Day: November 30, 2022

Choudhari, Alap A. published the artcileMicroencapsulation of solid dispersions of felodipine and characterization of release mechanism, HPLC of Formula: 72509-76-3, the main research area is felodipine microencapsulation sustained release solid dispersion.

The study was aimed at increase the solubility of poorly soluble drug Felodipine and formulating it in sustained release dosage form. Solid dispersion of drug was prepared using Poly vinyl pyrollidone (PVP) and hydroxyl Pr Me cellulose (HPMC) as inert hydrophilic carriers by kneading method. A 17-fold increase in dissolution rate of Felodipine was observed with solid dispersion prepared with HPMC. Optimized solid dispersion was further characterized by Powder X-ray diffraction (PXRD) which suggest transformation of crystalline Felodipine in amorphous form and Fourier transform IR spectroscopy (FTIR) suggesting no possible interaction. Sustained release microcapsules of Felodipine were formulated using Et cellulose (EC) and Eudragit RL 100 (EDRL) as coating material with solid dispersion of Felodipine as core by emulsion solvent evaporation method. Gelatin was used as microencapsulating agent employing coacervation-phase separation technique. Microcapsules from all the batches were found to discrete, spherical and free flowing and % entrapment efficiency was found to be in range of 88% to 96%. All the batches of microcapsules showed sustained release curve in pH 7.4 phosphate buffer up to eight hours with microcapsules prepared with gelatin giving Felodipine release up to 86% after 8 h. XRD pattern studies of the microcapsules made of gelatin showed drug still present in the amorphous form and thus maintaining its solubility in the microcapsule system.

International Journal of Drug Development & Research published new progress about Amorphous materials. 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, HPLC of Formula: 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

El Sayed, Mira published the artcileInsights into Dissolution and Solution Chemistry of Multidrug Formulations of Antihypertensive Drugs, COA of Formula: C18H19Cl2NO4, the main research area is antihypertensive dissolution solubility supersaturation formulation; amorphous; fixed dose combinations; multidrug formulations; solubility; supersaturation.

Using fixed dose combinations of drugs instead of administering drugs sep. can be beneficial for both patients and the health care system, but the current understanding of how multidrug formulations work at the mol. level is still in its infancy. Here, we explore dissolution, solubility, and supersaturation of various drug combinations in amorphous formulations. The effect of chem. structural similarity on combination behavior was investigated by using structurally related compounds of both drugs. The effect of polymer type on solution behavior was also evaluated using chem. diverse polymers. Indapamide (IPM) concentration decreased when combined with felodipine (FDN) or its analogs, which occurred even when the IPM solution was undersaturated The extent of solubility decrease of FDN was less than that of IPM from the dissolution of an equimolar formulation of the drugs. No significant solubility decrease was observed for FDN at low contents of IPM which was also observed for other dihydropyridines, whereas FDN decreases at high contents of IPM. This was explained by the complex nature of the colloidal precipitates of the combinations which impacts the chem. potential of the drugs in solution at different levels. The maximum achievable concentration of FDN and IPM during dissolution of the polyvinylpyrrolidone-based amorphous solid dispersion was higher than the value measured with the hydroxypropyl methylcellulose acetate succinate-based formulation. This emphasizes the significance of mol. properties and chem. diversity of drugs and polymers on solution chem. and solubility profiles. These findings may apply to drugs administered as a single dosage form or in sep. dosage forms and hence need to be well controlled to assure effective treatments and patient safety.

Molecular Pharmaceutics published new progress about Amorphous materials. 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

Morgan, John A. published the artcileChronic hypertension in pregnancy: are outcomes the same in patients on antihypertensives?*, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is antihypertensive chronic hypertension pregnancy maternal outcomes; Antihypertensives; chronic hypertension; maternal outcomes; neonatal outcomes; pregnancy.

To investigate differences in maternal and fetal outcomes among pregnant patients with chronic hypertension requiring antihypertensives for adequate control vs. those who do not require antihypertensives. Single-site retrospective cohort study including pregnant patients with chronic hypertension from 2015-2018. Two groups included those who required antihypertensives vs. those who did not. Primary outcome is composite morbidity: pregnancy loss after 20 wk, IUGR, maternal death, maternal stroke or TIA, pulmonary edema, renal failure, hypertensive emergency, HELLP syndrome, placental abruption or delivery before 34 wk. Secondary outcomes included development of severe features, indication for preterm labor less than 37 wk, incidence of severe range blood pressures, and neonatal outcomes. Student t, chi square, and Kruskal-Wallis tests where appropriate. Logistic regression used to account for potential confounders. Study cohort included 117 on antihypertensives and 114 not on antihypertensives. Use of antihypertensives was associated with the composite primary outcome (Odds ratio [OR], 3.88; 95% confidence interval [CI], 1.66-9.78). Use of antihypertensive medications was also associated with increased risk of prenatal diagnosis of IUGR, delivery prior to 34 wk, development of severe features, severe blood pressure during pregnancy, earlier mean gestational age at delivery, lower mean birth weight, and higher risk of NICU admission. Logistic regression anal. showed that the association between medication requirement and our composite primary outcome persisted even after adjustment for age, BMI, and presence of gestational diabetes. Our findings show an association between the requirement of antihypertensive medication use a significantly higher risk of composite primary outcome, prenatal diagnosis of IUGR, delivery prior to 34 wk, and the development of severe features.

Journal of Maternal-Fetal & Neonatal Medicine published new progress about Acute renal failure. 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Suzuki, Hiroyuki published the artcileAcute kidney injury successfully treated with autologous granulocyte colony-stimulating factor-mobilized peripheral blood CD34 -positive cell transplantation: A first-in-human report, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is autologous GCSF peripheral blood cell transplantation acute kidney injury; CD34+; clinical trials; granulocyte-colony stimulating factor (G-CSF); hematopoietic stem cells (HSCs); kidney; stem cell transplantation.

A 36-yr-old man with severe acute kidney injury (AKI) was admitted to Shonan Kamakura General Hospital in Japan. He was diagnosed with refractory hypertension based on a severely elevated blood pressure of 224/116 mmHg and retinal, cardiac, and brain damage revealed by ECG, fundoscopy, and magnetic resonance imaging, resp. Although hemodialysis was withdrawn following strict blood pressure control by an angiotensin receptor blocker, severe kidney insufficiency persisted. Therefore, we performed an autologous granulocyte colonystimulating factor-mobilized peripheral blood CD34-pos. cell transplantation. Collected CD34-pos. cells were directly infused to both renal arteries. The patient’s general condition was unremarkable after intervention, and the serum creatinine level gradually improved to 2.96 mg/dL 23 wk after cell therapy. Although transient fever and thrombocytosis were observed after intervention, no major adverse events were observed This patient is the first case in a phase I/II clin. trial of autologous granulocyte colony-stimulating factor-mobilized peripheral blood CD34-pos. cell transplantation for severe AKI with a CD34-pos. cell doseescalating protocol (trial number jRCTb030190231).

Stem Cells Translational Medicine published new progress about Acute kidney injury. 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

Lee, Chien-Chang published the artcileUse of calcium channel blockers and risk of active tuberculosis disease a population-based analysis, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is calcium channel blocker tuberculosis disease human; calcium channel blockers; heart failure; hypertension; pharmacoepidemiology; tuberculosis.

Calcium channel blockers (CCBs) are known to reduce the availability of iron-an important mineral for intracellular pathogens. Nonetheless, whether the use of CCBs modifies the risk of active tuberculosis in the clin. setting remains unclear. To determine whether CCBs may modify the risk of active tuberculosis disease, we conducted a nested case-control study using the National Health Insurance Research Database of Taiwan between Jan. 1999 and Dec. 2011. Conditional logistic regression and disease risk score adjustment were used to calculate the risk of active tuberculosis disease associated with CCB use. Subgroup anal. investigated the effect of different types of CCBs and potential effect modification in different subpopulations. A total of 8164 new active tuberculosis cases and 816 400 controls were examined Use of CCBs was associated with a 32% decrease in the risk of active tuberculosis (relative risk [RR], 0.68 [95% CI, 0.58-0.78]) after adjustment with disease risk score. Compared with nonuse of CCBs, the use of dihydropyridine CCBs was associated with a lower risk of tuberculosis (RR, 0.63 [95% CI, 0.53-0.79]) than nondihydropyridine CCBs (RR, 0.73 [95% CI, 0.57-0.94]). In contrast, use of β-blockers (RR, 0.99 [95% CI, 0.83-1.12]) or loop diuretics (RR, 0.88 [95% CI, 0.62-1.26]) was not associated with lower risk of tuberculosis. In subgroup anal., the risk of tuberculosis associated with the use of CCBs was similar among patients with heart failure or cerebrovascular diseases. Our study confirms that use of dihydropyridine CCBs decreases the risk of active tuberculosis.

Hypertension published new progress about Acute heart failure. 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rajendran, Venugopal published the artcileUltrasound assisted dichlorocarbene addition to 1,3-bis(allyloxy)-5-methylbenzene under biphasic condition: a kinetic study, HPLC of Formula: 36437-30-6, the main research area is bis allyloxy methylbenzene dichlorocarbene phase transfer catalyst cyclopropanation kinetics.

A new multi-site phase-transfer catalyst (MPTC), viz., N,N’-dioctyl-4,4′-bipyridium dibromide containing bi-site was prepared and proved by FT-IR, 1H NMR, 13C NMR, mass and elemental anal. The enhancement of C-N+ peak intensity at 1179 cm-1 noticed in FT-IR, the agreement of m/z values, viz., 542.43 bi-site resp. with their theor. values and the percentage of C, H, N elements noticed in elemental anal. has strongly supported the presence of tri-site MPTC catalysts. Further, the presence of number of active-sites in the catalyst was again confirmed by determining their pseudo-first order rate constant for dichlorocarbene addition to 1,3-bis(allyloxy)-5-methylbenzene in the presence of ultrasonic irradiation/mech. stirring. The comparative study reveals that the kapp determined with the combination of ultrasound and mech. stirring showed more activity than with their individual effect. Further, the detailed kinetic study performed with superior di-site MPTC reveals that the kapp are dependent with the stirring speed, [substrate], [catalyst], [NaOH] and temperature Based on the kinetic results, thermodn. parameters are evaluated.

Iranian Chemical Communication published new progress about Activation enthalpy. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, HPLC of Formula: 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Khattab, Sherine N. published the artcileSynthesis and aminolysis of 2,4-dinitrophenyl and 5-nitropyridine N-hydroxy oxime derivatives, Application In Synthesis of 26820-62-2, the main research area is aminolysis dinitrophenyl nitropyridine oxime morpholine nucleophilic aromatic substitution kinetics.

The 2,4-dinitrophenoxy derivatives 12-16 and the 5-nitro-2-pyridyloxy derivatives 18-22 were prepared The products were identified by elemental anal., IR, and NMR. The reaction of 12-16 and 18-22 with morpholine as nucleophile in CH3CN occurs through nucleophilic aromatic substitutions to give N-(2,4-dinitrophenyl)morpholine (23) and N-(5-nitro-2-pyridyl)morpholine (24) resp. Spectrophotometric measurements of the kinetics of these reactions in CH3CN at a range of temperatures indicated that they are not morpholine-catalyzed. The Bronsted-type plots for the reactions of 12-16 and 18-22 with morpholine are linear with slopes, β12-16 = -1.58 ± 0.1 and β18-22 = -1.15 ± 0.25 resp. The relative rate constants compared to the least reactive substrate, as well as the low neg. β values, supported that the decomposition of the zwitterionic intermediate is a slow process. The low activation parameters (ΔH# and ΔS#) are in accordance with the proposed transition state (T#). The expulsion of RO- anion in the rate-determining step is assisted by intramol. hydrogen-bonding with the ammonio-hydrogen present in the intermediate T#.

Bulletin of the Chemical Society of Japan published new progress about Activation enthalpy. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Application In Synthesis of 26820-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Khattab, Sherine N. published the artcileAminolysis of 1-(1-hydroxybenzotriazolyl)-2,4-dinitrobenzene and 2-(1-hydroxybenzotriazolyl)-5-nitropyridine, Application of 4-(5-Nitropyridin-2-yl)morpholine, the main research area is hydroxybenzotriazole aminolysis reaction mechanism kinetics solvent effect.

The reaction 1-(1-hydroxybenzotriazolyl)-2,4-dinitrobenzene and 2-(1-hydroxybenzotriazolyl)-5-nitropyridine with amines undergoes amination followed by elimination of the 1-hydroxyl benzotriazolyl anion. The kinetic data for the reaction of 1-(1-hydroxybenzotriazolyl)-2,4-dinitrobenzene and 2-(1-hydroxybenzotriazolyl)-5-nitropyridine with morpholine (Mo), cyclohexylamine (CHA) and aniline (An) in MeOH and acetonitrile (AN) proceeded by uncatalyzed mechanism in which the rate limiting step is the leaving group departure, whereas the reaction with Mo in toluene proceeded by uncatalyzed mechanism in which the formation of the zwitterionic intermediate is the rate determining step. While the reactions of 1-(1-hydroxybenzotriazolyl)-2,4-dinitrobenzene with CHA and An and the reaction of 2-(1-hydroxybenzotriazolyl)-5-nitropyridine with CHA in toluene proceeded by the specific base (SB) mechanism in which the rate determining step is the proton transfer process. The reactions of 1-(1-hydroxybenzotriazolyl)-2,4-dinitrobenzene and 2-(1-hydroxybenzotriazolyl)-5-nitropyridine with Mo in the three solvents and with CHA and An in MeOH and AN is greatly dependent on the stability of the zwitterionic intermediate. The effect of ring activation is due to the ground state stabilization and the more efficient delocalization of the neg. charge with a nitro group than with a ring-nitrogen in the transition state. The low activation enthalpies ΔH# and the highly neg. activation entropies ΔS# are due to the intramol. hydrogen bonding with the ammonio hydrogen present in the transition state.

Open Journal of Physical Chemistry published new progress about Activation enthalpy. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Application of 4-(5-Nitropyridin-2-yl)morpholine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Tsai, Yuan-Ming published the artcileVascular Kv7 channels control intracellular Ca2+ dynamics in smooth muscle, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is retigabine vasopressin calcium phospholipase smooth muscle; Calcium; Kv7; Phospholipase C; Retigabine; T-type Ca(2+)channels; Vascular smooth muscle cell; Vasopressin.

Voltage-gated Kv7 (or KCNQ) channels control activity of excitable cells, including vascular smooth muscle cells (VSMCs), by setting their resting membrane potential and controlling other excitability parameters. Excitation-contraction coupling in muscle cells is mediated by Ca2+ but until now, the exact role of Kv7 channels in cytosolic Ca2+ dynamics in VSMCs has not been fully elucidated. We utilized microfluorimetry to investigate the impact of Kv7 channel activity on intracellular Ca2+ levels and elec. activity of rat A7r5 VSMCs and primary human internal mammary artery (IMA) SMCs. Both, direct (XE991) and G protein coupled receptor mediated (vasopressin, AVP) Kv7 channel inhibition induced robust Ca2+ oscillations, which were significantly reduced in the presence of Kv7 channel activator, retigabine, L-type Ca2+ channel inhibitor, nifedipine, or T-type Ca2+ channel inhibitor, NNC 55-0396, in A7r5 cells. Membrane potential measured using FluoVolt exhibited a slow depolarisation followed by a burst of sharp spikes in response to XE991; spikes were temporally correlated with Ca2+ oscillations. Phospholipase C inhibitor (edelfosine) reduced AVP-induced, but not XE991-induced Ca2+ oscillations. AVP and XE991 induced a large increase of [Ca2+]i in human IMA, which was also attenuated with retigabine, nifedipine and NNC 55-0396. RT-PCR, immunohistochem. and electrophysiol. suggested that Kv7.5 was the predominant Kv7 subunit in both rat and human arterial SMCs; CACNA1C (Cav1.2; L-type) and CACNA1 G (Cav3.1; T-type) were the most abundant voltage-gated Ca2+ channel gene transcripts in both types of VSMCs. This study establishes Kv7 channels as key regulators of Ca2+ signalling in VSMCs with Kv7.5 playing a dominant role.

Cell Calcium published new progress about Immunohistochemistry. 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 of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Shujuan published the artcileBile acid transporter mediated STC/Soluplus self-assembled hybrid nanoparticles for enhancing the oral drug bioavailability, Synthetic Route of 72509-76-3, the main research area is sodium taurocholate Soluplus nanoparticle bioavailability bile acid transporter; ASBT; Felodipine; P4; Self-assembled hybrid nanoparticles; Sodium taurocholate; Soluplus.

The nano-particulate system for oral delivery faces a big challenge across the gastrointestinal bio-barriers. The aim was to explore the potential applications of bile acid transporter mediated the self-assembled hybrid nanoparticles (SHNPs) of sodium taurocholate (STC) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) for augmenting the oral delivery of poorly water-soluble drugs. Felodipine (FLDP) was chosen as a model drug. The self-assembly of STC with Soluplus to load FLDP and the microstructure of the SHNPs were confirmed using mol. simulation, STC determination by high performance liquid chromatog. (HPLC) and transmission electron microscope. Results showed that STC was integrated with Soluplus on the surface of nanoparticles by hydrophobic interactions. The permeability of FLDP loaded STC/Soluplus SHNPs was STC dependent in the ileum, which was inhibited by the higher concentrations of STC and the inhibitor of apical sodium-dependent bile acid transporter (ASBT). STC/Soluplus (1:9) SHNPs significantly improved the drug loading of FLDP, achieved the highest permeability of FLDP and realized 1.6-fold of the area under the curve (AUC) of Soluplus self-assembled nanoparticles (SNPs). A water-quenching fluorescent probe P4 was loaded into the STC/Soluplus SHNPs, which verified that the SHNPs were transferred intactly across the ileum. In conclusion, STC/Soluplus SHNPs via ASBT are a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Drug bioavailability. 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, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem