Tag: 221.2524

Preparation and characterization of metaxalone nanoparticles prepared by high pressure homogenization was written by Gubbala, Lakshmi Prasanna;Arutla, Srinivas;Venkateshwarlu, Vobalaboina. And the article was included in American Journal of PharmTech Research in 2016.Synthetic Route of C12H15NO3 This article mentions the following:

The aim of present work was to enhance the dissolution of poorly soluble drug metaxalone by particle size reduction Metaxalone nanoparticles are obtained by high pressure homogenization followed by drying, which are characterized for mean particle size (MPS), polydispersityindex( PDI), zeta-potential(ZP), X-ray diffraction(XRD), Differential scanning calorimetry(DSC), Fourier-transform infra-red(FTIR), SEM (SEM), flow properties, saturation solubility and in-vitro release. The MPS of nanoparticles was observed to be less than 200 nm. The neg. ZP indicates the stable nanoparticles obtained by sufficient adsorption of the stabilizers onto drug surface. The XRD and DSC show the retention of drug crystallinity. Out of three drying methods, SD and SG have obtained stable nanoparticles with improved flow properties. Nanoparticles increased the drug solubility by approx. 4 folds with Hydroxy Pr Me cellulose and sodium lauryl sulfate as surface stabilizers. In-vitro release studies showed a remarkable increase in rate of drug release from 3 % (pure drug) to 34-36 % (nanoparticles) after 15 min and at the end of dissolution study almost 95 % of drug dissolved when compared to only 30 % of pure drug. The combining methods of HPH followed by SD/SG was observed to be promising method to produce stable nanoparticles of metaxalone with remarkable increase dissolution rate.. Results from this study suggest that these metaxalone nanoparticles may be a potential candidate for oral administration with quick onset of action for relief of acute painful musculoskeletal conditions. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Synthetic Route of C12H15NO3).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives.Oxazolidines are readily available also from propargyl amines. Oxazolidines are cyclic condensation products of β-amino alcohols and aldehydes or ketone, and they undergo a facile and complete hydrolysis in aqueous solution. Alterations in carbonyl moiety control the rate of formation of a given β-amino alcohol. Oxazolidines are weaker bases (pKa 6–7) than parent β-amino alcohols and found to be more lipophilic than the parent compound at physiological pH.Synthetic Route of C12H15NO3

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Regioselective C-H Thioarylation of Electron-Rich Arenes by Iron(III) Triflimide Catalysis was written by Dodds, Amy C.;Sutherland, Andrew. And the article was included in Journal of Organic Chemistry in 2021.HPLC of Formula: 1665-48-1 This article mentions the following:

A mild and regioselective method for the preparation of unsym. biaryl sulfides using iron(III) catalysis is described. Activation of N-(arylthio)succinimides using the powerful Lewis acid iron(III) triflimide allowed the efficient thiolation of a range of arenes, including anisoles, phenols, acetanilides, and N-heterocycles. The method was applicable for the late-stage thiolation of tyrosine and tryptophan derivatives and was used as the key step for the synthesis of pharmaceutically relevant biaryl sulfur-containing compounds such as the antibiotic dapsone and the antidepressant vortioxetine. Kinetic studies revealed that while N-(arylthio)succinimides bearing electron-deficient arenes underwent thioarylation catalyzed entirely by iron(III) triflimide, N-(arylthio)succinimides with electron-rich arenes displayed an autocatalytic mechanism promoted by the Lewis basic product. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1HPLC of Formula: 1665-48-1).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Oxazolidines are commonly used as metal ligands in asymmetric catalysis, synthetic intermediates in organic synthesis, and also used as the protecting groups.HPLC of Formula: 1665-48-1

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Quantitative determination of drugs in bulk and pharmaceutical dosage forms by using 2,3-dichloro-5,6-dicyanobenzoquinone was written by Srinivas, Bathini;Yadagiriswamy, P.;Venkateshwarlu, G.. And the article was included in World Journal of Pharmacy and Pharmaceutical Sciences in 2015.Application of 1665-48-1 This article mentions the following:

The present work narrates determination of drugs viz,. Metaxalone (MTX), Rasagiline (RSG), Aprepitant (APR) and Linezolid (LZD) based on formation of Charge Transfer Complex of drugs as n-electron donor with 2,3-dichloro-5,6-dicyanobenzoquinone(DDQ) as π-acceptor in bulk and pharmaceutical dosage forms. The selected drugs turned the yellow color solution of DDQ in Acetonitrile to thick brown color and exhibited a band at 585nm due to the formation of Complex of drugs with DDQ. Under the optimized exptl. conditions, Beer, s law is obeyed over the concentration ranges of 15-75 μg/mL, 10-50 μg/mL, 5-25 μg/mL and 10-50 μg/mL for, MTX, RSG, APR and LZD resp. The sensitivity, accuracy of methods, effect of reagent concentrations, polarity of solvents and effect of reaction time have been studied and optimized. The stoichiometric relationship was determined by Job’s continuous method and is found to be 1:1 in each case. These methods have been validated in terms of ICH guidelines and applied to the quantification of selected drugs in bulk and dosage forms. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Application of 1665-48-1).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. In another report, the incorporation of an additional substituted oxazolidine ring over a range of new biphenylazepinium salt organocatalysts for the asymmetric epoxidation of alkenes improved enantiocontrol over the parent structures.Application of 1665-48-1

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

A new method development and validation of dual wavelength UV spectro- photometric method for simultaneous estimation of Metaxolone and Diclofenac potassium in combined dosage form was written by Mallela, Vijaya Jyothi;Kovvuru, Praneeth Kumar Reddy;Amulya, B.;Latha, Sree P.. And the article was included in Indo American Journal of Pharmaceutical Research in 2016.Safety of 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one This article mentions the following:

A simple, accurate, and precise dual wavelength UV spectrophotometric method was developed for simultaneous determination of Metaxolone and Diclofenac potassium in combined pharmaceutical dosage forms. The literature review reveals that there is no dual wavelength method development for this combination of drugs, hence this method was developed. The wavelengths selected for determination of Metaxolone were 270 nm and 280 nm, whereas, the wavelengths selected for determination of Diclofenac potassium were 265 nm and 278 nm. Methanol and distilled water were used as solvents. Regression anal. of Beer’s plots showed good correlation in concentration range of 15-90 μg/mL for Metaxolone and 2-12 μg/mL for Diclofenac potassium. Accuracy of method was found between 98.0-102.0%. The intra-day and inter-day precision studies of the method were found to be within limits. Limit of Detection was found to be 0.780μg and 0.0456 μg for Metaxolone and Diclofenac potassium resp. and Limit of Quantitation was found to be 2.36μg and 0.1382 μg for Metaxolone and Diclofenac potassium resp. The developed method is validated as per ICH guidelines and the results were found to be within the results. Hence, the proposed method can be successfully applied for determination of these drugs in com. tablets. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Safety of 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidine-based compounds have started to attract attention also in the medicinal and materials chemistry fields. Oxazolidines are cyclic condensation products of β-amino alcohols and aldehydes or ketone, and they undergo a facile and complete hydrolysis in aqueous solution. Alterations in carbonyl moiety control the rate of formation of a given β-amino alcohol.Safety of 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Increasing efficacy and reducing side effects in treatment of chronic anal fissures: A study of topical diazepam therapy was written by Hang, Minh Tuan H.;Smith, Betsy E.;Keck, Carson;Keshavarzian, Ali;Sedghi, Shahriar. And the article was included in Medicine (Philadelphia, PA, United States) in 2017.Reference of 1665-48-1 This article mentions the following:

This is a single institution nonexperimental study intended to analyze the therapeutic efficacy of topical diazepam in treating symptoms of chronic anal fissures.Anal fissures are a common cause of anal pain. Conventional treatments include nonsteroidal anti-inflammatory drugs, topical creams, such as nitroglycerin and nifedipine, and surgery. However, these treatments are usually suboptimally efficacious or have deterring side effects.Patients at an outpatient community center with a diagnosis of a chronic anal fissure were prescribed either topical 2% (n=19) or 4% (n=18) diazepam cream between Jan. 2013 and Feb. 2015. We retrospectively analyzed their responses to treatment.All 19 patients using 2% diazepam cream experienced a pos. response in pain, whereas 47.4% experienced a complete response, with a numerical rating scale (NRS) score of 0 (0-10). Eighty-eight percent of patients using 4% dose had a pos. response in pain, whereas 23.5% experienced a complete response. Ninety-four percent of patients using 2% dose had a pos. response in anal bleeding, whereas 68.8% experienced a complete response with an anal bleeding score (ABS) of 2 (2-9). Ninety-four percent of patients using 4% dose had a pos. response in anal bleeding, whereas 64.7% experienced a complete response. Only 1 patient reported a side effect from diazepam cream-perianal pruritus.Both 2% and 4% topical diazepam provided significant pain and bleeding relief from chronic anal fissures that were refractory to conventional therapies. There were insignificant differences when assessing independent comparisons for pain and bleeding between the doses. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Reference of 1665-48-1).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidines are commonly obtained by reaction of strained heterocycles, mainly aziridines. Some reports highlighted again the effectiveness of oxazolidine-based compounds in driving the stereo- or diastereotopic outcome of chemical reactions.Reference of 1665-48-1

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Drug screening method development for paper spray coupled to a triple quadrupole mass spectrometer was written by Jett, Rachel;Skaggs, Christine;Manicke, Nicholas E.. And the article was included in Analytical Methods in 2017.Safety of 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one This article mentions the following:

Paper spray mass spectrometry is a direct anal. method in which compounds are extracted and ionized from biofluids dried on paper. It is an attractive option for performing rapid drug screening because it is fast (the entire sample anal. takes <2 min), simple (there is no sample preparation or chromatog.), and sensitive (low ng mL-1 levels of many drugs can be detected from dried blood spots). Here, we discuss method development for paper spray mass spectrometry on a triple quadrupole mass spectrometer. Specifically, detection criteria, selected reaction monitoring (SRM) ratio tolerance, fragment ion selection, selectivity, and signal to blank considerations are all addressed. 134 drugs and drug metabolites commonly encountered in forensic toxicol. analyses were spiked into blood at concentrations reasonable for post-mortem drug screening applications. Detection of some 130 drug and drug metabolites using a single paper spray MS/MS is shown for these spike and recover experiments In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Safety of 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries. Oxazolidines are well known as key portions of bioactive molecules or precursors of chiral molecules, as well as established chiral auxiliaries.Safety of 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Serotonin syndrome following metaxalone overdose and therapeutic use of a selective serotonin reuptake inhibitor was written by Martini, Dyllon Ivy;Nacca, Nicholas;Haswell, David;Cobb, Timothy;Hodgman, Michael. And the article was included in Clinical Toxicology in 2015.Reference of 1665-48-1 This article mentions the following:

Metaxalone has only recently been associated with serotonin syndrome. The mechanism of action of this centrally acting muscle relaxant is unknown; however, the observation of serotonin syndrome in patients with metaxalone overdose suggests a role in the serotonergic pathway. Case report. (Case 1) A 29-yr-old woman with overdose of metaxalone presented to the emergency department with altered mental status, seizure-like activity, hyperthermia, rigidity in the lower extremities, myoclonus, and hyperreflexia. Vital signs on arrival include blood pressure of 168/80 mmHg, heart rate of 208 beats per min (bpm), respirations of 20/min, a temperature of 41.6° C rectally, and room air oxygen saturation of 97%. She was intubated and sedated with benzodiazepines, and actively cooled. Serum paroxetine concentration was 23 (therapeutic range: 20-200) ng/mL, and serum metaxalone concentration was 31 mcg/mL (peak plasma concentrations average 0.9 mcg/mL at 3.3 h following a single oral dose of 400 mg). (Case 2) A 27-yr-old man presented to the emergency department with altered mental status, rigidity in his lower extremities, myoclonus, and hyperreflexia. Vital signs on arrival include blood pressure of 158/131 mmHg, heart rate of 126 bpm, respiratory rate of 20 breaths per min, and temperature of 37.2°C, with oxygen saturation of 98% on room air. His medication list included metaxalone and escitalopram. He was managed aggressively with IV boluses of diazepam, in total 80 mg, in the emergency department. Serum escitalopram concentration was 24 ng/mL with a therapeutic range of 21-64 ng/mL, and serum metaxalone concentration was 58 mcg/mL. Conclusion. These two cases suggest that at supratherapeutic concentrations metaxalone has serotonergic effects. Severe serotonin toxicity may result from metaxalone abuse in individuals using a selective serotonin reuptake inhibitor therapeutically. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Reference of 1665-48-1).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidines that are the precursor to bisoxazolidines are in effect mono-oxazolidines. They are also used as moisture scavengers in polyurethane and other systems. Chiral oxazolidines are widely used as chiral auxiliaries, chiral ligands, protecting and/or directing groups in a variety of asymmetric transformations, thanks also to their easy cleavage or their further elaboration possibilities.Reference of 1665-48-1

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem

Bioanalytical and analytical method development, validation approaches for Metaxalone: a brief review was written by Yamgar, Dilip B.;Desale, Mayur N.;Prajapati, Malesh S.;Fegade, Bharti;Vaidhun, Bhaskar. And the article was included in World Journal of Pharmacy and Pharmaceutical Sciences in 2021.Category: oxazolidine This article mentions the following:

Metaxalone (MTX), a non-benzodiazepine antispasmodics, resembling in structure to mephenaxalone is a BCS Class II drug that acts centrally to skeletal muscle relaxant drug with antispasmodic effect. Although the exact mode of action of MTX is not fully understood, it has been stated that it acts via the general CNS depression method resulting in relaxation of skeletal muscles and also sedation. It has been formulated under the brand name of SKELAXIN and distributed by King Pharmaceuticals. The dosage form available in the market for the drug contains 400 and 800 mg of drug with excipients. The bioavailability of Metaxalone has been found to increase when taken on a full stomach. After intake of MTX in any form strictly avoid excessive or chronic consumption of alc. This often leads to an increase in CNS depressant effects. Literature survey has demonstrated that fewer methods are available to perform the characterization of Metaxalone in bulk solution as well as biol. fluids. Some of the methods are electrospray ionization (ESI), LC-MS/MS, UV spectroscopy combined with LC chromatog., HPLC-UV, GC with flame ionization detector, GC with MS. The present review comprehensively overlooks the all of above methods for estimation of Metaxalone in its bulk solution as well formulation and in biol. fluids. In the experiment, the researchers used many compounds, for example, 5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1Category: oxazolidine).

5-((3,5-Dimethylphenoxy)methyl)oxazolidin-2-one (cas: 1665-48-1) belongs to oxazolidine derivatives. Oxazolidines that are the precursor to bisoxazolidines are in effect mono-oxazolidines. They are also used as moisture scavengers in polyurethane and other systems. Oxazolidines are cyclic condensation products of β-amino alcohols and aldehydes or ketone, and they undergo a facile and complete hydrolysis in aqueous solution. Alterations in carbonyl moiety control the rate of formation of a given β-amino alcohol.Category: oxazolidine

Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem