Day: December 21, 2022

Lu, Yang published the artcileEnhanced felodipine dissolution from high drug loading amorphous solid dispersions with PVP/VA and sodium dodecyl sulfate, Application In Synthesis of 72509-76-3, the main research area is felodipine dissolution amorphous solid dispersion sodium dodecyl sulfate PVP.

The objective of this study was to investigate the mechanisms of sodium dodecyl sulfate (SDS) and Copovidone (PVP/VA) enhancing the dissolution of high loaded felodipine (FLDP) amorphous extrudates. The rheol. results indicated that PVP/VA inhibited FLDP crystallization and the binary FLDP-PVP/VA (1:1 and 1:3) and ternary FLDP-PVP/VA-SDS (1:1:0.02-0.16 and 1:3:0.02-0.32) extrudates were amorphous solid dispersions (ASDs). Internal SDS (5%-20%) decreased glass transition temperature (Tgs) of FLDP-PVP/VA ternary ASDs. The enhanced dissolution rate of binary or ternary PVP/VA-rich ASDs in the non-sink condition of 0.05%SDS was achieved. SDS enhanced the dissolution of PVP/VA-rich ASDs via wettability and complexation with PVP/VA to accelerate the medium uptake and erosion kinetics of extrudates, but induced FLDP recrystallization and resulted in incomplete dissolution of FLDP-rich extrudates. Interestingly, when the ratio of FLDP-SDS was 1:0.08-0.12, the addition of SDS can significantly promote drug dissolution To confirm the in vitro relevance of these mol. interaction mechanisms, we prepared two tablet formulations which internal or external added SDS, resp., the ratio of FLDP-SDS was 1:0.1. The results show that SDS can promote the dissolution of FLDP when only SDS was internal added.

Journal of Drug Delivery Science and Technology published new progress about Absorption. 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

Seibertz, Fitzwilliam published the artcileSingle-cell optical action potential measurement in human induced pluripotent stem cell-derived cardiomyocytes, Related Products of pyridine-derivatives, the main research area is singlecell optical action potential human pluripotent stem cell cardiomyocyte.

Conventional intracellular microelectrode techniques to quantify cardiomyocyte electrophysiol. are extremely complex, labor intensive, and typically carried out in low throughput. Rapid and ongoing expansion of induced pluripotent stem cell (iPSC) technol. presents a new standard in cardiovascular research and alternate methods are now necessary to increase throughput of electrophysiol. data at a single cell level. VF2.1Cl is a recently derived voltage sensitive dye which provides a rapid single channel, high magnitude response to fluctuations in membrane potential. It possesses kinetics superior to those of other existing voltage indicators and makes available functional data equivalent to that of traditional microelectrode techniques. Here, we demonstrate simplified, non-invasive action potential characterization in externally paced human iPSC derived cardiomyocytes using a modular and highly affordable photometry system.

Journal of Visualized Experiments 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Maafi, Mounir published the artcilePhotokinetics of Dacarbazine and Nifedipine under polychromatic light irradiation and their application as new reliable actinometers for the ultraviolet range, Application In Synthesis of 21829-25-4, the main research area is photokinetics dacarbazine nifedipine polychromatic light irradiation reliable actinometer UV.

The photokinetic behavior of drugs driven by polychromatic light is an area of pharmaceutics that has not received a lot of attention. Most often, such photokinetic data is treated by thermal kinetic models (i.e., the classical 0th-, 1st- or 2nd-order equations). Such models were not anal. derived from the rate-laws of the photodegradation reactions. Polychromatic light kinetic modeling is hence of importance, as a means to providing adequate toolkits and metrics. This paper aims at proposing two reliable drug-actinometers useful for polychromatic UVA range. The general actinometric methodol. offered here is also useful for any drugs/materials obeying a primary photoprocess where both reactant and photoproduct absorb the incident light, of the AB(1φ)εB≠0 type. The present method has been consolidated by the η-order kinetics. This framework further demonstrated the lamp-specificity of actinometers. Overall, Dacarbazine and Nifedipine photodegradations obeyed η-order kinetics, and stand as effective actinometers that can be recommended for the ICH Q1b photostability testing.

Scientific Reports 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 In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bochmann, Esther S. published the artcileMicro-scale solubility assessments and prediction models for active pharmaceutical ingredients in polymeric matrices, Quality Control of 72509-76-3, the main research area is polyvinylpyrrolidone polyvinyl acetate active pharmaceutical ingredient; Amorphous solid dispersion; Bisacodyl (PubChem CID: 2391); Carbamazepine (PubChem CID: 2554); Celecoxib (PubChem CID: 2662); Cilostazol (PubChem CID: 2754); Clozapine (PubChem CID: 2818); Copovidone (PubChem CID: 25086-89-9); Data review; Dipyridamole (PubChem CID: 3108); Felodipine (PubChem CID: 3333); Gliclazide (PubChem CID: 3475); Griseofulvin (PubChem CID: 441140); Indomethacin (PubChem CID: 3715); Itraconazole (PubChem CID: 55283); Lamotrigine (PubChem CID: 3878); Loratadine (PubChem CID: 3957); Naproxen (PubChem CID: 156391); Nifedipine (PubChem CID: 4485); Posaconazole (PubChem CID: 468595); Praziquantel (PubChem CID: 4891); Prediction model; Probucol (PubChem CID: 4912); Ritonavir (PubChem CID: 392622); Solubility; Telmisartan (PubChem CID: 65999); Verapamil-HCl (PubChem CID: 62969).

The number of models for assessing the solubility of active pharmaceutical ingredients (APIs) in polymeric matrixes on the one hand and the extent of available associated data on the other hand has been rising steadily in the past few years. However, according to our knowledge an overview on the methods used for prediction and the resp. exptl. data is missing. Therefore, we compiled exptl. data, the techniques used for their determination and the models used for estimating the solubility Our focus was on polymers commonly used in spray drying and hot-melt extrusion to form amorphous solid dispersions (ASDs), namely polyvinylpyrrolidone grades (PVP), polyvinyl acetate (PVAc), vinylpyrrolidone-vinyl acetate copolymer (copovidone, COP), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft polymer (Soluplus, SOL), different types of methacrylate copolymers (PMMA), polyethylene glycol grades (PEG) and hydroxypropyl-methylcellulose grades (HPMC). The literature data were further supplemented by our own results. The final data set included 37 APIs and two sugar derivatives The majority of the prediction models was constituted by the m.p. depression method, dissolution endpoint measurements, indirect solubility determination by Tg and the use of low mol. weight analogs. We observed that the API solubility depended more on the working group which conducted the experiments than on the measuring technique used. Furthermore, this compilation should assist researchers in choosing a prediction method suited for their investigations. Furthermore, a statistical assessment using recursive feature elimination was performed to identify descriptors of mols., which are connected to the API solubility in polymeric matrixes. It is capable of predicting the criterium 20% API soluble at 100°C (Yes/No) for an unknown compound with a balanced accuracy of 71%. The identified 8 descriptors to be connected to API solubility in polymeric matrixes were the number of hydrogen bonding donors, three descriptors related to the hydrophobicity of the mol., glass transition temperature, fractional neg. polar van der Waals surface area, out-of-plane potential energy and the fraction of rotatable bonds. Finally, in addition to our own model, the data set should help researchers in training their own solubility prediction models.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Flexibility. 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, Quality Control of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xiong, Zhihui published the artcileFour kinds of tocolytic therapy for preterm delivery: Systematic review and network meta-analysis, Formula: C17H18N2O6, the main research area is meta analysis preterm delivery tocolytic therapy safety; Atosiban; Indomethacin; Nifedipine; Ritodrine; network meta-analysis; preterm delivery; tocolysis.

Meta-anal. of premature birth affects more than 15 million infants, as well as mothers and families around the world. With the relaxation of the two-child policy, the problem of premature birth has become relatively prominent in China. According to statistics, China had a birth population of 15.23 million in 2018, with a considerably large number of premature births. This study aims to evaluate the efficacy and safety of tocolysis in the treatment of preterm delivery, provide clin. evidence for medical staff and promote the self-management of patients with premature births. Four English databases (PubMed, Embase, Cochrane Library and Web of Science) were retrieved by computer, the retrieval time was from the establishment of each database to Nov. 2021, and the randomized controlled trials for the treatment of preterm delivery were screened according to the pre-set natriuretic exclusion criteria. After literature screening, data selection and risk of bias evaluation were independently conducted by two researchers. R 4.1.1 and Stata 17.0 software were used for statistical anal. A total of 44 RCTs were included, including 6939 patients. The results of network meta-anal. reveal that in terms of effectiveness, indomethacin was the most effective intervention measure, followed by nifedipine, and the difference was statistically significant; regarding safety, nifedipine was the safest intervention measure, followed by indomethacin, and the difference was statistically significant; and in respect of adverse reactions, ritodrine had the highest probability, and the difference was statistically significant. Nifedipine may be better for delayed delivery and less likely to produce adverse pregnancy outcomes, followed by indomethacin. Limited by the number and quality of recipient studies, the aforementioned conclusions need to be verified through more high-quality studies. At the same time, the focus should be on patients with twin pregnancy and patients with clin. manifestations of extreme preterm delivery.

Journal of Clinical Pharmacy and Therapeutics published new progress about Drug safety. 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, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Okada, Hitomi published the artcileCorrelation between drug dissolution and resistance to water-induced phase separation in solid dispersion formulations revealed by solid-state NMR spectroscopy, Synthetic Route of 21829-25-4, the main research area is pharmaceutical solid dispersion dissolution miscibility hypromellose methacrylic acid copolymer; Dissolution; Drug-polymer interaction; Miscibility; Phase separation; Solid dispersion.

We aimed to elucidate the dissolution mechanism of solid dispersions (SDs) according to the carrier polymers used. Nifedipine (NIF) and polymers dissolved simultaneously from NIF/Eudragit S (EUD-S), NIF/Eudragit L (EUD-L), and NIF/hypromellose (HPMC)/EUD-S spray-dried samples (SPDs). In contrast, NIF dissolved sep. from polymers from NIF/HPMC and NIF/HPMC/EUD-L SPDs due to the formation of an amorphous NIF-rich interface. Solid-state NMR spectroscopy indicated that NIF-EUD interactions were stronger than NIF-HPMC interactions. NIF/HPMC SPD exhibited weak interactions; thus, it failed to inhibit phase separation during the dissolution process and control NIF dissolution The hygroscopicity of SPDs was higher with HPMC mixing and increased substitution ratio of methacrylic acid in EUD. Moreover, solid-state NMR spectroscopy revealed that the NIF-EUD interactions were hindered to a large extent by the absorbed water. During the dissolution process of NIF/HPMC/EUD-L SPD, the introduction of water to the NIF-EUD-L interaction site could induce the phase separation and poor controllability of NIF dissolution Water-induced phase separation should be considered based on mol.-level characterization to obtain SDs with enhanced drug dissolution An investigation of the mol. state change caused by the absorbed water using solid-state NMR spectroscopy will be helpful in understanding the dissolution mechanism of SDs.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Dissolution. 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, Synthetic Route of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Alshahrani, Saad M. published the artcileEffect of lutrol F grades (poloxamer) on dissolution of hot-melt extruded Kollidon VA64-felodipine matrices, Application In Synthesis of 72509-76-3, the main research area is felodipine poloxamer lutrol F grade dissolution hot melt extrusion.

The objective of this study was to assess the potential of Lutrol F grades as polymeric surfactants for dissolution enhancement of Kollidon VA64-drug matrixes produced by hot-melt extrusion (HME). The poorly soluble model drug felodipine (FEL) with a medium m.p. was selected for this study. Two different grades of Lutrol F (also called Kolliphor P grades) were added into the HME systems to investigate their influence on the drug-incorporated matrixes. Two grades of Lutrols i.e., Lutrol F 68 (KolliphorP 188) and Lutrol F 127 (KolliphorP 407) were studied as polymeric solubilizers. FEL was mixed with KollidonVA64, with or without LutrolF (alone or in combination) at predetermined amounts which resulted in 8 different formulations. Each blend was melt-extruded at the same extrusion conditions. Differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) analyses were performed to evaluate their physicochem. properties. DSC and PXRD studies suggested the formation of amorphous solid dispersion for all extruded formulations. Dissolution studies revealed that the extrudates with Lutrol F grades exhibited faster and higher release compared to formulations without Lutrol F grades. Formulations with high drug loading, which did not include Lutrol F grades, demonstrated low drug release profiles when compared with the same formulations containing Lutrol F grades. Fourier transform IR (FTIR) studies suggested that a stronger hydrogen bond has occurred between the (-NH) of FEL and (C = O) of the pyrrolidone group in Kollidon VA 64. Overall, these studies suggested the potential of Lutrols in enhancing the dissolution rate of poorly soluble model drug FEL.

Acta Poloniae Pharmaceutica published new progress about Dissolution. 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

Lal, Chiman published the artcileFormulation and optimization by applying 32 full factorial design of mucoadhesive microspheres of nifedipine, Formula: C17H18N2O6, the main research area is nifedipine mucoadhesive microsphere drug delivery controlled release formulation.

Objective: The purpose of this research work is to formulate and optimize mucoadhesive microspheres of nifedipine using Carbopol 934P as mucoadhesive and Et cellulose as a carrier polymer for controlling the release of nifedipine. Methods: The emulsion solvent evaporation technique was used for the preparation of microspheres and the 32 full factorial designs were employed for optimization of microspheres. The developed microspheres were characterized for percent yield, entrapment efficiency, particle size, in vitro release study, percent mucoadhesion, surface morphol., and stability study. Results: Evaluating outcomes of preliminary batches indicated that 100 mL volume of processing medium, 5 h stirring time and 2% concentration of emulsifying agent were suitable for spherical, free-flowing microspheres and high percentage drug entrapment efficiency. The optimized batch exhibited 84.35% drug entrapment efficiency, 61.78% mucoadhesion and drug release were also sustained for more than 12 h. SEM study revealed that produced microspheres were spherical in shape. Conclusion: Exptl. responses of the optimized batch have close proximity with the predicted value and stability study of the optimized formulation proved the formulation is stable for a long period of time; hence, it is an excellent alternative over the conventional delivery system.

Asian Journal of Pharmaceutical and Clinical Research published new progress about Dissolution. 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, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ito, Daishi published the artcileIdentification of the hypertension drug niflumic acid as a glycine receptor inhibitor, Related Products of pyridine-derivatives, the main research area is hypertension niflumic acid glycine inhibitor.

Glycine is one of the major neurotransmitters in the brainstem and the spinal cord. Glycine binds to and activates glycine receptors (GlyRs), increasing Cl- conductance at postsynaptic sites. This glycinergic synaptic transmission contributes to the generation of respiratory rhythm and motor patterns. Strychnine inhibits GlyR by binding to glycine-binding site, while picrotoxin blocks GlyR by binding to the channel pore. We have previously reported that bath application of strychnine to zebrafish embryos causes bilateral muscle contractions in response to tactile stimulation. To explore the drug-mediated inhibition of GlyRs, we screened a chem. library of ∼1,000 approved drugs and pharmacol. active mols. by observing touch-evoked response of zebrafish embryos in the presence of drugs. We found that exposure of zebrafish embryos to nifedipine (an inhibitor of voltage-gated calcium channel) or niflumic acid (an inhibitor of cyclooxygenase 2) caused bilateral muscle contractions just like strychnine-treated embryos showed. We then assayed strychnine, picrotoxin, nifedipine, and niflumic acid for concentration-dependent inhibition of glycine-mediated currents of GlyRs in oocytes and calculated IC50s. The results indicate that all of them concentration-dependently inhibit GlyR in the order of strychnine > picrotoxin > nifedipine > niflumic acid.

Scientific Reports published new progress about Danio rerio. 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lavado, Giovanna J. published the artcileZebrafish AC50 modelling: (Q)SAR models to predict developmental toxicity in zebrafish embryo, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Danio developmental toxicity QSAR model; AC(50); Classification; Developmental toxicity; In silico aquatic toxicology; QSAR; Regression; Zebrafish embryo.

Developmental toxicity refers to the occurrence of adverse effects on a developing organism as a consequence of exposure to hazardous chems. The assessment of developmental toxicity has become relevant to the safety assessment process of chems. The zebrafish embryo developmental toxicol. assay is an emerging test used to screen the teratogenic potential of chems. and it is proposed as a promising test to replace teratogenic assays with animals. Supported by the increased availability of data from this test, the developmental toxicity assay with zebrafish has become an interesting endpoint for the in silico modeling. The purpose of this study was to build up quant. structure-activity relationship (QSAR) models. In this work, new in silico models for the evaluation of developmental toxicity were built using a well-defined set of data from the ToxCast Phase I chem. library on the zebrafish embryo. Categorical and continuous QSAR models were built by gradient boosting machine learning and the Monte Carlo technique resp., in accordance with Organization for Economic Co-operation and Development principles and their statistical quality was satisfactory. The classification model reached balanced accuracy 0.89 and Matthews correlation coefficient 0.77 on the test set. The regression model reached correlation coefficient R2 0.70 in external validation and leave-one-out cross-validated Q2 0.73 in internal validation.

Ecotoxicology and Environmental Safety published new progress about Danio rerio. 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