Pub Date : 2023-10-11DOI: 10.3897/pharmacia.70.e111593
Stela Dragomanova, Velichka Andonova
Adamantane is a weakly functional hydrocarbon widely used to develop new drug molecules to improve their pharmacokinetic and pharmacodynamic parameters. The compound has an affinity for the lipid bilayer of liposomes, enabling its application in targeted drug delivery and surface recognition of target structures. This review presents the available data on developed liposomes, cyclodextrin complexes, and adamantane-based dendrimers. Adamantane has been used in two ways – as a building block to which various functional groups are covalently attached (adamantane-based dendrimers) or as a part of self-aggregating supramolecular systems, where it is incorporated based on its lipophilicity (liposomes) and strong interaction with the host molecule (cyclodextrins). Adamantane represents a suitable structural basis for the development of drug delivery systems. The study of adamantane derivatives is a current topic in designing safe and selective drug delivery systems and molecular carriers.
{"title":"Adamantane-containing drug delivery systems","authors":"Stela Dragomanova, Velichka Andonova","doi":"10.3897/pharmacia.70.e111593","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111593","url":null,"abstract":"Adamantane is a weakly functional hydrocarbon widely used to develop new drug molecules to improve their pharmacokinetic and pharmacodynamic parameters. The compound has an affinity for the lipid bilayer of liposomes, enabling its application in targeted drug delivery and surface recognition of target structures. This review presents the available data on developed liposomes, cyclodextrin complexes, and adamantane-based dendrimers. Adamantane has been used in two ways – as a building block to which various functional groups are covalently attached (adamantane-based dendrimers) or as a part of self-aggregating supramolecular systems, where it is incorporated based on its lipophilicity (liposomes) and strong interaction with the host molecule (cyclodextrins). Adamantane represents a suitable structural basis for the development of drug delivery systems. The study of adamantane derivatives is a current topic in designing safe and selective drug delivery systems and molecular carriers.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"35 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136062662","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}
The paediatric population is composed of several very different subgroups, each with its own specific characteristics. For this reason, children cannot be considered “small adults”. The development of formulations suitable for children is a complex process, as it must consider the physiological changes that occur during childhood and the impact they have on the absorption of drugs. Sildenafil citrate is a drug with a narrow therapeutic index used in paediatrics to treat pulmonary hypertension. In the present work, technological approaches for extemporaneous preparation of paediatric oral forms containing sildenafil citrate for personalized therapy in children were studied. The prepared formulations were tested for physical and microbiological stability, in-use stability, and determination of active substance content. All tested oral formulations remained unchanged in terms of appearance during the entire period of stability monitoring at the selected storage conditions – room temperature 25 °C ± 5 °C and in a refrigerator at 5 °C ± 2 °C. The established pH values suggest that the formulations remained chemically stable during the stability study. The content of sildenafil citrate in all prepared oral formulations remained above 95% w/v. The microbiological quality of the prepared compositions was confirmed. Rational strategies for preparation of extemporaneous formulations were proposed based on the analysis of experimental data.
{"title":"Extemporaneous preparation of paediatric oral formulations with sildenafil citrate","authors":"Milen Dimitrov, Dilyana Georgieva, Valentina Petkova","doi":"10.3897/pharmacia.70.e111611","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111611","url":null,"abstract":"The paediatric population is composed of several very different subgroups, each with its own specific characteristics. For this reason, children cannot be considered “small adults”. The development of formulations suitable for children is a complex process, as it must consider the physiological changes that occur during childhood and the impact they have on the absorption of drugs. Sildenafil citrate is a drug with a narrow therapeutic index used in paediatrics to treat pulmonary hypertension. In the present work, technological approaches for extemporaneous preparation of paediatric oral forms containing sildenafil citrate for personalized therapy in children were studied. The prepared formulations were tested for physical and microbiological stability, in-use stability, and determination of active substance content. All tested oral formulations remained unchanged in terms of appearance during the entire period of stability monitoring at the selected storage conditions – room temperature 25 °C ± 5 °C and in a refrigerator at 5 °C ± 2 °C. The established pH values suggest that the formulations remained chemically stable during the stability study. The content of sildenafil citrate in all prepared oral formulations remained above 95% w/v. The microbiological quality of the prepared compositions was confirmed. Rational strategies for preparation of extemporaneous formulations were proposed based on the analysis of experimental data.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"48 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136098012","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}
Pub Date : 2023-10-10DOI: 10.3897/pharmacia.70.e109086
Avetis Tsaturyan, Lilya Arstamyan, Anyuta Sargsyan, Jaklina Saribekyan, Ani Voskanyan, Ella Minasyan, Monika Israelyan, Tatevik Sargsyan, Lala Stepanyan
Taking into account a wide range of lactulose application in pharmaceutics, baby food production and other fields, along with the importance of technological solutions for its extraction from milk whey, the presented work was carried out to obtain lactulose in one cycle with simultaneous alkaline treatment and desalting of whey by the electromembrane method. Based on the data obtained, an effective method for obtaining a protein concentrate, lactose, and its isomer – lactulose from whey has been developed. The processes of pre-treatment and desalting of milk whey by the electromembrane method were studied and the optimal parameters for the processes implementation were determined. The curves of changes in the concentration of inorganic ions in whey in the desalination process, depending on the degree of demineralization, were plotted.
{"title":"Development of an efficient method for obtaining lactose and lactulose from whey","authors":"Avetis Tsaturyan, Lilya Arstamyan, Anyuta Sargsyan, Jaklina Saribekyan, Ani Voskanyan, Ella Minasyan, Monika Israelyan, Tatevik Sargsyan, Lala Stepanyan","doi":"10.3897/pharmacia.70.e109086","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e109086","url":null,"abstract":"Taking into account a wide range of lactulose application in pharmaceutics, baby food production and other fields, along with the importance of technological solutions for its extraction from milk whey, the presented work was carried out to obtain lactulose in one cycle with simultaneous alkaline treatment and desalting of whey by the electromembrane method. Based on the data obtained, an effective method for obtaining a protein concentrate, lactose, and its isomer – lactulose from whey has been developed. The processes of pre-treatment and desalting of milk whey by the electromembrane method were studied and the optimal parameters for the processes implementation were determined. The curves of changes in the concentration of inorganic ions in whey in the desalination process, depending on the degree of demineralization, were plotted.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136295506","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}
Pub Date : 2023-10-10DOI: 10.3897/pharmacia.70.e113014
Emilio Mateev, Maya Georgieva
Considering the complex pathophysiology of Alzheimer’s disease (AD), the multitarget ligand strategy is expected to provide superior effects for the treatment of the neurological disease compared to the classic single target strategy. Thus, six pyrrole-based compounds were evaluated for their dual monoamine oxidase type B (MAO-B) and acetylcholinesterase (AChE) inhibitory capacities. Most of the compounds revealed good AChE activities at 10 µM concentrations. 5d most potently inhibited AChE with 75%, while the hydrazide 5 demonstrated blocking effect of 51% at 10 µM concentrations. However, limited MAO-B inhibitory effects were observed with the exception of compounds 3, and especially 5 (30% inhibition at 1 µM). The in vitro assessments showed that the unsubstituted pyrrole-based hydrazide 5 is the best dual inhibitor of MAO-B/AChE enzymes. Subsequent in silico molecular docking simulations of 5 in the active sites of MAO-B (2V5Z) and AChE (4EY6) displayed the formation of stable enzyme-ligand complexes. To rationalize the biological assays, density functional theory (DFT) calculations were carried out at the B3LYP/6-311 ++ (d,p) level of theory. Overall, the results demonstrated that the pyrrole-based hydrazide 5 is a dual-acting AchE/MAO-B inhibitor with good antioxidant properties, which could be considered as a candidate for future lead-optimizations.
{"title":"Biological evaluation, molecular docking and DFT calculations of pyrrole-based derivatives as dual acting AChE/MAO-B inhibitors","authors":"Emilio Mateev, Maya Georgieva","doi":"10.3897/pharmacia.70.e113014","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113014","url":null,"abstract":"Considering the complex pathophysiology of Alzheimer’s disease (AD), the multitarget ligand strategy is expected to provide superior effects for the treatment of the neurological disease compared to the classic single target strategy. Thus, six pyrrole-based compounds were evaluated for their dual monoamine oxidase type B (MAO-B) and acetylcholinesterase (AChE) inhibitory capacities. Most of the compounds revealed good AChE activities at 10 µM concentrations. 5d most potently inhibited AChE with 75%, while the hydrazide 5 demonstrated blocking effect of 51% at 10 µM concentrations. However, limited MAO-B inhibitory effects were observed with the exception of compounds 3, and especially 5 (30% inhibition at 1 µM). The in vitro assessments showed that the unsubstituted pyrrole-based hydrazide 5 is the best dual inhibitor of MAO-B/AChE enzymes. Subsequent in silico molecular docking simulations of 5 in the active sites of MAO-B (2V5Z) and AChE (4EY6) displayed the formation of stable enzyme-ligand complexes. To rationalize the biological assays, density functional theory (DFT) calculations were carried out at the B3LYP/6-311 ++ (d,p) level of theory. Overall, the results demonstrated that the pyrrole-based hydrazide 5 is a dual-acting AchE/MAO-B inhibitor with good antioxidant properties, which could be considered as a candidate for future lead-optimizations.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"49 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136352440","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}
Glimepiride (GMP) is an oral antidiabetic drug classified as BCS class II, demonstrating extremely limited solubility, with a solubility level below 0.00384 mg/mL. Some generic drug manufacturers producing GMP (copy product) tablets encountered bioavailability issues due to poor dissolution, which did not meet the requirements. Therefore, measures were taken to enhance solubility through the modification of polymorphs. It is known that GMP exists in two polymorphic forms, namely Form I and an alternative Form II, which exhibits higher solubility in water. This study aims to produce and characterize the polymorph-modified GMP compared to non-modified GMP, develop an optimal formulation for polymorph-modified GMP tablets that adhere to pharmaceutical requirements as a representative copy drug model, and determine its similarity factor to Amaryl® as the innovator. The research methodology involved initiating the study by examining the polymorph transformation of GMP through the utilization of techniques such as neat grinding, solvent drop grinding, and solvent evaporation. The resulting samples were characterized using DSC, PXRD, and SEM analysis. The performance assessment encompassed the evaluation of flow properties, compressibility index, solubility, and dissolution rate compared to the non-modified GMP. Based on the characterization results, the best polymorph-modified GMP sample was used to produce a tablet formulation containing 4 mg of GMP using the direct compression method as a copy tablet model. In vitro equivalence testing was performed using a comparative dissolution test on the polymorph-modified GMP tablet compared to its innovator, Amaryl® 4 mg, in three different dissolution media, followed by determining the equivalence status using the similarity factor (f2) calculation. Based on the screening results of polymorph transformation, it was determined that the polymorph-modified GMP, using all three techniques, did not undergo a transition from Form I to Form II. Instead, it underwent amorphization, primarily observed in the solvent evaporation technique. Tablets containing polymorph-modified GMP using the solvent evaporation technique were able to enhance the in vitro dissolution rate profile compared to non-modified GMP tablets. The f2 values for the comparative in vitro dissolution test in acetate buffer pH 4.5 and phosphate buffer pH 6.8 were 60.15 ± 0.27 and 88 ± 0.35, respectively within acceptance criteria of 50–100. However, in KCl/HCl buffer pH 1.2, the f2 value was 45.15 ± 0.23. It was concluded that the polymorph-modified GMP tablet was not similar to its innovator, Amaryl®.
{"title":"The in vitro equivalence study of polymorph-modified glimepiride tablets compared to Amaryl®","authors":"Fitrianti Darusman, Taofik Rusdiana, Iyan Sopyan, Ratih Aryani, Gita Cahya Eka Darma","doi":"10.3897/pharmacia.70.e110374","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110374","url":null,"abstract":"Glimepiride (GMP) is an oral antidiabetic drug classified as BCS class II, demonstrating extremely limited solubility, with a solubility level below 0.00384 mg/mL. Some generic drug manufacturers producing GMP (copy product) tablets encountered bioavailability issues due to poor dissolution, which did not meet the requirements. Therefore, measures were taken to enhance solubility through the modification of polymorphs. It is known that GMP exists in two polymorphic forms, namely Form I and an alternative Form II, which exhibits higher solubility in water. This study aims to produce and characterize the polymorph-modified GMP compared to non-modified GMP, develop an optimal formulation for polymorph-modified GMP tablets that adhere to pharmaceutical requirements as a representative copy drug model, and determine its similarity factor to Amaryl® as the innovator. The research methodology involved initiating the study by examining the polymorph transformation of GMP through the utilization of techniques such as neat grinding, solvent drop grinding, and solvent evaporation. The resulting samples were characterized using DSC, PXRD, and SEM analysis. The performance assessment encompassed the evaluation of flow properties, compressibility index, solubility, and dissolution rate compared to the non-modified GMP. Based on the characterization results, the best polymorph-modified GMP sample was used to produce a tablet formulation containing 4 mg of GMP using the direct compression method as a copy tablet model. In vitro equivalence testing was performed using a comparative dissolution test on the polymorph-modified GMP tablet compared to its innovator, Amaryl® 4 mg, in three different dissolution media, followed by determining the equivalence status using the similarity factor (f2) calculation. Based on the screening results of polymorph transformation, it was determined that the polymorph-modified GMP, using all three techniques, did not undergo a transition from Form I to Form II. Instead, it underwent amorphization, primarily observed in the solvent evaporation technique. Tablets containing polymorph-modified GMP using the solvent evaporation technique were able to enhance the in vitro dissolution rate profile compared to non-modified GMP tablets. The f2 values for the comparative in vitro dissolution test in acetate buffer pH 4.5 and phosphate buffer pH 6.8 were 60.15 ± 0.27 and 88 ± 0.35, respectively within acceptance criteria of 50–100. However, in KCl/HCl buffer pH 1.2, the f2 value was 45.15 ± 0.23. It was concluded that the polymorph-modified GMP tablet was not similar to its innovator, Amaryl®.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"33 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136295665","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}
In the current study, RP-HPLC method for evaluation of 2 pyrrol-based hydrazones in isolated rat synaptosomes was optimized and validated according to ICH guidelines. The synaptosomes were obtained by multiple centrifugations with Percoll reagent and the selected 2 N-pyrollyl hydrazide-hydrazones were incubated for 2 hours at 37 °C. Subsequently, the purified fraction through protein precipitation was analyzed by an UltiMateDionex 3000 DAD system with Purospher STAR C18 (4.6 x 12.5 cm, 5 µm) column. The mobile phase, consisting of acetonitrile: phosphate buffer pH 3.5: methanol in ratio 42/36/22 (v/v/v), was eluted isocratically with 0.8 mL/min flow rate. Afterwards, the novel and rapid method was applied effectively for identification of biotransformation in isolated rat brain synaptosomes. The analysis results indicated an absence of new peaks and persistent sample concentration which determined the stability of the analyzed ethyl 5-(4-bromophenyl)-1-(2-(2-(2-hydroxybenzylidene) hydrazinyl)-2- oxoethyl)-2-methyl- 1H-pyrrole-3-carboxylate ( 11b ) and ethyl 5-(4-bromophenyl)-1-(3-(2-(2-hydroxybenzylidene)hydrazinyl)-3-oxopropyl)-2-methyl-1H-pyrrole-3-carboxylate ( 12b ) and pointed these structures as promising.
本研究根据ICH指南，优化并验证了RP-HPLC评价大鼠离体突触体中2个吡咯基腙的方法。用Percoll试剂多次离心得到突触体，选择的2个n -热解酰肼-腙在37℃下孵育2小时。随后，通过蛋白沉淀纯化的部分用UltiMateDionex 3000 DAD系统与Purospher STAR C18 (4.6 x 12.5 cm, 5µm)柱进行分析。流动相为乙腈:pH为3.5的磷酸盐缓冲液:甲醇，体积比为42/36/22 (v/v/v)，流速为0.8 mL/min。随后，该方法被有效地应用于离体大鼠脑突触体生物转化的鉴定。分析结果表明，没有新峰出现，样品浓度持续存在，这决定了所分析的5-(4-溴苯基)-1-(2-(2-(2-羟基苄基)肼基)-2-甲基- 1h -吡咯-3-羧酸酯(11b)和5-(4-溴苯基)-1-(3-(2-(2-羟基苄基)肼基)-3-氧丙基)-2-甲基- 1h -吡咯-3-羧酸酯(12b)的稳定性，并指出这些结构具有发展前景。
{"title":"Optimization and validation of RP-HPLC method for evaluation of pyrrole -containing hydrazones in isolated rat synaptosomes","authors":"Alexandrina Mateeva, Magdalena Kondeva-Burdina, Lily Peikova, Maya Georgieva","doi":"10.3897/pharmacia.70.e113039","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113039","url":null,"abstract":"In the current study, RP-HPLC method for evaluation of 2 pyrrol-based hydrazones in isolated rat synaptosomes was optimized and validated according to ICH guidelines. The synaptosomes were obtained by multiple centrifugations with Percoll reagent and the selected 2 N-pyrollyl hydrazide-hydrazones were incubated for 2 hours at 37 °C. Subsequently, the purified fraction through protein precipitation was analyzed by an UltiMateDionex 3000 DAD system with Purospher STAR C18 (4.6 x 12.5 cm, 5 µm) column. The mobile phase, consisting of acetonitrile: phosphate buffer pH 3.5: methanol in ratio 42/36/22 (v/v/v), was eluted isocratically with 0.8 mL/min flow rate. Afterwards, the novel and rapid method was applied effectively for identification of biotransformation in isolated rat brain synaptosomes. The analysis results indicated an absence of new peaks and persistent sample concentration which determined the stability of the analyzed ethyl 5-(4-bromophenyl)-1-(2-(2-(2-hydroxybenzylidene) hydrazinyl)-2- oxoethyl)-2-methyl- 1H-pyrrole-3-carboxylate ( 11b ) and ethyl 5-(4-bromophenyl)-1-(3-(2-(2-hydroxybenzylidene)hydrazinyl)-3-oxopropyl)-2-methyl-1H-pyrrole-3-carboxylate ( 12b ) and pointed these structures as promising.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"8 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136295680","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}
Pub Date : 2023-10-06DOI: 10.3897/pharmacia.70.e110412
Emir Behluli, Thomas Liehr, Rifat Hadziselimovic, Gazmend Temaj
Systemic lupus erythematosus (SLE) is a disease associated with an impaired autoimmune response; the immune system attacks erroneously own tissues, which leads to inflammation, tissue damage and complement activation. The latter plays a pivotal role in SLE pathology, as complement level is suited as histological marker for disease diagnoses and management. Besides, environmentally factors have been highlighted and their significant contribution for individual genetic predisposition has been pointed out. Here complement factors, their activity and their ability to modify DNA with histone proteins are reviewed; known gene mutations involved in SLE, and new therapeutic approaches suggested for SLE are discussed and summarized, as well.
{"title":"Epigenetics and treatment of systemic lupus erythematosus","authors":"Emir Behluli, Thomas Liehr, Rifat Hadziselimovic, Gazmend Temaj","doi":"10.3897/pharmacia.70.e110412","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110412","url":null,"abstract":"Systemic lupus erythematosus (SLE) is a disease associated with an impaired autoimmune response; the immune system attacks erroneously own tissues, which leads to inflammation, tissue damage and complement activation. The latter plays a pivotal role in SLE pathology, as complement level is suited as histological marker for disease diagnoses and management. Besides, environmentally factors have been highlighted and their significant contribution for individual genetic predisposition has been pointed out. Here complement factors, their activity and their ability to modify DNA with histone proteins are reviewed; known gene mutations involved in SLE, and new therapeutic approaches suggested for SLE are discussed and summarized, as well.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"66 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135347686","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}
Pub Date : 2023-10-05DOI: 10.3897/pharmacia.70.e110439
Khairi M. S. Fahelelbom, Abdullah Saleh, Ramez Mansour, Rami Abujarad
Aim : The aim of this study is to propose a green and nondestructive method using the ATR-FTIR method for the quantitative analysis of Ibuprofen tablet dosage forms. Herein, the technique has been validated as an alternative green tool that evades necessary sample preparation procedures required in traditional quantitative methods. Methods : The method depends on selecting CO of the Ibuprofen stretching band in the range 1620–1750 cm -1 to quantitatively determine Ibuprofen in original samples. The pack area (AUC) from ATR-FTIR spectral scanning of samples has been determined through the first derivative measurements. Results : The assay results indicated that no interferences between the excipients or additives and the active ingredients of the commercial tablets interferences. The linearity is excellent within the concentration range of 0.2 to 1.5 w/w % (r = 0.9994). A percentage of recoveries ranged between 99.7–10.5 which are in good agreement with the pharmacopeial percent recovery standards. The high degree of sensitivity of the technique was demonstrated by obtaining a 0.028 w/w % detection limit and a 0.1599 w/w % limit of quantification values.
{"title":"Utilization of green ATR-FTIR spectroscopic method for quantitative analysis of Ibuprofen tablets","authors":"Khairi M. S. Fahelelbom, Abdullah Saleh, Ramez Mansour, Rami Abujarad","doi":"10.3897/pharmacia.70.e110439","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110439","url":null,"abstract":"Aim : The aim of this study is to propose a green and nondestructive method using the ATR-FTIR method for the quantitative analysis of Ibuprofen tablet dosage forms. Herein, the technique has been validated as an alternative green tool that evades necessary sample preparation procedures required in traditional quantitative methods. Methods : The method depends on selecting CO of the Ibuprofen stretching band in the range 1620–1750 cm -1 to quantitatively determine Ibuprofen in original samples. The pack area (AUC) from ATR-FTIR spectral scanning of samples has been determined through the first derivative measurements. Results : The assay results indicated that no interferences between the excipients or additives and the active ingredients of the commercial tablets interferences. The linearity is excellent within the concentration range of 0.2 to 1.5 w/w % (r = 0.9994). A percentage of recoveries ranged between 99.7–10.5 which are in good agreement with the pharmacopeial percent recovery standards. The high degree of sensitivity of the technique was demonstrated by obtaining a 0.028 w/w % detection limit and a 0.1599 w/w % limit of quantification values.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134975161","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}
Pub Date : 2023-10-05DOI: 10.3897/pharmacia.70.e112215
Ahmad Habibie, Tri Joko Raharjo, Respati Dwi Swasono, Endah Retnaningrum
Macroalgae is a protein source with the potential to yield antimicrobial peptides (AMPs) that exhibit a wide range of biological activities. This study aimed to find bioactive peptide-based antibacterial compounds from marine macroalgae Chondrus crispus protein hydrolysate. The peptides were isolated by solid phase extraction with a strong cation exchanger from trypsin-digested and α -chymotrypsin-digested hydrolysates. Certain fractions of the hydrolyzed protein displayed a good inhibition zone, with the α-chymotrypsin-digested fraction eluted at pH 9 exhibiting the highest inhibition against Gram-negative bacteria Staphylococcus aureus . Several peptides were characterized as cationic helical peptides with hydrophobicity percentages of 16.67–77.78%. The potential antibacterial peptide P01 KKNVTTLAPLVF was identified as an α -helical cationic antibacterial peptide with 0.525 GRAVY value, amphipathic structure, and +2 total charge. Moreover, strong interaction was observed between P07 SAGSGNEGLSGW and P20 RTASSR peptide with DNA gyrase and DHFR receptors from S. aureus with binding energy -8.0 and -7.3 kcal/mol, respectively.
{"title":"Antibacterial activity of active peptide from marine macroalgae Chondrus crispus protein hydrolysate against Staphylococcus aureus","authors":"Ahmad Habibie, Tri Joko Raharjo, Respati Dwi Swasono, Endah Retnaningrum","doi":"10.3897/pharmacia.70.e112215","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e112215","url":null,"abstract":"Macroalgae is a protein source with the potential to yield antimicrobial peptides (AMPs) that exhibit a wide range of biological activities. This study aimed to find bioactive peptide-based antibacterial compounds from marine macroalgae Chondrus crispus protein hydrolysate. The peptides were isolated by solid phase extraction with a strong cation exchanger from trypsin-digested and α -chymotrypsin-digested hydrolysates. Certain fractions of the hydrolyzed protein displayed a good inhibition zone, with the α-chymotrypsin-digested fraction eluted at pH 9 exhibiting the highest inhibition against Gram-negative bacteria Staphylococcus aureus . Several peptides were characterized as cationic helical peptides with hydrophobicity percentages of 16.67–77.78%. The potential antibacterial peptide P01 KKNVTTLAPLVF was identified as an α -helical cationic antibacterial peptide with 0.525 GRAVY value, amphipathic structure, and +2 total charge. Moreover, strong interaction was observed between P07 SAGSGNEGLSGW and P20 RTASSR peptide with DNA gyrase and DHFR receptors from S. aureus with binding energy -8.0 and -7.3 kcal/mol, respectively.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"126 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135482521","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}
Pub Date : 2023-10-05DOI: 10.3897/pharmacia.70.e110336
Wafa Hourani, Mohammad Amayreh, Mohammed Khair Hourani
While platinum electrode shows hyperactivity towards adsorption and surface processes, iodine-coated platinum electrode offers remarkable inertness toward them. Therefore, iodine-coated platinum electrodes lend themselves to probe chemical species in the bulk solution without intervention from adsorption and surface processes. The current work presents utilization of iodine-coated polycrystalline platinum electrode as a voltammetric sensor for determination of dopamine in serum and urine samples. Differential pulse voltammetry (DPV) at iodine coated polycrystalline platinum electrode is the technique of choice whenever higher sensitivity is sought. DPV with a scan rate of 5 mV/s was applied for determination of dopamine in PBS at pH 7. The anodic peak related to dopamine oxidation in the above-mentioned solution was centered at ~0.1V vs. Ag/AgCl quasi reference electrode. The linear range for the developed method was between 1.0 and 100 µM. The anodic peak current showed excellent linearity with dopamine concentration (R 2 =0.9977) over the above-mentioned range. The limit of detection (LOD) and limit of quantitation (LOQ) were 0.29 µM and 0.96 µM respectively which attests to the high sensitivity of the developed method. The proposed method was successfully applied to the analysis of dopamine in serum and urine samples. The percent recovery values ranged from 94.4 to 104.5% attesting to the accuracy of the developed method and absence of determinate errors.
{"title":"Determination of dopamine in blood serum and urine samples by differential pulse voltammetry at an iodine-coated platinum electrode","authors":"Wafa Hourani, Mohammad Amayreh, Mohammed Khair Hourani","doi":"10.3897/pharmacia.70.e110336","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110336","url":null,"abstract":"While platinum electrode shows hyperactivity towards adsorption and surface processes, iodine-coated platinum electrode offers remarkable inertness toward them. Therefore, iodine-coated platinum electrodes lend themselves to probe chemical species in the bulk solution without intervention from adsorption and surface processes. The current work presents utilization of iodine-coated polycrystalline platinum electrode as a voltammetric sensor for determination of dopamine in serum and urine samples. Differential pulse voltammetry (DPV) at iodine coated polycrystalline platinum electrode is the technique of choice whenever higher sensitivity is sought. DPV with a scan rate of 5 mV/s was applied for determination of dopamine in PBS at pH 7. The anodic peak related to dopamine oxidation in the above-mentioned solution was centered at ~0.1V vs. Ag/AgCl quasi reference electrode. The linear range for the developed method was between 1.0 and 100 µM. The anodic peak current showed excellent linearity with dopamine concentration (R 2 =0.9977) over the above-mentioned range. The limit of detection (LOD) and limit of quantitation (LOQ) were 0.29 µM and 0.96 µM respectively which attests to the high sensitivity of the developed method. The proposed method was successfully applied to the analysis of dopamine in serum and urine samples. The percent recovery values ranged from 94.4 to 104.5% attesting to the accuracy of the developed method and absence of determinate errors.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135482364","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：