{"title":"From Mahidol University Journal of Pharmaceutical Sciences to Pharmaceutical Sciences Asia, From MUJPS to PSA","authors":"M. Chomnawang","doi":"10.29090/psa.2022.01.01","DOIUrl":"https://doi.org/10.29090/psa.2022.01.01","url":null,"abstract":"","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"56 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78054250","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 : 2022-01-01DOI: 10.29090/psa.2022.04.22.040
Kiatkriangkrai Koyratkoson, Nattapong Tidwong, Suwida Tangtrakultham, P. Montakantikul
Chloroquine (CQ) efficacy was shown in some coronavirus disease 2019 (COVID-19) adult clinical studies. However, its data in children is still limited. Therefore, this study aims to assess the suitability of the dosage regimens from the literature and regimens proposed by the authors for pediatric COVID-19 patients aged 2-12 years old. The efficacy pharmacodynamic (PD) target was calculated for CQ blood concentration based on the literature's successfully treated COVID-19 adult regimen. The safety PD targets were derived from the literature regarding any adverse effects (AEs) and QTc prolongation. The adult pharmacokinetic (PK) parameters were transformed into pediatrics by allometric scaling (AS) method. A 10,000-time Monte Carlo simulation (MCS) was performed to calculate the percentage of probability to target attainment (%PTA). The literature's regimens were not capable of achieving 90%PTA efficacy PD target. The proposed regimens without loading dose (LD) achieved the efficacy target at day 8-10 which was later than the proposed regimens with LD (day 4-7). The 90%PTA below any AEs target was achieved in the first few days of the literature and proposed regimens but was unavoidable thereafter. Nevertheless, the 90%PTA below QTc prolongation target was favorably achieved by all regimens. This study revealed that the proposed regimen with LD seems to be the optimal dosage regimen. Additional studies are needed to validate our proposed regimens, especially among early-stage COVID-19 patients and recent major variants.
{"title":"Chloroquine dosage regimen simulation for pediatric patients with coronavirus disease 2019","authors":"Kiatkriangkrai Koyratkoson, Nattapong Tidwong, Suwida Tangtrakultham, P. Montakantikul","doi":"10.29090/psa.2022.04.22.040","DOIUrl":"https://doi.org/10.29090/psa.2022.04.22.040","url":null,"abstract":"Chloroquine (CQ) efficacy was shown in some coronavirus disease 2019 (COVID-19) adult clinical studies. However, its data in children is still limited. Therefore, this study aims to assess the suitability of the dosage regimens from the literature and regimens proposed by the authors for pediatric COVID-19 patients aged 2-12 years old. The efficacy pharmacodynamic (PD) target was calculated for CQ blood concentration based on the literature's successfully treated COVID-19 adult regimen. The safety PD targets were derived from the literature regarding any adverse effects (AEs) and QTc prolongation. The adult pharmacokinetic (PK) parameters were transformed into pediatrics by allometric scaling (AS) method. A 10,000-time Monte Carlo simulation (MCS) was performed to calculate the percentage of probability to target attainment (%PTA). The literature's regimens were not capable of achieving 90%PTA efficacy PD target. The proposed regimens without loading dose (LD) achieved the efficacy target at day 8-10 which was later than the proposed regimens with LD (day 4-7). The 90%PTA below any AEs target was achieved in the first few days of the literature and proposed regimens but was unavoidable thereafter. Nevertheless, the 90%PTA below QTc prolongation target was favorably achieved by all regimens. This study revealed that the proposed regimen with LD seems to be the optimal dosage regimen. Additional studies are needed to validate our proposed regimens, especially among early-stage COVID-19 patients and recent major variants.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"218 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75621575","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 : 2022-01-01DOI: 10.29090/psa.2022.06.22.104
Van Duong Thi Thanh, Thang Nguyen, T. Van, Thu Pham Thi Minh
Antimicrobial resistance (AMR) has become a concerning health issue worldwide, and this resistance leads to poor treatment outcomes and high mortality, especially, AMR of NP in ICU. To determine the reality of AMR and find the factors related to AMR of NP in the ICU. We performed a cross-sectional study in the ICU Department from July 2015 to July 2019. We calculated the incidence of the degree of multidrug-resistant strains and the percentages of factors related to AMR. Data management and analysis were performed by SPSS version 22.0. Of the initial observation of 281 patients, all participants had NP due to gram-negative bacteria; 91 (32.4%) were early-onset and 190 (67.6%) were lately-onset NP. Out of all pathogens examined, above 80% were resistant to quinolone, carbapenem, and cephalosporin. Moreover, multiple drug resistance in bacteria was about 87.5%. Furthermore, bacteria, changed anti-biotics have been significantly associated with the multi-resistance of bacteria. Besides, the increase in antibiotic use, especially ciprofloxacin and imipenem, is also related to antibiotic resistance. These results show that the resistance to quinolones, carbapenem, and cephalosporin is high in the ICU, with rates exceeding 80%. Furthermore, the bacteria, change of antibiotics, and the increasing use of antibiotics have been significantly associated with multiple antibiotic resistance.
{"title":"Prevalence and determinants of antimicrobial resistance of gram-negative bacteria in intensive care unit","authors":"Van Duong Thi Thanh, Thang Nguyen, T. Van, Thu Pham Thi Minh","doi":"10.29090/psa.2022.06.22.104","DOIUrl":"https://doi.org/10.29090/psa.2022.06.22.104","url":null,"abstract":"Antimicrobial resistance (AMR) has become a concerning health issue worldwide, and this resistance leads to poor treatment outcomes and high mortality, especially, AMR of NP in ICU. To determine the reality of AMR and find the factors related to AMR of NP in the ICU. We performed a cross-sectional study in the ICU Department from July 2015 to July 2019. We calculated the incidence of the degree of multidrug-resistant strains and the percentages of factors related to AMR. Data management and analysis were performed by SPSS version 22.0. Of the initial observation of 281 patients, all participants had NP due to gram-negative bacteria; 91 (32.4%) were early-onset and 190 (67.6%) were lately-onset NP. Out of all pathogens examined, above 80% were resistant to quinolone, carbapenem, and cephalosporin. Moreover, multiple drug resistance in bacteria was about 87.5%. Furthermore, bacteria, changed anti-biotics have been significantly associated with the multi-resistance of bacteria. Besides, the increase in antibiotic use, especially ciprofloxacin and imipenem, is also related to antibiotic resistance. These results show that the resistance to quinolones, carbapenem, and cephalosporin is high in the ICU, with rates exceeding 80%. Furthermore, the bacteria, change of antibiotics, and the increasing use of antibiotics have been significantly associated with multiple antibiotic resistance.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74435496","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 : 2022-01-01DOI: 10.29090/psa.2022.01.21.096
N. Nguyen, Thang Nguyen, S. T. Pham, T. H. Nguyen
Inappropriate prescribing reduces the quality of treatment and leads to a waste of resources. The World Health Organization estimates that more than half of all drugs are prescribed, dispensed, or sold inappropriately, and that half of all patients do not take them correctly. Drug-related problems can increase the risk of side effects, drug interactions, antimicrobial resistance, increase costs for treatment (in terms of both direct medication costs and indirect medication costs), and pressure the insurance budget society. According to the studies, about 50% to 80% of drug-related problems may be preventable. In particular, clinical pharmacists help identify, treat and have a crucial role in preventing drug-related problems through specific interventions. The pharmacist's contribution to improving the quality of medication use and patient safety can be assessed directly or indirectly by determining the number of drug-related problems being managed/prevented or by cost-effective treatment. All over the world, many studies are showing the critical role of pharmacists in identifying and managing drug-related problems in prescribing. In Sweden, pharmacists' recommendations on DRPs might positively influence physicians’ prescribing quality and contribute to better and safer drug therapy for patients. In addition, Japanese pharmacists also had an essential role in providing medication safety, with potential cost savings.
{"title":"Pharmacist-led interventions to reduce drug-related problems in prescribing for Vietnamese outpatients","authors":"N. Nguyen, Thang Nguyen, S. T. Pham, T. H. Nguyen","doi":"10.29090/psa.2022.01.21.096","DOIUrl":"https://doi.org/10.29090/psa.2022.01.21.096","url":null,"abstract":"Inappropriate prescribing reduces the quality of treatment and leads to a waste of resources. The World Health Organization estimates that more than half of all drugs are prescribed, dispensed, or sold inappropriately, and that half of all patients do not take them correctly. Drug-related problems can increase the risk of side effects, drug interactions, antimicrobial resistance, increase costs for treatment (in terms of both direct medication costs and indirect medication costs), and pressure the insurance budget society. According to the studies, about 50% to 80% of drug-related problems may be preventable. In particular, clinical pharmacists help identify, treat and have a crucial role in preventing drug-related problems through specific interventions. The pharmacist's contribution to improving the quality of medication use and patient safety can be assessed directly or indirectly by determining the number of drug-related problems being managed/prevented or by cost-effective treatment. All over the world, many studies are showing the critical role of pharmacists in identifying and managing drug-related problems in prescribing. In Sweden, pharmacists' recommendations on DRPs might positively influence physicians’ prescribing quality and contribute to better and safer drug therapy for patients. In addition, Japanese pharmacists also had an essential role in providing medication safety, with potential cost savings.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74344210","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 study aims to investigate the effect of formulation variables on the characteristics of azithromycin (AZI) nanoparticles using a quality by design approach. AZI nanoparticles were prepared by the emulsification solvent diffusion method. Two critical factors, the ratio of AZI: Eudragit EPO (X 1 ) and volume of outer aqueous medium (X 2 ), were chosen as independent variables for central composite design. The optimized formulation was further characterized by Fourier transform infrared spectroscopy, X-ray diffractometry, transmission electron microscopy, and dissolution test. The obtained results showed variability of mean particle size, entrapment efficacy, and zeta potential from 200 to 1232 nm, 10.78 to 75.9%, and 31 to 43 mV, respectively. The main coefficients indicated that the ratio of AZI: polymer (X 1 ) possessed a synergistic effect on mean particle size (Y 1 ), and volume of outer aqueous medium (X 2 ) had an antagonistic effect on particle size. The interaction between the ratio of AZI: Eudragit EPO (X 1 ) and volume of outer aqueous medium (X 2 ) exhibited a significant antagonistic effect on entrapment efficacy (Y 2 ) ( p <0.05). AZI existed in an amorphous state in nanoparticles that were spherical and homogeneous in shape. The nanoparticles revealed the Korsmeyer-Peppas release model, from which AZI was released faster compared to raw material.
{"title":"Evaluation of formulation variables on azithromycin nanoparticles prepared by emulsification solvent diffusion method using quality by design approach","authors":"Nguyen-Thach Tung, Canh-Hung Nguyen, Huu-Manh Nguyen","doi":"10.29090/psa.2022.02.21.141","DOIUrl":"https://doi.org/10.29090/psa.2022.02.21.141","url":null,"abstract":"The study aims to investigate the effect of formulation variables on the characteristics of azithromycin (AZI) nanoparticles using a quality by design approach. AZI nanoparticles were prepared by the emulsification solvent diffusion method. Two critical factors, the ratio of AZI: Eudragit EPO (X 1 ) and volume of outer aqueous medium (X 2 ), were chosen as independent variables for central composite design. The optimized formulation was further characterized by Fourier transform infrared spectroscopy, X-ray diffractometry, transmission electron microscopy, and dissolution test. The obtained results showed variability of mean particle size, entrapment efficacy, and zeta potential from 200 to 1232 nm, 10.78 to 75.9%, and 31 to 43 mV, respectively. The main coefficients indicated that the ratio of AZI: polymer (X 1 ) possessed a synergistic effect on mean particle size (Y 1 ), and volume of outer aqueous medium (X 2 ) had an antagonistic effect on particle size. The interaction between the ratio of AZI: Eudragit EPO (X 1 ) and volume of outer aqueous medium (X 2 ) exhibited a significant antagonistic effect on entrapment efficacy (Y 2 ) ( p <0.05). AZI existed in an amorphous state in nanoparticles that were spherical and homogeneous in shape. The nanoparticles revealed the Korsmeyer-Peppas release model, from which AZI was released faster compared to raw material.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78791583","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 : 2022-01-01DOI: 10.29090/psa.2022.04.22.058
Khanit Sa-ngiamsuntorn, Piyanoot Thongsri, Yongyut Pewkliang, A. Wongkajornsilp
COVID-19 was declared by WHO as a pandemic since March 2020. The vaccination program has been implemented worldwide. Specific antiviral drugs such as remdesivir, molnupiravir and ritonavir-based nirmatrelvir were effective against SARS-CoV-2 infection. However, the new SARS-CoV-2 variants have been elevated due to viral mutation causing vaccine resistance and rapid spreading. Long-term COVID-19 complications have been lifethreatening in some recovery cases. To overcome viral adaptation, cell culture model is essential to comprehend SARS-CoV-2 infection, pathophysiology, complications, and drug target alterations. The classical 2D culture cell was frequency used for viral propagation and high-throughput screening. Modern 3D culture has recapitulated key cellular and molecular events of tissue physiology. Here, we reviewed the cell lines, 3D culture, organoid and relevant models for the aforementioned applications.
{"title":"Cell culture models for SARS-CoV-2 infectivity and systemic complications","authors":"Khanit Sa-ngiamsuntorn, Piyanoot Thongsri, Yongyut Pewkliang, A. Wongkajornsilp","doi":"10.29090/psa.2022.04.22.058","DOIUrl":"https://doi.org/10.29090/psa.2022.04.22.058","url":null,"abstract":"COVID-19 was declared by WHO as a pandemic since March 2020. The vaccination program has been implemented worldwide. Specific antiviral drugs such as remdesivir, molnupiravir and ritonavir-based nirmatrelvir were effective against SARS-CoV-2 infection. However, the new SARS-CoV-2 variants have been elevated due to viral mutation causing vaccine resistance and rapid spreading. Long-term COVID-19 complications have been lifethreatening in some recovery cases. To overcome viral adaptation, cell culture model is essential to comprehend SARS-CoV-2 infection, pathophysiology, complications, and drug target alterations. The classical 2D culture cell was frequency used for viral propagation and high-throughput screening. Modern 3D culture has recapitulated key cellular and molecular events of tissue physiology. Here, we reviewed the cell lines, 3D culture, organoid and relevant models for the aforementioned applications.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75334627","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 : 2022-01-01DOI: 10.29090/psa.2022.04.22.061
Gajanand R Pujari, V. Subramanian, S. Rao
{"title":"Antibacterial hydrogel containing Piper Betel L. extract for acne treatment, an ex vivo investigation","authors":"Gajanand R Pujari, V. Subramanian, S. Rao","doi":"10.29090/psa.2022.04.22.061","DOIUrl":"https://doi.org/10.29090/psa.2022.04.22.061","url":null,"abstract":"","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77225564","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 : 2022-01-01DOI: 10.29090/psa.2022.02.21.158
Yanti Herawati, U. Kalsum, I. W. Arsana, L. Yuniarti, Teguh Wahju Sardjono
The phytochemical compounds contained in papaya leaves are known to have a galactopoietic effect. This study aims to analyze the effect of ethanol extract of Carica papaya leaves on β-casein gene expression, β-casein levels, total protein, and milk volume. This in vivo was an experimental study including a posttest control group that was conducted on one control group and three treatment groups. Each group consisted of six lactating rats. The control group rats were given ordinary food, while the treatment group rats, D1, D2, and D3, were given ethanol extract of Carica papaya leaves with the dose of 0.95 mg, 1.9 mg, and 3.8 mg/200 g Body weight (BW)/ day, respectively, from day 1 to day 13 of lactation. On day 14, all of the rats were sacrificed. Breastmilk volume taken from all breasts of lactating rats was measured individually in milliliters, β-casein gene expressions in the mammary tissues were measured using reverse transcription polymerase chain reaction (RT-PCR), while serum β-casein levels were measured using ELISA, and total protein was measured using bicinchoninic acid (BCA) protein assay. Statistical analysis was carried out using one-way ANOVA, Tukey test, and Games-Howell test at 95% confidence level. Milk volume, β-casein gene expression, β-casein levels, and total protein levels of all treatment rat groups were significantly higher than the control group ( p <0.05). The increases of all parameters were consistent; the most effective dose was 1.9 mg/200g BW. Carica papaya leaf ethanol extract can increase milk volume, β-casein gene (Csn2) expression, β-casein levels, and total protein levels.
{"title":"Carica papaya leaf ethanol extract effect on milk volume, β-casein gene (Csn2) expression, β-casein levels, and milk total protein levels","authors":"Yanti Herawati, U. Kalsum, I. W. Arsana, L. Yuniarti, Teguh Wahju Sardjono","doi":"10.29090/psa.2022.02.21.158","DOIUrl":"https://doi.org/10.29090/psa.2022.02.21.158","url":null,"abstract":"The phytochemical compounds contained in papaya leaves are known to have a galactopoietic effect. This study aims to analyze the effect of ethanol extract of Carica papaya leaves on β-casein gene expression, β-casein levels, total protein, and milk volume. This in vivo was an experimental study including a posttest control group that was conducted on one control group and three treatment groups. Each group consisted of six lactating rats. The control group rats were given ordinary food, while the treatment group rats, D1, D2, and D3, were given ethanol extract of Carica papaya leaves with the dose of 0.95 mg, 1.9 mg, and 3.8 mg/200 g Body weight (BW)/ day, respectively, from day 1 to day 13 of lactation. On day 14, all of the rats were sacrificed. Breastmilk volume taken from all breasts of lactating rats was measured individually in milliliters, β-casein gene expressions in the mammary tissues were measured using reverse transcription polymerase chain reaction (RT-PCR), while serum β-casein levels were measured using ELISA, and total protein was measured using bicinchoninic acid (BCA) protein assay. Statistical analysis was carried out using one-way ANOVA, Tukey test, and Games-Howell test at 95% confidence level. Milk volume, β-casein gene expression, β-casein levels, and total protein levels of all treatment rat groups were significantly higher than the control group ( p <0.05). The increases of all parameters were consistent; the most effective dose was 1.9 mg/200g BW. Carica papaya leaf ethanol extract can increase milk volume, β-casein gene (Csn2) expression, β-casein levels, and total protein levels.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"59 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79799709","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 : 2022-01-01DOI: 10.29090/psa.2022.04.22.095
F. A. Saputri, A. N. Hasanah, Mutakin, T. Rusdiana, I. Surono, R. Abdulah
Type 2 diabetes mellitus triggers hypertension as a complication. The use of amlodipine and glibenclamide drugs simultaneously results in a synergistic and effective lowering of blood sugar and blood pressure. In the testing of bioavailability and bioequivalence, as well as the monitoring of drug concentrations in the blood, a sensitive bioanalytical approach that meets existing reference requirements, such as the European Medicines Agency (EMA) recommendation, is required. Presently, there is no simultaneous bioanalytical method of amlodipine and glibenclamide that meets EMA requirements. This study aimed to develop a sensitive bioanalytical method that fulfills EMA requirements for determining the levels of amlodipine and glibenclamide simultaneously. Amlodipine and glibenclamide in plasma were extracted with acetonitrile at 10°C. The derivatization was conducted using 0.08% 4-chloro-7-nitrobenzofurazan at pH 8.6 with Teorell and Stenhagen buffer for 20 min at 70°C, followed by the addition of 0.1 N sulfuric acid. High-performance liquid chromatography analysis used a LiChrospher RP 18 column with a size of 125×40 mm ID; mobile phase, acetonitrile: 0.01% phosphoric acid (52:48); flow rate of 1 mL/min; and emission and excitation wavelength for glibenclamide and amlodipine at 346 and 300 nm and 535 and 480 nm, respectively. The concentration ranges were 0.1-20 ng/mL for amlodipine and 1-200 ng/mL for glibenclamide. The average ranges of percentage coefficient of variation and percentage difference were 1.76%-14.62% and 4.48%-11.18% for amlodipine and 0.56%-11.92% and 2.92%-12.75% for glibenclamide. This sensitive and simultaneous bioanalytical method for amlodipine and glibenclamide fulfills the EMA requirements.
{"title":"A sensitive bioanalytical method for the simultaneous determination of amlodipine and glibenclamide","authors":"F. A. Saputri, A. N. Hasanah, Mutakin, T. Rusdiana, I. Surono, R. Abdulah","doi":"10.29090/psa.2022.04.22.095","DOIUrl":"https://doi.org/10.29090/psa.2022.04.22.095","url":null,"abstract":"Type 2 diabetes mellitus triggers hypertension as a complication. The use of amlodipine and glibenclamide drugs simultaneously results in a synergistic and effective lowering of blood sugar and blood pressure. In the testing of bioavailability and bioequivalence, as well as the monitoring of drug concentrations in the blood, a sensitive bioanalytical approach that meets existing reference requirements, such as the European Medicines Agency (EMA) recommendation, is required. Presently, there is no simultaneous bioanalytical method of amlodipine and glibenclamide that meets EMA requirements. This study aimed to develop a sensitive bioanalytical method that fulfills EMA requirements for determining the levels of amlodipine and glibenclamide simultaneously. Amlodipine and glibenclamide in plasma were extracted with acetonitrile at 10°C. The derivatization was conducted using 0.08% 4-chloro-7-nitrobenzofurazan at pH 8.6 with Teorell and Stenhagen buffer for 20 min at 70°C, followed by the addition of 0.1 N sulfuric acid. High-performance liquid chromatography analysis used a LiChrospher RP 18 column with a size of 125×40 mm ID; mobile phase, acetonitrile: 0.01% phosphoric acid (52:48); flow rate of 1 mL/min; and emission and excitation wavelength for glibenclamide and amlodipine at 346 and 300 nm and 535 and 480 nm, respectively. The concentration ranges were 0.1-20 ng/mL for amlodipine and 1-200 ng/mL for glibenclamide. The average ranges of percentage coefficient of variation and percentage difference were 1.76%-14.62% and 4.48%-11.18% for amlodipine and 0.56%-11.92% and 2.92%-12.75% for glibenclamide. This sensitive and simultaneous bioanalytical method for amlodipine and glibenclamide fulfills the EMA requirements.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"125 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78474419","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 : 2022-01-01DOI: 10.29090/psa.2022.06.22.280
S. Tinrat
The rapidly growing antimicrobial resistance is a global problem. This made it necessary to search for new antimicrobial agents. In present study, agar well diffusion, broth microdilution and time-kill kinetic assays were used to determine the antimicrobial activities of the extracts against seven pathogens. The results showed that 75% acetonic and 95% ethanolic extracts of Garcinia cowa Roxb. leaves (GCL) showed the strongest broad-spectrum antibacterial effect towards both Gram-negative and Gram-positive bacteria with 9.67±0.57-22.83±0.45 mm of inhibition zones and MIC/MBC values ranging from 25-100 mg/mL. 95% ethanolic extract revealed the inhibiting and killing actions at rapid first 3 h of incubation, depending on concentration of extracts and had the best capacity to inhibit biofilm formation of all tested bacteria (gastrointestinal and urinary pathogens) with 73.43 0.20-90.14 0.10%. Pseudomonas aeruginosa ATCC 27853 displayed the highest sensitivity with all GCL extracts. Interestingly, 95% ethanolic extract and ampicillin combination showed a synergistic effect at FICI value of 0.0313-0.5 (1/16MIC×1/32MIC-1MIC×1/4MIC) against all microorganisms. The bioactive potency of constituents of the 95% ethanolic extract (saponins, tannins, flavonoids, steroids, terpenoids and alkaloids) play an important roles in the observed antibacterial, anti-biofilm and synergistic activities. The findings indicated that Garcinia cowa Roxb. leaves extracts had the strong broad-spectrum antibacterial, anti-biofilm and synergistic activities. Crude extracts possess time and concentration-dependent bactericidal actions. Thus, the present results that G. cowa Roxb. leaves extracts had potential as a natural alternative antimicrobials for fighting bacterial infections.
{"title":"Phytochemical screenings, antibacterial and anti-biofilm activities of Garcinia cowa Roxb. leaves extracts and its synergistic effect with antibiotic","authors":"S. Tinrat","doi":"10.29090/psa.2022.06.22.280","DOIUrl":"https://doi.org/10.29090/psa.2022.06.22.280","url":null,"abstract":"The rapidly growing antimicrobial resistance is a global problem. This made it necessary to search for new antimicrobial agents. In present study, agar well diffusion, broth microdilution and time-kill kinetic assays were used to determine the antimicrobial activities of the extracts against seven pathogens. The results showed that 75% acetonic and 95% ethanolic extracts of Garcinia cowa Roxb. leaves (GCL) showed the strongest broad-spectrum antibacterial effect towards both Gram-negative and Gram-positive bacteria with 9.67±0.57-22.83±0.45 mm of inhibition zones and MIC/MBC values ranging from 25-100 mg/mL. 95% ethanolic extract revealed the inhibiting and killing actions at rapid first 3 h of incubation, depending on concentration of extracts and had the best capacity to inhibit biofilm formation of all tested bacteria (gastrointestinal and urinary pathogens) with 73.43 0.20-90.14 0.10%. Pseudomonas aeruginosa ATCC 27853 displayed the highest sensitivity with all GCL extracts. Interestingly, 95% ethanolic extract and ampicillin combination showed a synergistic effect at FICI value of 0.0313-0.5 (1/16MIC×1/32MIC-1MIC×1/4MIC) against all microorganisms. The bioactive potency of constituents of the 95% ethanolic extract (saponins, tannins, flavonoids, steroids, terpenoids and alkaloids) play an important roles in the observed antibacterial, anti-biofilm and synergistic activities. The findings indicated that Garcinia cowa Roxb. leaves extracts had the strong broad-spectrum antibacterial, anti-biofilm and synergistic activities. Crude extracts possess time and concentration-dependent bactericidal actions. Thus, the present results that G. cowa Roxb. leaves extracts had potential as a natural alternative antimicrobials for fighting bacterial infections.","PeriodicalId":19761,"journal":{"name":"Pharmaceutical Sciences Asia","volume":"87 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79417121","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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