Pub Date : 2020-12-30DOI: 10.31351/vol29iss2pp231-238
Narmin H. Amin Huseen
The Coronavirus Disease (COVID-19) has recently emerged as a human pathogen caused by SARS-CoV-2 virus was first reported from Wuhan, China, on 31 December 2019. Upon study, it has been used molecular docking to binding affinity between COVID-19 protease enzyme and flavonoids with evaluations based on docking scores calculated by AutoDock Vina. Results showed that naringin suppressed COVID-19 protease, as it has the highest binding value than other flavonoids including quercetin, hesperetin, garcina and naringenin. An important finding in this study is that naringin with neighboring poly hydroxyl groups can serve as inhibitors of COVID-19 protease bind to the S pocket of protein, it is shown that residues His163, Glu166, Asn142, His41and PHe181 participate in the hydrogen bonding and pi-pi interactions, the same as happened with decahydroisoquinolin as a novel scaffold for SARS 3CL protease inhibitors.In other hand, some of the known protease inhibitors and anti-influenza drugs docked with COVID-19 protease, it has low binding value than naringin
{"title":"Docking Study of Naringin Binding with COVID-19 Main Protease Enzyme","authors":"Narmin H. Amin Huseen","doi":"10.31351/vol29iss2pp231-238","DOIUrl":"https://doi.org/10.31351/vol29iss2pp231-238","url":null,"abstract":"The Coronavirus Disease (COVID-19) has recently emerged as a human pathogen caused by SARS-CoV-2 virus was first reported from Wuhan, China, on 31 December 2019. Upon study, it has been used molecular docking to binding affinity between COVID-19 protease enzyme and flavonoids with evaluations based on docking scores calculated by AutoDock Vina. Results showed that naringin suppressed COVID-19 protease, as it has the highest binding value than other flavonoids including quercetin, hesperetin, garcina and naringenin. An important finding in this study is that naringin with neighboring poly hydroxyl groups can serve as inhibitors of COVID-19 protease bind to the S pocket of protein, it is shown that residues His163, Glu166, Asn142, His41and PHe181 participate in the hydrogen bonding and pi-pi interactions, the same as happened with decahydroisoquinolin as a novel scaffold for SARS 3CL protease inhibitors.In other hand, some of the known protease inhibitors and anti-influenza drugs docked with COVID-19 protease, it has low binding value than naringin","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69297426","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 : 2020-06-25DOI: 10.31351/vol29iss1pp195-206
Ihab D. Hammodi, S. N. A. Alhammid
Letrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.
{"title":"Preparation and Characterization of Topical Letrozole Nanoemulsion for Breast Cancer","authors":"Ihab D. Hammodi, S. N. A. Alhammid","doi":"10.31351/vol29iss1pp195-206","DOIUrl":"https://doi.org/10.31351/vol29iss1pp195-206","url":null,"abstract":"Letrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"29 1","pages":"195-206"},"PeriodicalIF":0.0,"publicationDate":"2020-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48194028","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 : 2019-12-23DOI: 10.31351/vol28iss2pp159-164
Isra Majeed, N. Al-Shawi
The purpose of this study was to investigate the effect of omega-3 poly unsaturated fatty-acids co-administered with the therapeutic dose of lornoxicam on liver of healthy rats. Twenty-eight adults male rats weighing 180-200g were used in this study and the animals were randomly divided into four groups of seven rats each. Group I: negative control/rats intraperitoneally injected with normal saline in a dose 5ml/kg/day; Group II: rats intraperitoneally injected with lornoxicam at dose 0.7 mg/kg/day; Group III: rats orally-administered omega-3 only at a dose 185mg/kg/day; Group IV: rats co-administered omega-3 (185mg/kg/day) orally and intra-peritoneal injection of lornoxicam (0.7 mg/kg/day). Duration of treatment was 14-day; and at day 15 of the study, the liver of each rat was excised for the preparation of tissue-homogenate to be utilized for the estimation of ALT, AST, TNF-alpha and IL-10. Omega-3 can reduce signs of inflammation through the reduction- of TNF-alpha level and elevation of IL-10 with a significant reduction in ALT enzyme activity level in rats' liver tissue homogenate. In conclusion, Omega-3 poly-unsaturated fatty-acids may have a protective effect against hepatocytes inflammation when co-administered with lornoxicam.
{"title":"Effects of Omega-3 Co-Administered with Therapeutic Dose of lornoxicam on Male Rats' Liver","authors":"Isra Majeed, N. Al-Shawi","doi":"10.31351/vol28iss2pp159-164","DOIUrl":"https://doi.org/10.31351/vol28iss2pp159-164","url":null,"abstract":"The purpose of this study was to investigate the effect of omega-3 poly unsaturated fatty-acids co-administered with the therapeutic dose of lornoxicam on liver of healthy rats. Twenty-eight adults male rats weighing 180-200g were used in this study and the animals were randomly divided into four groups of seven rats each. Group I: negative control/rats intraperitoneally injected with normal saline in a dose 5ml/kg/day; Group II: rats intraperitoneally injected with lornoxicam at dose 0.7 mg/kg/day; Group III: rats orally-administered omega-3 only at a dose 185mg/kg/day; Group IV: rats co-administered omega-3 (185mg/kg/day) orally and intra-peritoneal injection of lornoxicam (0.7 mg/kg/day). Duration of treatment was 14-day; and at day 15 of the study, the liver of each rat was excised for the preparation of tissue-homogenate to be utilized for the estimation of ALT, AST, TNF-alpha and IL-10. Omega-3 can reduce signs of inflammation through the reduction- of TNF-alpha level and elevation of IL-10 with a significant reduction in ALT enzyme activity level in rats' liver tissue homogenate. In conclusion, Omega-3 poly-unsaturated fatty-acids may have a protective effect against hepatocytes inflammation when co-administered with lornoxicam.","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"28 1","pages":"159-164"},"PeriodicalIF":0.0,"publicationDate":"2019-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48108301","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 : 2019-12-22DOI: 10.31351/vol28iss2pp105-114
S. K. Ali, Eman B. H. Al-Khedairy
Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .
阿托伐他汀(ATR)是一种难溶性抗高脂血症药物;根据生物制药分类系统(BCS)，它属于II类，由于其溶解度低，生物利用度低。固体分散体吸附是提高难溶性药物溶解度和溶出度的有效技术。本研究旨在通过与普通固体分散体相比，采用固体分散体吸附技术提高ATR的溶解度和溶解速率。以聚乙二醇4000 (PEG 4000)、聚乙二醇6000 (PEG 6000)、Poloxamer188和poloxamer407为亲水性载体，以Aerosil 200、Aerosil 300和硅酸铝镁(MAS)为吸附剂。采用x射线粉末衍射(XRD)、差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)测定药物载体与吸附物的相互作用，对固体分散吸附物(SDA)配方的水溶性、产率、药物含量、溶出度、晶体结构进行了评价。所制备的SDA在各制剂中的溶解度均有显著提高。以SDA12(ATR:Poloxamer407: MAS 1:1:1)为最佳配方，其溶解度比纯ATR和固体分散体(SD4)(阿托伐他汀:Poloxamer407 1:1)分别提高了8.07倍和5.38倍，这是由于药物的润湿性增加，结晶度降低，从而提高了药物的溶解度和溶出度。
{"title":"Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique","authors":"S. K. Ali, Eman B. H. Al-Khedairy","doi":"10.31351/vol28iss2pp105-114","DOIUrl":"https://doi.org/10.31351/vol28iss2pp105-114","url":null,"abstract":"Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. \u0000 The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. \u0000 All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. \u0000 The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 \u0000fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"28 1","pages":"105-114"},"PeriodicalIF":0.0,"publicationDate":"2019-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41361997","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 : 2019-12-22DOI: 10.31351/vol28iss2pp115-123
A. M. Shanshal, Ahmed H. Ataimish
Abstract The present study aims to assess the knowledge, attitude, and experience of off-label prescribing practice among physicians in Baghdad city hospitals. This cross-sectional study was performed through the period from November 1st 2018 to March 2019 at 17 hospitals, a self-administered questionnaire was utilized to collect data from the physicians, and the targeted hospitals were randomly selected at different regions in Baghdad City area. Out of the 400 distributed questionnaires to the physicians, 383 of them were returned completed, 57.2% indicated that they were reasonably familiar with the term “off label drug”, 57.7% mentioned that the most common medical reasons for the prescribing off-label drugs were unavailability of alternatives, 67.6%, 65.5% had concerns regarding its safety and efficacy respectively, 62.7% agreed that the (MOH) authority should provide an incentive to stimulate pharmaceutical companies to perform clinical trials in Iraqi patients, 49.1% believed that clinical trials that recruit volunteers involve ethical issues. Extensive efforts are required to implant programs, regulations and guidelines to control the off-label prescribing practice among the Iraqi healthcare providers who are authorized to prescribe medications at different healthcare settings.
{"title":"Evaluation of Knowledge, Attitudes and Experience of off-label Drug Prescribing Practice among Physicians in Baghdad City Hospitals","authors":"A. M. Shanshal, Ahmed H. Ataimish","doi":"10.31351/vol28iss2pp115-123","DOIUrl":"https://doi.org/10.31351/vol28iss2pp115-123","url":null,"abstract":"Abstract \u0000The present study aims to assess the knowledge, attitude, and experience of off-label prescribing practice among physicians in Baghdad city hospitals. This cross-sectional study was performed through the period from November 1st 2018 to March 2019 at 17 hospitals, a self-administered questionnaire was utilized to collect data from the physicians, and the targeted hospitals were randomly selected at different regions in Baghdad City area. Out of the 400 distributed questionnaires to the physicians, 383 of them were returned completed, 57.2% indicated that they were reasonably familiar with the term “off label drug”, 57.7% mentioned that the most common medical reasons for the prescribing off-label drugs were unavailability of alternatives, 67.6%, 65.5% had concerns regarding its safety and efficacy respectively, 62.7% agreed that the (MOH) authority should provide an incentive to stimulate pharmaceutical companies to perform clinical trials in Iraqi patients, 49.1% believed that clinical trials that recruit volunteers involve ethical issues. Extensive efforts are required to implant programs, regulations and guidelines to control the off-label prescribing practice among the Iraqi healthcare providers who are authorized to prescribe medications at different healthcare settings.","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"28 1","pages":"115-123"},"PeriodicalIF":0.0,"publicationDate":"2019-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69297373","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 : 2018-12-07DOI: 10.31351/vol27iss2pp115-122
Hayder T. Hasan, Eman J. Kadhim
The aim of our study was to investigate the antiviral activity of the Corchorus olitorius family Tiliaceae cultivated in Iraq against measles virus, and to demonstrate an overview about chemical constituents and pharmacological activity of Corchorus olitorius L. About150 gm Leaves of Corchorus. olitorius were defatted by maceration in hexane for 24 hrs. The defatted plant materials were subjected for extraction after filtration using Soxhlet apparatus, with aqueous methanol 85% as a solvent extraction for 24 hours, the extract was filtered, and the solvent was evaporated under reduced pressure using a rotary evaporator to get a dry extract of about 12 gm. About 4 gm from the residue was suspended in 100ml water, about 3-4ml of 5% sodium hydroxide was added to obtain a basic solution having PH 10 and partitioned with ethyl acetate (3x100ml), the aqueous layer collected and evaporated to dryness. MTT-cell viability assay (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) was conducted on 96-well plates (Falcon), Vero cells were seeded at 1× 104 cells/well to obtain a multiplicity of infection (MOI 10), and at 5 × 103 cells/well to obtain a multiplicity of infection (MOI 5). Different statistical result revealed a significant antiviral activity of the aqueous layer of Corchorus olitorius leaves against measles virus. The preliminary phytochemical tests showed the presence of phenols and flavonoids in the aqueous layer of Corchorus olitorius leaves. The antiviral activity of Corchorus olitorius leaves is mainly due to the phenolics and flavonoids that detected in the aqueous layer.
{"title":"Phytochemical Investigation of Corchorus olitorius L. Leaves Cultivated in Iraq and it’s In Vitro Antiviral Activity","authors":"Hayder T. Hasan, Eman J. Kadhim","doi":"10.31351/vol27iss2pp115-122","DOIUrl":"https://doi.org/10.31351/vol27iss2pp115-122","url":null,"abstract":"The aim of our study was to investigate the antiviral activity of the Corchorus olitorius family Tiliaceae cultivated in Iraq against measles virus, and to demonstrate an overview about chemical constituents and pharmacological activity of Corchorus olitorius L. \u0000About150 gm Leaves of Corchorus. olitorius were defatted by maceration in hexane for 24 hrs. The defatted plant materials were subjected for extraction after filtration using Soxhlet apparatus, with aqueous methanol 85% as a solvent extraction for 24 hours, the extract was filtered, and the solvent was evaporated under reduced pressure using a rotary evaporator to get a dry extract of about 12 gm. About 4 gm from the residue was suspended in 100ml water, about 3-4ml of 5% sodium hydroxide was added to obtain a basic solution having PH 10 and partitioned with ethyl acetate (3x100ml), the aqueous layer collected and evaporated to dryness. MTT-cell viability assay (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide) was conducted on 96-well plates (Falcon), Vero cells were seeded at 1× 104 cells/well to obtain a multiplicity of infection (MOI 10), and at 5 × 103 cells/well to obtain a multiplicity of infection (MOI 5). \u0000Different statistical result revealed a significant antiviral activity of the aqueous layer of Corchorus olitorius leaves against measles virus. The preliminary phytochemical tests showed the presence of phenols and flavonoids in the aqueous layer of Corchorus olitorius leaves. \u0000The antiviral activity of Corchorus olitorius leaves is mainly due to the phenolics and flavonoids that detected in the aqueous layer.","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69297369","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}
Cefixime (CFX) was treated with sodium nitrite and hydrochloric acid for diazotization reaction followed by coupling with ?-Naphthol in alkaline medium to form, a yellow colored azo dye compound which exhibits maximum absorption (?max) at 412 nm where the concentration of (CFX) was determined spectrophotometrically. The optimum reaction conditions and other analytical parameters were evaluated. Beer’s law was obeyed in the concentration range of (1-20) ?g.mL-1 with a molar absorptivity of 34870.5 L.mol-1.cm-1. The limit of detection was found to be 0.1090 ?g.mL-1 and the Sandell's sensitivity value was 0.0130 ?g.cm-2. The proposed method could be successfully applied to the determination of (CFX) in pharmaceutical formulations.
{"title":"Spectrophotometric Determination of Cefixime Following Simple Diazotization and Coupling with ?-Naphthol","authors":"S. A. Darweesh","doi":"10.1234/ijps.v26i2.726","DOIUrl":"https://doi.org/10.1234/ijps.v26i2.726","url":null,"abstract":"Cefixime (CFX) was treated with sodium nitrite and hydrochloric acid for diazotization reaction followed by coupling with ?-Naphthol in alkaline medium to form, a yellow colored azo dye compound which exhibits maximum absorption (?max) at 412 nm where the concentration of (CFX) was determined spectrophotometrically. The optimum reaction conditions and other analytical parameters were evaluated. Beer’s law was obeyed in the concentration range of (1-20) ?g.mL-1 with a molar absorptivity of 34870.5 L.mol-1.cm-1. The limit of detection was found to be 0.1090 ?g.mL-1 and the Sandell's sensitivity value was 0.0130 ?g.cm-2. The proposed method could be successfully applied to the determination of (CFX) in pharmaceutical formulations.","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"26 1","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2017-12-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46125445","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 effective surface area of drug particle is increased by a reduction in the particle size. Since dissolution takes place at the surface of the solute, the larger the surface area, the further rapid is the rate of drug dissolution. Ketoprofen is class II type drug according to (Biopharmaceutics Classification System BCS) with low solubility and high permeability. The aim of this investigation was to increase the solubility and hence the dissolution rate by the preparation of ketoprofen nanosuspension using solvent evaporation method. Materials like PVP K30, poloxamer 188, HPMC E5, HPMC E15, HPMC E50, Tween 80 were used as stabilizers in perpetration of different formulas of Ketoprofen nanosuspensions. These formulas were evaluated for particle size, entrapment efficiency of drug (EE), effect of stabilizer type, effect of stabilizer concentration and in-vitro dissolution studies. All of the prepared Ketoprofen nanosuspensions formulas showed a particle size result within Nano range. The average particle size of Ketoprofen nanosuspensions formulas was observed from 9.4 nm to 997 nm. Entrapment efficiency was ranged from 79.23% to 95.41 %. The in vitro dissolution studies showed a significant (p<0.01) enhancement in dissolution rate of nanosuspension formulas compared to pure drug (drug alone) and physical mixture (drug and stabilizer). The results indicate the suitability of solvent evaporation method for Ketoprofen with improved in vitro dissolution rate and thus perhaps enhance fast onset of action for drug.
{"title":"Preparation and Evaluation of Ketoprofen Nanosuspension Using Solvent Evaporation Technique","authors":"Hayder K. Abbas, F. M. H. Wais, A. N. Abood","doi":"10.1234/IJPS.V26I2.727","DOIUrl":"https://doi.org/10.1234/IJPS.V26I2.727","url":null,"abstract":" \u0000 \u0000The effective surface area of drug particle is increased by a reduction in the particle size. Since dissolution takes place at the surface of the solute, the larger the surface area, the further rapid is the rate of drug dissolution. Ketoprofen is class II type drug according to (Biopharmaceutics Classification System BCS) with low solubility and high permeability. The aim of this investigation was to increase the solubility and hence the dissolution rate by the preparation of ketoprofen nanosuspension using solvent evaporation method. Materials like PVP K30, poloxamer 188, HPMC E5, HPMC E15, HPMC E50, Tween 80 were used as stabilizers in perpetration of different formulas of Ketoprofen nanosuspensions. These formulas were evaluated for particle size, entrapment efficiency of drug (EE), effect of stabilizer type, effect of stabilizer concentration and in-vitro dissolution studies. All of the prepared Ketoprofen nanosuspensions formulas showed a particle size result within Nano range. The average particle size of Ketoprofen nanosuspensions formulas was observed from 9.4 nm to 997 nm. Entrapment efficiency was ranged from 79.23% to 95.41 %. The in vitro dissolution studies showed a significant (p<0.01) enhancement in dissolution rate of nanosuspension formulas compared to pure drug (drug alone) and physical mixture (drug and stabilizer). The results indicate the suitability of solvent evaporation method for Ketoprofen with improved in vitro dissolution rate and thus perhaps enhance fast onset of action for drug.","PeriodicalId":14600,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2017-12-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"66008384","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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