Alireza Shafaati
Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
[ 1 ] - Rapamycin-Loaded, CapryolTM 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment
This study was planned to explore the capability of nanoemulsions (NEs) consisting of CapryolTM 90 and oleic acid for the delivery of rapamycin (RAP). Permeability and cytotoxicity of RAP-loaded NEs were also inspected. Pseudo-ternary phase diagrams were created with oleic acid and CapryolTM 90 (as oil phase) and four surfactants and co-surfactants at various weight ratios (Rsm). Selected NEs f...
[ 2 ] - Application of Guanidine Hcl to Improve Enantioseparation of a Model Basic Drug, Cetirizine, By Capillary Electrophoresis Using Sulfated Β-Cyclodextrin
A common approach in resolving enantiomers of chiral basic drugs by capillary electrophoresis (CE) is to use cyclodextrins (especially their anionic derivatives) as chiral selector in the acidic buffer (pH ≤ 3) in normal or reversed (carrier) mode. Then, some organic modifiers are added to the buffer solution if the resolution is not satisfactory. In case of cetirizine (CTN), applying the same ...
[ 3 ] - Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats
Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX1 and COX 2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al. reported 6-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 101) as a novel derivative of...
[ 4 ] - Physicochemical, stress degradation evaluation and pharmacokinetic study of AZGH102, a new synthesized COX2 inhibitors after I.V. and oral administration in male and female rats
Coxibs such as celecoxib, rofecoxib and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and slow the progress of Alzheimer’s disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 102) ...
[ 5 ] - A Simple and Specific Stability- Indicating RP-HPLC Method for Routine Assay of Adefovir Dipivoxil in Bulk and Tablet Dosage Form
A simple and reliable stability-indicating RP-HPLC method was developed and validated for analysis of adefovir dipivoxil (ADV).The chromatographic separation was performed on a C18 column using a mixture of acetonitrile-citrate buffer (10 mM at pH 5.2) 36:64 (%v/v) as mobile phase, at a flow rate of 1.5 ml/min. Detection was carried out at 260 nm and a sharp peak was obtained for ADV at a reten...
[ 6 ] - Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection
A rapid, sensitive and reproducible HPLC method was developed and validatedfor the analysis of amifostine (AMF) and/or its metabolite, WR-1065 inhuman plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite witho-phthaldialdehyde (OPA) andUVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted i...
[ 7 ] - Formulation Development and Toxicity Assessment of Triacetin Mediated Nanoemulsions as Novel Delivery Systems for Rapamycin
The aim of this investigation was to design and develop nanoemulsions as novel delivery systems for rapamycin. Phase behavior of quaternary systems composed of Traicetin (as oil), various surfactants and co-surfactants and water at different surfactant/co-surfactant weight ratios were investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase...
[ 8 ] - Study on the Effect of Solution Conditions on Heat Induced-Aggregation of Human Alpha Interferon
A major problem in the formulation of therapeutic proteins is the irreversible protein aggregation. Recombinant human interferon alpha2b (rhIFN2b) has poor stability and undergoes physical degradation. The aim of this study was to investigate the effect of solution conditions on the heat-induced aggregation of rhIFNα2b. The protein was incubated for 1 h at 40°C–70°C and for up to 240 h at 50C...
[ 9 ] - Development of a Combined Solution Formulation of Atropine Sulfate and Obidoxime Chloride for Autoinjector and Evaluation of Its Stability
Atropine (AT) and oximes, alone or in combination, have been proven greatly valuable therapeutics in the treatment of organophosphates intoxications. An injectable mixture of AT and obidoxime (OB) was formulated for administration by automatic self-injector. The aqueous single dose solution contained 275 mg obidoxime chloride and 2.5 mg atropine sulfate per 1 ml (220 mg and 2 mg per 0.8 effecti...
[ 10 ] - Rapid High Performance Liquid Chromatographic Method for Determination of Clarithromycin in Human Plasma Using Amperometric Detection: Application in Pharmacokinetic and Bioequivalence Studies
A rapid, sensitive and reproducible HPLC method using amperometric detector was developed and validated for the analysis of clarithromycin in human plasma. The separation was achieved on a monolithic silica column (MZ- C8 125×4.0 mm) using acetonitrile- methanol-potassium dihydrogen phosphate buffer (40:6:54,v/v), with pH of 7.5, as the mobile phase at a flow rate of 1.5 mL/min. The assay enabl...
[ 11 ] - Improvement of Capillary Electrophoretic Enantioseparation of Fluoxetine by a Cationic Additive
One of the problems encountered in CE separations of basic compounds is the adsorption of analytes onto the negatively charged capillary wall which could lead to poor repeatability of migration time and peak area. Additionally, separation of enantiomers of chiral of basic drugs is commonly carried out in low pH buffer which contributes to strong ionic interaction of the cationic drug ions with ...
[ 12 ] - A Reversed Phase High Performance Liquid Chromatographic Method for Determination of Rapamycin
Easily degradating and various isomeric forms of rapamycin (Sirolimus) face the determination of this compound to many challenges. In this study, we developed and validated the isocratic reversed phase high performance liquid chromatographic (RP-HPLC) method for rapamycin. Separation was performed on a C8 column (MZ, 15 × 4.6 mm, 5 µm particle size) using methanol:water (80:20 v/v) as the mobil...
[ 13 ] - Improvement of Electrophoretic Enantioseparation of Amlodipine by Polybrene
In chiral and non-chiral electrophoretic resolution of basic drugs, adsorption of analytes to negatively charged capillary wall could lead to poor repeatability of migration time and peak area. In addition, chiral resolutions of basic drugs are commonly performed in low pH buffers. Therefore, longer analysis time due to suppression of electroosmotic flow (EOF) is another dilemma. In this wor...
[ 14 ] - Exposure Assessment of the Tehran Population (Iran) to Zearalenone Mycotoxin
Zearalenone (ZEA) mycotoxin is a potent estrogenic metabolite. It is the primary toxin causing infertility, abortion or other breeding problems. A HPLC method was validated for ZEA in foods using a monolithic column with sample clean-up on an immunoaffinity column. A certified reference material (CRM) from FAPAS (UK) was analyzed. A survey of ZEA was performed on the 72 samples of rice, bread, ...
[ 15 ] - Rapamycin-Loaded, CapryolTM 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment
This study was planned to explore the capability of nanoemulsions (NEs) consisting of CapryolTM 90 and oleic acid for the delivery of rapamycin (RAP). Permeability and cytotoxicity of RAP-loaded NEs were also inspected. Pseudo-ternary phase diagrams were created with oleic acid and CapryolTM 90 (as oil phase) and four surfactants and co-surfactants at various weight ratios (Rsm). Selected NEs f...
[ 16 ] - Application of Guanidine Hcl to Improve Enantioseparation of a Model Basic Drug, Cetirizine, By Capillary Electrophoresis Using Sulfated Β-Cyclodextrin
A common approach in resolving enantiomers of chiral basic drugs by capillary electrophoresis (CE) is to use cyclodextrins (especially their anionic derivatives) as chiral selector in the acidic buffer (pH ≤ 3) in normal or reversed (carrier) mode. Then, some organic modifiers are added to the buffer solution if the resolution is not satisfactory. In case of cetirizine (CTN), applying the same ...
[ 17 ] - Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats
Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (COX) isoenzymes (COX1 and COX 2). Selective COX-2 inhibitors which are also known as coxibs provide the main therapeutic effects of NSAIDs. Zarghi et al. reported 6-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 101) as a novel derivative of...
[ 18 ] - Physicochemical, stress degradation evaluation and pharmacokinetic study of AZGH102, a new synthesized COX2 inhibitors after I.V. and oral administration in male and female rats
Coxibs such as celecoxib, rofecoxib and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and slow the progress of Alzheimer’s disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 102) ...
[ 19 ] - A Simple and Specific Stability- Indicating RP-HPLC Method for Routine Assay of Adefovir Dipivoxil in Bulk and Tablet Dosage Form
A simple and reliable stability-indicating RP-HPLC method was developed and validated for analysis of adefovir dipivoxil (ADV).The chromatographic separation was performed on a C18 column using a mixture of acetonitrile-citrate buffer (10 mM at pH 5.2) 36:64 (%v/v) as mobile phase, at a flow rate of 1.5 ml/min. Detection was carried out at 260 nm and a sharp peak was obtained for ADV at a reten...
[ 20 ] - Development and Validation of an HPLC Method for Determination of Amifostine and/or Its Metabolite (WR-1065) In Human Plasma Using OPA Derivatization and UV Detection
A rapid, sensitive and reproducible HPLC method was developed and validatedfor the analysis of amifostine (AMF) and/or its metabolite, WR-1065 inhuman plasma. The method involves the alkylation of free sulfydryl group with iodoacetic acid followed by derivatization of the drug and its metabolite witho-phthaldialdehyde (OPA) andUVdetection at 340 nm. The derivatized AMF and WR-1065 were eluted i...
[ 21 ] - Formulation Development and Toxicity Assessment of Triacetin Mediated Nanoemulsions as Novel Delivery Systems for Rapamycin
The aim of this investigation was to design and develop nanoemulsions as novel delivery systems for rapamycin. Phase behavior of quaternary systems composed of Traicetin (as oil), various surfactants and co-surfactants and water at different surfactant/co-surfactant weight ratios were investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase...
[ 22 ] - Study on the Effect of Solution Conditions on Heat Induced-Aggregation of Human Alpha Interferon
A major problem in the formulation of therapeutic proteins is the irreversible protein aggregation. Recombinant human interferon alpha2b (rhIFN2b) has poor stability and undergoes physical degradation. The aim of this study was to investigate the effect of solution conditions on the heat-induced aggregation of rhIFNα2b. The protein was incubated for 1 h at 40°C–70°C and for up to 240 h at 50C...
[ 23 ] - Development of a Combined Solution Formulation of Atropine Sulfate and Obidoxime Chloride for Autoinjector and Evaluation of Its Stability
Atropine (AT) and oximes, alone or in combination, have been proven greatly valuable therapeutics in the treatment of organophosphates intoxications. An injectable mixture of AT and obidoxime (OB) was formulated for administration by automatic self-injector. The aqueous single dose solution contained 275 mg obidoxime chloride and 2.5 mg atropine sulfate per 1 ml (220 mg and 2 mg per 0.8 effecti...
[ 24 ] - Rapid High Performance Liquid Chromatographic Method for Determination of Clarithromycin in Human Plasma Using Amperometric Detection: Application in Pharmacokinetic and Bioequivalence Studies
A rapid, sensitive and reproducible HPLC method using amperometric detector was developed and validated for the analysis of clarithromycin in human plasma. The separation was achieved on a monolithic silica column (MZ- C8 125×4.0 mm) using acetonitrile- methanol-potassium dihydrogen phosphate buffer (40:6:54,v/v), with pH of 7.5, as the mobile phase at a flow rate of 1.5 mL/min. The assay enabl...
[ 25 ] - Improvement of Capillary Electrophoretic Enantioseparation of Fluoxetine by a Cationic Additive
One of the problems encountered in CE separations of basic compounds is the adsorption of analytes onto the negatively charged capillary wall which could lead to poor repeatability of migration time and peak area. Additionally, separation of enantiomers of chiral of basic drugs is commonly carried out in low pH buffer which contributes to strong ionic interaction of the cationic drug ions with ...
[ 26 ] - A Reversed Phase High Performance Liquid Chromatographic Method for Determination of Rapamycin
Easily degradating and various isomeric forms of rapamycin (Sirolimus) face the determination of this compound to many challenges. In this study, we developed and validated the isocratic reversed phase high performance liquid chromatographic (RP-HPLC) method for rapamycin. Separation was performed on a C8 column (MZ, 15 × 4.6 mm, 5 µm particle size) using methanol:water (80:20 v/v) as the mobil...
[ 27 ] - Improvement of Electrophoretic Enantioseparation of Amlodipine by Polybrene
In chiral and non-chiral electrophoretic resolution of basic drugs, adsorption of analytes to negatively charged capillary wall could lead to poor repeatability of migration time and peak area. In addition, chiral resolutions of basic drugs are commonly performed in low pH buffers. Therefore, longer analysis time due to suppression of electroosmotic flow (EOF) is another dilemma. In this wor...
[ 28 ] - Exposure Assessment of the Tehran Population (Iran) to Zearalenone Mycotoxin
Zearalenone (ZEA) mycotoxin is a potent estrogenic metabolite. It is the primary toxin causing infertility, abortion or other breeding problems. A HPLC method was validated for ZEA in foods using a monolithic column with sample clean-up on an immunoaffinity column. A certified reference material (CRM) from FAPAS (UK) was analyzed. A survey of ZEA was performed on the 72 samples of rice, bread, ...
[ 29 ] - Pharmacokinetics and Biodistribution of Pegylated Methotrexate after IV Administration to Mice
The efficacy of methotrexate (MTX) as an antimetabolite chemotherapeutic agent highly depends on its blood circulation half-life. In our previous study, different conjugates of MTX (MTX-PEG) were synthesized, their physicochemical properties were investigated and MTX-PEG5000 was finally selected as optimum drug-conjugate for further investigations. In the current work, first the stability of MT...
[ 30 ] - Pharmacokinetics and Biodistribution of Pegylated Methotrexate after IV Administration to Mice
The efficacy of methotrexate (MTX) as an antimetabolite chemotherapeutic agent highly depends on its blood circulation half-life. In our previous study, different conjugates of MTX (MTX-PEG) were synthesized, their physicochemical properties were investigated and MTX-PEG5000 was finally selected as optimum drug-conjugate for further investigations. In the current work, first the stability of MT...
نویسندگان همکار