Objective: Two highly sensitive, accurate, inexpensive, and simple spectrophotometric assays were developed and validated for the determination of an anti-fungal drug, Terbinafine HCl (TBH), in pure drug and tablets using potassium permanganate (PP) and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate (DSOQ). Material and Method: In the present study, Sebifin and Terbiforce 250 mg tablets were used as pharmaceuticals, potassium permanganate KMnO4 and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate in water were used as reagents, and DR 3900 spectrophotometer equipped with 1cm matched quartz cells was used for absorbance measurements. Result and Discussion: The amount of terbinafine hydrochloride reacting with permanganate and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate in an acidic medium has been determined. The colored reaction products in both cases were measured at the maximum absorptions of 540 nm and 440 nm, respectively. The absorbance measured in each assay as a function of TBH concentration was related to TBH concentrations. Different experimental and variable conditions of assays were done carefully, accurately studied, and optimized. The validation of two assays also was done by following the current guidelines of the International Conference on Harmonization (ICH). Beer’s law for the two methods is obeyed over the concentration ranges 1-15 µg/ml (Correlation coefficient = 0.9983) and 1-18 µg/ml (Correlation coefficient = 0.9989) for methods PP and DSOQ, respectively. Molar absorptivity, limits of detection, and quantification (LOD & LOQ) values were (1.38×104 l/ mol cm, 0.92 & 2.78 µg/ml) for PP assay, and (1.73×104 l/ mol cm, 0.09 & 0.27 µg/ml) for DSOQ assay, respectively. The two assays were successfully applied for the determination of TBH in commercial tablets with reliable and satisfactory results, and hence the proposed assays can be applied in pharmaceutical laboratories of quality control.
{"title":"SIMPLE AND SENSITIVE SPECTROPHOTOMETRIC ASSAYS FOR THE DETERMINATION OF TERBINAFINE HCL ANTIFUNGAL DRUG IN PHARMACEUTICALS","authors":"N. Qarah, Ezzouhra El-maaıden, K. Basavaiah","doi":"10.33483/jfpau.1348367","DOIUrl":"https://doi.org/10.33483/jfpau.1348367","url":null,"abstract":"Objective: Two highly sensitive, accurate, inexpensive, and simple spectrophotometric assays were developed and validated for the determination of an anti-fungal drug, Terbinafine HCl (TBH), in pure drug and tablets using potassium permanganate (PP) and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate (DSOQ).\u0000Material and Method: In the present study, Sebifin and Terbiforce 250 mg tablets were used as pharmaceuticals, potassium permanganate KMnO4 and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate in water were used as reagents, and DR 3900 spectrophotometer equipped with 1cm matched quartz cells was used for absorbance measurements.\u0000Result and Discussion: The amount of terbinafine hydrochloride reacting with permanganate and disodium 2-(1,3-dioxo-2,3-dihydro-1H-inden-2-yl)quinoline-6,8-disulfonate in an acidic medium has been determined. The colored reaction products in both cases were measured at the maximum absorptions of 540 nm and 440 nm, respectively. The absorbance measured in each assay as a function of TBH concentration was related to TBH concentrations. Different experimental and variable conditions of assays were done carefully, accurately studied, and optimized. The validation of two assays also was done by following the current guidelines of the International Conference on Harmonization (ICH). Beer’s law for the two methods is obeyed over the concentration ranges 1-15 µg/ml (Correlation coefficient = 0.9983) and 1-18 µg/ml (Correlation coefficient = 0.9989) for methods PP and DSOQ, respectively. Molar absorptivity, limits of detection, and quantification (LOD & LOQ) values were (1.38×104 l/ mol cm, 0.92 & 2.78 µg/ml) for PP assay, and (1.73×104 l/ mol cm, 0.09 & 0.27 µg/ml) for DSOQ assay, respectively. The two assays were successfully applied for the determination of TBH in commercial tablets with reliable and satisfactory results, and hence the proposed assays can be applied in pharmaceutical laboratories of quality control.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"48 9","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141650076","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}
Hendrawan Hm, Nur Khairi, Alfat Fadri, Wahyuddin Wahyuddin, A. Aisyah, A. Sapra, Maulita Indrisari, Lukman Lukman
Objective: Cultivation location and maturity levels could affect Muntingia calabura's bioactive compounds and biological activities. The present investigation evaluated two different maturity stages (young and ripened) of Indonesian M. calabura on their phytochemical constituents (total phenolic [TP] and total flavonoid [TF]), antioxidant activity, and nutrition composition. Material and Method: The TP and TF were measured using the Folin-Ciocalteau reagent and ammonium chloride (AlCl3). Antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS). Nutrition composition: total soluble solids (TSS) were determined by the gravimetric method; soluble sugars used anthrone-sulfuric acid colorimetric assays; and vitamin C established 2,6-dichloroindophenol (DCIP) titration. Result and Discussion: The ripened fruit presented the most potent antioxidant activity. DPPH and ABTS IC50 values were 28.38 ± 0.84 µg/ml and 29.92 ± 3.05 µg/ml, respectively. In contrast, the young fruit exhibited the highest TP (56.85 ± 1.08 mg/g GAE) and TF (8.45 ± 0.65 mg QE). Our findings additionally suggested that ripened fruit was a good source of nutrients, such as soluble sugar (SS; 12.34 ± 0.76%) and vitamin C (21.88 ± 2.73 mg/g).
{"title":"THE EFFECT OF MATURITY ON PHYTOCHEMICAL CONSTITUENT, ANTIOXIDANT ACTIVITY, AND NUTRIENT COMPOSITION OF MUNTINGIA CALABURA FRUITS CULTIVATED IN INDONESIA","authors":"Hendrawan Hm, Nur Khairi, Alfat Fadri, Wahyuddin Wahyuddin, A. Aisyah, A. Sapra, Maulita Indrisari, Lukman Lukman","doi":"10.33483/jfpau.1452000","DOIUrl":"https://doi.org/10.33483/jfpau.1452000","url":null,"abstract":"Objective: Cultivation location and maturity levels could affect Muntingia calabura's bioactive compounds and biological activities. The present investigation evaluated two different maturity stages (young and ripened) of Indonesian M. calabura on their phytochemical constituents (total phenolic [TP] and total flavonoid [TF]), antioxidant activity, and nutrition composition.\u0000Material and Method: The TP and TF were measured using the Folin-Ciocalteau reagent and ammonium chloride (AlCl3). Antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS). Nutrition composition: total soluble solids (TSS) were determined by the gravimetric method; soluble sugars used anthrone-sulfuric acid colorimetric assays; and vitamin C established 2,6-dichloroindophenol (DCIP) titration.\u0000Result and Discussion: The ripened fruit presented the most potent antioxidant activity. DPPH and ABTS IC50 values were 28.38 ± 0.84 µg/ml and 29.92 ± 3.05 µg/ml, respectively. In contrast, the young fruit exhibited the highest TP (56.85 ± 1.08 mg/g GAE) and TF (8.45 ± 0.65 mg QE). Our findings additionally suggested that ripened fruit was a good source of nutrients, such as soluble sugar (SS; 12.34 ± 0.76%) and vitamin C (21.88 ± 2.73 mg/g).","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"51 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141650431","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}
Objective: The objective of this study is to characterize the aerial parts of S. orientalis using Fourier Transform Infrared (FTIR) spectroscopy, evaluate the phenolic content and antioxidant activity of seeds, stems, and flowers, and conduct quantitative analysis of phenolic compounds using LC-MS/MS. Material and Method: Fourier Transform Infrared (FTIR) spectroscopy was employed to characterize the aerial parts of S. orientalis. The analysis focused on identifying various functional groups such as -OH vibrations associated with polysaccharides, C-H vibrations from lipids and lignin compounds, and C=O vibrations related to cellulose derivatives. The total phenolic, flavonoid, flavanol, tannin, and proanthocyanidin contents of S. orientalis seeds, stems, and flowers were evaluated using standard analytical methods. DPPH radical scavenging activity was determined to assess antioxidant potential, with IC50 values calculated for each plant part. Quantitative analysis of phenolic compounds in the plant extract was conducted using LC-MS/MS. The abundance of various phenolic acids including P-coumaric acid, trans-ferulic acid, caffeic acid, and vanillic acid was determined. Additionally, other phenolic compounds such as gallic acid, chlorogenic acid, salicylic acid, (+) taxifolin, rutin hydrate, ellagic acid, quercetin dihydrate, and apigenin were also detected and quantified. Result and Discussion: The evaluation of phenolic content showed differences among different plant parts, with flowers exhibiting the highest total phenolic and proanthocyanidin content. Seeds demonstrated superior DPPH radical scavenging activity. Quantitative analysis of phenolic compounds using LC-MS/MS highlighted the abundance of various phenolic acids and other phenolic compounds in S. orientalis. These findings underscore the potential of S. orientalis as a valuable source of natural antioxidants. Overall, the results suggest that S. orientalis possesses significant phenolic diversity and antioxidant activity, which could contribute to its potential applications in various industries, including pharmaceuticals and nutraceuticals.
{"title":"PHENOLIC AND ANTIOXIDANT PROFILE: FTIR AND LC-MS ANALYSES OF SERAPIAS ORIENTALIS","authors":"E. C. Aytar, Yasemin Özdener Kömpe","doi":"10.33483/jfpau.1448197","DOIUrl":"https://doi.org/10.33483/jfpau.1448197","url":null,"abstract":"Objective: The objective of this study is to characterize the aerial parts of S. orientalis using Fourier Transform Infrared (FTIR) spectroscopy, evaluate the phenolic content and antioxidant activity of seeds, stems, and flowers, and conduct quantitative analysis of phenolic compounds using LC-MS/MS.\u0000Material and Method: Fourier Transform Infrared (FTIR) spectroscopy was employed to characterize the aerial parts of S. orientalis. The analysis focused on identifying various functional groups such as -OH vibrations associated with polysaccharides, C-H vibrations from lipids and lignin compounds, and C=O vibrations related to cellulose derivatives. The total phenolic, flavonoid, flavanol, tannin, and proanthocyanidin contents of S. orientalis seeds, stems, and flowers were evaluated using standard analytical methods. DPPH radical scavenging activity was determined to assess antioxidant potential, with IC50 values calculated for each plant part. Quantitative analysis of phenolic compounds in the plant extract was conducted using LC-MS/MS. The abundance of various phenolic acids including P-coumaric acid, trans-ferulic acid, caffeic acid, and vanillic acid was determined. Additionally, other phenolic compounds such as gallic acid, chlorogenic acid, salicylic acid, (+) taxifolin, rutin hydrate, ellagic acid, quercetin dihydrate, and apigenin were also detected and quantified.\u0000Result and Discussion: The evaluation of phenolic content showed differences among different plant parts, with flowers exhibiting the highest total phenolic and proanthocyanidin content. Seeds demonstrated superior DPPH radical scavenging activity. Quantitative analysis of phenolic compounds using LC-MS/MS highlighted the abundance of various phenolic acids and other phenolic compounds in S. orientalis. These findings underscore the potential of S. orientalis as a valuable source of natural antioxidants. Overall, the results suggest that S. orientalis possesses significant phenolic diversity and antioxidant activity, which could contribute to its potential applications in various industries, including pharmaceuticals and nutraceuticals.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":" 11","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141668748","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}
Objective: Vegetable oils have various biologically active components, including antibacterial, antioxidant, and anti-inflammatory properties. These oils help control nausea, vomiting, coughing and gas, as well as diarrhea and dyspepsia. It also helps to reduce stomach bloating and intestinal spasm pain. To sum up, the objective of this investigation was to assess the antibacterial and antibiofilm properties of twelve different vegetable oils against the reference strain of Helicobacter pylori, NTCC 11637. Material and Method: For antibacterial activity, the minimum inhibitory concentration and the agar-well diffusion method were employed, and for antibiofilm activity, the microplate method. Result and Discussion: Vegetable oils showed antimicrobial activity at concentrations of 62.5-15.625 μg/ml and antibiofilm activity at concentrations of 250-15.625 μg/ml. According to our findings, the vegetable oils we utilized may have the ability to form a novel class of Helicobacter pylori inhibitors with anti-H. pylori properties.
{"title":"ANTIMICROBIAL AND ANTIBIOFILM ACTIVITIES OF VARIOUS VEGETABLE OILS AGAINST HELICOBACTER PYLORI","authors":"Elif Aydın","doi":"10.33483/jfpau.1438607","DOIUrl":"https://doi.org/10.33483/jfpau.1438607","url":null,"abstract":"Objective: Vegetable oils have various biologically active components, including antibacterial, antioxidant, and anti-inflammatory properties. These oils help control nausea, vomiting, coughing and gas, as well as diarrhea and dyspepsia. It also helps to reduce stomach bloating and intestinal spasm pain. To sum up, the objective of this investigation was to assess the antibacterial and antibiofilm properties of twelve different vegetable oils against the reference strain of Helicobacter pylori, NTCC 11637.\u0000Material and Method: For antibacterial activity, the minimum inhibitory concentration and the agar-well diffusion method were employed, and for antibiofilm activity, the microplate method.\u0000Result and Discussion: Vegetable oils showed antimicrobial activity at concentrations of 62.5-15.625 μg/ml and antibiofilm activity at concentrations of 250-15.625 μg/ml. According to our findings, the vegetable oils we utilized may have the ability to form a novel class of Helicobacter pylori inhibitors with anti-H. pylori properties.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":" 571","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141669632","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}
Objective: This study aimed to synthesize and evaluate the cytotoxic activities of four platinum(II) complexes with 2-substituted or nonsubstituted 1H-benzo[d]imidazole and 1H-1,3-diazole derivatives as carrier ligands (L1-L4), which may have potent cytotoxic activity and low side effects. Material and Method: K1-K4 complexes were synthesized by heating and mixing K2PtCl4 and the appropriate L1-L4. The chemical structures of K1-K4 were elucidated by Infrared and 1H Nuclear Magnetic Resonance spectroscopic methods. In vitro, cytotoxic effects of K1-K4 complexes against prostate (DU-145), endometrial adenocarcinoma (Ishikawa), and breast cancer (MCF-7) cell lines were tested by the MTT method. Result and Discussion: According to the IC50 values of the tested cell lines, K1 and K2 derivatives bearing unsubstituted 1H-benzo[d]imidazole (L1) and 1H-1,3-diazole (L2) were found to be the most effective compounds among these synthesized complexes.
{"title":"IN VITRO CYTOTOXIC ACTIVITIES OF PLATINUM(II) COMPLEXES CONTAINING 1H-BENZO[d]IMIDAZOLE AND 1H-1,3-DIAZOLE DERIVATIVES","authors":"Tuğçe Yılmaz, Elif Ergin, Hatice Oruç Demirbağ, Semra Utku","doi":"10.33483/jfpau.1461131","DOIUrl":"https://doi.org/10.33483/jfpau.1461131","url":null,"abstract":"Objective: This study aimed to synthesize and evaluate the cytotoxic activities of four platinum(II) complexes with 2-substituted or nonsubstituted 1H-benzo[d]imidazole and 1H-1,3-diazole derivatives as carrier ligands (L1-L4), which may have potent cytotoxic activity and low side effects.\u0000Material and Method: K1-K4 complexes were synthesized by heating and mixing K2PtCl4 and the appropriate L1-L4. The chemical structures of K1-K4 were elucidated by Infrared and 1H Nuclear Magnetic Resonance spectroscopic methods. In vitro, cytotoxic effects of K1-K4 complexes against prostate (DU-145), endometrial adenocarcinoma (Ishikawa), and breast cancer (MCF-7) cell lines were tested by the MTT method. \u0000Result and Discussion: According to the IC50 values of the tested cell lines, K1 and K2 derivatives bearing unsubstituted 1H-benzo[d]imidazole (L1) and 1H-1,3-diazole (L2) were found to be the most effective compounds among these synthesized complexes.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"113 36","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141668036","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}
Objective: This study aimed to create an orally disintegrating tablet (ODT) formulation using an itraconazole (ITZ)-beta-cyclodextrin (β-CD) complex to enhance itraconazole's solubility, a drug with limited solubility. β-CD was chosen for its compatibility with ITZ. Material and Method: The study prepared equimolar mixtures of ITZ and β-CD through kneading, assessing their solubility and dissolution rates. The inclusion complexes significantly increased ITZ's solubility. This complex was used to develop directly compressed ODTs with a lower ITZ content (25 mg), incorporating D-Mannitol as a bulking agent, sweetener, and to enhance mouthfeel, facilitating rapid disintegration and drug release. Result and Discussion: ODT formulations containing the ITZ-β-CD complex showed a significantly higher dissolution rate of ITZ compared to formulations with pure ITZ. This enhancement in dissolution is expected to significantly improve ITZ's bioavailability, suggesting a potential for reducing ITZ dosage and minimizing adverse effects.
{"title":"ENHANCING SOLUBILITY AND DEVELOPING AN ITRACONAZOLE-BETA-CYCLODEXTRIN COMPLEX FOR ANTIFUNGAL THERAPY IN ORALLY DISINTEGRATING TABLETS","authors":"T. Çomoğlu","doi":"10.33483/jfpau.1465360","DOIUrl":"https://doi.org/10.33483/jfpau.1465360","url":null,"abstract":"Objective: This study aimed to create an orally disintegrating tablet (ODT) formulation using an itraconazole (ITZ)-beta-cyclodextrin (β-CD) complex to enhance itraconazole's solubility, a drug with limited solubility. β-CD was chosen for its compatibility with ITZ.\u0000Material and Method: The study prepared equimolar mixtures of ITZ and β-CD through kneading, assessing their solubility and dissolution rates. The inclusion complexes significantly increased ITZ's solubility. This complex was used to develop directly compressed ODTs with a lower ITZ content (25 mg), incorporating D-Mannitol as a bulking agent, sweetener, and to enhance mouthfeel, facilitating rapid disintegration and drug release.\u0000Result and Discussion: ODT formulations containing the ITZ-β-CD complex showed a significantly higher dissolution rate of ITZ compared to formulations with pure ITZ. This enhancement in dissolution is expected to significantly improve ITZ's bioavailability, suggesting a potential for reducing ITZ dosage and minimizing adverse effects.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"48 7","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141697810","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}
Amaç: Sanal biyoeşdeğerlik çalışmaları hem yeni ilaçların hem de jenerik ilaçların geliştirme süreçlerini kolaylaştırma ve optimize etmede kritik rol oynamaktadır. Bu yaklaşım, ilaçların insan vücudundaki davranışlarını taklit etmek ve kestirebilmek için matematiksel hesaplamalara dayanmaktadır. Sanal biyoeşdeğerlik çalışmaları ile in vitro, in siliko ve in vivo veriler kullanılarak, test ve referans formülasyonlar arasındaki farmakokinetik ve klinik performans değerlendirebilir. Bu modeller, ilaçların vücutta nasıl dağıldığını, metabolize olduğunu ve atıldığını daha duyarlı bir şekilde tahmin edebilir. Bu sayede ilaçların etkilerinin kestirilebilmesi ve dozun optimize edilmesine olanak sağlar. Sonuç ve Tartışma: Sanal biyoeşdeğerlik çalışmalarının yasal düzenlemelerdeki yeri henüz tam olarak belirlenememiştir, bu nedenle ilaçla ilgili yasal otoriteler, ilaç endüstrisi, üniversiteler ve araştırma kuruluşlarının iş birliği yapması oldukça önemlidir. Özellikle ağız yolu ve diğer uygulama yolları ile kullanılan sistemik etki gösteren ilaçların, fizyolojik temelli farmakokinetik ve biyofarmasötik modelleme çalışmalarının çerçevesinin belirlenmesi, in vivo klinik çalışmalardan muafiyetin ve optimizasyonunun desteklenmesi için sanal biyoeşdeğerlik çalışmaları önemlidir. Sanal biyoeşdeğerlik çalışmaları, ilaç geliştirme süreçlerini iyileştirmek, süreyi kısaltmak ve maliyetleri düşürmek için önemli bir araç olabilir, ancak bu alandaki ilerlemelerin devam etmesi ve bu yöntemlerin ilaçla ilgili yasal düzenleme süreçlerine daha fazla entegre edilmesi gerekmektedir.
{"title":"İLAÇLARDA SANAL BİYOEŞDEĞERLİK UYGULAMALARI","authors":"Tuğba Gülsün, Huriye Demir, Levent Öner","doi":"10.33483/jfpau.1456868","DOIUrl":"https://doi.org/10.33483/jfpau.1456868","url":null,"abstract":"Amaç: Sanal biyoeşdeğerlik çalışmaları hem yeni ilaçların hem de jenerik ilaçların geliştirme süreçlerini kolaylaştırma ve optimize etmede kritik rol oynamaktadır. Bu yaklaşım, ilaçların insan vücudundaki davranışlarını taklit etmek ve kestirebilmek için matematiksel hesaplamalara dayanmaktadır. Sanal biyoeşdeğerlik çalışmaları ile in vitro, in siliko ve in vivo veriler kullanılarak, test ve referans formülasyonlar arasındaki farmakokinetik ve klinik performans değerlendirebilir. Bu modeller, ilaçların vücutta nasıl dağıldığını, metabolize olduğunu ve atıldığını daha duyarlı bir şekilde tahmin edebilir. Bu sayede ilaçların etkilerinin kestirilebilmesi ve dozun optimize edilmesine olanak sağlar. \u0000Sonuç ve Tartışma: Sanal biyoeşdeğerlik çalışmalarının yasal düzenlemelerdeki yeri henüz tam olarak belirlenememiştir, bu nedenle ilaçla ilgili yasal otoriteler, ilaç endüstrisi, üniversiteler ve araştırma kuruluşlarının iş birliği yapması oldukça önemlidir. Özellikle ağız yolu ve diğer uygulama yolları ile kullanılan sistemik etki gösteren ilaçların, fizyolojik temelli farmakokinetik ve biyofarmasötik modelleme çalışmalarının çerçevesinin belirlenmesi, in vivo klinik çalışmalardan muafiyetin ve optimizasyonunun desteklenmesi için sanal biyoeşdeğerlik çalışmaları önemlidir. Sanal biyoeşdeğerlik çalışmaları, ilaç geliştirme süreçlerini iyileştirmek, süreyi kısaltmak ve maliyetleri düşürmek için önemli bir araç olabilir, ancak bu alandaki ilerlemelerin devam etmesi ve bu yöntemlerin ilaçla ilgili yasal düzenleme süreçlerine daha fazla entegre edilmesi gerekmektedir.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"40 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141340139","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}
Metin Çapa, Y. Kadioglu, Elif Çadırcı, M. Albayrak
Objective: The goal of the present work was to investigate the antioxidant properties of the extracts of Hippophae rhamnoides L. and to determine their effects on liver toxicity in rats. Material and Method: Metal chelation, reducing power and DPPH radical scavenging methods were used in the antioxidant activity analysis of extracts. The total phenolic content was determined using the folin-ciocalteu reagent. Plant extracts were administered orally to the rats at doses of 500 µg/kg for 2 days. Each animal group was composed of six female Albino Wistar rats with an average weight of 250 g. Microscopic examination was carried out to observe any pathological changes in the rat livers. Result and Discussion: Water extract showed the highest radical scavenging activity (48.65%), reducing power (0.291 absorbance at 700 nm) and metal chelating (35.40%) at 1 mg/ml concentration. Histopathological studies showed that especially water extract reduced the severity of CCl4-induced intoxication. Hippophae rhamnoides L. extracts were found to have antioxidant activity, and also Hippophae rhamnoides L. water extract was shown to be particularly effective in preventing liver damage.
{"title":"DETERMINATION OF ANTIOXIDANT ACTIVITY OF HIPPOPHAE RHAMNOIDES L. GROWING IN TURKEY AND INVESTIGATION OF ITS EFFECTS ON THE LIVER TOXICITY IN RATS","authors":"Metin Çapa, Y. Kadioglu, Elif Çadırcı, M. Albayrak","doi":"10.33483/jfpau.1404302","DOIUrl":"https://doi.org/10.33483/jfpau.1404302","url":null,"abstract":"Objective: The goal of the present work was to investigate the antioxidant properties of the extracts of Hippophae rhamnoides L. and to determine their effects on liver toxicity in rats.\u0000Material and Method: Metal chelation, reducing power and DPPH radical scavenging methods were used in the antioxidant activity analysis of extracts. The total phenolic content was determined using the folin-ciocalteu reagent. Plant extracts were administered orally to the rats at doses of 500 µg/kg for 2 days. Each animal group was composed of six female Albino Wistar rats with an average weight of 250 g. Microscopic examination was carried out to observe any pathological changes in the rat livers.\u0000Result and Discussion: Water extract showed the highest radical scavenging activity (48.65%), reducing power (0.291 absorbance at 700 nm) and metal chelating (35.40%) at 1 mg/ml concentration. Histopathological studies showed that especially water extract reduced the severity of CCl4-induced intoxication. Hippophae rhamnoides L. extracts were found to have antioxidant activity, and also Hippophae rhamnoides L. water extract was shown to be particularly effective in preventing liver damage.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"5 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141350988","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}
Objective: Creatinine-based equations are generally used in clinical practice to estimate glomerular filtration rates (GFR), but values are not usually consistent. This study aimed to evaluate the difference between estimated GFR values using different equations. Material and Method: Adult Turkish patients with serum creatinine measurements between January to December 2021 and complete demographic data were included. GFR values were calculated using 5 different formulas. GFR calculated with Cockcroft-Gault were normalized to body surface area and added to the comparison. Difference between GFR values and KDIGO stages were evaluated. Albunin/creatinine ratio (ACR) of patients was also assessed. Result and Discussion: A total of 305 patients with average age of 52.92 years were included. Six different GFR calculations were recorded with median values between 51.70 to 71.77 ml/min/1.73m2. Formula of The Modification of Diet in Renal Disease with the race factor for Turkish population resulted in the lowest eGFR values. The ACR values of only 42 patients were available and it was negatively correlated to all GFR values and positively correlated to all KDIGO stages (p<0.05). There were noteworthy variations in GFR values, based on patient demographics and/or equations. The need for novel practical methods for estimating GFR in general and specific patient populations are necessary.
目的：临床实践中通常使用基于肌酐的方程来估算肾小球滤过率（GFR），但其数值通常并不一致。本研究旨在评估使用不同方程估算的 GFR 值之间的差异：研究纳入了 2021 年 1 月至 12 月间测量血清肌酐并提供完整人口统计学数据的土耳其成年患者。使用 5 种不同的公式计算 GFR 值。用 Cockcroft-Gault 计算出的 GFR 值按体表面积归一化后加入比较。评估 GFR 值与 KDIGO 分期之间的差异。还评估了患者的白蛋白/肌酐比值（ACR）：共纳入 305 名患者，平均年龄为 52.92 岁。共记录了六种不同的 GFR 计算方法，中位值介于 51.70 至 71.77 毫升/分钟/1.73 平方米之间。根据 "肾病饮食调整 "公式和土耳其人的种族因素计算得出的 eGFR 值最低。只有 42 名患者的 ACR 值与所有 GFR 值呈负相关，与所有 KDIGO 分期呈正相关（P<0.05）。根据患者的人口统计学特征和/或方程，GFR 值存在显著差异。有必要采用新的实用方法来估算一般和特定患者群体的 GFR 值。
{"title":"COMPARISON OF ESTIMATED GLOMERULAR FILTRATION RATE USING DIFFERENT FORMULAS IN TURKISH POPULATION","authors":"B. Çattık, R. Umar","doi":"10.33483/jfpau.1458525","DOIUrl":"https://doi.org/10.33483/jfpau.1458525","url":null,"abstract":"Objective: Creatinine-based equations are generally used in clinical practice to estimate glomerular filtration rates (GFR), but values are not usually consistent. This study aimed to evaluate the difference between estimated GFR values using different equations.\u0000Material and Method: Adult Turkish patients with serum creatinine measurements between January to December 2021 and complete demographic data were included. GFR values were calculated using 5 different formulas. GFR calculated with Cockcroft-Gault were normalized to body surface area and added to the comparison. Difference between GFR values and KDIGO stages were evaluated. Albunin/creatinine ratio (ACR) of patients was also assessed.\u0000Result and Discussion: A total of 305 patients with average age of 52.92 years were included. Six different GFR calculations were recorded with median values between 51.70 to 71.77 ml/min/1.73m2. Formula of The Modification of Diet in Renal Disease with the race factor for Turkish population resulted in the lowest eGFR values. The ACR values of only 42 patients were available and it was negatively correlated to all GFR values and positively correlated to all KDIGO stages (p<0.05). There were noteworthy variations in GFR values, based on patient demographics and/or equations. The need for novel practical methods for estimating GFR in general and specific patient populations are necessary.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"102 7","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141361581","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}
Objective: Orally Disintegrating Tablets (ODTs) have revolutionized pharmaceutical drug delivery, offering a patient-friendly alternative for those struggling with conventional tablet swallowing. This study delves into the impact of superdisintegrants (crospovidone, sodium starch glycolate, and croscarmellose sodium) on the in vitro characterization of Ketoprofen-containing ODTs. ODTs are designed to rapidly disintegrate in the oral cavity without water, enhancing patient compliance, ensuring faster therapeutic onset, and providing convenience. Material and Method: The micromeritic properties of pre-compression Ketoprofen ODT blends were assessed for bulk density, tapped density, Hausner ratio, and compressibility index. ODTs were formulated using a direct compression method to maintain component uniformity. Comprehensive characterization included weight variation, tablet hardness, friability, wetting time, and in vitro disintegration time assessments. The drug content was determined through UV spectrophotometry of dissolved ODTs, and dissolution studies were conducted in pH 6.8 phosphate buffer using USP apparatus XXIV. Result and Discussion: Results showed uniform tablet mass and favorable powder mixture flowability, ensuring ODT physical properties. Tablets exhibited excellent mechanical resistance with consistent hardness and low friability loss. All formulations demonstrated high and uniform drug content. Different superdisintegrants influenced wetting, disintegration, and dissolution times. Crospovidone exhibited the fastest wetting time but longer disintegration times, attributed to increased tablet hardness. Dissolution studies revealed that crospovidone-containing ODTs had faster drug release compared to croscarmellose sodium and sodium starch glycolate, aligning with literature findings. The study emphasized the importance of considering both wetting and disintegration times for a comprehensive evaluation of ODT performance. Croscarmellose sodium and sodium starch glycolate hindered drug release, forming gel-like masses impeding dissolution, while crospovidone enhanced drug release in formulated ODTs. In conclusion, the study provides valuable insights for pharmaceutical development and patient-centric drug delivery solutions, showcasing the influence of superdisintegrants on ODT performance and emphasizing the importance of considering various parameters for comprehensive evaluation.
{"title":"FARKLI SÜPER DAĞITICILARIN KETOPROFEN İÇEREN AĞIZDA DAĞILAN TABLETLERİN İN VİTRO KARAKTERİZASYON PARAMETRELERİ ÜZERİNDEKİ ETKİSİNİN DEĞERLENDİRİLMESİ","authors":"Tansel Çomoğlu","doi":"10.33483/jfpau.1425266","DOIUrl":"https://doi.org/10.33483/jfpau.1425266","url":null,"abstract":"Objective: Orally Disintegrating Tablets (ODTs) have revolutionized pharmaceutical drug delivery, offering a patient-friendly alternative for those struggling with conventional tablet swallowing. This study delves into the impact of superdisintegrants (crospovidone, sodium starch glycolate, and croscarmellose sodium) on the in vitro characterization of Ketoprofen-containing ODTs. ODTs are designed to rapidly disintegrate in the oral cavity without water, enhancing patient compliance, ensuring faster therapeutic onset, and providing convenience.\u0000Material and Method: The micromeritic properties of pre-compression Ketoprofen ODT blends were assessed for bulk density, tapped density, Hausner ratio, and compressibility index. ODTs were formulated using a direct compression method to maintain component uniformity. Comprehensive characterization included weight variation, tablet hardness, friability, wetting time, and in vitro disintegration time assessments. The drug content was determined through UV spectrophotometry of dissolved ODTs, and dissolution studies were conducted in pH 6.8 phosphate buffer using USP apparatus XXIV.\u0000Result and Discussion: Results showed uniform tablet mass and favorable powder mixture flowability, ensuring ODT physical properties. Tablets exhibited excellent mechanical resistance with consistent hardness and low friability loss. All formulations demonstrated high and uniform drug content. Different superdisintegrants influenced wetting, disintegration, and dissolution times. Crospovidone exhibited the fastest wetting time but longer disintegration times, attributed to increased tablet hardness. Dissolution studies revealed that crospovidone-containing ODTs had faster drug release compared to croscarmellose sodium and sodium starch glycolate, aligning with literature findings. The study emphasized the importance of considering both wetting and disintegration times for a comprehensive evaluation of ODT performance. Croscarmellose sodium and sodium starch glycolate hindered drug release, forming gel-like masses impeding dissolution, while crospovidone enhanced drug release in formulated ODTs. In conclusion, the study provides valuable insights for pharmaceutical development and patient-centric drug delivery solutions, showcasing the influence of superdisintegrants on ODT performance and emphasizing the importance of considering various parameters for comprehensive evaluation.","PeriodicalId":7891,"journal":{"name":"Ankara Universitesi Eczacilik Fakultesi Dergisi","volume":"24 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140229894","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}
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