Tag: M.W=350-400

Guo, Changchuan published the artcileTargeted and nontargeted screening and identification of 50 antihypertensive adulterants in dietary supplements and herbal medicines using quadrupole-orbitrap high resolution mass spectrometry with compound database, Category: pyridine-derivatives, the main research area is antihypertensive dietary supplement adulterant screening spectrometry; adulteration; antihypertensives; identification; mass spectrometry; orbitrap; traditional Chinese medicine.

In the present work, a novel database of drug compounds and a rapid screening method based on ultra-high performance liquid chromatog. coupled to high resolution orbitrap mass spectrometry were developed and applied in the screening and identification of targeted and nontargeted antihypertensive adulterants in dietary supplements and herbal medicines. The established screening database includes retention time, exact mass, fragments, isotopic pattern, and MS2 spectra library of the target compounds and thus provides automated search and identification of the targets with a single injection. The nontargeted compounds in the samples are identified through the full MS scan and MS2 data by using the Chemspider database and the data anal. in XCalibur, MassFrontier and TraceFinder software. In addition, this method possesses excellent quant. capacity. The novel approach was applied to 65 batches of samples that are claimed as “”all-natural”” products having the antihypertensive function, among which nine batches were found to be pos. Multiple targeted and nontargeted antihypertensive adulterants were detected at levels ranging from 2.8 to 27.9 mg/g. The novel database and screening method demonstrated herein will be promising and powerful tools for rapid screening of antihypertensive adulterants in dietary supplements and herbal medicines.

Journal of Separation Science published new progress about Adulterants. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zadymova, N. M. published the artcileNanoemulsions Containing Incorporated Lipophilic Drug, Felodipine, and Microheterogeneous Adhesive Polymer Matrices Based on These Nanoemulsions, SDS of cas: 72509-76-3, the main research area is lipophilic felodipine microheterogeneous adhesive polymer matrix nanoemulsion.

Oil-in-water nanoemulsions (NEs) have been obtained with a simple composition, in which a lipophilic non-micelle-forming nonionic surfactant (Tween 85) serves as both a dispersed phase and a stabilizer. The NEs remain in a metastable state for a long time (several months) and have a highly developed sp. surface area (Ssp ≃ 63 m2/g) and a high solubilization capacity with respect to a lipophilic hypotensive drug, felodipine (FD). Nanosized droplets (dav ≃ 95 nm) of the NEs efficiently transport FD in an aqueous medium. The oil-in-water NEs of Tween 85 with incorporated FD and a solution of a polymer adhesive (a blend of polyisobutylenes having different mol. weights and polybutene) in heptane have been used to obtain oil1/water/oil2 double emulsions, which are used as premixes for polymer microheterogeneous matrixes. Obtained polymer films are characterized by a good adhesion to skin, the absence of FD crystallization, and a constant rate of its release for several hours.

Colloid Journal published new progress about Aggregation. 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, SDS of cas: 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Buchwald, Peter published the artcileSoft drugs: design principles, success stories, and future perspectives, Quality Control of 72509-76-3, the main research area is Soft drug design success story future perspective; Antedrug; drug metabolism; esterases; methylphenidate; prodrug; sofpironium; therapeutic index; toxic metabolite.

In the present study, the SD concept is part of the more general recognition that drug design needs to fully integrate metabolic con-siderations from the very beginning as metabolites contribute significantly to the overall activity and toxicity profile of the original drug and focus not on improving activity alone, but on improving the activity/toxicity ratio. This is usually characterized by the therapeutic index, typically defined as the ratio between the half-maximal toxic and effec-tive doses: TI = TD50/ED50. These ideas are the main underlying principles of retrometabolic drug design, which incorporates both SD and chem. delivery system (CDS) design. For most drugs, several metabolites are formed following administration, and they can contribute significantly not just to the overall activity, but also to toxicity and side effects. This can lead to complex time-profiles as illustrated in Figure 1(a), which shows the case of a hypothetical drug D that is present together with its active, toxic, and inactive metabolites. In light of these, the SD approach, which provides general drug design strategies, has particular potential. Because it often starts from a known active structure and focuses on designing safer drugs by decreasing side effects and toxicity, the likelihood of success is increased, especially considering the perspective highlighted by Sir James Black: the most fruitful basis for the discovery of a new drug is to start with an old drug.

Expert Opinion on Drug Metabolism & Toxicology published new progress about Anesthetics. 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

Dzodic, Predrag published the artcileA reliable chromatographic method for the simultaneous determination of ciprofloxacin and moxifloxacin in human serum, Synthetic Route of 72509-76-3, the main research area is serum ciprofloxacin moxifloxacin high performance liquid chromatog.

Purpose: To develop and validate a simple chromatog. method for the anal. of ciprofloxacin and moxifloxacin in human serum. Methods: After protein precipitation had been performed, high performance liquid chromatog. (HPLC) with UV detection was utilized for the anal. of ciprofloxacin and moxifloxacin in human serum. Anal. column Zorbax SB-C18 (150 mm x 4.6 mm i.d., particle size 3.5μm) was used as a stationary phase. Chromatog. separation was realized with the mobile phase 0.1% trifluoroacetic acid in water for chromatog. – methanol (66:34, volume/volume), at the flow rate of 1 mL/min, temperature of 35°C and detection at 280 nm. The method validation was performed according to the guidelines of the European Medicines Agency (EMA). Results: The chromatog. run time was about 12 min and no interference was observed For ciprofloxacin, the method was linear over a concentration range of 0.5-50μg/mL, with a correlation coefficient of 0.9874. For moxifloxacin, the method was linear over a concentration range of 0.5-50μg/mL, with a correlation coefficient of 0.9946. Since relative standard deviation (RSD) and relative recovery values were within acceptable limits according to EMA guidelines, good intra-day precision, inter-day precision, as well as the accuracy of the method, were observed Conclusion: A simple and reliable HPLC-UV method has been developed and validated for the simultaneous determination of ciprofloxacin and moxifloxacin in human serum. The method can be applied for therapeutic drug monitoring but also and pharmacokinetic studies of ciprofloxacin and moxifloxacin.

Tropical Journal of Pharmaceutical Research published new progress about Blood serum. 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

Wang, Dongdong published the artcileCyclosporin population pharmacokinetics in pediatric refractory nephrotic syndrome based on real-world studies: effects of body weight and spirolactone administration, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is refractory nephrotic syndrome cyclosporin spirolactone body weight pharmacokinetics pediatrics; cyclosporin; pediatric refractory nephrotic syndrome; population pharmacokinetics; real-world study; spirolactone; weight.

Different models of population pharmacokinetics (PPK) of cyclosporin have been established in various populations. However, the cyclosporin PPK model in patients with pediatric refractory nephrotic syndrome (PRNS) has yet to be constructed. The present study aimed to establish the cyclosporin PPK model in PRNS, and to identify factors that may account for any variability. Chinese patients with PRNS treated with cyclosporin between June 2014 and June 2018 at the Children’s Hospital of Fudan University (Shanghai, China) were retrospectively analyzed. The impact of demog. features, laboratory parameters and concomitant medications was evaluated. A total of 18 PRNS patients from real-world studies were analyzed by non-linear mixed-effects modeling. A one-compartment model with first-order absorption and elimination was selected as the appropriate model in PRNS. Body weight (WT) and spirolactone intake were included as significant covariates for the apparent oral clearance (CL/F), and the WT was revealed to significantly influence the apparent volume of distribution (V/F). The final covariate models were as follows: CL/F = 80.7 × (WT/70)0.75 × (1-0.265 × θspirolactone), and V/F = 2,030 × (WT/70), where θspirolactoneis the coefficient of spirolactone. The inter-individual variability in CL/F and V/F was 44.6 and 53.1%, resp. In conclusion, in the present study, a cyclosporin PPK model for patients with PRNS was successfully constructed, and the presence of a clin. significant interaction between spirolactone and cyclosporin in PRNS patients was determined based on real-world studies, indicating that concomitant medication with spirolactone was able to reduce cyclosporin clearance in the patients with PRNS.

Experimental and Therapeutic Medicine published new progress about Body weight. 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

Salunkhe, N. H. published the artcileValidated RP-HPLC method for quantification of felodipine in rabbit plasma: Application in a bioequivalence study, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is RP HPLC method felodipine rabbit plasma; Felodipine; La nimodipine; Nimodipine; Plasma de lapin; RP-HPLC; Rabbit plasma; Validation.

The aim of present study was to develop a simple, rapid, selective, sensitive and robust reverse phase high performance liquid chromatog. method for quantification of felodipine in rabbit plasma at the wavelength of 360 nm. Protein was precipitated from rabbit plasma sample by addition of acetonitrile as a vehicle. An isocratic elution of samples was performed on capcell pak C8 DD S5 column (4.6 mm × 250 mm particle size 5μm) column with mobile phase consisting 5 mM Phosphate Buffer (pH 4.8 adjusted with dilute ortho-phosphoric acid solution): acetonitrile (25:75:volume/volume) delivered at flow rate 1.0 mL min-1. A good linear response was achieved over the range of 0.25-20.00 g mL-1. LODs and LOQs for felodipine were found to be 0.055 and 0.201μg mL-1, resp. The method was quant. evaluated in terms of linearity, precision, accuracy (recovery), selectivity robustness and stability study as per standard guidelines. The validated RP-HPLC method was successfully applied for the bioavailability studies of felodipine. The pharmacokinetic parameters were calculated for all the investigated drugs in rabbit after single-dose administrations of pure drug and formulation of felodipine. Finally, the obtained results for the application of the proposed RP-HPLC method proved its efficiency to be applied to the therapeutic drug monitoring (TDM) and bioequivalence (BE) studies. Thus, developed method is simple, convenient and suitable for the anal. of felodipine in bulk and pharmaceutical formulations.

Annales Pharmaceutiques Francaises published new progress about Blood plasma. 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, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Iwasaki, Shinji published the artcileApplication of unbound liver-to-plasma concentration ratio to quantitative projection of cytochrome P450-mediated drug-drug interactions using physiologically based pharmacokinetic modelling approach, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is liver plasma cytochrome drug interaction PBPK modeling approach; Drug–drug interaction; K; human cryopreserved hepatocytes; physiologically based pharmacokinetic model.

1. This study evaluated the prediction accuracy of cytochrome P 450 (CYP)-mediated drug-drug interaction (DDI) using minimal physiol.-based pharmacokinetic (PBPK) modeling incorporating the hepatic accumulation factor of an inhibitor (i.e. unbound liver/unbound plasma concentration ratio [Kp,uu,liver]) based on 22 clin. DDI studies.2. Kp,uu,liver values were estimated using three methods: (1) ratio of cell-to-medium ratio in human cryopreserved hepatocytes (C/Mu) at 37°C to that on ice (Kp,uu,C/M), (2) multiplication of total liver/unbound plasma concentration ratio (Kp,u,liver) estimated from C/Mu at 37°C with unbound fraction in human liver homogenate (Kp,uu,cell) and (3) observed Kp,uu,liver in rats after i.v. infusion (Kp,uu,rat).3. PBPK model using each Kp,uu,liver projected the area under the curve (AUC) increase of substrates more accurately than the model assuming a Kp,uu,liver of 1 for the average fold error and root mean square error did. Particularly, the model with a Kp,uu,liver of 1 underestimated the AUC increase of triazolam following co-administration with CYP3A4 inhibitor itraconazole by five-fold, whereas the AUC increase projected using the model incorporating the Kp,uu,C/M, Kp,uu,cell, or Kp,uu,rat of itraconazole and hydroxyitraconazole was within approx. two-fold of the actual value.4.

Xenobiotica published new progress about Blood plasma. 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 of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Carling, Carl-Johan published the artcileMilling of poorly soluble crystalline drug compounds to generate appropriate particle sizes for inhaled sustained drug delivery, Quality Control of 72509-76-3, the main research area is lung inhaled sustained drug delivery; particle size AZD4854 milling dissolution; Dissolution; Inhaled sustained drug delivery; Milling; Nebulization; Suspension; Ultrasound.

One of the simplest design concepts of inhaled sustained drug delivery to the lung is to utilize the slow dissolution of drug crystals with poor aqueous solubility An optimum dissolution rate, and thereby a delivery profile locally in the lung tissue, can be achieved in a reliable way by selecting a compound with an appropriate combination of solubility and particle size. It is in our experience relatively straightforward to manufacture monomodal particle size distributions of poorly soluble drug crystals in the mass median diameter range of either a few micrometers or a few hundred nanometers, but very challenging to manufacture a monomodal distribution in the range intermediate to these two. In this manuscript, we describe an investigation with the objective of generating desired particle sizes in the whole size range from a few micrometers to a few hundred nanometers for inhaled sustained drug delivery, by utilizing Adaptive Focused Acoustic (AFA) milling and planetary bead-milling. By combining the two different milling techniques it was possible to produce two to three distinctly different monomodal or almost monomodal particle size distributions in the desired particle size range of each of the model drug compounds in milligram scale. The dissolution kinetics of the different particle sizes of the model drugs were measured exptl. as well as predicted theor., showcasing that the dissolution kinetics can be characterized, predicted and significantly changed in a controlled way by modifying the particle size. For one of the model drugs, it was shown in an in vivo rat study that the inhaled sustained drug delivery profile in the lung tissue could be significantly changed by modifying the particle size of the drug.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Blood plasma. 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

Poulin, Patrick published the artcileApplication of the Tissue Composition-Based Model to Minipig for Predicting the Volume of Distribution at Steady State and Dermis-to-Plasma Partition Coefficients of Drugs Used in the Physiologically Based Pharmacokinetics Model in Dermatology, Computed Properties of 72509-76-3, the main research area is dermis partition drug pharmacokinetics model dermatol; IVIVE; PBPK modeling; discovery; in silico; pharmacokinetics; tissue composition; topical; transdermal.

The minipig continues to build a reputation as a viable alternative large animal model to predict humans in dermatol. and toxicol. studies. Therefore, it is essential to describe and predict the pharmacokinetics in that species to speed up the clin. candidate selection. Essential input parameters in whole-body physiol. based pharmacokinetic models are the tissue-to-plasma partition coefficients and the resulting volume of distribution at steady-state (Vss). Mechanistic in vitro- and in silico-based models used for predicting these parameters of tissue distribution of drugs refer to the tissue composition-based model (TCM). Robust TCMs were initially developed for some preclin. species (e.g., rat and dog) and human; however, there is currently no model available for the minipig. Therefore, the objective of this present study was to develop a TCM for the minipig and to estimate the corresponding tissue composition data. Drug partitioning into the tissues was predominantly governed by lipid and protein binding effects in addition to drug solubilization and pH gradient effects in the aqueous phase on both sides of the biol. membranes; however, some more complex tissue distribution processes such as drug binding to the collagen-laminin material in dermis and a restricted drug partitioning into membranes of tissues for compounds that are amphiphilic and contain sulfur atom(s) were also challenged. The model was validated by predicting Vss and the dermis-to-plasma partition coefficients (Kp-dermis) of 68 drugs. The prediction of Kp-dermis was extended to humans for comparison with the minipig. The results indicate that the extended TCM provided generally good agreements with observations in the minipig showing that it is also applicable to this preclin. species. In general, up to 86% and 100% of the predicted Vss values are resp. within 2-fold and 3-fold errors compared to the exptl. determined values, whereas these numbers are 78% and 94% for Kp-dermis when the anticipated outlier compounds are not included. Binding data to dermis are comparable between minipigs and humans. Overall, this study is a first step toward developing a mechanistic TCM for the minipig, with the aim of increasing the use of physiol. based pharmacokinetic models of drugs for that species in addition to rats, dogs, and humans because such models are used in preclin. and clin. transdermal studies.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Blood plasma. 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, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dilip, Kinkar Viki published the artcileResearch article on to investigate, develop and evaluate pharmaceutical excipient from orange peel powder, Application In Synthesis of 72509-76-3, the main research area is orange peel powder pharmaceutical excipient.

The present study aimed to investigate, develop and evaluate pharmaceutical excipients from orange peel powder and assess its binding property in tablets by using perindopril erbumine as a modal drug. Now a day′s synthetic polymers are mostly used in the pharmaceutical industry they have many disadvantages such as harmful effects on the human body, highly costly but recently natural polymers are used as a pharmaceutical application like orange peel waste material is used as an excipient have many advantages such as nontoxic, nonirritants easily available, it is economically and biocompatible. There are two basic categories of orange: sweet orange and bitter orange. Orange peel consists of several important constituents such as limonene, citral, vitamin c, hesperidin, and pectin are used as pharmaceutical additives. Manufacturing of tablets was done by using direct compression method on lab level tablet press (CEMACH) by direct compression method. Evaluations tests performed on tablets such as Hardness, Weight variation, friability, disintegration test, etc.

International Journal of Pharmacy and Pharmaceutical Research published new progress about Body remains. 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