Avinash Pore, G. Gaikwad, S. Hegade, Y. Jadhav, R. Mane, R. Kumbhar
{"title":"Analyzing the Impact of the Substituent on the Quinazolinone Schiff Base and the Interaction of the Fe (III) and Cr (III) with Different Quinazolinone Schiff Base for Antioxidant and Anti-inflammatory Activity","authors":"Avinash Pore, G. Gaikwad, S. Hegade, Y. Jadhav, R. Mane, R. Kumbhar","doi":"10.1080/22297928.2023.2173647","DOIUrl":"https://doi.org/10.1080/22297928.2023.2173647","url":null,"abstract":"Abstract Schiff base and their Fe (III), Cr (III) complexes stood vetted for Antioxidant, Anti-inflammatory activities and docking study. Mixed ligand complexes had strong antioxidant and anti-inflammatory properties. Docking study of mixed ligand complexes reveals substantial binding affinity for COX2 and STAT3 receptors. The experimental and computational anti-inflammatory and antioxidant activity results are more consistent. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"4 1","pages":"39 - 59"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80080119","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Stability Indicating Method for the Assay of Remogliflozin Etabonate and its Related Substances by RP-HPLC","authors":"Ramjilal Yadav, R. Dev, Ruchita Santra, P. Jain","doi":"10.1080/22297928.2023.2176785","DOIUrl":"https://doi.org/10.1080/22297928.2023.2176785","url":null,"abstract":"Abstract Simple, accurate, precise and stable indicating HPLC methods were developed and validated to determine both related substances and the assay content of Remogliflozin etabonate (RME). The separation was established under optimized chromatographic condition using Waters e2695 HPLC coupled to Ultraviolet detector (UV) at 228 nm with Inertsil ODS-3V C18 column (250 mm x 4.6 mm, 5 μm), injection volume 10 μl for related substances and 20 μl for assay content determination. The mobile phase consisted of 10 mM KH2PO4 buffer with ortho-phosphoric acid pH 2.5. Gradient elution was maintained at a flow rate of 1.0 ml/min using 45°C column oven temperature for determination of the related substances and isocratic elution was maintained at a flow rate of 1.2 ml/min for assay content. The retention time for RME-01, RME-02, RME-03 and RME-04, RME-05 and RME were about 41.74 min, 11.42 min, 20.38 min, 37.16 min, 49.93 min, 25.05 min respectively. The linearity was found to be in the concentration range of 0.312-2.341 μg/ mL for RME-01, 0.306-2.292 μg/ mL for RME-02, 0.306-2.297 μg/ ml for RME-03 and 0.294-2.203 μg/mL for RME-04. The RME was subjected to acid, base, oxidation, and thermal degradation stress conditions. The method was validated according to the ICH guidelines for specificity, precision, linearity, accuracy and robustness and the values were found to be within the limits. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"45 1","pages":"73 - 81"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81720040","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Norsyazwani Muhamad Dah, Wan Yaacob Wan Ahmad, Mohd Syafiq Aiman Mat Noor, S. S. S. Abdul Azziz
{"title":"Chemical Composition of Goniothalamus andersonii Bark and its Mosquito Repellent Activity","authors":"Norsyazwani Muhamad Dah, Wan Yaacob Wan Ahmad, Mohd Syafiq Aiman Mat Noor, S. S. S. Abdul Azziz","doi":"10.1080/22297928.2023.2178327","DOIUrl":"https://doi.org/10.1080/22297928.2023.2178327","url":null,"abstract":"Abstract This study sought to identify the chemical composition of smoke condensate of Goniothalamus andersonii (Annonaceae) and comparatively evaluate the effectiveness of smoke condensate. The chemical composition has been determined by GC-MS. Five main components were contained in aqueous fraction, namely eugenol (25.31%), (E)-cinnamaldehyde (21.13%), hexamethylene diacrylate (7.0%), caryophyllene (6.25%), and ethyl oleate (4.3%). While, three main components were detected in the n-hexane fractions, namely guaiol (8.98%), α-eudesmol (5.71%), and (-)-cyperene (3.06%). Laboratory research was conducted to determine the repellency of the smoke condensate of Aedes aegypti mosquitoes at two levels of concentration (5.0% and 10.0%). Tests were carried out to establish the percentage reduction of mosquito landing for each of the concentrations. The synthetic insect repellent, N, N-diethyl-m-toluamide (DEET), was used as a standard at a similar level of concentration. At 5.0% concentration, DEET provided a better percentage reduction with 70.5% for up to 4 hours, compared to smoke condensate (44.5%). At 10.0%, DEET provided an 80.9% reduction in mosquito landing, which was significantly better, as compared to smoke condensate (61.9%). However, data analysis through a t-test demonstrated a significant difference between smoke condensate and DEET efficacy in both concentrations, with regards to treated and untreated arms (P < 0.05). GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"8 1","pages":"17 - 27"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90358251","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Devangkumar Tandel, K. Patel, V. Thakkar, A. Sakure, T. Gandhi
{"title":"Bioanalytical Method Development and Validation for Determination of Rifampicin and Quercetin in Rat Plasma by UHPLC-MS/MS: Applications to Pharmacokinetic Study","authors":"Devangkumar Tandel, K. Patel, V. Thakkar, A. Sakure, T. Gandhi","doi":"10.1080/22297928.2022.2162830","DOIUrl":"https://doi.org/10.1080/22297928.2022.2162830","url":null,"abstract":"Abstract UHPLC-MS/MS was utilised to quantitatively analyse Rifampicin and Quercetin-loaded Liquisolid compact in rat plasma. The UPLC Acquity C18 (1.7 μm, 2.1 × 15 mm) column and 0.5 ml/min were used to separate the analyte. In a low-pressure gradient mode, A: In water 0.1 % formic acid and B: In acetonitrile 0.1 % formic acid as the mobile phase. Sample pre-treatment was performed by protein precipitation technique with methanol and acetonitrile (1:1) from rat plasma. As an internal standard (IS), the analyte was found by tracking precursor-to-product ion transformations of 823 → 791.3 m/z for rifampicin, 303 → 257 m/z for quercetin, and 138 → 121 m/z for isoniazid in MRM mode. The proposed technique was validated for precisions (Intraday and Interday) accuracy, linearity, quantification at lower limits, and analyte recovery. The findings showed that the plasma samples inter and intra-day precision and consistency values were determined to be within the acceptable range. After orally administering Liquid solid compact and pure drug solution, which showed a substantial difference in the pace and extent of absorption, the method’s suitability for determining the pharmacokinetic profile of each drug was tested. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"21 1","pages":"60 - 72"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82543216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dhavalsinh P. Solanki, Krunal H. Solanki, Jaineel Desai, D. Shah, U. Chhalotiya
{"title":"HPTLC-Densitometric Estimation of Anti-hypertensive Drug Combination Azilsartan Medoxomil and Cilnidipine in Combined Dosage Form","authors":"Dhavalsinh P. Solanki, Krunal H. Solanki, Jaineel Desai, D. Shah, U. Chhalotiya","doi":"10.1080/22297928.2023.2195862","DOIUrl":"https://doi.org/10.1080/22297928.2023.2195862","url":null,"abstract":"Abstract A combination of Azilsartan Medoxomil and Cilnidipine is prescribed in the treatment of Hypertension. The present work represents an accurate and precise high-performance thin layer chromatographic method for the estimation of Azilsartan Medoxomil (AZL) and Cilnidipine (CLN) in combined tablet dosage form. Pre-coated silica gel- G60 F254 aluminum sheet (100 × 100 mm, 0.2 mm layer thickness) were used as stationary phase and Ethyl Acetate: Toluene: Glacial Acetic Acid (5: 4.9: 0.1 %v/v/v) in the mixture was used as mobile phase. The method was linear in the concentration range of 200 - 2000 ng/band for AZL and 50 -500 ng/band for CLN with a correlation coefficient (r2) of 0.996 for AZL and 0.999 for CLN. The proposed method was validated with respect to linearity, accuracy, precision, and robustness as per ICH Q2 (R1) guideline. A forced degradation study was performed to assess the stability indicating the nature of the method. All the degradant peaks were well resolved from the peak of the drug without any interference. The method was successfully applied for the analysis of AZL and CLN in combined tablet formulation. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"8 1","pages":"82 - 94"},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81500138","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Enantioselective Green HPLC Method for Simultaneous Determination of Enantiomer, and Potential Impurities in Apremilast Drug Substance","authors":"C. Vijaykumar, Y. Kumar, P. Aparna, V. Marisetti","doi":"10.1080/22297928.2022.2155071","DOIUrl":"https://doi.org/10.1080/22297928.2022.2155071","url":null,"abstract":"Abstract A single reversed-phase HPLC method was developed for the quantification of seven impurities of Apremilast and its enantiomer in the drug substance. An immobilized chiral stationary phase with a chiral selector “tris (3,5-dimethyl phenyl carbamate) derivative of amylose-Chiralpak IA-3 (250 mm × 4.6 mm, 3 μm) was employed to achieve the desired separation. A mobile phase consists of buffer (0.01M NH4HCO3, PH 8.0) and acetonitrile in the ratio 50:50 (v/v) and is pumped at a flow rate of 0.4 mL/min with an isocratic elution mode. The column oven temperature is set at 25°C, and the chromatographic output is monitored at 225 nm with a total run time of 45 min. A test concentration of 500 µg/mL of Apremilast in the mobile phase is used with an injection volume of 10 µL. Induced degradation studies were carried out to study the intrinsic chemical behavior of the drug. The degradation sample solutions were utilized to demonstrate the stability-indicating nature of the developed analytical method. The obtained mass number [M+H]+ for the primary degradation product formed in acid hydrolysis was identified as 418.36 and in base hydrolysis 478.12. The two impurities were identified as impurity-5(Deacetylated impurity), and impurity-2(open ring acid impurity), respectively, and the degradation pathways were established. Following ICH Q2 and USP<1225>guidelines, complete method validation was carried out. The RSD for the drug and impurities in interday and intraday studies are less than 4.0%, and the recoveries for the impurities are between 96.1-102.1% and linearity r ≥ 0.9997. LOQ results for the drug and impurities are between 0.052 µg/mL and 0.107 µg/mL, and LOD results are between 0.016 µg/mL and 0.032 µg/mL. The greenness of the method was evaluated by using an analytical eco scale, GAPI, and AGREE, and it was found that the method is green. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"30 1","pages":"691 - 714"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75316774","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Execution of Quality by Design Approach for Preparation and Optimization of Inclusion Complexes: In-vivo and ex-vivo Assessment","authors":"Neha Bajwa, P. Singh, Srishti Naryal, Trisha Sharma, Puran Singh Sijwal, Ashish Baldi","doi":"10.1080/22297928.2022.2159521","DOIUrl":"https://doi.org/10.1080/22297928.2022.2159521","url":null,"abstract":"Abstract The inclusion complex of α, β-arteether with β-cyclodextrin was prepared. The ratio was selected by implementing the QbD approach to get the best host-guest complex ratio. Further, the formation of the best complex was compared with stability analysis. Also, the enhancement in dissolution profile, as well as solubility, was compared with the pure α, β-arteether. The cyclodextrin derivative with maximum enhanced solubility and best dissolution profile was further used for PKPD modeling, permeability studies, and in-vivo and ex-vivo studies. By QbD approach as well as phase solubility studies it was confirmed that 1:1 fits best for the ART-CD inclusion complex formation. This was substantiated by a saturation solubility investigation, which found that in the presence of PVPK30, the solubility of α, β-arteether was enhanced by 77.05 times. The crystalline nature of the drug was lost or diminished greatly in the inclusion complex, showing the drug was present in a solubilized form in the formulation, according to scanning electron microscopy, X-ray diffraction, and differential scanning calorimetry. Further, the complex powder was converted into spheroids by the spheronization technique and filled in empty enteric-coated shells. In vitro release studies for spheroids-filled enteric capsules were carried out for 6 h by progressive dissolution technique. The pharmacokinetic model using Ecosim Pro 6.2.0 software confirms the enhancement of the bioavailability of the arteether. Further, the in vivo studies also confirm the enhancement in absolute bioavailability by 48.29% when compared with i.v. data of pure drugs. The complex shows an 11% maximum enhancement in antimalarial activity when compared with pure drugs. From the research, it was concluded that inclusion complexation is a suitable approach to improvise the solubility as well as bioavailability of hydrophobic drugs like α, β-arteether. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"26 1","pages":"715 - 729"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86105409","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Repurposing of Existing Pharmaceutical Drugs Against Monkey-pox Virus: An In Silico Study","authors":"K. Sarkar, R. Das","doi":"10.1080/22297928.2022.2157224","DOIUrl":"https://doi.org/10.1080/22297928.2022.2157224","url":null,"abstract":"Abstract Monkeypox virus (MPXV) is considered as zoonotic disease with characteristics comparable to smallpox virus. The disease is now a global epidemic concern. Currently, tecovirimat is approved by US Food and Drug Administration (FDA) for MPXV treatment. The aim of this in silico study is to repurpose approved pharmaceutical drugs as potential inhibitors of MPXV target. In this study, molecular docking was performed on 406 pharmaceutical drugs, and results were compared with reference tecovirimat. Results showed that 7 compounds, bictegravir, glimepiride, glyburide, lasmiditan, olaparib, rimegepant, and ubrogepant, have shown higher binding energies compared to the reference. After that, these best hits were further assessed by 100 ns molecular dynamics simulation and the best results were observed for bictegravir, glimepiride, glyburide, olaparib, and ubrogepant. The docking analysis was further validated by molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) binding free energy calculations. In addition, pharmacokinetics and density functional theory (DFT) studies were also discussed for these best hits. In conclusion, three compounds, bictegravir, glimepiride, and glyburide, have satisfied all the criteria for better leads against MPXV. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"81 1","pages":"655 - 670"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85137016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Sushank Suryawanshi, R. Pawar, R. Gonnade, Sharvil Patil
{"title":"Hot Melt Extrusion Assisted Felodipine Loaded Liquid Crystal Precursor with Enhanced Solubility and Sustained Drug Release Characteristics","authors":"Sushank Suryawanshi, R. Pawar, R. Gonnade, Sharvil Patil","doi":"10.1080/22297928.2022.2159523","DOIUrl":"https://doi.org/10.1080/22297928.2022.2159523","url":null,"abstract":"Abstract Glyceryl monooleate (GMO) forms cubic mesophase upon hydration with sustained drug release characteristics. However its stickiness and stiffness often creates processing challenges for preparation of formulations. Felodipine (FLD), BCS class II molecule was used as model drug. Thus objective of the current work was to increase manufacturing feasibility of GMO using polymer and to enhance the release of felodipine by preparing LC precursors using HME. HPMC E5 polymer was selected for processing of FLD. Batch optimization was done using 23 Factorial design. The prepared batches were characterized for DSC, FTIR, hot stage microscopy (HSM), plane polarized light microscopy (PPL), PXRD and in vitro dissolution studies. The processing of FLD using HME process showed amorphization as revealed by PXRD studies. DSC and HSM studies showed solubilization of FLD in the molten mass of GMO and HPMC E5 confirming formation of solid dispersion. PPL demonstrated formation of cubic LC phase by GMO upon hydration of prepared formulations. The optimized batch of felodipine showed significant improvement in the dissolution profile of FLD with extended release profile. HME assisted liquid crystal precursors could act as promising formulations for BCS II drugs requiring extended drug release profile with improved processing feasibility of GMO. GRAPHICAL ABSTRACT","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"86 1","pages":"745 - 760"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89866523","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Rony Bhowal, Sony Kumari, C. Sarma, P. Suprasanna, Puja Roy
{"title":"Phytochemical Constituents and Bioactivity Profiles of Citrus Genus from India","authors":"Rony Bhowal, Sony Kumari, C. Sarma, P. Suprasanna, Puja Roy","doi":"10.1080/22297928.2022.2157223","DOIUrl":"https://doi.org/10.1080/22297928.2022.2157223","url":null,"abstract":"Abstract Citrus plants have a secure and important place in human health. Citrus is not only significant for its delicious fruits but also because of certain medicinal and pharmacological properties. The presence of secondary metabolites like flavonoids, limonoids, alkaloids, phenolics and coumarins has dramatically increased its efficacy in treating bacterial and fungal infections. Emergence of new and improved extraction techniques has helped researchers to isolate novel phytochemicals from citrus species, and there is a greater attention. Numerous studies throughout the world have focused to isolate novel metabolites from citrus plants. There is a rich biodiversity of citrus species in the Indian subcontinent based on climatic condition which supported the growth and maintenance of diverse varieties. Analysis of metabolomic and medicinal properties of local citrus plant will aid in understanding their importance in pharmacological industry. The present review is focused on the medicinal and secondary metabolite profile of citrus plants from India.","PeriodicalId":7793,"journal":{"name":"Analytical Chemistry Letters","volume":"10 1","pages":"770 - 787"},"PeriodicalIF":0.0,"publicationDate":"2022-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81102367","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}