation; anti-inflammatory drugs; antihypertensive drugs; antiparasitic drugs; lipophilicity.

The aim of this study was to assess the lipophilicity of selected antiparasitic, antihypertensive and non-steroidal anti-inflammatory drugs (NSAIDs) by means of reversed phase-thin layer chromatog. (RP-TLC) as well by using Soczewinski-Wachtmeister’s and J. Oscik’s equations. The lipophilicity parameters of all examined compounds obtained under various chromatog. systems (i.e., methanol-water and acetone-water, resp.) and those determined on the basis of Soczewinski-Wachtmeister’s and Oscik’s equations (i.e., RMWS and RMWO) were compared with the theor. ones (e.g., AlogPs, AClogP, milogP, AlogP, MlogP, XlogP2, XlogP3) and the exptl. value of the partition coefficient (logPexp). It was found that the RMWS parameter may be a good alternative tool in describing the lipophilic nature of biol. active compounds with a high and low lipophilicity (i.e., antihypertensive and antiparasitic drugs). Meanwhile, the RMWO was more suitable for compounds with a medium lipophilicity (i.e., non-steroidal anti-inflammatory drugs). The chromatog. parameter f0(a) can be helpful for the prediction of partition coefficients, i.e., AClogP, XlogP3, as well as logPexp of examined compounds

Molecules published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jhanwar, Anshul published the artcilePharmacoeconomic analysis of various brands of commonly prescribed oral antihypertensive medicines in Indian market, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is nifedipine antihypertensive agent pharmacoeconomic hypertension.

Objectives: The objective of the study was to analyze the percentage cost variations among various brands of the commonly prescribed antihypertensive medicines in India. Cost of a particular medicine (cost per 10 tablets) in the same strength and dosage forms being produced by various pharmaceutical companies was taken from Current Index of Medical specialties and Drug Today. Difference between the highest and lowest cost of the same drug manufactured by various pharmaceutical industries was obtained and percentage cost variation was calculated The percentage variation in the price was above 100% with almost all of the commonly prescribed antihypertensive medicines. The cost of a total of 23 drugs (14 single and nine combination preparations), available in forty nine different formulations were studied. Overall, Amlodipine (5 mg) shows highest price difference of 982.3%, while Nifedipine (5 mg) shows lowest price difference of 39%. Telmisartan + Hydrochlorthiazide (80 + 12.5 mg) combinations shows highest price variation of 318.9%, while Amlodipine + Losartan (5 + 50 mg) shows lowest price difference of 50%. Conclusion: The average percentage price difference of the same antihypertensive medicine manufactured by various pharmaceuticals company in India is very huge. Hence, Government, Pharmaceutical companies, prescribing health care workers should educate themselves about huge variation in price of brand drugs in comparison with their cheap generic counterpart to provide maximum benefits with min. financial burden to the patients receiving antihypertensive drugs.

Asian Journal of Pharmaceutical and Clinical Research published new progress about Antihypertensives. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

He, Yingmeng published the artcileEnhanced Oral Bioavailability of Felodipine from Solid Lipid Nanoparticles Prepared Through Effervescent Dispersion Technique, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is felodipine solid lipid nanoparticle delivery glyceryl behenate oral bioavailability; effervescent dispersion technique; felodipine; oral bioavailability; solid lipid nanoparticles.

Felodipine (FLD), a dihydropyridine calcium channel blocker with excellent antihypertensive effect, is poorly soluble and undergoes extensive hepatic metabolism, which lead to poor oral bioavailability (about 15%) and limit its clinic application. The goal of this study was to develop solid lipid nanoparticles (SLNs) loading FLD to improve the oral bioavailability. The FLD loaded solid lipid nanoparticles (FLD-SLNs) were prepared by the effervescent dispersion technique developed by our laboratory, which might have some advantages over traditional methods. The FLD-SLNs showed desired particle characteristics with particle size (198.15 ± 1.82 nm), poly dispersity index (0.26 ± 0.02), zeta-potential (- 25.53 ± 0.60 mV), entrapment efficiency (95.65 ± 0.70%), drug loading (2.33 ± 0.10%), and a spherical appearance. Pharmacokinetic results showed that the FLD-SLNs presented 3.17-fold increase in area under the curve (AUC(0-t)) compared with free FLD after oral administration in beagle dogs, which indicated that SLNs prepared using the effervescent dispersion technique can improve the bioavailability of lipophilic drugs like felodipine by enhancement of absorption and reduction first-pass metabolism

AAPS PharmSciTech published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Amssayef, Ayoub published the artcileAqueous extract of oakmoss produces antihypertensive activity in L-NAME-induced hypertensive rats through sGC-cGMP pathway, Product Details of C17H18N2O6, the main research area is norepinephrine oakmoss antihypertensive agent hypertension; Hypertension; lichens; oakmoss; pathways; vasorelaxant.

BackgroundLichens are a symbiotic association of a fungus with a green alga or cyanobacterium. They are widely used in traditional medicine as a treatment against skin disorders, diabetes and hypertension. The Aim of the StudyThe goal of this paper was to assess the possible antihypertensive and vasorelaxant capacity of the aqueous extract of a lichen species called Oakmoss or Evernia prunastri (L.). Material and MethodsIn the present study, the aqueous extract of Oakmoss was prepared, its antihypertensive activity was examined in N(ω)-nitro-L-arginine Me ester (L-NAME)-induced hypertensive rats, and its vasorelaxant ability was performed in rat isolated thoracic aorta. ResultsThe results proved that Oakmoss reduced the systolic, diastolic, mean arterial blood pressure, and heart rate in hypertensive rats but not in normotensive rats. Besides, the data showed that Oakmoss exerts its antihypertensive effect through vasorelaxant ability. ConclusionThe present study presents the favorable action of Oakmoss as an antihypertensive agent.

Clinical and Experimental Hypertension published new progress about Antihypertensives. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yin, Xuezhi published the artcileA Novel Micron-Size Particulate Formulation of Felodipine with Improved Release and Enhanced Oral Bioavailability Fabricated by Coaxial Electrospray, Formula: C18H19Cl2NO4, the main research area is felodipine coaxial electrospray povidone K30 HPMC; absorption; bioavailability; micron particles.

The antihypertensive drug felodipine (FD) is a typical biopharmaceutics classification system (BCS) II drug; thus, improving the dissolution rate of FD is very important to enhance its bioavailability. Besides, according to the in situ “”close loop”” perfusion assay, we found that the jejunum is the main absorptive site, then the duodenum and ileum. Consequently, a novel micron-size particulate of FD in a core-shell structure was fabricated by a coaxial electrospray technique; within the drug delivery system, Hypromellose K4M (HPMC K4M) was selected as a sheath material to prolong the retention time in the upper GI tract, while povidone K30 (PVP K30) was mixed with FD in the inner layer. The dissolution study in three different media (0.02% Tween-80 solution; phosphate buffer containing 0.02% Tween-80, pH 6.8; and HCl solution containing 0.02% Tween-80, pH 1.2) demonstrated that FD-loaded coaxial electrospray particles (F-COES) could greatly improve the dissolution of FD. Furthermore, in vivo pharmacokinetics revealed that F-COES emerged no changes in the half-life but significantly prolonged the tmax and increased the oral bioavailability. Collectively, this work supplies a promising drug release system that will improve the dissolution and enhance the bioavailability simultaneously for those poorly water-soluble drugs mainly absorbed in the upper GI tract.

AAPS PharmSciTech published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bezencon, Olivier published the artcileDesign and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors, Safety of 2-chloro-3-methylisonicotinaldehyde, the main research area is aryl substituted diazabicyclononenecarboxamide preparation selective renin inhibitor antihypertensive; potent nonpeptidic bioavailable diazabicyclononenecarboxamide renin inhibitor; structure aryl substituted diazabicyclononenecarboxamide inhibition renin; mol crystal structure renin bound nonracemic aryloxyethylphenyl diazabicyclononenecarboxamide.

Aryl-substituted diazabicyclononenecarboxamides such as I are prepared as selective human renin inhibitors for potential use as antihypertensive agents. Aryl substituents and the carboxamide moiety of the diazabicyclononenecarboxamides are essential for selective binding to renin; attachment of a substituent to the methyleneaminomethylene bridge of the diazabicyclononenecarboxamides does not modify the binding affinity but alters the pharmacokinetics of the product. I inhibits renin with an IC50 of 0.20 nM in buffer and 19 nM in plasma; a 10 mg/kg dose of I lowers the blood pressures of transgenic rats over a period of 36 h. The structures of both enantiomers of an aryloxyethylphenyl diazabicyclononenecarboxamide sep. bound to human renin are determined by X-ray crystallog.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 790696-96-7 belongs to class pyridine-derivatives, name is 2-chloro-3-methylisonicotinaldehyde, and the molecular formula is C7H6ClNO, Safety of 2-chloro-3-methylisonicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zadymova, Natalia M. published the artcileMicroemulsions and microheterogeneous microemulsion-based polymeric matrices for transdermal delivery of lipophilic drug (Felodipine), Application In Synthesis of 72509-76-3, the main research area is microemulsion polymeric matrix transdermal drug delivery felodipine.

Transdermal administration of drugs is more effective than traditional methods: metabolism of a drug in the gastrointestinal tract and liver is excluded, and its constant concentration in blood is provided. In most cases, the main part of the transdermal patch (TP) is a polymer film (matrix) with good adhesion to skin, which contains a skin permeability enhancer (SPE) and a drug. Types of TPs differ in a way of drug incorporating into the matrix. In this work, a new type of polymer matrixes for the delivery of lipophilic drugs based on microemulsions is developed. An optimized direct microemulsion (IV type according to Winsor) is obtained; practically, all its components are SPEs. Microemulsion (ME) type is confirmed by conductometry and dynamic light-scattering methods. Solubilization capacity of ME in relation to the antihypertensive drug felodipine (FEL) is studied. This drug is characterized by poor water solubility and, consequently, by low bioavailability at oral administration (âˆ?15%). FEL solubility in ME exceeds its solubility in water by 2.2 × 104 times. ME efficiency as a carrier of FEL is shown using Franz diffusion cell and UV spectroscopy. The FEL-loaded microemulsion was used as the dispersed phase of the emulsion, and the dispersion medium of the emulsion was a solution of polymer adhesive (a mixture of polyisobutylenes with different mol. weights and polybutene) in heptane with optimized rheol. properties. This emulsified ME (i.e., inverse emulsion) is served as a basis for the microheterogeneous polymer matrix, which provides FEL release at a constant target rate during the day.

Colloid and Polymer Science published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fathima, Nazish published the artcilePrescribing pattern of drugs in the treatment of hypertension in a tertiary care teaching hospital: a prospective observational study, COA of Formula: C18H19Cl2NO4, the main research area is hypertension antihypertension morbidity combination therapy.

Hypertension is a common chronic medical condition which is identified as the 3rd leading risk factor for global burden of diseases. According to Joint National Committee guidelines, hypertension is defined as elevated systolic blood pressure of =140mmHg or diastolic blood pressure of �90mmHg. The objective of this study is to analyze the prescribing pattern associated with antihypertensives. A Prospective Observational study was carried out for a period of 6 mo in an inpatient department in Shamanur Shivashankarappa Institute of Medical Science and Research Center, a tertiary care teaching hospital, Davangere. The data was collected from case sheets of all inpatients taking at least one antihypertensive. A total of 150 prescriptions were analyzed, out of which, 88(58.66%) were males and 62(41.33%) were females. The mean age group of study population was found to be 60-80 years (52%). The most commonly reported co- morbidity along with hypertension was Diabetes mellitus 80 (53.33%). Monotherapy was most preferred therapy which was given in almost 76 (50.66%) followed by combination therapy. In monotherapy Calcium channel blockers 35(46.04%) was most commonly prescribed. The present study confirms that the Prescribing patterns of antihypertensive drugs were in concordance with joint national committee 8 guidelines for patients with different compelling indications. The most frequently prescribed class of drug as monotherapy was Calcium Channel Blockers, followed by diuretics, which was also the most commonly used class of drugs in combination therapy.

World Journal of Pharmaceutical Research published new progress about Antihypertensives. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem