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Biological Potential and Pharmacological Activity of Columbianetin in Chronic Diseases. 哥伦布黄酮素在慢性疾病中的生物潜力和药理活性
Drug metabolism and bioanalysis letters Pub Date : 2023-01-24 DOI: 10.2174/1872312815666230124154630
Dinesh Kumar Patel, Kanika Patel
{"title":"Biological Potential and Pharmacological Activity of Columbianetin in Chronic Diseases.","authors":"Dinesh Kumar Patel, Kanika Patel","doi":"10.2174/1872312815666230124154630","DOIUrl":"10.2174/1872312815666230124154630","url":null,"abstract":"<p><strong>Background: </strong>Herbal medicine is widely used in different systems of traditional and complementary medicine including. People believe that herbal medicines are safe and more cost-effective than other synthetic medicines. Herbal medicines are also used as a promising source of new drug discovery molecules in modern medicines. Coumarins are polyphenols class phytochemical that naturally occurs in higher plants and are used in medicine for the treatment of human disorders and associated secondary complications. Columbianetin is a coumarin class phytochemical found in Angelica archangelica L.</p><p><strong>Methods: </strong>The aim of the present work is to review the medicinal importance and pharmacological activities of columbianetin and to provide a summary of the medicinal importance and pharmacological activities of columbianetin in medicine. Further scientific progress of columbianetin in the fields of Ethnopharmacology, Phytochemistry and Pharmacology has been analyzed and discussed in the present work. However, possible future research on columbianetin has been also discussed in the present work. Scientific information on columbianetin was collected from PubMed, Elsevier, Google, Google Scholar, and Europe PMC using herbal medicine, columbianetin and coumarin as important keywords. Other published books and journal data have also been included in the present work to know the therapeutic potential of columbianetin in medicine.</p><p><strong>Results: </strong>Scientific data analysis of columbianetin signified the biological importance of phytochemicals belonging to the coumarins. Biological effectiveness of coumarins for their antioxidative, cytotoxic, and anti-inflammatory potential has been discussed in the research fields. Columbianetin has analgesic, antioxidative, anti-inflammatory, anti-proliferative, and anti-allergic activities in medicine. However, its biological effectiveness on neuroprotection, keratinocyte damage and platelet aggregation has also been discussed in the present work. Further tissue distribution of columbianetin in different biological tissue has been estimated through different analytical methods and scientific data are also presented in the present work.</p><p><strong>Conclusion: </strong>The present work summarized the biological importance and pharmacological activities of columbianetin in medicine. Analytical methods developed for the quantitative and qualitative estimation of columbianetin have also been reviewed.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10643934","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}
引用次数: 0
A Novel Spectrophotometric Method Development for Quantification of Desidustat in Bulk and Pharmaceutical Dosage Form. 一种新的分光光度法定量散装和药用剂型中杀菌素的研究。
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230828150206
Sanjay Sharma, Sunidhi Jain
{"title":"A Novel Spectrophotometric Method Development for Quantification of Desidustat in Bulk and Pharmaceutical Dosage Form.","authors":"Sanjay Sharma, Sunidhi Jain","doi":"10.2174/2949681016666230828150206","DOIUrl":"10.2174/2949681016666230828150206","url":null,"abstract":"<p><strong>Background: </strong>Desidustat (DES) belongs to a new category of drugs, i.e., Hypoxia-Inducible Factor (HIF) propyl hydroxylase inhibitor, and is used for the treatment of anemia in chronic kidney disease. However, no method has yet been reported in the literature for the estimation of drugs.</p><p><strong>Objective: </strong>The objective of the study is to develop a simple, precise, and accurate method for determining DES in bulk and pharmaceutical dose form.</p><p><strong>Methods: </strong>The physicochemical characterization of the drug was performed using methanol as a solvent to establish the identity. According to ICH Q2 criteria, validation characteristics, such as specificity, linearity, accuracy, precision, limits of detection and quantification, and robustness, were assessed.</p><p><strong>Results: </strong>Maximum absorbance wavelength was observed at 229 nm. The sample solution remained stable for up to 12 hours. The linear response from 2 to 12 μg/ml of DES was y = 0.1087x + 0.0962 and r2 = 0.9963. The accuracy was between 100 to 101%. Precision was recorded under three criteria: repeatability, intraday and interday, for which results fell within the acceptable ranges (<2%). The limit of detection (LOD) and limit of quantification (LOQ) of the technique were 0.434 μg/ml and 1.316 μg/ml, respectively.</p><p><strong>Conclusion: </strong>The proposed method was found to be beneficial for drug monitoring and the ongoing analysis of DES in research and quality control laboratories. This approach is simple, precise, rapid, economical, and sensitive.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"133-139"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10467209","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}
引用次数: 0
Stimulatory and Inhibitory Effects of Steroid Hormones and Human Cytochrome P450 (CYP) 3A Inhibitors on Cortisol 6β-Hydroxylation Catalyzed by CYP3A Subfamilies. 类固醇激素和人细胞色素P450 (CYP) 3A抑制剂对CYP3A亚家族催化的皮质醇6β-羟基化的刺激和抑制作用
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230830125358
Toshiro Niwa, Misaki Tani, Anna Suzuki, Mizuho Murakami
{"title":"Stimulatory and Inhibitory Effects of Steroid Hormones and Human Cytochrome P450 (CYP) 3A Inhibitors on Cortisol 6β-Hydroxylation Catalyzed by CYP3A Subfamilies.","authors":"Toshiro Niwa, Misaki Tani, Anna Suzuki, Mizuho Murakami","doi":"10.2174/2949681016666230830125358","DOIUrl":"10.2174/2949681016666230830125358","url":null,"abstract":"<p><strong>Objective: </strong>The inhibitory and stimulatory effects of several compounds, including steroid hormones and azole antifungal agents, on cortisol 6β-hydroxylation activity by cytochrome P450 (CYP) 3A4, polymorphically expressed CYP3A5, and fetal CYP3A7 were compared with those on testosterone 6β-hydroxylation to clarify the catalytic properties of the predominant forms of the human CYP3A subfamily.</p><p><strong>Methods: </strong>6β-Hydroxylation activities of cortisol and testosterone by CYP3A4, CYP3A5, and CYP3A7 in the absence or presence of dehydroepiandrosterone (DHEA), α-naphthoflavone (ANF), ketoconazole, itraconazole, and voriconazole were measured using high-performance liquid chromatography.</p><p><strong>Results: </strong>Lower concentrations of DHEA and ANF increased cortisol 6β-hydroxylation activities catalyzed by CYP3A4 but not those catalyzed by CYP3A5 and CYP3A7. The inhibition strength of azole antifungal agents against cortisol 6β-hydroxylation catalyzed by all CYP3A subfamilies was similar to that of testosterone 6β-hydroxylation. Although the Michaelis constant (<i>K<sub>m</sub></i>) increased 2-fold in the presence of 20 μM DHEA compared to that of the control, the maximal velocity (<i>V<sub>max</sub></i>) values gradually increased with increasing DHEA. For ANF, both <i>K<sub>m</sub></i> and <i>V<sub>max</sub></i> values increased, although the <i>K<sub>m</sub></i> value decreased at 2.5 μM concentrations. Ketoconazole and itraconazole competitively inhibited cortisol 6β-hydroxylation mediated by CYP3A4 with similar inhibition constants.</p><p><strong>Conclusion: </strong>The inhibitory/stimulatory pattern among CYP3A subfamily members differed between cortisol and testosterone, and CYP3A4 was found to be the most sensitive in terms of inhibition by azole antifungals among the CYP3A subfamily members investigated.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"73-80"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10121314","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}
引用次数: 0
A Promising Approach of Dermal Targeting of Antipsoriatic Drugs via Engineered Nanocarriers Drug Delivery Systems for Tackling Psoriasis. 通过工程纳米载体给药系统治疗银屑病的抗银屑病药物的皮肤靶向治疗方法。
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230803150329
Devika Tripathi, Mansi Srivastava, Krislay Rathour, Awani Kumar Rai, Pranay Wal, Jagannath Sahoo, Ritesh Kumar Tiwari, Prashant Pandey
{"title":"A Promising Approach of Dermal Targeting of Antipsoriatic Drugs <i>via</i> Engineered Nanocarriers Drug Delivery Systems for Tackling Psoriasis.","authors":"Devika Tripathi, Mansi Srivastava, Krislay Rathour, Awani Kumar Rai, Pranay Wal, Jagannath Sahoo, Ritesh Kumar Tiwari, Prashant Pandey","doi":"10.2174/2949681016666230803150329","DOIUrl":"10.2174/2949681016666230803150329","url":null,"abstract":"<p><p>Psoriasis is a complex autoimmune skin condition with a significant genetic component. It causes skin inflammation and is characterized by flaky, silvery reddish spots that can worsen with age. This condition results from an impaired immunological response of T-cells and affects 2-5% of the global population. The severity of the illness determines the choice of treatment. Topical treatments are commonly used to treat psoriasis, but they can have several adverse effects. Biological therapy is another option for treating specific types of psoriasis. Recently, new nanoformulations have revolutionized psoriasis treatment. Various nanocarriers, such as liposomes, nanostructured lipid nanoparticles, niosomes, and nanoemulsions, have been developed and improved for drug delivery. The use of nanocarriers enhances patient compliance, precise drug delivery, and drug safety. This review aims to suggest new nanocarrier-based drug delivery systems for treating psoriasis. It discusses the importance of nanocarriers and compares them to traditional treatments. Anti-psoriatic drugs have also been investigated for cutaneous delivery using nanocarriers. The review also covers various factors that influence dermal targeting. By highlighting several relevant aspects of psoriasis treatment, the review emphasizes the current potential of nanotechnology. Using nanocarriers as a drug delivery technique may be a promising alternative treatment for psoriasis.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"89-104"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10302454","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}
引用次数: 0
Comparison of Ussing Chamber and Caco-2 Model in Evaluation of Intestinal Absorption Mechanism of Compounds from Different BCS Classifications. 不同BCS分类化合物肠道吸收机制评价的实验与Caco-2模型比较
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230913105920
Dong Tian, Yingxin Yang, Huiying Zhang, Hongwen Du, Hongyu Zhou, Tao Wang
{"title":"Comparison of Ussing Chamber and Caco-2 Model in Evaluation of Intestinal Absorption Mechanism of Compounds from Different BCS Classifications.","authors":"Dong Tian, Yingxin Yang, Huiying Zhang, Hongwen Du, Hongyu Zhou, Tao Wang","doi":"10.2174/2949681016666230913105920","DOIUrl":"10.2174/2949681016666230913105920","url":null,"abstract":"<p><strong>Background: </strong>Oral bioavailability (F), which is evaluated by permeability and solubility, is one of the key parameters in drug discovery. Currently, Caco-2 and Ussing chamber are both used in the study of intestinal permeability of drugs at different stages of drug development. However, comparative research between the Ussing chamber and Caco-2 for predicting the intestinal availability data (<i>F<sub>a</sub>×F<sub>g</sub></i>) in humans has not been reported.</p><p><strong>Methods: </strong>In the present study, we evaluated the permeability of 22 drugs in rat intestines by Ussing chamber and compared them with the reported permeability data from Caco-2. In addition, the active transport of gabapentin was evaluated by Ussing Chamber.</p><p><strong>Results: </strong>Intestine segments were selected by corresponding absorption site for Ussing chamber analysis. BCS Class I and II compounds were more absorbed in the duodenum and jejunum, and Class III and IV compounds were more absorbed in the ileum. P<sub>app</sub> values in the Caco-2 model were moderately correlated with human <i>F<sub>a</sub>×F<sub>g</sub></i> (<i>R<sup>2</sup></i>=0.722), and the P<sub>app</sub> of the rat in the Ussing chamber revealed a better correlation with human <i>F<sub>a</sub>×F<sub>g</sub></i> (<i>R<sup>2</sup></i>=0.952). In addition, we also used the Ussing chamber to identify the transporter of gabapentin, and the results showed that the active absorption of gabapentin was related to LAT1.</p><p><strong>Conclusion: </strong>Ussing chamber combined with rat intestinal tissue would be a significant tool for predicting the intestinal absorption and metabolism of compounds with diverse physiochemical characteristics.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"105-112"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10241753","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}
引用次数: 0
Therapeutic Importance and Pharmacological Activities of Norisoboldine in Medicine for the Treatment of Human Disorders. 诺里斯波尔丁在人类疾病治疗中的重要性和药理活性。
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230914103740
Dinesh Kumar Patel, Kanika Patel
{"title":"Therapeutic Importance and Pharmacological Activities of Norisoboldine in Medicine for the Treatment of Human Disorders.","authors":"Dinesh Kumar Patel, Kanika Patel","doi":"10.2174/2949681016666230914103740","DOIUrl":"10.2174/2949681016666230914103740","url":null,"abstract":"<p><strong>Background: </strong>Natural products constitute a unique source of chemical compounds with multi-target potential for the treatment of complex human disorders. Phytochemicals are pure phytoconstituents of plants, mainly responsible for their therapeutic potential and pharmacological activities. Natural products isolated from medicinal plants have been used as a lead source of drug. Norisoboldine is an important isoquinoline alkaloid found to be present in the dry root of <i>Lindera aggregate</i>.</p><p><strong>Methods: </strong>In the present paper, scientific data of norisoboldine have been collected from Google, Google Scholar, PubMed, Science Direct and Scopus and analyzed in order to know the biological potential and therapeutic effectiveness of norisoboldine in medicine. Scientific data of medicinal importance and therapeutic potential of norisoboldine has been collected and analyzed in the present work. Moreover, all the collected scientific data have been separated into different sub-section <i>i.e.</i> Medicinal importance, pharmacological activities and analytical aspects. Detailed pharmacological activity data of norisoboldine have been analyzed in the present work to know the therapeutic effectiveness of norisoboldine in medicine. Analytical data of norisoboldine have also been collected and analyzed in the present work.</p><p><strong>Results: </strong>Scientific data analysis revealed the biological importance of isoquinoline alkaloids in medicine. Isoquinoline alkaloids are pure, active phytochemical present in several natural edible products including vegetables, plants, and fruits. Norisoboldine has a biological effect on arthritis, colitis, apoptosis, osteoclast differentiation, inflammatory pain, renal ischemia-reperfusion injury, acute lung injury, pro-inflammatory cytokines, tumor, regulatory T cells, and endothelial cell migration. However nanoemulsifying drug delivery system of norisoboldine has also been prepared in order to get better therapeutic value. Further analytical parameters of norisoboldine were also discussed in the present work in order to get the scientific information of separation, isolation and identification parameter of norisoboldine.</p><p><strong>Conclusion: </strong>Present work revealed the therapeutic potential of norisoboldine in medicine.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"81-88"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10234816","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}
引用次数: 0
Effect of Saccharolactone on CYP-mediated Metabolism of Xenobiotics. 糖内酯对cyp介导的外源性代谢的影响。
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230823094423
Dayanidhi Behera, Pankaj Jain, Vishwanath Kurawattimath, Nagaraj Gowda
{"title":"Effect of Saccharolactone on CYP-mediated Metabolism of Xenobiotics.","authors":"Dayanidhi Behera, Pankaj Jain, Vishwanath Kurawattimath, Nagaraj Gowda","doi":"10.2174/2949681016666230823094423","DOIUrl":"10.2174/2949681016666230823094423","url":null,"abstract":"<p><strong>Background: </strong>Saccharolactone is used as a β-glucuronidase inhibitor in in vitro microsomal and recombinant uridine diphosphoglucuronosyl transferases (rUGTs) incubations to enhance glucuronide pathway and, thereby, formation of glucuronide metabolites. We investigated its effect on CYP mediated metabolism of drugs (compound-174, phenacetin and quinidine) using human liver microsomes (HLM) supplemented with Phase-1 and Phase-2 co-factors.</p><p><strong>Methods: </strong>Compounds were incubated in HLM supplemented with co-factors to assess Phase-1 (NADPH) and Phase-2 (NADPH, alamethicin, saccharolactone and UDPGA) metabolism. CYP phenotype assay for compound-174 was conducted in HLM (± 1-ABT) and human recombinant CYP isoforms. CYP inhibition profile of saccharolactone was also generated in HLM.</p><p><strong>Results: </strong>The metabolism of compound-174, phenacetin and quinidine in HLM significantly decreased in reactions containing additional components like alamethicin, saccharolactone and UDPGA and indicated that the addition of saccharolactone inhibited the metabolism. Phenacetin and quinidine are known substrates of CYP1A2 and CYP3A4 isoforms. The metabolism of compound- 174 was significantly inhibited in the presence of 1-ABT in HLM, and CYP3A4 and CYP2C8 isoforms were found to be the predominant isoforms responsible for its metabolism. Further evaluation of CYP inhibition in HLM indicated saccharolactone to be a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms with IC<sub>50</sub> values of less than 4 mM.</p><p><strong>Conclusion: </strong>The findings indicated that saccharolactone being a strong inhibitor of CYP1A2, 2D6, 3A4 and 2C8 isoforms (IC<sub>50</sub> < 4 mM), resulted in significant inhibition of the metabolism of compound-174, phenacetin and quinidine in HLM and caution should be exercised in using it with proper titration of the concentrations.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"121-132"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10292482","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}
引用次数: 0
Analytical Method Development, Validation and Forced Degradation Study of Dapagliflozin by RP-HPLC. 达格列净的RP-HPLC分析方法建立、验证及强制降解研究。
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230823091112
Ujwal Chaudhari, Jagdish K Sahu, Payal R Dande
{"title":"Analytical Method Development, Validation and Forced Degradation Study of Dapagliflozin by RP-HPLC.","authors":"Ujwal Chaudhari, Jagdish K Sahu, Payal R Dande","doi":"10.2174/2949681016666230823091112","DOIUrl":"10.2174/2949681016666230823091112","url":null,"abstract":"<p><strong>Background: </strong>Worldwide, it is projected that 285 million individuals have diabetes, and by 2030, this number is expected to climb to 438 million. About 90% of cases of diabetes mellitus are type 2 (T2DM). Insulin sensitizers, such as metformin and thiazolidinediones; insulin secretagogues, such as sulfonylureas and glinides; dipeptidyl peptidase 4 (DPP-4) inhibitors; glucosidase inhibitors, or oral combination therapy are currently available treatments for type 2 diabetes. Some of these drugs exhibit serious limitations; thus, it is crucial to design an innovative therapy that is efficient and depends on a new channel.</p><p><strong>Aim: </strong>In the current work, a stability-indicating reverse phase HPLC (RP-HPLC) technique was developed and subsequently validated for the detection of dapagliflozin in its API.</p><p><strong>Methods: </strong>The stability-indicating HPLC method for assay included the use of Kromasil 100-5-C8 (100 mm × 4.6 mm) column, UV detector 224 nm, mobile phase composition involving a mixture of acetonitrile:water (52:48), and a flow rate of 1.0 mL/min. ICH guidelines were followed for the method's validation. To assess the method's specificity and stability in showing characteristics, stress degradation studies were carried out. The working standard solution of dapagliflozin was exposed to 1 and 2 N HCl by refluxing 1 and 2 N NaOH with 30% hydrogen peroxide by volume and UV radiation in order to conduct a degradation study.</p><p><strong>Results: </strong>All system suitability parameters were determined to be within the intended ranges, and the drug's retention duration was discovered to be 1.67 minutes. It was also investigated as to how the drug degraded under various circumstances. The drug was discovered to be stable under situations of photolytic, thermal, neutral, alkaline, and oxidative deterioration. The developed stabilityindicating HPLC technique was validated in accordance with ICH Q2 recommendations, and the validation parameters, such as linearity, precision, and robustness, were achieved within the approved standards.</p><p><strong>Conclusion: </strong>It may be concluded that this method is stability-indicating and specific, and it can be successfully applied to analyze tablet dosage forms containing dapagliflozin.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"140-152"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10414936","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}
引用次数: 0
A Simplified Method for Determining Blood-to-Plasma Ratios in vitro and ex vivo by Matrix Matching with Blank Blood or Plasma. 用空白血或血浆基质匹配法测定体外和离体血浆比的简化方法。
Drug metabolism and bioanalysis letters Pub Date : 2023-01-01 DOI: 10.2174/2949681016666230817150551
Xiaomei Zhang, Gary J Jenkins, Kelly E Desino, Jinrong Liu, Mary Larsen, David M Stresser
{"title":"A Simplified Method for Determining Blood-to-Plasma Ratios <i>in vitro</i> and <i>ex vivo</i> by Matrix Matching with Blank Blood or Plasma.","authors":"Xiaomei Zhang, Gary J Jenkins, Kelly E Desino, Jinrong Liu, Mary Larsen, David M Stresser","doi":"10.2174/2949681016666230817150551","DOIUrl":"10.2174/2949681016666230817150551","url":null,"abstract":"<p><strong>Objective: </strong>This work describes a simplified, 96-well plate method for determining the blood-to-plasma concentration ratio (BP ratio) for small molecules.</p><p><strong>Methods: </strong>The need for calibration curves was eliminated using a matrix-matching approach in which blood samples were mixed with blank plasma and plasma samples were mixed with blank blood. As a result, both blood- and plasma-origin samples shared an equivalent matrix ahead of bioanalysis. In the <i>in vitro</i> assay, identical sample matrices were achieved by using the same source of blank plasma and blood.</p><p><strong>Results: </strong>In humans, a good correlation (R2 = 0.84) was observed between the data obtained in this matrix-matching method and literature values for 11 commercial compounds possessing a wide range of logD values across multiple chemical classes. In addition, this method showed good agreement with <i>in vitro</i> BP ratios for 10 proprietary compounds determined radiometrically (R2 = 0.72) in human and preclinical species. Finally, the <i>in vitro</i> matrix matching method compared favorably to BP ratios determined <i>ex vivo</i> for 13 proprietary and literature compounds (R2 = 0.87) in rat.</p><p><strong>Conclusion: </strong>This method, suitable for <i>in vitro</i> and <i>ex vivo</i> BP ratio determinations, is operationally efficient, robust, and a useful improvement upon previously published methods.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"113-120"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10078110","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}
引用次数: 0
CYP2D6 and CYP2C19 Genes Associated with Tricontinental and Latin American Ancestry of Pe-ruvians. CYP2D6 和 CYP2C19 基因与 Pe-ruvians 的三大陆和拉丁美洲血统有关。
Drug metabolism and bioanalysis letters Pub Date : 2022-12-13 DOI: 10.2174/1872312815666221213151140
Angel T Alvarado, María Saravia, Ricardo Losno, Ricardo Pariona, Ana María Muñoz, Roberto O Ybañez-Julca, Berta Loja, María R Bendezú, Jorge A García, Felipe Surco-Laos, Doris Laos-Anchante, Haydee Chávez, Priscilia Aguilar, Mario Pineda
{"title":"CYP2D6 and CYP2C19 Genes Associated with Tricontinental and Latin American Ancestry of Pe-ruvians.","authors":"Angel T Alvarado, María Saravia, Ricardo Losno, Ricardo Pariona, Ana María Muñoz, Roberto O Ybañez-Julca, Berta Loja, María R Bendezú, Jorge A García, Felipe Surco-Laos, Doris Laos-Anchante, Haydee Chávez, Priscilia Aguilar, Mario Pineda","doi":"10.2174/1872312815666221213151140","DOIUrl":"10.2174/1872312815666221213151140","url":null,"abstract":"<p><p>Precision medicine seeks to individualize the dose from the beginning of phar-macological therapy based on the characteristics of each patient, genes involved in the metabolic phenotype, ethnicity or miscegenation, with the purpose to minimize adverse effects and optimize drug efficacy. The objective was to re-view studies that describe the association of the CYP2D6 and CYP2C19 genes with the tricontinental and Latin American ancestry of Peruvians. A biblio-graphic search was carried out in PubMed/Medline and SciELO, with various descriptors in Spanish and English. The results of this review confirm that the ethnic origin of Peruvians is triconti-nental due to European (mainly Spanish), African and Asian migration, in addi-tion to Latin American migration, being 60.2% mixed, 25.8% Amerindian, 5.9% white, 3.6% African descent, 1.2% Chinese and Japanese descent, and 3.3% unspecified. Studies on CYP2C19*3, CYP2D6*2, *3 and *6 have been reported in Peruvians, and the frequency is similar to that studied in Ecuadori-ans and Colombians. The CYP2C19*3, CYP2D6*3, and CYP2D6*6 alleles found in Peruvians are common in Europeans, Africans, and Asians; while CYP2D6*4 in Africans and CYP2D6*2 related to Asians. In some studies, the ethnic/gene association has not been demonstrated; while others have shown a significant association, which is why further investigation is warranted. It is concluded that the studies on CYP2D6 and CYP2C19 genes associated with the tricontinental and Latin American ancestry of Peruvians are little, and ac-cording to what has been investigated, the CYP2C19*3, CYP2D6*2, *3, *4 and *6 alleles have more related to their ancestry.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-12-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10436705/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10043248","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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