Pub Date : 2017-07-23DOI: 10.21065/1920-4159.1000246
M. Xue, Y. Cheng, L. Xu, L. Zhang
Curcumin is the yellow pigment of turmeric. In addition to its positive safety profile, curcumin is reported to have beneficial pharmacologic effects as an antioxidant, antitumor, and anti-inflammatory agent, along with other promising pharmacologic effects on the cardiovascular and digestive systems. Curcumin is poorly absorbed, which limits its value in clinical application. In order to improve the poor bioavailability and enhance the pharmacologic action of curcumin, we studied its absorption mechanisms in an animal model in vivo and in a Caco-2 cell model in vitro. The absorption rates of curcumin at different concentrations in blank intestinal juice were not the same. The absorption rate of curcumin solution at a concentration of 5 μg/mL was the highest, followed by 10 μg/mL, and the minimum absorption occurred at 20 μg/mL. The absorption rate in the ileum decreased as the concentration of curcumin increased, which reminds us that absorption in the ileum does not result from simple passive diffusion but rather shows the characteristics of active transport. Curcumin may be a P-glycoprotein (P-gp) substrate and thus may be affected by P-gp efflux, and thus the addition of a P-gp inhibitor such as verapamil can promote the intestinal absorption of curcumin. A Caco-2 cell model was established to accurately study curcumin’s absorption mechanisms. We found that, for curcumin in a 5 μg/mL solution, the Caco-2 cell monolayer transport was passive, and when the concentration was increased to 10 μg/mL efflux influenced the transport but not extensively. The transport mode of curcuminthe appears to be passive diffusion at concentrations 10 μg/mL active transport is involved. In summary, curcumin is transported by a combination of passive diffusion and active transport, curcumin is a substrate for the intestinal transporter P-gp, and intestinal absorption of curcumin is regulated by intestinal P-gp transport.
{"title":"Study of the Intestinal Absorption Characteristics of Curcumin In Vivoand In Vitro","authors":"M. Xue, Y. Cheng, L. Xu, L. Zhang","doi":"10.21065/1920-4159.1000246","DOIUrl":"https://doi.org/10.21065/1920-4159.1000246","url":null,"abstract":"Curcumin is the yellow pigment of turmeric. In addition to its positive safety profile, curcumin is reported to have beneficial pharmacologic effects as an antioxidant, antitumor, and anti-inflammatory agent, along with other promising pharmacologic effects on the cardiovascular and digestive systems. Curcumin is poorly absorbed, which limits its value in clinical application. In order to improve the poor bioavailability and enhance the pharmacologic action of curcumin, we studied its absorption mechanisms in an animal model in vivo and in a Caco-2 cell model in vitro. The absorption rates of curcumin at different concentrations in blank intestinal juice were not the same. The absorption rate of curcumin solution at a concentration of 5 μg/mL was the highest, followed by 10 μg/mL, and the minimum absorption occurred at 20 μg/mL. The absorption rate in the ileum decreased as the concentration of curcumin increased, which reminds us that absorption in the ileum does not result from simple passive diffusion but rather shows the characteristics of active transport. Curcumin may be a P-glycoprotein (P-gp) substrate and thus may be affected by P-gp efflux, and thus the addition of a P-gp inhibitor such as verapamil can promote the intestinal absorption of curcumin. A Caco-2 cell model was established to accurately study curcumin’s absorption mechanisms. We found that, for curcumin in a 5 μg/mL solution, the Caco-2 cell monolayer transport was passive, and when the concentration was increased to 10 μg/mL efflux influenced the transport but not extensively. The transport mode of curcuminthe appears to be passive diffusion at concentrations 10 μg/mL active transport is involved. In summary, curcumin is transported by a combination of passive diffusion and active transport, curcumin is a substrate for the intestinal transporter P-gp, and intestinal absorption of curcumin is regulated by intestinal P-gp transport.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"56 1","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2017-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90598703","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 : 2017-06-30DOI: 10.21065/1920-4159.1000247
A. Maa, Al'-Kadi Km, Alawdi Sm
The aim of this study was to determine the prescriptions pattern of antibiotic in paediatric in-patient department of General Thamar Hospital in Yemen. The method was prospective and observational study which was carried out for 2 months duration between March- April 2015. Patient’s data was being recorded in a specific format and results were analysed by descriptive statistic and expressed as mean ± SD. The result was out of 148 patients, 95 prescriptions were taken antibiotics, where 59 were male child and 36 were female child. The mean age of patient on antibiotic was 1.49 ± 2.12 years. The total antibiotics were prescribed to the patients was 194 and the average number of antibiotics per prescription was 2.04 ± 0.55. The most prevalent diseases among studied patients was bronchitis (27.4%) followed by asthma (15.8%), and lower respiratory tract infection (9.5%). Cephalosporin (51.5%) was found to be widely prescribed antibiotic followed by penicillin (25.3), aminoglycosides (13.4), metronidazole (5.7%), vancomycin (2.6%), and azithromycin. The most of the antibiotics were administered for inpatients 183 (94.3%) prescribed parenteral, and 11 (5.7%) prescribed oral. The conclusion of study was Ceftriaxone and penicillin was identified to be the most prescribed medications in the General Thamar hospital. The selection of antibiotic should be based on culture and sensitivity test to avoid the development of bacterial resistance; however prescription of antibiotic should be done in accordance with WHO guidelines and rational strategies.
{"title":"Study of Antibiotics Prescribing Pattern in Paediatric Patients of ThamarProvince, in Republic of Yemen","authors":"A. Maa, Al'-Kadi Km, Alawdi Sm","doi":"10.21065/1920-4159.1000247","DOIUrl":"https://doi.org/10.21065/1920-4159.1000247","url":null,"abstract":"The aim of this study was to determine the prescriptions pattern of antibiotic in paediatric in-patient department of General Thamar Hospital in Yemen. The method was prospective and observational study which was carried out for 2 months duration between March- April 2015. Patient’s data was being recorded in a specific format and results were analysed by descriptive statistic and expressed as mean ± SD. The result was out of 148 patients, 95 prescriptions were taken antibiotics, where 59 were male child and 36 were female child. The mean age of patient on antibiotic was 1.49 ± 2.12 years. The total antibiotics were prescribed to the patients was 194 and the average number of antibiotics per prescription was 2.04 ± 0.55. The most prevalent diseases among studied patients was bronchitis (27.4%) followed by asthma (15.8%), and lower respiratory tract infection (9.5%). Cephalosporin (51.5%) was found to be widely prescribed antibiotic followed by penicillin (25.3), aminoglycosides (13.4), metronidazole (5.7%), vancomycin (2.6%), and azithromycin. The most of the antibiotics were administered for inpatients 183 (94.3%) prescribed parenteral, and 11 (5.7%) prescribed oral. The conclusion of study was Ceftriaxone and penicillin was identified to be the most prescribed medications in the General Thamar hospital. The selection of antibiotic should be based on culture and sensitivity test to avoid the development of bacterial resistance; however prescription of antibiotic should be done in accordance with WHO guidelines and rational strategies.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"42 1","pages":"1-4"},"PeriodicalIF":0.0,"publicationDate":"2017-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81541074","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 : 2017-06-14DOI: 10.21065/1920-4159.1000245
Poonam Vasantrao Mogal, D. Derle
Cefixime is BCS class 2/4 drug whose oral absorption is limited by its solubility and/or permeability. The use of HPBCD is proved to be better complexing agent for enhancing solubility as well as permeability of drugs. At the same time spray drying is the one step continuous drying process making it attractive technique for industrial application. Therefore, the current study was undertaken to unite the use of HPBCD and spray drying alongside with optimizing it through Design of Experiments (DOE) approach by means of Box–Behnken design for the benefit of drugs like Cefixime that needs to be redeveloped for better therapeutic efficacy. These formulations were evaluated by solubility studies, process yield and total drug content with help of independent variables like air inlet temperature, aspirator rate and pump feed rate. The optimized formulation was also characterized by SEM, FTIR analysis and in vitro dissolution study. Inlet air temperature was found to be the most important parameter for the spray dried material characteristics, followed by the aspirator flow rate whereas Feed flow rate was found less significant. The results indicate that formulation parameters are at least important than process parameters when designing a proper process for spray drying inclusion complex. The optimized formulation was also then compressed into tablet and was compared with marketed formulation where it showed comparable dissolution.
{"title":"Optimization and Formulation Development of Cefixime Complex UsingSpray Drying Technique: DOE Approach","authors":"Poonam Vasantrao Mogal, D. Derle","doi":"10.21065/1920-4159.1000245","DOIUrl":"https://doi.org/10.21065/1920-4159.1000245","url":null,"abstract":"Cefixime is BCS class 2/4 drug whose oral absorption is limited by its solubility and/or permeability. The use of HPBCD is proved to be better complexing agent for enhancing solubility as well as permeability of drugs. At the same time spray drying is the one step continuous drying process making it attractive technique for industrial application. Therefore, the current study was undertaken to unite the use of HPBCD and spray drying alongside with optimizing it through Design of Experiments (DOE) approach by means of Box–Behnken design for the benefit of drugs like Cefixime that needs to be redeveloped for better therapeutic efficacy. These formulations were evaluated by solubility studies, process yield and total drug content with help of independent variables like air inlet temperature, aspirator rate and pump feed rate. The optimized formulation was also characterized by SEM, FTIR analysis and in vitro dissolution study. Inlet air temperature was found to be the most important parameter for the spray dried material characteristics, followed by the aspirator flow rate whereas Feed flow rate was found less significant. The results indicate that formulation parameters are at least important than process parameters when designing a proper process for spray drying inclusion complex. The optimized formulation was also then compressed into tablet and was compared with marketed formulation where it showed comparable dissolution.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"18 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2017-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85426322","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 : 2017-06-06DOI: 10.21065/1920-4159.1000244
S. Bakhshaei
Anxiety, stress and depression are characterized by widespread and highly comorbid psychiatric conditions in the world that are defined as a negative emotional experience and are associated with biochemical, cognitive, behavioural and psychological changes. Herbal medicine has been widely used among suffering and anxiety disorders since ancient times. The modern pharmacological therapy is costly and associated with multiple side effects resulting in patient non-compliance. Thus there is a need to explore alternative therapies particularly from herbal sources as these are cost effective and possess minimal side effects. This review investigates the available studies on the pharmacological effects of some medicinal plants on depression. The studied plants include: Melissa officinalis, Lavandula angustifolia, Cinnamomum zeylanicum, Viola odorata, Echium amoneum, Valeriana officinalis, Aloysia triphylla, Citrus aurantium and Salix aegyptica. The present article is a comprehensive review of the pharmacological properties, especially anti-depressants, anti-anxiety of nine medicinal plants that could be useful for clinical studies to produce an herbal product which use treat depression.
{"title":"Phyto-Pharmacological Effect of Nine Medicinal Plants as a TraditionalTreatment on Depression","authors":"S. Bakhshaei","doi":"10.21065/1920-4159.1000244","DOIUrl":"https://doi.org/10.21065/1920-4159.1000244","url":null,"abstract":"Anxiety, stress and depression are characterized by widespread and highly comorbid psychiatric conditions in the world that are defined as a negative emotional experience and are associated with biochemical, cognitive, behavioural and psychological changes. Herbal medicine has been widely used among suffering and anxiety disorders since ancient times. The modern pharmacological therapy is costly and associated with multiple side effects resulting in patient non-compliance. Thus there is a need to explore alternative therapies particularly from herbal sources as these are cost effective and possess minimal side effects. This review investigates the available studies on the pharmacological effects of some medicinal plants on depression. The studied plants include: Melissa officinalis, Lavandula angustifolia, Cinnamomum zeylanicum, Viola odorata, Echium amoneum, Valeriana officinalis, Aloysia triphylla, Citrus aurantium and Salix aegyptica. The present article is a comprehensive review of the pharmacological properties, especially anti-depressants, anti-anxiety of nine medicinal plants that could be useful for clinical studies to produce an herbal product which use treat depression.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"8 1","pages":"1-5"},"PeriodicalIF":0.0,"publicationDate":"2017-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84490322","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 : 2017-05-25DOI: 10.21065/1920-4159.1000243
S. El-Adl, M. El-Sadek, Saeed Nm
A new spectrophotometric method is described for the determination of nicorandil in bulk and pharmaceutical dosage form. It is based on the reduction of nitrate in nicorandil to nitrite ion by using vanadium chloride, and reduction of phosphomolybdic acid to phospho-molybdenum blue complex by sodium sulfide, phospho-molybdenum blue complex is then oxidized by nitrite ion leading to a decrease in blue color intensity which found to be directly proportional to the concentration of nicorandil. Maximum absorbance was measured at 827 nm. Effect of acidity, volume of Sodium Sulfide, stability of complex, volume of vanadium chloride, time and temperature of the reaction were completely studied. The proposed method was satisfactorily applied for the determination of the drug in both bulk and pharmaceutical forms, the calibration curve was linear over the range (60–200 μg/ml) and the results were compared statistically with reference methods.
{"title":"Spectrophotometric Determination of Nicorandil in Bulk andPharmaceutical Formulation Using Phospho-Molybdenum Blue Complex","authors":"S. El-Adl, M. El-Sadek, Saeed Nm","doi":"10.21065/1920-4159.1000243","DOIUrl":"https://doi.org/10.21065/1920-4159.1000243","url":null,"abstract":"A new spectrophotometric method is described for the determination of nicorandil in bulk and pharmaceutical dosage form. It is based on the reduction of nitrate in nicorandil to nitrite ion by using vanadium chloride, and reduction of phosphomolybdic acid to phospho-molybdenum blue complex by sodium sulfide, phospho-molybdenum blue complex is then oxidized by nitrite ion leading to a decrease in blue color intensity which found to be directly proportional to the concentration of nicorandil. Maximum absorbance was measured at 827 nm. Effect of acidity, volume of Sodium Sulfide, stability of complex, volume of vanadium chloride, time and temperature of the reaction were completely studied. The proposed method was satisfactorily applied for the determination of the drug in both bulk and pharmaceutical forms, the calibration curve was linear over the range (60–200 μg/ml) and the results were compared statistically with reference methods.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"15 1","pages":"1-7"},"PeriodicalIF":0.0,"publicationDate":"2017-05-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85110087","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 : 2017-05-10DOI: 10.21065/1920-4159.1000241
Yeo Qq, Chong Jbk, Chung Wl, C. Ll
Singapore is facing an imminent silver tsunami with an increase in the percentage of older people aged 65 years and older, from 8.4% in 2006 to 12.4% in 2016 [1]. The number of chronic illnesses and frequency of medication use increase with age, which often result in polypharmacy and Drug Related Problems (DRPs) that can lead to significant drug related morbidity and mortality [2]. Pharmacists play a pivotal role in the healthcare team to manage polypharmacy, improve patient health outcomes and reduce drug related hospital readmissions [3]. Studies have also suggested that collaborations between hospital and community pharmacies can increase the detection and resolution of DRPs [4].
随着65岁及以上老年人比例从2006年的8.4%上升到2016年的12.4%，新加坡正面临迫在眉睫的“银发海啸”[1]。慢性疾病的数量和用药频率随着年龄的增长而增加，这往往导致多重用药和药物相关问题(Drug Related Problems, DRPs)，从而导致显著的药物相关发病率和死亡率[2]。药剂师在医疗团队中发挥着关键作用，管理多种用药，改善患者健康结果，减少与药物相关的再入院率[3]。研究还表明，医院和社区药房之间的合作可以提高DRPs的检测和解决[4]。
{"title":"Drug Related Problems Detected During a Brown Bag Review by aPharmacistâÂÂInitiated Octo-Pills Programme in Singapore","authors":"Yeo Qq, Chong Jbk, Chung Wl, C. Ll","doi":"10.21065/1920-4159.1000241","DOIUrl":"https://doi.org/10.21065/1920-4159.1000241","url":null,"abstract":"Singapore is facing an imminent silver tsunami with an increase in the percentage of older people aged 65 years and older, from 8.4% in 2006 to 12.4% in 2016 [1]. The number of chronic illnesses and frequency of medication use increase with age, which often result in polypharmacy and Drug Related Problems (DRPs) that can lead to significant drug related morbidity and mortality [2]. Pharmacists play a pivotal role in the healthcare team to manage polypharmacy, improve patient health outcomes and reduce drug related hospital readmissions [3]. Studies have also suggested that collaborations between hospital and community pharmacies can increase the detection and resolution of DRPs [4].","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"25 1","pages":"1-4"},"PeriodicalIF":0.0,"publicationDate":"2017-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90461069","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 : 2017-03-07DOI: 10.21065/1920-4159.1000239
A. Salahuddin, M. Katary
Oxidative stress is a major cause for development and progression of diabetic mediated peripheral and central complications. The aim of this work is to evaluate the role of Grape Seed Proanthocyanidin (GSPE) extract in attenuating diabetic complications. Forty-five adult male Wistar rats were divided into three groups. Control, non-treated diabetic and diabetic rats treated with GSPE. Diabetes was induced by intraperitoneal injection of streptozotocin. After eight weeks; urine, blood and brain, heart, kidneys, liver tissue homogenate parameters were evaluated. The results showed a reduction in both renal and hepatic function in non-treated group as well as an elevated serum inflammatory markers (TNF-α, hs-CRP and IL-6). In addition, there were an elevation in both serum and different tissue homogenate oxidative stress parameters (SOD, GPx, Catalase and MDA). Treatments with GSPE improve the oxidative stress status in different tissue and improve renal and kidney functions. These finding suggested that GSPE is effective as adjuvant therapy for protection from diabetic complications as well as its potent antioxidant and anti-inflammatory activity.
{"title":"Effects of Grape Seed Proanthocyanidin Extract in Attenuating DiabeticComplications in Streptozotocin-Induced Diabetic Rats","authors":"A. Salahuddin, M. Katary","doi":"10.21065/1920-4159.1000239","DOIUrl":"https://doi.org/10.21065/1920-4159.1000239","url":null,"abstract":"Oxidative stress is a major cause for development and progression of diabetic mediated peripheral and central complications. The aim of this work is to evaluate the role of Grape Seed Proanthocyanidin (GSPE) extract in attenuating diabetic complications. Forty-five adult male Wistar rats were divided into three groups. Control, non-treated diabetic and diabetic rats treated with GSPE. Diabetes was induced by intraperitoneal injection of streptozotocin. After eight weeks; urine, blood and brain, heart, kidneys, liver tissue homogenate parameters were evaluated. The results showed a reduction in both renal and hepatic function in non-treated group as well as an elevated serum inflammatory markers (TNF-α, hs-CRP and IL-6). In addition, there were an elevation in both serum and different tissue homogenate oxidative stress parameters (SOD, GPx, Catalase and MDA). Treatments with GSPE improve the oxidative stress status in different tissue and improve renal and kidney functions. These finding suggested that GSPE is effective as adjuvant therapy for protection from diabetic complications as well as its potent antioxidant and anti-inflammatory activity.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"27 1","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2017-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87360624","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 : 2017-02-25DOI: 10.21065/1920-4159.1000237
Koji Komori, M. Fukuda, T. Matsuura, Shota Yamada, Shinobu Mitamura, Reiko Konishi, Maho Kikuta, Masahiro Takada, M. Shuto, Yumiko Hane
Consumption of alcohol concomitantly with a drug may increase absorption of the active ingredients, leading to dose dumping. In this study, ibuprofen was administered to mice along with rice wine or beer. Blood concentrations of ibuprofen were lower when taken with alcohol than when taken with water. The ibuprofen formulation was suspended in rice wine, beer, 15% ethanol, or 20% mannitol, and then administered to male ddY mice. In a separate experiment, mice were pretreated with rice wine per os (p.o.) or loperamide (p.o.) 30 min before administering ibuprofen with water. Ibuprofen doses for oral administration and tail vein injection were 40 mg/kg and 0.75 mg/kg, respectively. Maximum blood concentrations (Cmax) were lower in mice pretreated with rice wine or beer. There were no significant differences in ibuprofen clearance between animals pretreated with rice wine by tail vein injection and controls. Pretreatment with 20% mannitol or loperamide lowered the blood concentration of ibuprofen. These results suggest that alcoholic beverages affect drug pharmacokinetics. In particular, absorption may be affected by an increase in osmotic pressure and inhibition of gastrointestinal transit.
{"title":"Effect of Alcoholic Beverages on Drug Absorption: Blood ConcentrationProfile of Ibuprofen in Mice","authors":"Koji Komori, M. Fukuda, T. Matsuura, Shota Yamada, Shinobu Mitamura, Reiko Konishi, Maho Kikuta, Masahiro Takada, M. Shuto, Yumiko Hane","doi":"10.21065/1920-4159.1000237","DOIUrl":"https://doi.org/10.21065/1920-4159.1000237","url":null,"abstract":"Consumption of alcohol concomitantly with a drug may increase absorption of the active ingredients, leading to dose dumping. In this study, ibuprofen was administered to mice along with rice wine or beer. Blood concentrations of ibuprofen were lower when taken with alcohol than when taken with water. The ibuprofen formulation was suspended in rice wine, beer, 15% ethanol, or 20% mannitol, and then administered to male ddY mice. In a separate experiment, mice were pretreated with rice wine per os (p.o.) or loperamide (p.o.) 30 min before administering ibuprofen with water. Ibuprofen doses for oral administration and tail vein injection were 40 mg/kg and 0.75 mg/kg, respectively. Maximum blood concentrations (Cmax) were lower in mice pretreated with rice wine or beer. There were no significant differences in ibuprofen clearance between animals pretreated with rice wine by tail vein injection and controls. Pretreatment with 20% mannitol or loperamide lowered the blood concentration of ibuprofen. These results suggest that alcoholic beverages affect drug pharmacokinetics. In particular, absorption may be affected by an increase in osmotic pressure and inhibition of gastrointestinal transit.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"28 1","pages":"1-5"},"PeriodicalIF":0.0,"publicationDate":"2017-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81288651","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 : 2017-02-22DOI: 10.21065/1920-4159.1000238
Ghare Jl, Mundada As
The objective of this work was to assess the new polymer obtained from natural source (Helianthus annuus) in the formation of floating in situ gel of Ranitidine HCl. Low Methoxy Pectin (LMP), calcium carbonate, sodium citrate, D-mannitol, methylparaben and propylparaben were utilized in developing floating in situ gelling formulations. The developed formulations were evaluated for various physicochemical properties like viscosity, floating lag time, and duration of floating, in vitro gelation and in vitro drug release. The 32 full factorial design was applied wherein concentration of LMP and calcium carbonate were considered as independent variables whereas floating lag time and drug release after 8 h (Q8 ) were taken as dependent variables. All formulations (F1–F9) exhibited floating within 60 s and remained floated for around 24 h. All the formulations were pourable before coming in contact with gastric fluid. It was seen that floating lag time and cumulative percentage drug release was influenced by concentration of LMP and calcium carbonate. Formulation F5 showed optimum floating lag time (37 s) and drug release after 8 h (98.09%) amongst developed in situ gels. Thus it can be concluded that Ranitidine HCl can be formulated as floating in situ gel using LMP as a gelling polymer to sustain the drug release for 8 h.
{"title":"Evaluation of Novel Polymer in the Development of Floating In situ GellingSystem","authors":"Ghare Jl, Mundada As","doi":"10.21065/1920-4159.1000238","DOIUrl":"https://doi.org/10.21065/1920-4159.1000238","url":null,"abstract":"The objective of this work was to assess the new polymer obtained from natural source (Helianthus annuus) in the formation of floating in situ gel of Ranitidine HCl. Low Methoxy Pectin (LMP), calcium carbonate, sodium citrate, D-mannitol, methylparaben and propylparaben were utilized in developing floating in situ gelling formulations. The developed formulations were evaluated for various physicochemical properties like viscosity, floating lag time, and duration of floating, in vitro gelation and in vitro drug release. The 32 full factorial design was applied wherein concentration of LMP and calcium carbonate were considered as independent variables whereas floating lag time and drug release after 8 h (Q8 ) were taken as dependent variables. All formulations (F1–F9) exhibited floating within 60 s and remained floated for around 24 h. All the formulations were pourable before coming in contact with gastric fluid. It was seen that floating lag time and cumulative percentage drug release was influenced by concentration of LMP and calcium carbonate. Formulation F5 showed optimum floating lag time (37 s) and drug release after 8 h (98.09%) amongst developed in situ gels. Thus it can be concluded that Ranitidine HCl can be formulated as floating in situ gel using LMP as a gelling polymer to sustain the drug release for 8 h.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"23 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2017-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82428092","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 : 2017-02-17DOI: 10.21065/1920-4159.1000235
Shikha Baghel Chauhan
Penetration Enhancers have vast potential and if utilized thoroughly, can be beneficial route in the drug delivery. Penetration Enhancers facilitates the drug delivery in various ways. They are therefore also referred as sorption enhancers or accelerants. This review focusses on the various enhancement techniques which are widely used to increase the bioavailability of the drugs. This review explores the various penetration enhancers with their mechanism of action and their roles in enhancement techniques. One of the reasons why the Transdermal drug delivery has not been successful compared to other delivery system, is the impervious nature of the versatile skin. It has been reported that individual penetration enhancer are not able to bring that effect which is achieved by the combination of penetration enhancer or mixture of penetration enhancer. Different penetration enhancers act at different site of action and have different mechanism of action ranging from altering metabolic activity within the skin, or exerting an influence on the thermodynamic activity of the drug in its vehicle. The major limitation in transdermal drug delivery is the diffusion of drug molecules to cross, one of the most versatile barriers of skin. A number of skin penetrations enhancers have been investigated and explored for skin penetration enhancement. Further, developments and initiatives are required to evaluate the mechanism of enhancement techniques. A thorough understanding of this penetration enhancer has been discussed and future implications explored.
{"title":"Penetration Enhancement Techniques","authors":"Shikha Baghel Chauhan","doi":"10.21065/1920-4159.1000235","DOIUrl":"https://doi.org/10.21065/1920-4159.1000235","url":null,"abstract":"Penetration Enhancers have vast potential and if utilized thoroughly, can be beneficial route in the drug delivery. Penetration Enhancers facilitates the drug delivery in various ways. They are therefore also referred as sorption enhancers or accelerants. This review focusses on the various enhancement techniques which are widely used to increase the bioavailability of the drugs. This review explores the various penetration enhancers with their mechanism of action and their roles in enhancement techniques. One of the reasons why the Transdermal drug delivery has not been successful compared to other delivery system, is the impervious nature of the versatile skin. It has been reported that individual penetration enhancer are not able to bring that effect which is achieved by the combination of penetration enhancer or mixture of penetration enhancer. Different penetration enhancers act at different site of action and have different mechanism of action ranging from altering metabolic activity within the skin, or exerting an influence on the thermodynamic activity of the drug in its vehicle. The major limitation in transdermal drug delivery is the diffusion of drug molecules to cross, one of the most versatile barriers of skin. A number of skin penetrations enhancers have been investigated and explored for skin penetration enhancement. Further, developments and initiatives are required to evaluate the mechanism of enhancement techniques. A thorough understanding of this penetration enhancer has been discussed and future implications explored.","PeriodicalId":15238,"journal":{"name":"Journal of Applied Pharmacy","volume":"46 1","pages":"1-5"},"PeriodicalIF":0.0,"publicationDate":"2017-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82690040","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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