Metformin (MET) ist das Mittel der Wahl zur Behandlung von Patienten mit Typ-2-Diabetes. Das Ziel... more Metformin (MET) ist das Mittel der Wahl zur Behandlung von Patienten mit Typ-2-Diabetes. Das Ziel dieser Arbeit bestand in der Entwicklung einer Tablette für MET mit einem Freisetzungsprofil, das der zirkadiane Variation der Blutzuckerwerte folgt (Arbeitshypothese). Um die Tabletten herzustellen wurden Stearinsäure (SA) und Gummi aus Tamarindensamen (TSG) mit Hydroxypropylmethylcellulose (HPMC) und Polyvinylpyrrolidon (PVP) gemischt. Zur Messung der Haftkraft wurde ein neuer Apparat gebaut, der die Scherkraft horizontal misst. Ein statistischer Versuchsplan wurde verwendet, um die Auswirkungen der verschiedenen Polymere zu untersuchen. Der Herstellungsprozess wurde optimiert. Die Arbeitshypothese wurde bestätigt. SA wurde zur Kontrolle der Freigabe qualifiziert. Die Polymere konnten zur Einstellung der Quellung und MET-Freigabe dienen. Die kombinatorischen Effekte der Polymere und die Wechselwirkung zwischen HPMC und PVP wurden verifiziert. Die in-vitro-Ergebnisse wurden teilweise d...
A convenient and low cost thin layer chromatography (TLC) - image analysis method was developed f... more A convenient and low cost thin layer chromatography (TLC) - image analysis method was developed for the determination and quantification of propyl gallate PG in some vegetable oil samples. Chromatographic separation of PG was achieved on silica gel TLC plates using benzene-ethyl acetate-methanol-glacial acetic acid as a mobile phase and Folin-Denis , s reagent for spot detection . Image analysis of the TLC plates using a scanner linked to a computer was performed to quantify the amount of PG, the approach was accurate , specific, reliable for the analysis of PG in the selected oil samples, with the possibility of analyzing simultaneously 25 samples in addition to the standard curve spots. Propyl gallate calibration curve was linear up to 1 µg/spot with a detection limit 0.16 µg/spot. The results of analyzing PG using the previous approach were compared to a standard procedure employing HPLC method.
Die Erfindung betrifft eine pharmazeutische Zusammensetzung aus zwei Abteilungen, die Metformin o... more Die Erfindung betrifft eine pharmazeutische Zusammensetzung aus zwei Abteilungen, die Metformin oder dessen Salze enthalten und den Herstellungsprozess, der eine Zwei-Puls-Freisetzung des Arzneimittels ergibt. Metformin und Hilfsstoffe aus drei Gruppen genannter hydrophiler Mittel, hydrophober Mittel und Zerfallhilfsmittel werden in einem Doppelwandmischer gemischt und weiter durch Sieben verteilt, so dass ein Pulver heraus kommt, welches zu Tabletten gepresst oder in Kapseln gefullt werden kann. Die Arzneiform liefert zwei Gipfel in einer Darstellung der Blutplasmakonzentration in Abhangigkeit von der Zeit, so dass die gewunschten biologischen Rhythmen nachgeahmt werden. Die erfindungsgemase Formulierung steigert die therapeutische Effektivitat des Arzneimittels und verbessert die Patienten Compliance infolge der einmal taglichen Anwendung.
In Syria, high-Sensitive C-Reactive (hsCRP), folate, and, other health risk data in young women a... more In Syria, high-Sensitive C-Reactive (hsCRP), folate, and, other health risk data in young women are limited. This cross-sectional study evaluates hsCRP and folate levels along with anthropometric characteristics, lifestyle factors and some biomarkers linked to cardiovascular disease (CVD) risk factors in healthy female students (n = 207, 18–25 years old). Among participants, hsCRP level was at average or high risk of CVD in 20.7% and 2.5% respectively and it was significantly higher in participants who had high body mass index (BMI) (Nonparametric statistical tests, p value
In Syria, health risk data on young males are limited. Hence, the aim of the present study was to... more In Syria, health risk data on young males are limited. Hence, the aim of the present study was to evaluate cardiovascular disease (CVD) risk factors along with C-reactive protein levels measured by high-sensitive method (hsCRP) in a group of healthy males of university students (n=101, 18–25 years old). Participants’ anthropometric characteristics; alcohol drinking, smoking, and physical activity habits; parents medical history; and some inflammatory biomarkers were inspected for their associations with hsCRP. Results. Regarding hsCRP level, 19 participants were at average (1–3 mg/L) and 13 were at high (>3 mg/L) risk of CVD. Nonparametric statistical tests (p value < 0.05) revealed that hsCRP level was higher in participants who had high body mass index (BMI), had high BMI with high waist-to-hip ratio (WHR), or did not practice sport frequently. Unexpectedly, it did not vary between smokers and nonsmokers. In general, it correlated positively with anthropometric and erythrocy...
Abstract Discovering of new and effective antibiotics is a major issue facing scientists today. L... more Abstract Discovering of new and effective antibiotics is a major issue facing scientists today. Luckily, the development of computer science offers new methods to overcome this issue. In this study, a set of computer software was used to predict the antibacterial activity of nonantibiotic Food and Drug Administration (FDA)-approved drugs, and to explain their action by possible binding to well-known bacterial protein targets, along with testing their antibacterial activity against Gram-positive and Gram-negative bacteria. A three-dimensional virtual screening method that relies on chemical and shape similarity was applied using rapid overlay of chemical structures (ROCS) software to select candidate compounds from the FDA-approved drugs database that share similarity with 17 known antibiotics. Then, to check their antibacterial activity, disk diffusion test was applied on Staphylococcus aureus and Escherichia coli. Finally, a protein docking method was applied using HYBRID software to predict the binding ...
In Syria, a Mediterranean country, health risk data on young women are limited. The aim of study:... more In Syria, a Mediterranean country, health risk data on young women are limited. The aim of study: is to evaluate lifestyle factors, along with biomarkers related to cardiovascular risk factors in a group of university female students. Healthy female students (n = 206, 18-25 years old) participated in the study. Participant anthropometric characteristics and blood pressure were measured; alcohol drinking, smoking, and physical activity were assessed; the Mediterranean dietary pattern was evaluated; biomarkers such as glucose, uric acid, total cholesterol, triglycerides, alanine aminotransferase, red blood cell count, hemoglobin, and hematocrit were determined. Results: Among participants, 22.34% were overweight and obese; 10.2% were considered to be at high risk for type 2 diabetes, hypertension, and cardiovascular diseases associated to waist circumference (>88 cm); 47.58% have abdominal obesity; 94.17% were non-alcoholic beverage consumers; 70.87% were non-smokers; and 63% practice sport daily. The average of adherence to the Mediterranean dietary pattern was 49.14 ± 8%. No correlation was found between Mediterranean dietary score and anthropometric or biomarkers' measurements. Non-refined cereal consumption was inversely correlated with uric acid
This study optimizes the composition of an effervescent floating tablet (EFT) containing metformi... more This study optimizes the composition of an effervescent floating tablet (EFT) containing metformin hydrochloride (M) regarding tablet hardness (H), time to dissolve 60% of the embedded drug (t60%), and buoyancy, the floating lag time (FLT). A simplex lattice experimental design has been used comprising different levels of hydroxypropylmethylcellulose (HPMC), stearic acid (SA), sodium bicarbonate (SB) as tablet matrix components, and hardness (H), t60%, FLT as response variables. Two models have been applied to decide which composition will result in Fickian diffusion or in overlapping of two dissolution mechanisms, diffusion and matrix erosion. Three of EFT showed the two dissolution mechanisms but most of EFT showed Fickian diffusion only. Checking the experimental response by a linear, quadratic, special cubic and cubic model using multivariate regression analysis resulted in best fit for the cubic model. Overlaying the results for the cubic model under constraints defined shows t...
The in vitro performance of gastro-retentive tablets containing metformin was investigated compri... more The in vitro performance of gastro-retentive tablets containing metformin was investigated comprising work of adhesion (W), swelling and drug release. To measure W a method was adapted to apply shear stress horizontally. Tablets based on hydroxypropylmethylcellulose (HPMC) were compared with those containing a fraction of tamarind seed gum (TSG) or its derivatives instead of HPMC. Surprisingly, the TSG as well the derivatives investigated here were lowering W but they were increasing drug release rate and swelling of the tablets. TSG of carboxyl methyl type increased both dissolution and swelling significantly whilst W remained unchanged.
In France, the regional pharmacovigilance centres manage drug overdose as adverse drug reactions ... more In France, the regional pharmacovigilance centres manage drug overdose as adverse drug reactions (ADRs) using the French ADR causality assessment method, and some poison control centres (e.g. in Paris) do likewise for the most serious cases. The aim of the study was to analyse and compare the chronological and semiological scores calculated with this method, in cases of drug overdose and ADRs in children recorded in the French pharmacovigilance ADR database. In total, 7963 cases were analysed. The distribution of semiological criteria in drug overdose and ADR cases differed significantly (G-test), with a similar result for chronological criteria (but to a lesser degree). The distinction of two types of criteria in the French ADR causality assessment method appears useful for analysing cases of drug overdose in children. This finding triggers a renewed interest in the use of this method of causality assessment of drug overdose in children, and possibly in adults.
Context: The in vitro performance of floating mucoadhesive metformin tablets was optimized using ... more Context: The in vitro performance of floating mucoadhesive metformin tablets was optimized using different polymer ratios of polyvinylpyrrolidone (PVP) tamarind seed gum (TSG) and hydroxypropylmethylcellulose (HPMC). Objective: The objectives of this investigation were to investigate the combinatorial effects of PVP, TSG and HPMC; to study the work of adhesion measured on stainless steel (W ss) and on rabbit gastric mucosa (W gm); and a comparison of hydrophilic and more hydrophobic tablets. Material and methods: In vitro performance was measured as tablet hardness (H), tablet floating lag time (FLT), time needed to release 60% of drug content (t 60%), swelling thickness (S), W ss and W gm. To compare the effects, a simplex lattice mixture design was used. Results and discussion: H, FLT, W ss and W gm were found dependent on polymer ratio. H was increased when PVP ratio was increased. FLT, W ss and W gm were increased when HPMC ratio was increased. The p value for the lack of fit for all models were greater than 0.05. An approximate linear correlation between W gm and W ss was established (R 2 ¼ 0.71). The tablets containing PVP resulted in larger H, shorter FLT and t 60% , whereas W ss and W gm were enhanced. Conclusion: The different in vitro performance of tablets containing different water-soluble polymers could be explained partially by the differences in the hydrophilic properties of the polymers and the ability of PVP to interact with HPMC or TSG. An equation established is used to conclude mucoadhesion based on adhesion measurements on stainless steel.
Metformin (MET) ist das Mittel der Wahl zur Behandlung von Patienten mit Typ-2-Diabetes. Das Ziel... more Metformin (MET) ist das Mittel der Wahl zur Behandlung von Patienten mit Typ-2-Diabetes. Das Ziel dieser Arbeit bestand in der Entwicklung einer Tablette für MET mit einem Freisetzungsprofil, das der zirkadiane Variation der Blutzuckerwerte folgt (Arbeitshypothese). Um die Tabletten herzustellen wurden Stearinsäure (SA) und Gummi aus Tamarindensamen (TSG) mit Hydroxypropylmethylcellulose (HPMC) und Polyvinylpyrrolidon (PVP) gemischt. Zur Messung der Haftkraft wurde ein neuer Apparat gebaut, der die Scherkraft horizontal misst. Ein statistischer Versuchsplan wurde verwendet, um die Auswirkungen der verschiedenen Polymere zu untersuchen. Der Herstellungsprozess wurde optimiert. Die Arbeitshypothese wurde bestätigt. SA wurde zur Kontrolle der Freigabe qualifiziert. Die Polymere konnten zur Einstellung der Quellung und MET-Freigabe dienen. Die kombinatorischen Effekte der Polymere und die Wechselwirkung zwischen HPMC und PVP wurden verifiziert. Die in-vitro-Ergebnisse wurden teilweise d...
A convenient and low cost thin layer chromatography (TLC) - image analysis method was developed f... more A convenient and low cost thin layer chromatography (TLC) - image analysis method was developed for the determination and quantification of propyl gallate PG in some vegetable oil samples. Chromatographic separation of PG was achieved on silica gel TLC plates using benzene-ethyl acetate-methanol-glacial acetic acid as a mobile phase and Folin-Denis , s reagent for spot detection . Image analysis of the TLC plates using a scanner linked to a computer was performed to quantify the amount of PG, the approach was accurate , specific, reliable for the analysis of PG in the selected oil samples, with the possibility of analyzing simultaneously 25 samples in addition to the standard curve spots. Propyl gallate calibration curve was linear up to 1 µg/spot with a detection limit 0.16 µg/spot. The results of analyzing PG using the previous approach were compared to a standard procedure employing HPLC method.
Die Erfindung betrifft eine pharmazeutische Zusammensetzung aus zwei Abteilungen, die Metformin o... more Die Erfindung betrifft eine pharmazeutische Zusammensetzung aus zwei Abteilungen, die Metformin oder dessen Salze enthalten und den Herstellungsprozess, der eine Zwei-Puls-Freisetzung des Arzneimittels ergibt. Metformin und Hilfsstoffe aus drei Gruppen genannter hydrophiler Mittel, hydrophober Mittel und Zerfallhilfsmittel werden in einem Doppelwandmischer gemischt und weiter durch Sieben verteilt, so dass ein Pulver heraus kommt, welches zu Tabletten gepresst oder in Kapseln gefullt werden kann. Die Arzneiform liefert zwei Gipfel in einer Darstellung der Blutplasmakonzentration in Abhangigkeit von der Zeit, so dass die gewunschten biologischen Rhythmen nachgeahmt werden. Die erfindungsgemase Formulierung steigert die therapeutische Effektivitat des Arzneimittels und verbessert die Patienten Compliance infolge der einmal taglichen Anwendung.
In Syria, high-Sensitive C-Reactive (hsCRP), folate, and, other health risk data in young women a... more In Syria, high-Sensitive C-Reactive (hsCRP), folate, and, other health risk data in young women are limited. This cross-sectional study evaluates hsCRP and folate levels along with anthropometric characteristics, lifestyle factors and some biomarkers linked to cardiovascular disease (CVD) risk factors in healthy female students (n = 207, 18–25 years old). Among participants, hsCRP level was at average or high risk of CVD in 20.7% and 2.5% respectively and it was significantly higher in participants who had high body mass index (BMI) (Nonparametric statistical tests, p value
In Syria, health risk data on young males are limited. Hence, the aim of the present study was to... more In Syria, health risk data on young males are limited. Hence, the aim of the present study was to evaluate cardiovascular disease (CVD) risk factors along with C-reactive protein levels measured by high-sensitive method (hsCRP) in a group of healthy males of university students (n=101, 18–25 years old). Participants’ anthropometric characteristics; alcohol drinking, smoking, and physical activity habits; parents medical history; and some inflammatory biomarkers were inspected for their associations with hsCRP. Results. Regarding hsCRP level, 19 participants were at average (1–3 mg/L) and 13 were at high (>3 mg/L) risk of CVD. Nonparametric statistical tests (p value < 0.05) revealed that hsCRP level was higher in participants who had high body mass index (BMI), had high BMI with high waist-to-hip ratio (WHR), or did not practice sport frequently. Unexpectedly, it did not vary between smokers and nonsmokers. In general, it correlated positively with anthropometric and erythrocy...
Abstract Discovering of new and effective antibiotics is a major issue facing scientists today. L... more Abstract Discovering of new and effective antibiotics is a major issue facing scientists today. Luckily, the development of computer science offers new methods to overcome this issue. In this study, a set of computer software was used to predict the antibacterial activity of nonantibiotic Food and Drug Administration (FDA)-approved drugs, and to explain their action by possible binding to well-known bacterial protein targets, along with testing their antibacterial activity against Gram-positive and Gram-negative bacteria. A three-dimensional virtual screening method that relies on chemical and shape similarity was applied using rapid overlay of chemical structures (ROCS) software to select candidate compounds from the FDA-approved drugs database that share similarity with 17 known antibiotics. Then, to check their antibacterial activity, disk diffusion test was applied on Staphylococcus aureus and Escherichia coli. Finally, a protein docking method was applied using HYBRID software to predict the binding ...
In Syria, a Mediterranean country, health risk data on young women are limited. The aim of study:... more In Syria, a Mediterranean country, health risk data on young women are limited. The aim of study: is to evaluate lifestyle factors, along with biomarkers related to cardiovascular risk factors in a group of university female students. Healthy female students (n = 206, 18-25 years old) participated in the study. Participant anthropometric characteristics and blood pressure were measured; alcohol drinking, smoking, and physical activity were assessed; the Mediterranean dietary pattern was evaluated; biomarkers such as glucose, uric acid, total cholesterol, triglycerides, alanine aminotransferase, red blood cell count, hemoglobin, and hematocrit were determined. Results: Among participants, 22.34% were overweight and obese; 10.2% were considered to be at high risk for type 2 diabetes, hypertension, and cardiovascular diseases associated to waist circumference (>88 cm); 47.58% have abdominal obesity; 94.17% were non-alcoholic beverage consumers; 70.87% were non-smokers; and 63% practice sport daily. The average of adherence to the Mediterranean dietary pattern was 49.14 ± 8%. No correlation was found between Mediterranean dietary score and anthropometric or biomarkers' measurements. Non-refined cereal consumption was inversely correlated with uric acid
This study optimizes the composition of an effervescent floating tablet (EFT) containing metformi... more This study optimizes the composition of an effervescent floating tablet (EFT) containing metformin hydrochloride (M) regarding tablet hardness (H), time to dissolve 60% of the embedded drug (t60%), and buoyancy, the floating lag time (FLT). A simplex lattice experimental design has been used comprising different levels of hydroxypropylmethylcellulose (HPMC), stearic acid (SA), sodium bicarbonate (SB) as tablet matrix components, and hardness (H), t60%, FLT as response variables. Two models have been applied to decide which composition will result in Fickian diffusion or in overlapping of two dissolution mechanisms, diffusion and matrix erosion. Three of EFT showed the two dissolution mechanisms but most of EFT showed Fickian diffusion only. Checking the experimental response by a linear, quadratic, special cubic and cubic model using multivariate regression analysis resulted in best fit for the cubic model. Overlaying the results for the cubic model under constraints defined shows t...
The in vitro performance of gastro-retentive tablets containing metformin was investigated compri... more The in vitro performance of gastro-retentive tablets containing metformin was investigated comprising work of adhesion (W), swelling and drug release. To measure W a method was adapted to apply shear stress horizontally. Tablets based on hydroxypropylmethylcellulose (HPMC) were compared with those containing a fraction of tamarind seed gum (TSG) or its derivatives instead of HPMC. Surprisingly, the TSG as well the derivatives investigated here were lowering W but they were increasing drug release rate and swelling of the tablets. TSG of carboxyl methyl type increased both dissolution and swelling significantly whilst W remained unchanged.
In France, the regional pharmacovigilance centres manage drug overdose as adverse drug reactions ... more In France, the regional pharmacovigilance centres manage drug overdose as adverse drug reactions (ADRs) using the French ADR causality assessment method, and some poison control centres (e.g. in Paris) do likewise for the most serious cases. The aim of the study was to analyse and compare the chronological and semiological scores calculated with this method, in cases of drug overdose and ADRs in children recorded in the French pharmacovigilance ADR database. In total, 7963 cases were analysed. The distribution of semiological criteria in drug overdose and ADR cases differed significantly (G-test), with a similar result for chronological criteria (but to a lesser degree). The distinction of two types of criteria in the French ADR causality assessment method appears useful for analysing cases of drug overdose in children. This finding triggers a renewed interest in the use of this method of causality assessment of drug overdose in children, and possibly in adults.
Context: The in vitro performance of floating mucoadhesive metformin tablets was optimized using ... more Context: The in vitro performance of floating mucoadhesive metformin tablets was optimized using different polymer ratios of polyvinylpyrrolidone (PVP) tamarind seed gum (TSG) and hydroxypropylmethylcellulose (HPMC). Objective: The objectives of this investigation were to investigate the combinatorial effects of PVP, TSG and HPMC; to study the work of adhesion measured on stainless steel (W ss) and on rabbit gastric mucosa (W gm); and a comparison of hydrophilic and more hydrophobic tablets. Material and methods: In vitro performance was measured as tablet hardness (H), tablet floating lag time (FLT), time needed to release 60% of drug content (t 60%), swelling thickness (S), W ss and W gm. To compare the effects, a simplex lattice mixture design was used. Results and discussion: H, FLT, W ss and W gm were found dependent on polymer ratio. H was increased when PVP ratio was increased. FLT, W ss and W gm were increased when HPMC ratio was increased. The p value for the lack of fit for all models were greater than 0.05. An approximate linear correlation between W gm and W ss was established (R 2 ¼ 0.71). The tablets containing PVP resulted in larger H, shorter FLT and t 60% , whereas W ss and W gm were enhanced. Conclusion: The different in vitro performance of tablets containing different water-soluble polymers could be explained partially by the differences in the hydrophilic properties of the polymers and the ability of PVP to interact with HPMC or TSG. An equation established is used to conclude mucoadhesion based on adhesion measurements on stainless steel.
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