Tag: M.W=200-350

Bi, Ye published the artcileA liposomal formulation for improving solubility and oral bioavailability of nifedipine, COA of Formula: C17H18N2O6, the main research area is nifedipine liposome oral drug delivery formulation controlled release bioavailability; bioavailability; nifedipine; pharmacokinetics; proliposomes.

Proliposomes were used to improve the solubility and oral bioavailability of nifedipine. Nifedipine proliposomes were prepared by methanol injection-spray drying method. The response surface method was used to optimize formulation to enhance the encapsulation efficiency (EE%) of nifedipine. The particle size of nifedipine proliposomes after rehydration was 114 nm. Surface morphol. of nifedipine proliposomes was observed by a scanning electron microscope (SEM) and interaction of formulation ingredients was assessed by differential scanning calorimetry (DSC). The solubility of nifedipine is improved 24.8 times after forming proliposomes. In vitro release experiment, nifedipine proliposomes had a control release effect, especially in simulated gastric fluid. In vivo, nifedipine proliposomes significantly improved the bioavailability of nifedipine. The area under the concentration-time curve (AUC0-∞) of nifedipine proliposomes was about 10 times than nifedipine after oral administration. The elimination half-life (T1/2β) of nifedipine was increased from 1.6 h to 6.6 h. In conclusion, proliposomes was a promising system to deliver nifedipine through oral route and warranted further investigation.

Molecules published new progress about Absorption. 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, COA of Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Nakanishi, Atsushi published the artcileSpectral imaging of pharmaceutical materials with a compact terahertz difference-frequency generation semiconductor source, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is pharmaceutical material spectral imaging terahertz frequency generation semiconductor.

Spectral imaging of pharmaceutical material using a compact ultra-broadband (1-4 THz) terahertz semiconductor source was demonstrated. False-color RGB images could be obtained using a simple procedure (calibration free). The ability to distinguish the polymorphism of carbamazepine (CBZ), the hydrate forms of D-(+)-glucose and caffeine, and the crystallinity of nifedipine was demonstrated using the THz DFG source. Crystal forms of pharmaceutical materials can be distinguished using this method.

Analytical Methods published new progress about Absorption. 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

Tubtimsri, Sukannika published the artcileImprovement in Solubility and Absorption of Nifedipine Using Solid Solution: Correlations between Surface Free Energy and Drug Dissolution, COA of Formula: C17H18N2O6, the main research area is nifedipine absorption solubility surface free energy drug dissolution correlation; nifedipine; polysorbate; poorly water-soluble drug; solid solution; third generation solid dispersion.

Ternary solid solutions composed of nifedipine (NDP), amino methacrylate copolymer (AMCP), and polysorbate (PS) 20, 60, or 65 were prepared using a solvent evaporation method. The dissolution profiles of NDP were used to study the effect of the addition of polysorbate based on hydrophilic properties. A solid solution of NDP and AMCP was recently developed; however, the dissolution of NDP was <70%. In the present study, polysorbate was added to improve the dissolution of the drug by altering its hydrophilicity. The suitable formulation contained NDP and AMCP at a ratio of 1:4 and polysorbate at a concentration of 0.1%, 0.3%, or 0.6%. Differential scanning calorimetry and powder X-ray diffraction were used to examine the solid solutions No peak representing crystalline NDP was observed in any solid solution samples, suggesting that the drug was molecularly dispersed in AMCP. The NDP dissolution from NDP powder and solid solution without PS were 16.82% and 58.19%, resp. The highest dissolution of NDP of approx. 95.25% was noted at 120 min for the formulation containing 0.6% PS20. Linear correlations were observed between the surface free energy and percentages of dissolved NDP (R2 = 0.7115-0.9315). Cellular uptake across Caco-2 was selected to determine the drug permeability. The percentages of cellular uptake from the NDP powder, solid solution without and with PS20 were 0.25%, 3.60%, and 7.27%, resp. Polymers (Basel, Switzerland) published new progress about Absorption. 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, COA of Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ismail, Mai S. published the artcileDevelopment and assessment of oral nifedipine colloidal provesicles, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is review nifedipine colloidal provesicle assessment development.

Nifedipine(NIF), a well-known calcium channel blocker, is used in the management of hypertension especially if concomitant with kidney, heart or hormonal disorders in children. Colloidal vesicular systems were reported to improve oral absorption and bioavailability of hydrophobic drugs, so the current work embodies a new type of liquid oral colloidal provesicular nano-carrier of NIF. It was developed by simple slurry method. The optimum composition of appropriate lipid film, the effect of surfactant HLB values and cholesterol level on the entrapment efficiency of NIF within liberated vesicles were studied. Addnl., investigating the effect of both initial amount of NIF and the total lipid contents on NIF vesicular entrapment and drug loading were assessed. The morphol. and particle size of both provesicles and liberated nano-vesicles were estimated microscopically and by TEM. The study revealed that 300μmol total lipids of Span 20 /cholesterol at (9:1) molar ratio is an optimum lipid film for higher NIF encapsulation. The vesicular size attained was 209 nm and 79% EE. The in-vitro release study at pH 6.8 revealed an extended release pattern controlling both the release rate and extent. Furthermore, The DSC study showed The successful of intercalating NIF within the vesicle bilayer. This indicate the ability of these provesicles to load NIF successfully.

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

Abduljalil, Khaled published the artcilePrediction of maternal pharmacokinetics using physiologically based pharmacokinetic models: assessing the impact of the longitudinal changes in the activity of CYP1A2, CYP2D6 and CYP3A4 enzymes during pregnancy, Application In Synthesis of 21829-25-4, the main research area is metabolizing CYP1A2 CYP2D6 CYP3A4 impact pregnancy; CYP1A2; CYP2D6; CYP3A4; Inter-individual variability; PBPK; Pharmacokinetics; Pregnancy.

Concerns over gestational effects on the disposition of drugs has highlighted the need for a better understanding of drug distribution and elimination during pregnancy. This study aimed at predicting maternal drug kinetics using a physiol. based pharmacokinetic (PBPK) modeling approach focusing on the observed gestational changes in three important Cytochrome P 450 metabolizing enzymes, namely, CYP1A2, CYP2D6 and CYP3A4 at different gestational weeks (GWs). The Pregnancy PBPK model within the Simcyp Simulator V19 was used to predict the pharmacokinetics of sensitive probes to these enzymes; namely caffeine, theophylline, metoprolol, propranolol, paroxetine, midazolam, nifedipine and rilpivirine. PBPK model predictions were compared against clin. data collated from multiple studies for each compound to cover a wide spectrum of gestational ages. Pregnancy PBPK model predictions were within 2-fold error and indicated that CYP1A2 activity is approx. 0.70, 0.44 and 0.30 fold of the non-pregnant level at the end of the first, second and third trimesters, resp. On the other hand, CYP2D6 activity increases by 1.36, 2.16 and 3.10 fold of the non-pregnant level at the end of the first, second and third trimesters, resp. Likewise, CYP3A4 activity increases by 1.25, 1.75 and 2.32 fold of the non-pregnant level at the end of the first, second and third trimesters, resp. The enzymes activity have been qualified throughout pregnancy. Quantified changes in drug dosing are most relevant during the third trimester, especially for drugs that are mainly eliminated by CYP1A2, CYP2D6 and CYP3A4 enzymes. The provided functions describing the continuous changes to the activity of these enzymes during pregnancy are important when modeling long term pharmacokinetic studies where longitudinal modeling or time-varying covariates are used.

Journal of Pharmacokinetics and Pharmacodynamics published new progress about Homo sapiens. 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

Ngadjui, Esther published the artcileUterotonic Effects of Aqueous and Methanolic Extracts of Lannea acida in Wistar Rats: An In Vitro Study, Product Details of C17H18N2O6, the main research area is Lannea atosiban atropine nifedipine uterine contraction uterotonic; Calcium; In vitro; Lannea acida; Rats; Uterine contraction.

Lannea acida (Anacardiaceae), commonly called Kikie in the Noun division (West-Cameroon), is a tree whose bark is used locally to facilitate delivery. This study was aimed at evaluating the in vitro uterotonic effects of aqueous and methanol extracts of L. acida in Wistar rats. Uterine strips isolated from rats pretreated with 5μg estradiol (48 h) were mounted in a single-organ bath containing aerated and thermostated De Jalon solution (37°C). After equilibration, non-cumulative effects of L. acida extracts were recorded after application. The effect of the methanol extract (the most active extract) was monitored in the presence of atosiban (a competitive antagonist of oxytocin receptors), atropine (a specific type 3 muscarinic receptor antagonist), nifedipine (an L-type calcium channel antagonist), and 2-Aminoethoxydiphenyl borate (2-ADB, a specific antagonist of inositol 1,4,5-triphosphate receptors type 1), and in calcium-free medium containing EGTA to elucidate its mechanism of action. L. acida induced uterine contraction in a concentration-dependent manner with the methanol extract (1.506 ± 0.032 gf) being the most effective. Administration of atosiban (2μmol/L) and atropine (1μmol/L) reduced the contractile effect of L. acida. Complete inhibition was observed with nifedipine, 2-APB, and calcium-free medium containing EGTA. These results suggest that L. acida possesses uterotonic effects mediated through oxytocin receptors with mobilization of extracellular calcium.

Reproductive Sciences published new progress about Lannea acida. 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

Zhang, Shuo published the artcileCalcium plays a double-edged role in modulating cadmium uptake and translocation in rice, Application In Synthesis of 21829-25-4, the main research area is Oryza grain nifedipine calcium cadmium NRAMP1 translocation seedling; cadmium; calcium; crop safety; membrane transport; net Cd2+ influx; root-to-shoot translocation.

Cadmium (Cd) contamination in soils poses great risks to both agricultural production and human health. Calcium (Ca) is an essential element playing a significant role in protecting plants against Cd toxicity. However, how Ca affects Cd uptake and translocation in rice is still not fully elucidated. In this study, the regulatory role of Ca in Cd uptake and upward translocation was investigated in rice at different growth stages. Our results showed that the supplement of 5 mM Ca significantly reduced Cd uptake by rice roots, because of their competition for Ca-permeable channels as an absorption site and Ca-induced downregulation of OsNRAMP1 and OsNRAMP5. However, Ca application facilitated the upward translocation of Cd by both upregulating OsHMA2 to induce xylem loading of Cd and downregulating OsHMA3 to reduce vacuolar sequestration of Cd. Such contrary results suggested a double-edged role of Ca in regulating root Cd uptake and root-to-shoot Cd translocation in rice. Although it increased Cd content in the aboveground vegetative tissues during the whole growth period, the addition of 5 mM Ca eventually decreased Cd content in rice grains at the ripening stage. All these results suggest that Ca-based amendments possess great potential for the production of low-Cd rice grains.

International Journal of Molecular Sciences published new progress about Oryza sativa. 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

Sardesai, Mrunmayi published the artcileEngineering of Nanospheres Dispersed Microneedle System for Antihypertensive Action, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is engineering nanosphere microneedle system antihypertension; Hypertension; diltiazem; microneedles; nanospheres; nifedipine; vasodilator.

Background: A combinational therapy is mostly preferred in hypertension treatment because of low-dose and less side effects like pretibial edema, and gastrointestinal bleeding. Objective: So the objective of the present work was to formulate an advanced drug delivery system in the form of bio-responsive microneedles by incorporating nifedipine, a cardiodepressant and diltiazem, a vasodilator for effective synergism in the treatment of hypertension. Methods: The pH-responsive PLGA nanospheres of diltiazem were formulated using Water-in-Oil-in- Water (W/O/W) double emulsion and solvent-diffusion-evaporation technique. These nanospheres were added to nifedipine-PVP mixture and then incorporated into mold to develop microneedles. Results: The microneedles showed the release of nifedipine almost 96.93± 2.31% for 24 h due to high PVP solubilization. The nanospheres of diltiazem on contact with acidic pH of skin managed to form of CO2 bubbles and increase the internal pressure to burst PLGA shell due to pore formation. The mean blood pressure observed for the normal group was 89.58 ± 3.603 mmHg, whereas the treatment with the new formulation significantly reduced the mean blood pressure up to 84.11 ± 2.98 mmHg in comparison to the disease control group (109.9 ± 1.825 mm Hg). Conclusion: This system co-delivers the drugs nifedipine and diltiazem in hypertension and shows an advance alternative approach over conventional drug delivery system.

Current Drug Delivery published new progress about Aggregation. 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

Sehdev, Bhumika published the artcileEffect of calcium channel blockers on gingival tissues in hypertensive patients visiting Ayder Referral Hospital, Mekelle, Ethiopia, Category: pyridine-derivatives, the main research area is hypertensive patients gingival tissue calcium channel blocker.

Long term treatment of common chronic cardiac conditions such as hypertension with Calcium channel blockers (CCBs) has been associated with gingival hyperplasia. This oral side effect may affect esthetics and function, yet often overlooked and therefore underreported among hypertensive patients visiting in Ayder Comprehensive Specialized Hospital, Mekelle, Ethiopia. This study aims to determine the association of CCBs with gingival overgrowth in hypertensive patients. This is hospital based cross sectional study conducted among 50 hypertensive patients (25 CCBs and 25 non-CCBs age matched controls) attending the medical outpatient clinic of Ayder Comprehensive Specialized hospital. Data collection tools included interviewer administered questionnaires and periodontal examination Socio-demog. details, medical history and periodontal indexes (plaque index, papillary bleeding index, grade of GO according to DIGO clin. index) were recorded. The mean plaque index and mean papillary bleeding index for CCB users were 0.9±0.8 and 0.3±0.5 resp., while mean plaque index and mean papillary bleeding index for non-CCB users were 1.4±0.8 and 0.8±1.3 mm resp. Also, more females (44%) presented with DIGO compared to males (26%) in both the groups. Participants on CCBs had significantly increased probing depths than that of the non-CCB users (p = 0.001). The higher prevalence of DIGO among CCB users compared with non-CCB users has been reported. Furthermore, there was an increased risk of GO nearly 3 folds in CCB users compared with non-CCB users. The slightly higher finding of DIGO among Nifedipine users in the current study may be related to the fact that more patients were placed on Nifedipine. The significant association between increased probing depth and DIGO in our study was not unexpected owing to the formation of false pocketing in relation to GO. The study reveals that the risk of GO is nearly three times higher in CCB than non-CCB users and 2 folds in nifedipine than amlodipine users in Mekelle. Further studies intend to conduct multicenter studies with larger sample sizes to further elucidate the effect of the dose and duration of CCB on DIGO and also consider genetic studies for DIGO among Mekelle patients on CCB.

International Journal of Pharmaceutical, Chemical and Biological Sciences published new progress about Anesthetics. 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

Yu, Qiuli published the artcileEffects of drinking water fluorosis on L-type calcium channel of hippocampal neurons in mice, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is drinking water fluorosis calcium channel hippocampal neuron; Calcium imbalance; Fluorosis; Hippocampal CA1 region; LTCCs; Patch clamp.

The study aimed to investigate the effects of drinking water fluorosis on L-type calcium channels (LTCCs) in mouse hippocampal neurons. A total of 60 newly weaned ICR male mice were randomly divided into control, low fluoride and high fluoride groups. After 3 and 6 mo of exposure to fluoride, the patch clamp technique was used to detect the peak and relative values (I/Imax), steady-state activation curve ratio (G/Gmax), decay time constant, and tail current time constant of LTCCs currents in hippocampal CA1 region of mouse brain slices. Fluoride greatly reduced the serum and urinary calcium concentrations in mice, and the chronic fluorosis has a greater impact than subchronic fluorosis. The peak value of LTCCs current in pyramidal neurons of hippocampal CA1 area was significant and increased with the prolonged exposure time. The relative values of current and steady-state coefficients were changed greatly. The decay and tail current time increased significantly. High fluorine concentration indicates great peak value and open time of LTCCs opening. LTCCs are sensitive to fluoride exposure. The activation voltage of calcium channels induced by fluoride exposure is decreased, the opening time of calcium channels is prolonged, and the calcium influx per unit time increased, thereby overloading calcium concentration in neurons and this may be an explanation for intracellular calcium overload caused by fluoride. The imbalance of calcium metabolism caused by fluorosis may be a pathogenesis of brain injury induced by fluoride. Furthermore, the risk of brain damage from low-fluorine exposure cannot be ignored.

Chemosphere published new progress about Blood serum. 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