Category: 23828-92-4

Ijitsu, Shin published the artcilePreparation of novel functional drug particles embedded in a gelling-swelling layer (PEGS) for taste masking and subsequent rapid drug release, Application In Synthesis of 23828-92-4, the publication is Chemical & Pharmaceutical Bulletin (2021), 69(4), 383-390, database is CAplus.

The purpose of this research was to develop novel functional drug particles embedded in a gelling-swelling layer (PEGS) which are capable of achieving both taste-masking of unpalatable drugs and rapid drug elution. The functional particles had a three-layer structure consisting of a core drug layer, a gelling-swelling layer and an outer water-penetration control layer containing a water-insoluble polymer. The concept of formulation design was as follows: when water reaches the gelling-swelling layer, pulverized fine gelling-swelling particles gellate and swell from water absorption to form a rigid layer, thereby preventing drug release. After a defined lag time, the increased volume of the gelling-swelling layer breaks down the outer water-penetration control layer, leading to rapid drug release. In order to adapt this system for use in orally disintegrating tablets, PEGS were prepared at a size of about 250μm using a fine particle-coating method. Ambroxol hydrochloride was used as a model drug for bitterness and the effects of different gelling-swelling agents and water-insoluble polymers on drug release characteristics from PEGS were examined In in vitro dissolution tests, it was shown that the drug dissolution rate from PEGS could be suppressed to about 5% after 2 min and increased to more than 85% after 30 min by adjusting the composition and thickness of the outer layer. The PEGS expanded about 1.5-fold and the outer layer was ruptured after 5 min in water.

Chemical & Pharmaceutical Bulletin published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application In Synthesis of 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Sun, Shuzhou published the artcileDetermination of 26 chemical drugs for the treatment of cough and asthma added illegally in herbal tea by high performance liquid chromatography-tandem mass spectrometry, Quality Control of 23828-92-4, the publication is Jinri Yaoxue (2021), 31(3), 195-199, database is CAplus.

OBJECTIVE To establish a rapid screening method for determination of 26 chem. drugs for the treatment of cough and asthma added illegally in herbal tea. METHODS This method involved liquid chromatog.-tandem mass spectrometry. The samples were extracted with methanol, filtrated by 0.22 μm microporous filters and finally separated on a C₁₈ column (2.1 mm×150 mm, 3.5 μm) by using acetonitrile and water (containing 5 mmol·L^-1 ammonium formate and 0.1% formic acid) as mobile phase. Qual. and quant. anal. were carried out in multiple reaction monitoring (MRM) model. RESULTS The correlative coefficient of 26 chem. drugs were above 0.995. The average recoveries were 61.2% ∼ 115.6%, the relative standard deviations ranged from 1.0% to 2.0% (n=6). CONCLUSION The method is simple, rapid and sensitive. It is suitable for the determination of 26 chem. drugs for the treatment of cough and asthma added illegally in herbal tea.

Jinri Yaoxue published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C12H15ClO3, Quality Control of 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Chen, Shi-yun published the artcileSynthesis of related substances for ambroxol hydrochloride glucose injection, Category: alcohols-buliding-blocks, the publication is Huaxue Shiji (2019), 41(10), 1098-1100, database is CAplus.

To perform the quality control of ambroxol hydrochloride glucose injection, related substance 4-(6, 8-dibromo-3, 4-dihydroquinazoline-3-yl)-cyclohexanol was prepared 4-(6, 8-Dibromo-3, 4-dihydroquinazoline-3-yl)-cyclohexanol was synthesized from ambroxol hydrochloride and formaldehyde by cyclization and oxidation reactions. The structure of 4-(6, 8-dibromo-3, 4-dihydroquinazoline-3-yl)-cyclohexanol was confirmed by IR, ¹HNMR, ¹³CNMR and ESI-MS. The synthetic route designed in this work is simple and the post-processing is convenient, can be used to provide the material foundation for ambroxol hydrochloride related substances 4-(6,8-dibromo-3,4-dihydroquinazoline-3-yl)-cyclohexanol reference substance preparation

Huaxue Shiji published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Category: alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lee, Sie Huey published the artcileInhaled mucoactive particles with tailored architecture for enhanced aerodynamicity, stability and efficacy, Application In Synthesis of 23828-92-4, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2019), 118740, database is CAplus and MEDLINE.

In respiratory and genetic disorders such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis and cystic fibrosis (CF), the lungs produce excess mucus, resulting in a thickened mass, which clogs up the airways and reduces airflow. Consequently, breathing becomes more difficult. Medications that break down the structure of mucus will be especially useful in managing the early symptoms of these diseases and preventing their progression into the more severe forms. This work therefore seeks to develop an inhaled mucoactive dry powder formulation that is efficacious on multiple fronts. As an innovative step, sodium chloride was used to tailor the surface architecture of ambroxol hydrochloride particles, such that the resulting angular features on the surfaces contributed to the creation of corrugated particles with enhanced aerodynamicity. The optimized spray-dried powder particles were of respirable-size (d₅₀ of 2.85 ± 0.15 μm) and moderately corrugated. When the crystalline powder was dispersed via an Aerolizer inhaler at 60 L/min, it gave a fine particle fraction (FPF) of ∼31%, which was a ten-fold improvement over the unmodified species (i.e. ambroxol hydrochloride alone). Tests on artificial sputum medium (ASM) showed that the optimized formulation was potentially useful in liquefying the mucus, which favorably pointed towards the effectiveness of the formulation. In addition, the formulation was also stable to moisture ingress (up to ∼60% RH) and had good flowability. Hence, the advent of angular adjuvant sodium chloride particles in a mucoactive formulation conferred a three-fold benefit to the product: (1) Improved aerodynamicity and flowability, (2) Enhanced moisture stability and (3) Synergistic mucolytic properties.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application In Synthesis of 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

El-Sayed, Heba M. published the artcileQuality by Design Strategy for Simultaneous HPLC Determination of Bromhexine HCl and Its Metabolite Ambroxol HCl in Dosage Forms and Plasma, Application In Synthesis of 23828-92-4, the publication is Chromatographia (2020), 83(9), 1075-1085, database is CAplus.

Abstract: The quality by design strategy was applied for the simultaneous chromatog. quantification of a binary mixture of bromhexine HCl and its pharmacol. active metabolite ambroxol HCl in dosage forms as well as in human plasma. In this study, five independent parameters were screened by fractional factorial design to specify the critical ones. The optimal conditions were determined by a response surface methodol. using a central composite design. Response surface methodol. enabled the best separation in minimal run time, as well as, prediction of separation and retention parameters with min. error. Separation and quantitation were carried out on BDS Hypersil C₈ (250 × 4.6 mm, 5μm) RP-column at 1.1 mL min^-1 flow rate, 25 mM of KH₂PO₄ (pH 3.5) in aqueous mobile phase, 65% MeOH, 210 nm wavelength of detection and 10μL injection volume After optimization of the chromatog. parameters, validation of the method was achieved according to ICH guidelines. Linearity ranged from 0.195 to 100μg mL^-1 ambroxol HCl, and 0.391-100μg mL^-1 bromhexine HCl, with R² values of 0.9998 and 0.9999 and limits of detection of 0.098 and 0.195μg mL^-1, resp. Recovery results ranged from 98.06 to 100.18 and 97.88 to 100.68 for bromhexine HCl and ambroxol HCl, resp., with RSD less than 1.80.

Chromatographia published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application In Synthesis of 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Panchale, Wrushali A. published the artcileSimultaneous estimation of salbutamol sulphate and ambroxol HCl from their combined dosage form by UV-VIS spectroscopy using simultaneous equation method, COA of Formula: C13H19Br2ClN2O, the publication is GSC Biological and Pharmaceutical Sciences (2020), 13(3), 127-134, database is CAplus.

A simple UV-Vis Spectrophometric method was developed for the simultaneous determination of salbutamol sulfate and ambroxol HCl (AMB) from their combined dosage form. The method employs formation and solving of simultaneous equation using 242 nm and 272 nm as two anal. wavelengths (λMax of the drugs) of detection. Both the drugs obeyed Beer-Lambert’s law over the concentration range 1-50μg/mL for salbutamol sulfate and 10-50μg/mL for ambroxol HCl, resp. The developed method was validated for Accuracy, Precision, Limit of Detection and Limit of Quantification as per ICH guidelines and results of anal. were validated statistically.

GSC Biological and Pharmaceutical Sciences published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, COA of Formula: C13H19Br2ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

He, Meilian published the artcileDetermination of ambroxol hydrochloride in human plasma by ultra high performance liquid chromatography-tandem mass spectrometry and bioequivalence evaluation of its preparation, Related Products of alcohols-buliding-blocks, the publication is Sepu (2018), 36(11), 1099-1104, database is CAplus and MEDLINE.

A rapid, simple and sensitive ultra high performance liquid chromatog.-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the determination of ambroxol hydrochloride in human plasma, and bioequivalence of its preparation was evaluated. The 50 μL-plasma sample was treated with methanol for protein precipitation, while ambroxol-d5 was used as an internal standard (IS). The separation was carried out on a Waters XBridge BEH C18 column (50 mm × 2.1 mm, 2.5 μm) by gradient elution at a flow rate of 0.4 mL/min, with 0.1% (volume/volume) formic acid aqueous solution and methanol containing 0.1% (volume/volume) formic acid as the mobile phases. The analyte was detected using an electrospray ionization source in pos. ion multiple reaction monitoring (MRM) mode. The calibration curves were linear in the range of 2-400 ng/mL (r = 0.998). The intra- and inter-run accuracies were 97.1-108.7%, and the intra- and inter-run precisions were 1.0-5.6%. The method was applied to the determination of the plasma concentration of the six healthy subjects after the oral administration of 30 mg of test and reference preparations The bioavailability was (102.3 ± 14.8)%. The 90% confidence intervals of the test preparation’s pharmacokinetic parameters were 80.0-125.0% of the reference preparation’s corresponding parameters. Thus, it is proved that the test preparation and reference preparation are bioequivalent.

Sepu published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Skarzynska, Magdalena Beata published the artcileEffectiveness of surgical approach of insertion ventilation tubes (Tympanostomy) and adenoidectomy in comparison with non-surgical approach (Watchful Waiting Approach) in children at the age between 1 and 6 and who suffer from otitis media with effusion (OME) in 12-month period of observation-the retrospective analysis, Application In Synthesis of 23828-92-4, the publication is International Journal of Environmental Research and Public Health (2021), 18(23), 12502, database is CAplus and MEDLINE.

Otitis media with effusion (OME) is one of the most common diseases in childhood. The objective was to assess clin. the effectiveness of the surgical approach (tube insertion with adenoidectomy) in comparison with the non-surgical approach (watchful waiting) during a 12-mo observation period. This study was retrospective and obtained approval from the bioethics committee. The criteria of inclusion in the first group (surgical approach) were: (1) a diagnosis of chronic otitis media with effusion in children aged between 1 and 6 years; (2) their medical history showed that they had undergone adenoidectomy and tympanostomy with the insertion of ventilation tubes (VTs). The criteria for inclusion in the second group (non-surgery) were similar to the first group except that their medical history showed they had not undergone adenoidectomy or tympanostomy with the insertion of VTs. There were 422 children included in the surgical group and 50 children in the non-surgical group, and the period of observation was 12 mo. For the entire surgical group, the number of healthy days ranged from 20 to 365, with a mean of 328.0 days (SD = 91.4).In the non-surgical group, the number of healthy days ranged from 13 to 365, with a mean of 169.2 days (SD = 127.3). The difference in the number of healthy days was statistically significant (p < 0.001). The certainty of treatment in the first group was higher than in the second group, and the number of days without recurrence was significantly higher than in the second group. In the first group, there were 71 recurrences from 422 children (16.8%), and, in the second subgroup, there were 40 recurrences of acute otitis media (AOM) from 50 children (80%). The RR was 0.21. The surgical approach in children aged 1-6 years who have been diagnosed with otitis media with effusion is reasonable and beneficial for the child.

International Journal of Environmental Research and Public Health published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C10H11NO4, Application In Synthesis of 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Thangavelu, Prabha published the artcileAnalytical method development and validation for the simultaneous estimation of salbutamol sulphate, guaifenesin, and ambroxol hydrochloride by RP-HPLC method in commercial oral liquid dosage form, Formula: C13H19Br2ClN2O, the publication is International Journal of Pharmaceutical Sciences and Research (2019), 10(1), 260-265, database is CAplus.

Salbutamol is a bronchodilator, Guaifenesin is an expectorant and Ambroxol is a mucolytic. Combination of these drugs is used in the formulation of cough syrups. In the literature, there is no method reported for the simultaneous estimation of the drugs in oral liquid dosage form. Hence, the present work is aimed to develop reverse phase HPLC method for the simultaneous determination of Salbutamol sulfate (SAL), Guaifenesin (GUA) and Ambroxol hydrochloride (AMB) in oral liquid dosage form and validation of the developed method. The chromatog. separation of the drugs was achieved with the mobile phase system sodium dihydrogen phosphate buffer pH 3.0: acetonitrile: methanol in the ratio of 65:10:25 with the flow rate of 1 mL/min and injection volume 10μL. An Inertsil C8-3 (250 × 4.6 mm, 5μm) column was used, and the detection wavelength was 276 nm. This system produced sharp peaks with good resolution, min. tailing and satisfactory retention times of SAL, GUA and AMB were found to be 3.157, 9.949 and 11.883 min resp. indicating the suitability of the system. The developed method was validated for various parameters accuracy, precision, linearity, robustness, and specificity as per ICH guidelines.

International Journal of Pharmaceutical Sciences and Research published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C18H26ClN3O, Formula: C13H19Br2ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Potawale, Rani S. published the artcileLiquid chromatography tandem-mass spectrometry method development and validation for simultaneous analysis of paracetamol, guaifenesin, phenylephrine hydrochloride, chlorpheniramine maleate, and ambroxol hydrochloride in bulk and in tablet dosage form, HPLC of Formula: 23828-92-4, the publication is Asian Journal of Pharmaceutical and Clinical Research (2018), 11(7), 1-8, database is CAplus.

Objective: The objective is to study liquid chromatog. tandem-mass spectrometry (LC/MS/MS) method for simultaneous quantification of paracetamol (PCM), guaifenesin (GUA), phenylephrine hydrochloride (PE), chlorpheniramine maleate (CPM), and ambroxol hydrochloride (AMB) in tablet dosage form developed and validated as per the International Conference on Harmonization Q2 (R1) guideline. Methods: The chromatograms were developed using a gradient mobile phase of WATER:methanol. Flow rate used was to 0.3 mL/min. Quantitation was performed using multiple reaction monitoring (MRM) mode to study parent to product ion transition, for paracetamol. (m/z 152.0 ≥ 110.0), guaifenesin (m/z 199.0 ≥ 163.0), phenylephrine hydrochloride (m/z 168.0 ≥ 150.0), chlorpheniramine maleate (m/z 275.0 ≥ 230.0) and ambroxol hydrochloride (m/z 379.0 ≥ 263.8). Results: The retention times were found to be 1.76, 1.81, 1.90, 2.10, and 2.33 min for PCM, GUA, PE, CPM, and AMB, resp. The linearity of the method was found to be in the concentration range of 10-200 ng/mL for PCM, GUA, PE, CPM, and AMB. Percentage relative standard deviation values for repeatability and intermediate precision studies were below 2%. Conclusion: Developed method was found to be robust, precise, accurate, rapid and can be used to analyze fixed-dose tablet formulation used in the study.

Asian Journal of Pharmaceutical and Clinical Research published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, HPLC of Formula: 23828-92-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts