Day: November 30, 2022

Ou, Xiao published the artcileA general method for cultivating single crystals from melt microdroplets, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is pharmaceutical crystal microdroplet.

The cultivation of single crystals from solution is usually a time-consuming trial-and-error process. Here, we report a general strategy for rapidly cultivating single crystals from melt microdroplets within tens of minutes at the microgram scale. This strategy was successfully applied to the important polymorphic system griseofulvin to provide missing structural information of Form III, for which single crystals could not be cultivated from solution, as well as to twenty clin. drugs to verify its generality.

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal polymorphs. 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, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

R., Hema published the artcileRole of coformers in solubility enhancement of poorly soluble drugs through cocrystallization: an overview, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is review coformer solubility soluble drug cocrystn.

Improving the solubility of poorly soluble pharmaceuticals is a key problem in the pharmaceutical industry, and it can be solved using a range of methods, such as particle size reduction, surface modification, and other procedures. Cocrystn. is a new method for enhancing solubility in the pharmaceutical industry, which can be done with the help of cocrystal former (Coformer). These are watersol. stoichiometric cocrystals of the active pharmaceutical ingredient (API) with water-soluble small mol. coformers such as ascorbic acid, Nicotinamide, etc. Selection of coformer is a principal challenge in evolution of cocrystals, which can be done by various approaches such as trial and error, supra mol. synthon, virtual screening, etc. Hydrogen bonding, halogen bonding, and π -π interactions all play a part in the development of cocrystals. Moisture absorption, cocrystal reactant dissolution, cocrystal nucleation, and growth are all factors that impact crystal formation. Cocrystals can be prepared by various methods such as Solution evaporation method, Solution cooling crystallization, Solid state grinding, Liquid assisted grinding method, Hot melt extrusion, etc. This review complies the various research works on cocrystals.

International Journal of Pharmaceutical Sciences Review and Research published new progress about Chemical stability. 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, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Patel, Nehanshu published the artcileComparative evaluation of different marketed brands of itraconazole, Formula: C18H19Cl2NO4, the main research area is itraconazole dissolution economic pharmaceutical analysis.

Efficacy of pharmaceutical dosage form generally depends on their formulation and manufacturing methods, hence it is likely that the quality of dosage form may vary. The free azole nitrogen competes for oxygen at the catalytic heme of cytochrome P 450 enzyme. Inhibition of cytochrome P 450 enzyme prevents the synthesis of ergosterolin fungal cell membranes by limiting the C14 demethylation of lanosterol, which is criticalfor the synthesis of ergosterol. The study was exclusively exptl. that used IP and otherstandard books to check in vitro quality of Itraconazole tablet using different anal. techniques and procedure. Test for weight variation, hardness, friability, disintegration time and dissolution were conducted. The dissolution test was performed at pH 6.8 for both brandsof the tablet. Further all the tablet passed weight variation, hardness, and friability and disintegration test as per the pharmacopoeial standard Hence we can conclude that both the brands of tablets are equal quantity of active pharmaceutical ingredient (API). Both the brands having higher and lower costs exert similar action.

World Journal of Pharmacy and Pharmaceutical Sciences published new progress about Cardiac arrhythmia. 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

Sueda, Shozo published the artcileSpasm provocation tests under medication may help decide on medical or mechanical therapy in patients with aborted sudden cardiac death due to coronary spasm, Product Details of C17H18N2O6, the main research area is aborted sudden cardiac death coronary spasm; aborted sudden cardiac death; coronary artery spasm; implantable cardioverter-defibrillator; medications; ventricular fibrillation.

Objective The decision to perform medical or mech. therapy in patients with aborted sudden cardiac death (ASCD) due to coronary spasm is controversial. The Japanese Circulation Society guidelines for the diagnosis and treatment of patients with coronary spastic angina mentioned that implantable cardioverterdefibrillator (ICD) is one option in patients with ASCD due to coronary spasm. We investigated the usefulness of spasm provocation tests under medications in five patients with ASCD due to coronary spasm. Methods We performed the spasm provocation tests under medications in five ASCD patients due to coronary spasm. Pharmacol. spasm provocation tests, including five acetylcholine (ACh) tests, two ergonovine (ER) tests, and two ACh added after ER tests, were performed to estimate the effect of medications to suppressing the next fatal spasms. Results ACh tests under medications did not provoke spasm in one patient but did provoke in two patients. In the remaining two patients, neither the ACh test nor the ER test provoked spasm, but the ACh added after ER test induced a focal spasm in one coronary artery. We increased the medication dosage in four patients. An ICD was implanted in two patients, including one with refractory spasm and one with left main trunk spasm. One patient died due to pulseless elec. activity without ventricular fibrillation, while the remaining four patients survived. Conclusion Spasm provocation tests under medication in patients with ASCD due to coronary spasm may be an option when deciding on medical or mech. therapy.

Internal Medicine (Tokyo, Japan) published new progress about Bioelectric charge. 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

Eid, Rania K. published the artcileEssential oils in niosomes for enhanced transdermal delivery of felodipine, COA of Formula: C18H19Cl2NO4, the main research area is felodipine essential oil niosome transdermal delivery; Lipid vesicles; dermal; eucalyptol; limonene; thermal analysis.

The fluidity of vesicular membrane affects vesicular transdermal drug delivery. Essential oils can be located in vesicular membrane imparting flexibility and influencing transdermal delivery. Accordingly, the objective was to investigate the effect of incorporation of essential oils in niosomes on felodipine transdermal delivery. Rigid niosomes comprising Span 60 with cholesterol (2:1, weight/weight) were used with clove, eucalyptus or lemon oils being incorporated in the vesicles at increasing concentrations The vesicle size and shape was monitored using SEM. Thermal anal. was used to monitor the thermal behavior. Drug entrapment efficiency, release and skin permeation were monitored. Niosomes were spherical with size ranging from 279 to 345 nm. The drug entrapment ranged from 97.9 to 98.8%. Thermal anal. confirmed the existence of oils within vesicular membrane and highlighted the membrane fluidizing effect. Drug release depended on the oil with clove oil or eucalyptus oil showing a trend of increased drug release compared with plain niosomes. In contrast, lemon oil reduced drug release rate. Skin permeation study reflected the superiority of oil containing niosomes. The results correlated with the fluidizing and penetration enhancing effects of oils. The study introduced essential oils as potential niosomes fluidizing agents for enhanced transdermal drug delivery.

Pharmaceutical Development and Technology published new progress about Behavior (thermal). 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

Faconti, Luca published the artcileArterial stiffness can be modulated by pressure-independent mechanisms in hypertension, Category: pyridine-derivatives, the main research area is blood pressure hypertension pulse wave velocity stiffness; autonomic nervous system; high blood pressure; hypertension; pulse wave velocity; stiffness.

Effects of short-term interventions on large-artery stiffness assessed by pulse wave velocity (PWV) have mainly been explained by concomitant changes in blood pressure (BP). However, lower body neg. pressure, which increases sympathetic activity and has other hemodynamic effects, has a specific effect on PWV in healthy volunteers. We examined effects of lower-limb venous occlusion (LVO), a similar intervention to lower-body neg. pressure that reduces BP but increases sympathetic activity and device-guided breathing (DGB), which reduces both BP and sympathetic activity, on PWV in patients with essential hypertension (n = 70 after LVO, n = 45 after DGB and LVO in random order). The short-acting calcium channel antagonist nifedipine was used as a control for changes in BP. LVO produced a small but significant reduction in mean arterial pressure of 1.8 (95% CI 0.3-3.4) mm Hg. Despite this, aortic and carotid-femoral PWV increased during LVO by 0.8 (0.2-1.4) m/s and 0.7 (0.3-1.05) m/s, resp. DGB reduced PWV by 1.2 (0.9-1.4) m/s, to a greater extent than did nifedipine 10 mg (reduction of 0.7 [0.1-1.3] m/s, P<0.05 compared with reduction during DGB). This occurred despite a greater decrease in BP with nifedipine compared with DGB. Arterial stiffness can be modulated independently of BP over the short term. The mechanism could involve alterations in sympathetic activity or other as yet uncharacterized effects of LVO and DGB. Journal of the American Heart Association published new progress about Arterial stiffness. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mizoguchi, Ryo published the artcileApplication of Co-Amorphous Technology for Improving the Physicochemical Properties of Amorphous Formulations, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is amorphous solid dispersion coamorhpous stability screening mixing enthalpy hygroscopicity; co-amorphous; hydrogen bonds; hygroscopicity; lipophilicity; mixing enthalpy; physical stability; screening.

Co-amorphous technol. was recently introduced to stabilize drugs in the amorphous state for drug development. We examined the predictability of the formation of co-amorphous systems and identified two reliable indicators of successful formation: (1) a neg. ΔHmix value and (2) small Δlog P between components. Moreover, we found that the stability of co-amorphous systems was improved when (1) ΔHmix was neg. and (2) amorphous forms of the constituent compounds were stable. Furthermore, we concluded that co-amorphous systems with small (neg. large) ΔHmix values had lower hygroscopicity. Typically, amorphous solid dispersions exhibit hygroscopicity because polymers exhibit large hygroscopicity. We proved the superiority of co-amorphous technol. over amorphous solid dispersion in this respect. Our results provide methods for (1) establishing a screening method and (2) improving hygroscopicity, which may make co-amorphous technol. more useful than amorphous solid dispersion technol.

Molecular Pharmaceutics published new progress about Amorphization (co). 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, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Leal-Junior, Carlos C. published the artcileEffectiveness of an oral versus sublingual loading dose of nifedipine for tocolysis, HPLC of Formula: 21829-25-4, the main research area is nifedipine tocolytic oral sublingual drug delivery premature labor; Nifedipine; Oral administration; Pregnant; Premature; Premature labor; Sublingual administration; Tocolysis.

Objective : To determine the effectiveness of an oral vs. sublingual loading dose of nifedipine for tocolysis. Methods : An open, randomized clin. trial conducted between March 1, 2013, and Apr. 31, 2014. Participants were pregnant women with a diagnosis of premature labor, single live fetus, topical pregnancy, gestational age 24-36 wk, normal fetal vitality, cervical dilatation less than or equal to 4 cm, cervical effacement less than or equal to 80%, and intact amniotic membranes. They were randomized into two groups, oral and sublingual nifedipine, 20 mg loading dose, repeated every 30 min (maximum dose of 60 mg). The primary endpoint was the time until tocolysis and the secondary endpoints were the effectiveness of tocolysis within 90 min, 12 h, and 48 h; premature delivery within 48 h; and maternal hemodynamic parameters and side effects. Results : There were 80 patients randomized to oral (n=40) and sublingual (n=40) nifedipine. The time required for tocolysis was significantly less with sublingual nifedipine (160 min vs 340 min; P=0.0003). Sublingual nifedipine was also more successful than oral nifedipine at inhibiting premature labor within 90 min (n=8 [20.0%] vs n=1 [2.5%], P=0.014). There was no statistically significant difference between the groups for the other secondary endpoints. Conclusion : Compared with oral administration, a sublingual loading dose of nifedipine resulted in faster tocolysis in patients with premature labor. Brazilian Clin. Trials Registry (ReBEC): U1111-11566186.

International Journal of Gynecology & Obstetrics published new progress about Amnion, epithelium. 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, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Hao published the artcileMechanism of contractile dysfunction induced by serotonin in coronary artery in spontaneously hypertensive rats, HPLC of Formula: 21829-25-4, the main research area is rottlerin U73122 Y27632 cardioprotectant serotonin coronary artery vasoconstriction hypertension; 5-HT; Coronary artery; Hypertension; Spontaneously hypertensive rats; Vasoconstriction.

Abstract: Hypertension is one of the risk factors for coronary heart disease. The present study investigated the mechanism of contractile dysfunction induced by serotonin (5-HT) in coronary artery in spontaneously hypertensive rats (SHRs). Coronary arteries were isolated form SHRs and Wistar rats. Arterial ring contraction was measured using a multi myograph system. Intracellular calcium concentration was measured with a Ca2+ probe fluo-4/AM in vascular smooth muscle cells (VSMCs) isolated from coronary arteries. Signaling pathway-related proteins were assayed by western blotting. A 5-HT2A receptor blocker, sarpogrelate, completely eliminated coronary artery contraction induced by 5-HT. PLCβ inhibitor U73122 also significantly inhibited the response to 5-HT. Compared with the Wistar rats, serotonin (5-HT)- and CaCl2-induced coronary vasoconstriction in the SHRs was significantly reduced. Rho-associated protein kinase inhibitor Y27632, PKC inhibitor rottlerin, and L-type calcium channel blocker nifedipine inhibited the 5-HT-induced coronary artery contraction in a dose-dependent manner in SHRs and Wistar rats. However, the inhibitory effects were reduced in SHRs. In addition, store-operated Ca2+ (SOC) induced an obvious Ca2+ influx in coronary arterial smooth muscle cells, whereas SOC-mediated contraction was very slight in coronary arteries. At the same time, it was found that 5-HT2AR, IP3R, and Cav1.2 protein expression and PKCδ activity were decreased, and STIM1 and Orai1 were increased in VSMCs from coronary arteries of SHRs compared with Wistar rats. These results implicate calcium-handling dysfunction mediated by the 5-HT2A receptor and downstream signaling pathway might lead to a reduction in 5-HT-induced contraction in SHR coronary arteries.

Naunyn-Schmiedeberg’s Archives of Pharmacology published new progress about 5-HT2A antagonists. 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, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Inan, Cihan published the artcileComparison of the efficacy of the immediate-release and osmotic push-pull system formulations of nifedipine for tocolysis, HPLC of Formula: 21829-25-4, the main research area is hemorrhage respiratory distress syndrome enterocolitis; neonate; nifedipine; preterm labor; tocolysis; uterine contraction.

To compare the immediate-release (IR) and osmotic push-pull system formulations of nifedipine used for tocolysis in prolonging pregnancy, neonatal outcomes and maternal-fetal adverse effects. We evaluated 140 pregnant women who received the IR (n = 72) and osmotic push-pull system (n = 68) formulations of nifedipine for tocolysis due to threatened preterm labor between 240/7 and 336/7 wk of gestation. Groups were compared in terms of efficacy of tocolysis in prolonging pregnancy for more than 48 h, 7 days and up to 37 wk of gestation, total number of days gained for prolonging pregnancy, delivery weeks, maternal-fetal adverse effects and neonatal outcomes including ventilation support, need for intubation or surfactant, intraventricular hemorrhage, respiratory distress syndrome, necrotizing enterocolitis, admission to neonatal intensive care unit, neonatal death, Apgar scores at the 1st and 5th minutes. There was no significant difference between the two groups in prolonging pregnancy for more than 48 h or 7 days, total number of days gained after tocolysis initiation, delivery weeks, the number of births at 340/7-366/7 wk or after 37 wk of gestation (P > 0.05). Maternal-fetal adverse effects and neonatal outcomes were similar in both groups (P > 0.05). The efficacy of IR and osmotic push-pull system formulations of nifedipine have similar effects in terms of tocolysis and neonatal outcomes, adverse effects. Osmotic push-pull system formulation of nifedipine may be an alternative medication in tocolytic therapy due to its ease of use and the absence of loading dose necessity.

Journal of Obstetrics and Gynaecology Research published new progress about Cervical dilatation. 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, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem