Current Pharmaceutical Analysis最新文献

{"title":"Determination of Antithyroid drug Propylthiouracil with Ru (III) in Pharmaceutical formulations and its characterization","authors":"Afraim Koty, Mukul Sharma","doi":"10.2174/1573412919666230524140341","DOIUrl":"https://doi.org/10.2174/1573412919666230524140341","url":null,"abstract":"\u0000\u0000Sulfur serves as a versatile element and an essential constituent of pharmaceutical industries, natural compounds, proteins, and biological systems. One of the fundamental constituents of sulfur is thiouracil, which forms several derivatives, including 6-methylthiouracil, 6-methyl-2-thiouracil, and 6-propylthiouracil. These derivatives act as effective chelating agents and can form complexes with metal ions.\u0000\u0000\u0000\u0000Sulfur serves as a versatile element and an essential constituent of pharmaceutical industries, natural compounds, proteins, and biological systems. One of the fundamental constituents of sulfur is thiouracil, which forms several derivatives, including 6-methylthiouracil, 6-methyl-2-thiouracil, and 6-propylthiouracil. These derivatives act as effective chelating agents and can form complexes with metal ions.\u0000Compared with other metals, ruthenium possesses unique chemical properties that make it an ideal therapeutic agent. Therefore, this study reports on the propylthiouracil: Ru(III) complex, considering these essential facts.\u0000\u0000\u0000\u0000An equimolar amount of ruthenium trichloride 3.34 x 10-5 M was added to various aliquots ranging from 0.4 mL to 8.8 mL of 3.26 x 10−5 M propylthiouracil. The volume was adjusted to 10 mL with double distilled water. After letting the solution stand for 10 min, we recorded the absorbance of different sets at λmax 376 nm. The Beer-Lambert's law graph demonstrated linearity in the concentration range of 3.18 x101 gmL-1 to 7.96 x102 gmL-1, with a linear regression equation of Y = 0.0354 + 0.1109 X. We determined the effective molar absorptivity (ε) to be 6.609 x 102 Lmole-1 cm-1, and the relative standard deviation (RSD %) was ± 0.34%.\u0000\u0000\u0000\u0000At room temperature, a yellow-colored complex of propylthiouracil: Ru(III) was formed within 10 min, with a λmax of 376 nm and constant color intensity for 24 h. We confirmed and characterized the formed complex using FTIR, ESR, 1HNMR, thermal analysis, magnetic susceptibility, and powder X-ray.\u0000\u0000\u0000\u0000This approach is notable for its precision, accuracy, rapidity, cost-effectiveness, and applicability in tablet form. The novel propylthiouracil: Ru(III) complex offers several advantages, including stability, low absorbance, and no interference with water-soluble ions, eliminating the need for an organic solvent to extract the reaction product. Therefore, this approach could be recommended for quality control in the pharmaceutical industry.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-05-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49559722","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pitfalls and Opportunities in the Execution of Quality by Design in Analytical\u0000Sciences","authors":"S. Chopra, Prashant K. Chaturvedi, Kalyani H. Joshi, S. Tauro, Pintu B. Prajapati","doi":"10.2174/1573412919666230517141015","DOIUrl":"https://doi.org/10.2174/1573412919666230517141015","url":null,"abstract":"\u0000\u0000Quality by Design (QbD) is a systematic approach integrated with quality risk management.\u0000It uses different design approaches followed by statistical analysis to yield a quality\u0000product. Now, the pharmaceutical industries are intrested in the application of QbD principles to\u0000analytical methods and term it as Analytical QbD (AQbD), which does not essentially mean less\u0000analytical testing; to a particular extent, it means the right analysis at the right time, supported by\u0000science and risk evaluation which ensures that the analytical method can be improved throughout\u0000its life cycle. However, for that, the analyst must have sound knowledge of Analytical Target Profile\u0000(ATP), method performance characteristics, risk assessment, choice of Design of Experiment\u0000(DoE), optimization of Method Operable Design Region (MODR). Some papers have cited the\u0000importance, regulatory flexibility, theoretical aspects, and statistical analysis of AQbD, but only a\u0000few discuss the core issue of gradual implementation of QbD in analytical sciences. For seamless\u0000transition, researchers need clarification on AQbD terminologies, acceptable methods, criteria to\u0000embrace critical quality attributes (CQAs), and standards to judge the adequacy of controls. This\u0000paper summarizes the challenges and solutions for the implementation of AQbD.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44426209","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Review on Determination of Berberine in Biological and Pharmaceutical Matrices: An Analytical and Therapeutic Perspective","authors":"Umang Shah, Meghana Patel, Alkesh Patel, K. Patel, Mehul Patel, A. Akabari, Samir G Patel, Veena S Patel, R. Maheshwari, A. Sen, N. Sethiya","doi":"10.2174/1573412919666230505095457","DOIUrl":"https://doi.org/10.2174/1573412919666230505095457","url":null,"abstract":"\u0000\u0000Berberine (BRB) is a natural alkaloid of the isoquinoline class, mostly isolated from the Berberis genus, which exhibits antibiotic, immunostimulant, antitumor, cardiovascular protection, endocrine regulator, antidepressant, neuroprotective, antioxidant, anti-inflammatory, and other pharmacological properties. The poor aqueous solubility of BRB is one roadblock in scaling up activities for the clinical drug. However, this can be overcome by its chemical modification into salt form. Extraction of this biologically beneficial component becomes one of the important aspects, and for that, several extraction techniques are available using a variety of solvents. Numerous analytical methods are reported for the quantification of extracted BRB as well as simultaneous estimation of BRB in the presence of other components. Among them, RP-HPLC, LC/MS, and UPLC/MS are the most frequently used methods. The effectiveness and preciseness of these advanced methods could be the reason for analysts’ preferred choice for analysis.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-05-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47068616","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Overview of Analytical Methods for the Identification and Quantification of Baclofen","authors":"João Augusto Oshiro-Junior, Milena Nogueira da Silva, João Victor Belo da Silva, Naara Felipe da Fonsêca, Ana Claudia Dantas Medeiros","doi":"10.2174/1573412919666230502124837","DOIUrl":"https://doi.org/10.2174/1573412919666230502124837","url":null,"abstract":"\u0000\u0000Baclofen is a potent antispasmodic agent, acting as an analgesic and central\u0000skeletal muscle relaxant. It is a GABA-B analog, and is widely used for the treatment of spasticity.\u0000Due to its therapeutic importance, various analytical techniques are used in the pharmaceutical industry and research to determine, identify, and characterize baclofen in bulk material, biological fluids,\u0000and pharmaceutical forms.\u0000\u0000\u0000\u0000This review aimed to collect information on reported analytical techniques commonly\u0000used to identify and quantify baclofen in pharmaceutical forms and biological samples.\u0000\u0000\u0000\u0000The authors explored various authenticated scientific journals using these descriptors: highperformance liquid chromatography, liquid chromatography-tandem mass spectrometry, capillary\u0000electrophoresis, differential scanning calorimetry, Fourier transform infrared spectroscopy, ultravioletvisible spectroscopy, near-infrared spectroscopy, nuclear magnetic resonance, potentiometry, and Xray diffraction.\u0000\u0000\u0000\u0000Quantification of the drug by all the methods evaluated in the review was possible. There\u0000were 73 articles reviewed, of which 26 used HPLC for baclofen quantification; the least used was near\u0000infrared spectroscopy and potentiometry, both with one article identified.\u0000\u0000\u0000\u0000This review has shed light on a wide variety of analytical methods that can be used to\u0000quantify and identify baclofen. The knowledge provided by the use of these analytical methods makes\u0000this document an important tool for developing pharmaceutical formulations containing baclofen.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45314297","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Experimental and Theoretical Study of Biosurfactants Functionalized Gold Nanoparticles for Mixture Detection and Chiral Recognition of Tryptophan by UV-Vis Spectroscopy","authors":"Lu Huang, Xiangzong Wu, Yanxia Li, Yiting Chen, Zhenli Qiu","doi":"10.2174/1573412919666230427110327","DOIUrl":"https://doi.org/10.2174/1573412919666230427110327","url":null,"abstract":"\u0000\u0000Tryptophan (Trp) is an essential amino acid and plays important roles in biological processes. The detection of Trp is very important for its biological and chemical study. Moreover, Trp is a chiral compound; due to its importance in biological processes, researchers have been\u0000long committed to the chiral recognition and sensing of Trp enantiomers.\u0000\u0000\u0000\u0000Two biosurfactants, sodium cholate and sodium deoxycholate, were used for the preparation of functionalized gold nanoparticles (AuNPs) which were characterized by transmission electron\u0000microscope and potentiometer. UV-Vis spectra of functionalized gold nanoparticle solutions with different concentrations of Trp, tyrosine, phenylalanine, D-Trp, and L-Trp were analyzed. Then, the discrimination mechanism was further investigated, and the promotion mechanism of biosurfactants was\u0000studied by density functional theory (DFT).\u0000\u0000\u0000\u0000Trp could induce the aggregation of unmodified AuNPs in 2 h, while phenylalanine and tyrosine could not. Adding biosurfactants promoted the aggregation process, and D- Trp rather than LTrp was found to be responsible for the aggregation. Therefore, there were interaction differences not\u0000only between Trp, phenylalanine, and tyrosine but also between Trp enantiomers.\u0000\u0000\u0000\u0000UV-vis spectroscopy could be applied for the direct detection of Trp in mixtures as well\u0000as the chiral recognition of Trp enantiomers. DFT calculations proved that the interactions of D-Trp\u0000with biosurfactants were the strongest, which contributes to the promotion of aggregation.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-04-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47131843","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The development and validation of simultaneous quantitative analysis reversed-phase high-performance liquid chromatography for sitagliptin phosphate monohydrate and dapagliflozin propanediol monohydrate fixed-dose combination dual-layered tablet","authors":"Joo-Eun Kim, So-Jin Kang","doi":"10.2174/1573412919666230417081123","DOIUrl":"https://doi.org/10.2174/1573412919666230417081123","url":null,"abstract":"\u0000\u0000Sitagliptin phosphate monohydrate-dapagliflozin propanediol hydrate fixeddose combination (FDC) dual-layered tablet is used for type 2 diabetes treatment. Simultaneous quantitative analysis can shorten the analysis time of sitagliptin phosphate monohydrate-dapagliflozin propanediol monohydrate FDC dual-layered tablets and increase their efficiency.\u0000\u0000\u0000\u0000This study aimed to develop the simultaneous quantitative analysis for sitagliptin phosphate\u0000monohydrate-dapagliflozin propanediol monohydrate FDC dual-layered tablet, a type 2 diabetes treatment.\u0000\u0000\u0000\u0000Simultaneous quantitative analysis using the rapid and selective reversed-phase highperformance liquid chromatography (RP-HPLC) method was developed and validated using method\u0000validation. RP-HPLC analysis was conducted using an ultraviolent absorption spectrophotometer and\u0000a Zorbax C18 column (4.6 x 150 mm, 5 µm). The flow rate and injection volume were set to 1.5 mL\u0000min-1 and 20 µL, respectively. The wavelength was set at 205 nm.\u0000\u0000\u0000\u0000The retention times of sitagliptin phosphate monohydrate and dapagliflozin propanediol\u0000monohydrate were 2.28 mins and 10.65 mins, respectively. The relative standard deviations of the\u0000system suitability for validation of simultaneous quantitative analysis were 0.03% for sitagliptin phosphate monohydrate and dapagliflozin propanediol monohydrate. The chromatogram confirmed that\u0000there was no peak interference between the two main components and between the main component\u0000and the excipients. In addition, It revealed a favorable linearity with correlation coefficients of 0.9999\u0000in the concentration range of 20–120% compared to the standard solution.\u0000\u0000\u0000\u0000The developed simultaneous quantitative analysis shortened the analysis time and high\u0000efficiency of the sitagliptin phosphate monohydrate-dapagliflozin propanediol monohydrate FDC bilayer tablet. The validity of the analytical method was verified through accuracy and precision, detection and quantitation limits, and solution stability tests. In addition, it was thought that it would be\u0000helpful in developing an analytical method by referring to the simultaneous quantitative analysis\u0000method for developing other FDC dual-layered tablets.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43203505","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Survey on Multi-omics, and Multi-omics Data Analysis, Integration and Application","authors":"","doi":"10.2174/1573412919666230406100948","DOIUrl":"https://doi.org/10.2174/1573412919666230406100948","url":null,"abstract":"\u0000\u0000Multi-omics approaches have developed as a profitable technique for plant systems, a\u0000popular method in medical and biological sciences underlining the necessity to outline new integrative technology and functions to facilitate the multi-scale depiction of biological systems. Understanding a biological system through various omics layers reveals supplementary sources of\u0000variability and probably inferring the sequence of cases leading to a definitive process. Manuscripts and reviews were searched on PubMed with the keywords of multi-omics, data analysis,\u0000omics, data analysis, data integration, deep learning multi-omics, and multi-omics integration. Articles that were published after 2010 were prioritized. The authors focused mainly on popular\u0000publications developing new approaches. Omics reveal interesting tools to produce behavioral\u0000and interactions data in microbial communities, and integrating omics details into microbial risk\u0000assessment will have an impact on food safety, and also on relevant spoilage control procedures.\u0000Omics datasets, comprehensively characterizing biological cases at a molecular level, are continually increasing in both dimensionality and complexity. Multi-omics data analysis is appropriate\u0000for treatment optimization, molecular testing and disease prognosis, and to achieve mechanistic\u0000understandings of diseases. New effective solutions for multi-omics data analysis together with\u0000well-designed components are recommended for many trials. The goal of this mini-review article\u0000is to introduce multi-omics technologies considering different multi-omics analyses.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47709311","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Validation of the T–47D Cell Culture Bioassay for the Potency Assessment of Botulinum Neurotoxin Type A","authors":"S. Dalmora, Bruna Xavier, Rafaela Ferreira Perobelli Dumoncel, Clóvis Dervil Appratto Cardoso Jr, F. S. da Silva","doi":"10.2174/1573412919666230320155755","DOIUrl":"https://doi.org/10.2174/1573412919666230320155755","url":null,"abstract":"\u0000\u0000Botulinum neurotoxins (BoNTs) are among the most potent toxins known and are also used for therapeutic and aesthetic applications.\u0000\u0000\u0000\u0000An alternative in vitro cell culture bioassay based on the induction of apoptosis on T−47D breast cancer cells, after exposure to BoNTA, was developed and validated.\u0000\u0000\u0000\u0000The T-47D cells (ATCC HTB−133) were seeded at a density of 3 × 105 cells mL−1, and the bioassay was performed with doses of BoNTA, between 3 and 81 U mL−1. The responses were assessed using 10 µL of Alamar Blue®. The absorbances were read at 570 and 600 nm.\u0000\u0000\u0000\u0000The results were compared with those of the in vivo LD50 mouse bioassay, showing a non-significant 1.08% higher, mean difference of the estimated potencies (p>0.05). Besides, the biopharmaceutics is analyzed by the size exclusion and reversed-phase liquid chromatography methods, showing a significant correlation with values 1.15% higher and 0.85% lower, respectively, related to the cell culture bioassay.\u0000\u0000\u0000\u0000It is concluded that the validated T−47D cell culture assay represents an advancement toward the establishment of an alternative approach for the potency assessment, in the context of the 3 Rs. Besides, the employment of chromatographic methods in conjunction with the bioassays contributes to assessing the quality attributes of the biopharmaceutical formulations of BoNTA.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-03-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47917653","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Stability Study and Simultaneous determination of Norepinephrine, Moxifloxacin, and Piperacillin + Tazobactam Mixtures applied in Intensive Care Medicine","authors":"J. Schmidt, M. Steppe","doi":"10.2174/1573412919666230315151351","DOIUrl":"https://doi.org/10.2174/1573412919666230315151351","url":null,"abstract":"\u0000\u0000In intensive care units intravenous medicine may be used in simultaneous infusion in the same intravenous site. Sometimes, the physical compatibility and stability of the combined solutions are unknown.\u0000\u0000\u0000\u0000The objective was to develop, optimize and validate a simple, fast and sensitive stability-indicating high-performance liquid chromatography (HPLC) for simultaneous quantification of binary mixtures of norepinephrine, piperacillin + tazobactam, moxifloxacin for intravenous (IV) administration in different diluents and physical compatibility with mannitol.\u0000\u0000\u0000\u0000The HPLC method was performed on a C18LUNA (4.6x250 mm 5-Micron) column, using acetonitrile: methanol: phosphate buffer pH 3.0 (20:30:50) as eluent and validated according to ICH guidelines and applied to mixtures of norepinephrine, moxifloxacin, piperacillin, tazobactam and mannitol at 0, 2, 6, 9 and 24 h. The substances and their mixtures were also evaluated by visual inspection and pH over time.\u0000\u0000\u0000\u0000The analytical method developed was specific, linear, precise, accurate and robust. No visual changes were observed in the mixtures over time, maintaining the pH values (except for piperacillin + tazobactam which changed 0.5 in 24 h) and losses of less than 10% of content over the 24 h under analyzed conditions.\u0000\u0000\u0000\u0000The proposed method is suitable for simultaneous analysis of norepinephrine, moxifloxacin, piperacillin and tazobactam. All tested mixtures were compatible and stable for up to 24 h, which is an important result for increasing patient safety in clinical practice since it has not been reported in the literature yet. The method can be further investigated and used for different concentration and diluent combinations.\u0000\u0000\u0000\u0000Conclusion: The proposed method is suitable for simultaneous analysis of norepinephrine, moxifloxacin, piperacillin and tazobactam. All tested mixtures were compatible and stable for up to 24 h, which is an important result for increase patient safety in clinical practice, since it has not been reported in literature yet. The method can be further investigated and used for different concentration and diluents combinations.\u0000\u0000\u0000\u0000HPLC\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48854962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigation of the Pharmacokinetic Properties and Theoretical Chemical Activities of 7,8-Dihydroxyflavone and 4'-Dimethylamino-7,8-Dihydroxyflavone","authors":"O. Korkmaz, M. F. Karakaya, Faik Gokalp, E. Şener","doi":"10.2174/1573412919666230313143549","DOIUrl":"https://doi.org/10.2174/1573412919666230313143549","url":null,"abstract":"\u0000\u0000Flavonoids naturally exist in plants as secondary metabolites. In this study, the aim is to determine and compare the theoretical and in vivo chemical activities of 7,8-dihydroxyflavone (7,8-DHF) and 4'dimethylamino-7,8-dihydroxyflavone (4’-DMA-7,8-DHF), tyrosine receptor kinase B (TrkB) receptor agonist flavonoid molecules with reported potent neuroprotective effects.\u0000\u0000\u0000\u0000BDNF has been thought to be a potent therapeutic agent against neurological disorders via its receptor TrkB. However, BDNF has poor pharmacokinetic properties and cannot cross the blood-brain barrier. It has been demonstrated that 7,8-DHF and 4''-DMA-7,8-DHF can bind and activate TrkB receptors and pass the blood-brain barrier. It has been thought that 4''-DMA-7,8-DHF may be more potent than 7,8-DHF due to strong TrkB activity and supporting neurogenesis at lower concentrations. However, there is no detailed study on this yet.\u0000\u0000\u0000\u0000method was used for the theoretical chemical analysis. For the in vivo studies, 6-month-old Wistar rats were used in two groups (n=8). 7,8-DHF and 4’-DMA-7,8-DHF (5 mg/kg) were administered intraperitoneally (ip) to each group. Then, plasma samples were collected by carotid catheterization, and brain samples by the microdialysis technique were collected simultaneously for 12 h from awake rats. The level of 7,8-DHF and 4’-DMA-7,8-DHF in blood and brain samples were analyzed and their pharmacokinetics were determined.\u0000\u0000\u0000\u0000Flavonoids naturally exist in plants as seconder metabolites. In this study, the aim is to determine and compare the theoretical and in vivo chemical activities of 7,8-DHF and 4’-DMA-7,8-DHF, tyrosine receptor kinase B (TrkB) receptor agonist flavonoid molecules with reported potent neuroprotective effects.\u0000\u0000\u0000\u0000Theoretical calculations show that 7,8-DHF is slightly more stable than 4’-DMA-7,8-DHF. The in vivo pharmacokinetic results show that the maximum concentration of 7,8-DHF was about 48 ng/mL, whereas it was only 8 ng/mL for 4’-DMA-7,8-DHF.\u0000\u0000\u0000\u0000Our results suggest that the 4'-DMA-7,8-DHF is more unstable and is more prone to binding to TrkB than 7,8-DHF. On the other hand, the in vivo pharmacokinetic results show that 7,8-DHF is more stable than 4’-DMA-7,8-DHF when it is applied systemically at therapeutic concentrations.\u0000\u0000\u0000\u0000Theoretical calculations show that 7,8-DHF is slightly more stable than 4’-DMA-7,8-DHF. The in vivo pharmacokinetic results show that the maximum concentration of 7,8-DHF was about 48 ng/mL, whereas it was only 8 ng/mL for 4’-DMA-7,8-DHF.\u0000\u0000\u0000\u00007.8-DHF seems more suitable for pharmacological applications.\u0000","PeriodicalId":10889,"journal":{"name":"Current Pharmaceutical Analysis","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47503732","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}