Category: pyridine-derivatives

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

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

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

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

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

Okuda, Shigenobu published the artcileThe constitution of matrine. XXVI. The constitution of dehydro-α-matrinidine, Safety of 4-Amino-2-picoline, the publication is Pharmaceutical Bulletin (1956), 257-61, database is CAplus.

cf. C.A. 49, 8316f. The decision between the 2 proposed structures of dehydro-α-matrinidine (I), upon which the structure of matrine depends, is based on spectrographic comparisons. Ultraviolet absorption maximum are recorded for: the degradation products of matrine, I, and the 2 bases C₁₂H₁₈N₂, m. 111° and 190°, resp.; the 4-aminopyridine group of 4-H₂N and 4-Et₂N derivatives of C₅H₅N, and 5,7-dimethyl-1,2,3,4-tetrahydro-1,6-naphthyridine (II); the 3-aminopyridine group of 3-H₂N (III) and 3-Me₂N (IV) derivatives of C₅H₅N, and 2,4-dimethyl-5,6,7,8-tetrahydro-1,5-naphthyridine (V); the 2-aminopyridine group of the 2-H₂N derivative of C₅H₅N, and 2,4-dimethyl-5,6,7,8-tetrahydro-1,8-naphthyridine. The solvents used were EtOH, 0.1N NaOH, 0.01N H₂SO₄, 50% H₂SO₄, and concentrated H₂SO₄. The spectra of 2,4-Me(H₂N) and 2,6,4-Me₂(H₂N) derivatives of C₅H₅N were determined in EtOH only. Only II and IV were previously unknown. The synthesis of II will be reported later. Methylation of III with H₂CO and HCO₂H gave IV, b₆ 95°; picrate, m. 179-81°. Study of the spectra led to the following generalizations: the 3-aminopyridine group form their di-salts even in 50% H₂SO₂, whereas the matrine products and the 4-aminopyridine group show the same absorption in 50% as in 0.01N H₃SO₃; I absorbs at much shorter wave lengths than III in EtOH, 0.1N NaOH, and 0.01N H₂SO₂; C₂H₂N₂ both have the same absorption in all solvents, very similar to that of II, and very different from that of V. It is concluded that all 3 matrine degradation compounds have the 4-aminopyridine skeleton, that I is 1-methyl-4,5,6,8,9,10-hexahydropyrido[3,4,5-ij]quinolizine, and that the C₁₂H₁₈N₂ are Me derivatives of 8-propyl-1,2,3,4-tetrahydro-1,6-naphthyridine.

Pharmaceutical Bulletin published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Safety of 4-Amino-2-picoline.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Profft, Elmar published the artcilePreparation and pharmacological properties of 1-(4-alkoxy-2-pyridyl)-2-ethylpiperidines, SDS of cas: 18437-58-6, the publication is Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft (1958), 429-36, database is CAplus.

The title compounds in which the alkoxy group was MeO, EtO, PrO, BuO, iso-BuO, AmO, iso-AmO, n-C₆H₁₃O, or n-C₇H₁₅O were prepared and tested for their activity as local anesthetics by surface application of a 1% solution of their HCl salts. The PrO compound was prepared by treating 24 g. 2,4-Me(PrO)C₅H₃N with 12 g. 40% HCHO and 3 drops of HOAc at 190° for 8 h. and working up with Et₂O to give 7 g. 2,4-HOCH₂CH₂(PrO)C₅H₃N (I), yellow oil, b₁₈ 182-6°. I (10 g.) kept with 2 g. KOH for 40 h., some hydroquinone added, and the product vacuum distilled gave 2,4-CH₂:CH(PrO)C₅H₃N (II), b₂₀ 125-7°. II (0.05 mol) heated with 0.033 mol piperidine and 0.0043 mol HOAc for 3 h. on a water bath at 95-110°, then vacuum distilled gave 1-(4-propoxy-2-pyridyl)-2-ethylpiperidine, a golden oil, b₁₆ 200.5°. The other members of the series were prepared in a similar manner. Only the n-C₆H₁₃O and n-C₇H₁₅O analogs showed any significant pharmacol. activity as local anesthetics. Quaternary iodides were also prepared from the 4-alkoxy-2-methylpyridines where the alkoxy group was MeO, EtO, PrO, BuO, or AmO by treatment of 0.02 mol of the picoline with 0.021 mol MeI in 3-5 mL. EtOH for 3 h.

Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, SDS of cas: 18437-58-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Saielli, Giacomo published the artcileOne-bond ¹J(¹⁵N-¹⁹F) spin-spin coupling constants of cationic fluorinating reagents: Insights from DFT calculations, Product Details of C6H5F4NO3S, the publication is Magnetic Resonance in Chemistry (2020), 58(6), 548-558, database is CAplus and MEDLINE.

We have investigated, by means of d. functional theory protocols, the one-bond ¹J(¹⁵N-¹⁹F) spin-spin coupling constants in a series of fluorinating reagents, containing the N-F bond, recently studied exptl. The results of the calculations show a very good linear relationship with the exptl. values, even though only the M06-2X(PCM)/pcJ-2//B3LYP/6-311G(d,p) level affords a very low mean absolute error. The calculations allow to analyze the various MOs contributions to the J coupling and to rationalize the observed pos. sign, corresponding to a neg. sign of the reduced spin-pin coupling constant K(N-F). Moreover, of the four Ramsey contributions, only the diamagnetic spin orbit is negligible, whereas the paramagnetic spin orbit and spin dipole terms decrease the magnitude of the Fermi contact (FC) term by an amount that goes from a min. of 35% up to more than 60% of the FC term itself. Several effects have been investigated, namely, the contribution of the long-range solvent reaction field, relativistic corrections, and conformational and vibrational effects.

Magnetic Resonance in Chemistry published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C6H5F4NO3S, Product Details of C6H5F4NO3S.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Shibata, Katsumi published the artcileNiacin activity of 3-cyanopyridine, pyridine 3-sulfonic acid, nicotinic acid N-oxide, and 6-hydroxynicotinic acid in rats, Application In Synthesis of 636-73-7, the publication is Bitamin (1995), 69(7), 357-64, database is CAplus.

Niacin activity of the niacin related compounds such as 3-cyanopyridine, pyridine 3-sulfonic acid, nicotinic acid N-oxide, and 6-hydroxynicotinic acid was investigated using rats. 3-Cyanopyridine, pyridine-3-sulfonic acid, and 6-hydroxynicotinic acid had not only niacin activity but also the antagonistic activity. Nicotinic acid N-oxide had niacin activity and the relative niacin activity to nicotinic acid was about 1/2 in molar ratio.

Bitamin published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C14H10O4S2, Application In Synthesis of 636-73-7.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Surov, O. V. published the artcileEnthalpies of Fusion, sublimation and vaporization of some hydrazones, Quality Control of 2215-33-0, the publication is Physical Chemistry: An Indian Journal (2017), 12(1), 1-15, database is CAplus.

Enthalpies of melting, sublimation and vaporization were determined for some hydrazones. The validity of thermogravimetric procedure for measuring enthalpy of vaporization of the compounds under investigation was demonstrated. Exploring packing modes and intermol. interactions in mol. crystals of the hydrazones using Hirshfeld surfaces was carried out.

Physical Chemistry: An Indian Journal published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C5H10Cl3O3P, Quality Control of 2215-33-0.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem