Pub Date : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02028
P. P. Amrutkar, S. Patil, Abhijeet N. Todarwal, M. Wagh, P. D. Kothawade, R. K. Surawase
Lamotrigine, an antiepileptic drug (AED) of the phenyltriazine class, is chemically unrelated to existing antiepileptic drugs. Lamotrigine is also used in the treatment of depression and bipolar disorder. But it is a bitter drug and slightly soluble in water. Thus, in the work under taken, an attempt was made to mask the taste and to formulate into a chewable dispersible tablet by complexation with Precirol ATO-05, which also acts as taste masking agent. Since, these tablets can be swallowed in the form of dispersion; it is suitable dosage form for paediatric and geriatric patients. Drug-Precirol ATO-05 was prepared in drug to Precirol ATO-05 ratio of 1:2, 1:1.5, 1:1, 1:0.5. The prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, taste evaluation, mouth feel, in vitro disintegration time, and in vitro dissolution studies. Tablets with Precirol ATO-05 have shown good disintegrating features, also, the dispersion not showing any bitter taste, indicate the capability of Precirol ATO-05 used, both as taste masking agents. Almost more than 90 percent of drug was released from the formulation within 1 h. Further formulations were subjected to stability testing for 3 months at temperatures 25±5oC/60±5%RH; 30±5oC/65±5%RH and 40±5oC/75±5%RH. Tablets have shown no appreciable changes with respect to taste, disintegration, and dissolution profiles. Keywords: Lamotrigine; Melt granulation; Precirol; Taste masking; Chewable dispersible tablets.
{"title":"Design and evaluation of taste masked chewable dispersible tablet of lamotrigine by melt granulation","authors":"P. P. Amrutkar, S. Patil, Abhijeet N. Todarwal, M. Wagh, P. D. Kothawade, R. K. Surawase","doi":"10.5138/IJDD.2010.0975.0215.02028","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02028","url":null,"abstract":"Lamotrigine, an antiepileptic drug (AED) of the phenyltriazine class, is chemically unrelated to existing antiepileptic drugs. Lamotrigine is also used in the treatment of depression and bipolar disorder. But it is a bitter drug and slightly soluble in water. Thus, in the work under taken, an attempt was made to mask the taste and to formulate into a chewable dispersible tablet by complexation with Precirol ATO-05, which also acts as taste masking agent. Since, these tablets can be swallowed in the form of dispersion; it is suitable dosage form for paediatric and geriatric patients. Drug-Precirol ATO-05 was prepared in drug to Precirol ATO-05 ratio of 1:2, 1:1.5, 1:1, 1:0.5. The prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, taste evaluation, mouth feel, in vitro disintegration time, and in vitro dissolution studies. Tablets with Precirol ATO-05 have shown good disintegrating features, also, the dispersion not showing any bitter taste, indicate the capability of Precirol ATO-05 used, both as taste masking agents. Almost more than 90 percent of drug was released from the formulation within 1 h. Further formulations were subjected to stability testing for 3 months at temperatures 25±5oC/60±5%RH; 30±5oC/65±5%RH and 40±5oC/75±5%RH. Tablets have shown no appreciable changes with respect to taste, disintegration, and dissolution profiles. Keywords: Lamotrigine; Melt granulation; Precirol; Taste masking; Chewable dispersible tablets.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77753202","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02019
M. El-Majri, R. Sharma
Piroxicam suppositories were prepared by using water soluble and oil soluble suppository bases. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness, melting point, disintegration and macromelting range. Invitro release study was performed USP type I apparatus using Sorensen's phosphate buffer pH 7.4 as dissolution media. The suppositories prepared with water soluble bases were within permissible range of all physical parameters. In vitro drug released from water soluble bases (hydrous PEG and anhydrous PEG) was greater than that from oil soluble bases. Keywords: Piroxicam; In vitro evaluation; Macromelting range; Water soluble bases; Suppositories
{"title":"Formulation and evaluation of piroxicam suppositories","authors":"M. El-Majri, R. Sharma","doi":"10.5138/IJDD.2010.0975.0215.02019","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02019","url":null,"abstract":"Piroxicam suppositories were prepared by using water soluble and oil soluble suppository bases. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness, melting point, disintegration and macromelting range. Invitro release study was performed USP type I apparatus using Sorensen's phosphate buffer pH 7.4 as dissolution media. The suppositories prepared with water soluble bases were within permissible range of all physical parameters. In vitro drug released from water soluble bases (hydrous PEG and anhydrous PEG) was greater than that from oil soluble bases. Keywords: Piroxicam; In vitro evaluation; Macromelting range; Water soluble bases; Suppositories","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87910727","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02027
Hima Bindu. Tvl, M. Vidyavathi, K. Kavitha, Sastry. Tp, S. Rv
Natural polymers are used as lead compounds for design of drugs in treatment of different ailments. Chitosan and gelatin have proven wound healing properties individually. As both have wound healing property, the combination of these two polymers and incorporation of drugs into the composite films may show improvement in wound healing activity. Thus, the composite films and drug loaded films were evaluated for various in vitro evaluation tests to ascertain the applicability of prepared combination for wound healing activity. The composite films were prepared with increase in gelatin concentration and the drug loaded films were prepared with increased concentrations of drug in optimized composite film. These films were evaluated for thickness, folding endurance, water absorption capacity, antibacterial activity, tensile strength, drug load, content uniformity, in vitro drug release by diffusion studies and in vivo wound healing studies by excision wound model using albino rats. The drug loaded films shown significant difference in folding endurance, water absorption capacity, antibacterial activity when compared to optimized blank composite film. There was no significant difference in thickness and tensile strength of drug loaded films when compared to blank composite films. Percentage of wound contraction was more for wounds treated with ciprofloxacin loaded composite film than blank composite film. With the above results, it was concluded that ciprofloxacin loaded chitosan-gelatin composite films had shown more wound healing property than chitosan-gelatin blank composite film and blank chitosan film without interfering in strength of film. Keywords: Ciprofloxacin; Chitosan; Gelatin; Drug loaded films; Wound healing; Tensile strength.
{"title":"Preparation and evaluation of ciprofloxacin loaded chitosan-gelatin composite films for wound healing activity","authors":"Hima Bindu. Tvl, M. Vidyavathi, K. Kavitha, Sastry. Tp, S. Rv","doi":"10.5138/IJDD.2010.0975.0215.02027","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02027","url":null,"abstract":"Natural polymers are used as lead compounds for design of drugs in treatment of different ailments. Chitosan and gelatin have proven wound healing properties individually. As both have wound healing property, the combination of these two polymers and incorporation of drugs into the composite films may show improvement in wound healing activity. Thus, the composite films and drug loaded films were evaluated for various in vitro evaluation tests to ascertain the applicability of prepared combination for wound healing activity. The composite films were prepared with increase in gelatin concentration and the drug loaded films were prepared with increased concentrations of drug in optimized composite film. These films were evaluated for thickness, folding endurance, water absorption capacity, antibacterial activity, tensile strength, drug load, content uniformity, in vitro drug release by diffusion studies and in vivo wound healing studies by excision wound model using albino rats. The drug loaded films shown significant difference in folding endurance, water absorption capacity, antibacterial activity when compared to optimized blank composite film. There was no significant difference in thickness and tensile strength of drug loaded films when compared to blank composite films. Percentage of wound contraction was more for wounds treated with ciprofloxacin loaded composite film than blank composite film. With the above results, it was concluded that ciprofloxacin loaded chitosan-gelatin composite films had shown more wound healing property than chitosan-gelatin blank composite film and blank chitosan film without interfering in strength of film. Keywords: Ciprofloxacin; Chitosan; Gelatin; Drug loaded films; Wound healing; Tensile strength.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83914319","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02020
V. Sinha, Vinay Jindal, S. Srivastava, H. Goel
Oral extended release products offer potential advantages in patient compliance and therapeutic outcomes like sustained blood levels with attenuation of adverse effects. In neuropsychiatric disorders like depression, most of the formulations serve a marketing objective rather than a clinical objective. The present investigation was aimed to develop a once daily sustained release formulation for delivery of an acid-labile, water soluble antidepressant, duloxetine HCl. The formulation was pragmatically designed using blend of natural and synthetic polymeric biomaterials that it releases the drug at alkaline pH in a sustained manner. The basic intention was to develop a tablet formulation with hydrophilic matrix core, using blend of release retarding natural biodegradable polymers such as guar gum, carbopol 71G-NF (a synthetic carbomer) and C-Pharm® gel. Barrier coating using HPMC-E5 was given to retard the initial release followed by enteric coating with HPMC-AS to prevent exposure of drug in acidic mileau of the stomach. The formulation exhibited desired release pattern and was described best-fit by Hixon-Crowell model. Stability analysis under stress conditions up to one month displayed good reproducibility. The matrix tablets successfully decreased the symptoms of depression (significant decrease in immobility time) in a rat forced swimming model. Pharmacokinetic data of the formulation revealed (tmax ~ 6 h, Cmax ~ 1157.58 ng/ml, mean AUCt~11145.04 ng*h/ml, and Ka~1.07h-1) good correlation in all animals. Keywords: Matrix tablets; Duloxetine HCl; Sustained release; Enteric coating; Hixon-crowell model
{"title":"Paradoxical effect of coating on natural guar gum blended carbomer matrix systems for the neurological depressive disorders","authors":"V. Sinha, Vinay Jindal, S. Srivastava, H. Goel","doi":"10.5138/IJDD.2010.0975.0215.02020","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02020","url":null,"abstract":"Oral extended release products offer potential advantages in patient compliance and therapeutic outcomes like sustained blood levels with attenuation of adverse effects. In neuropsychiatric disorders like depression, most of the formulations serve a marketing objective rather than a clinical objective. The present investigation was aimed to develop a once daily sustained release formulation for delivery of an acid-labile, water soluble antidepressant, duloxetine HCl. The formulation was pragmatically designed using blend of natural and synthetic polymeric biomaterials that it releases the drug at alkaline pH in a sustained manner. The basic intention was to develop a tablet formulation with hydrophilic matrix core, using blend of release retarding natural biodegradable polymers such as guar gum, carbopol 71G-NF (a synthetic carbomer) and C-Pharm® gel. Barrier coating using HPMC-E5 was given to retard the initial release followed by enteric coating with HPMC-AS to prevent exposure of drug in acidic mileau of the stomach. The formulation exhibited desired release pattern and was described best-fit by Hixon-Crowell model. Stability analysis under stress conditions up to one month displayed good reproducibility. The matrix tablets successfully decreased the symptoms of depression (significant decrease in immobility time) in a rat forced swimming model. Pharmacokinetic data of the formulation revealed (tmax ~ 6 h, Cmax ~ 1157.58 ng/ml, mean AUCt~11145.04 ng*h/ml, and Ka~1.07h-1) good correlation in all animals. Keywords: Matrix tablets; Duloxetine HCl; Sustained release; Enteric coating; Hixon-crowell model","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88453521","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02022
Ashok Kumar, Manisha Pandey, M. Koshy, S. Saraf
Fast swelling highly porous superporous hydrogels (SPH) are synthesized through a method utilizing rapid solution polymerization of acrylic acid for development of gastric retention devices. The swelling property, mechanical strength and release profile of SPH containing Metformin was investigated by changing the amount of crosslinking agents, (Bis) and AcDiSol. The results indicate that swelling ratio increases in the concentration range of 1%-2.5% w/v of Bis while beyond 2.5% w/v the swelling ratio slightly decreases but is not significant. Mechanical strength of the SPH was significantly increased by increasing the concentration of Bis from 1%-3.5% w/v. The release kinetics of SPH containing different crosslinker concentrations was measured in 0.1NHCl which was found to be consistent with the expected swelling behavior. AcDiSol was an important factor in maintaining the capillary structure required for fast swelling. Increase in AcDiSol resulted in decrease in swelling ratio of composite from 98.36±0.5% to 85.57±0.4%. As the amount of AcDiSol increases the mechanical strength increases due to increased cross linking density of the Superporous Hydrogel. This study indicates that superporous hydrogel composite possessed two properties necessary for gastric retention i.e., fast swelling and mechanical strength. Keywords: Superporous hydrogel; Croslinking agent; AcDiSol; Swelling ratio; Mechanical strength
{"title":"Synthesis of fast swelling superporous hydrogel: effect of concentration of crosslinker and acdisol on swelling ratio and mechanical strength","authors":"Ashok Kumar, Manisha Pandey, M. Koshy, S. Saraf","doi":"10.5138/IJDD.2010.0975.0215.02022","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02022","url":null,"abstract":"Fast swelling highly porous superporous hydrogels (SPH) are synthesized through a method utilizing rapid solution polymerization of acrylic acid for development of gastric retention devices. The swelling property, mechanical strength and release profile of SPH containing Metformin was investigated by changing the amount of crosslinking agents, (Bis) and AcDiSol. The results indicate that swelling ratio increases in the concentration range of 1%-2.5% w/v of Bis while beyond 2.5% w/v the swelling ratio slightly decreases but is not significant. Mechanical strength of the SPH was significantly increased by increasing the concentration of Bis from 1%-3.5% w/v. The release kinetics of SPH containing different crosslinker concentrations was measured in 0.1NHCl which was found to be consistent with the expected swelling behavior. AcDiSol was an important factor in maintaining the capillary structure required for fast swelling. Increase in AcDiSol resulted in decrease in swelling ratio of composite from 98.36±0.5% to 85.57±0.4%. As the amount of AcDiSol increases the mechanical strength increases due to increased cross linking density of the Superporous Hydrogel. This study indicates that superporous hydrogel composite possessed two properties necessary for gastric retention i.e., fast swelling and mechanical strength. Keywords: Superporous hydrogel; Croslinking agent; AcDiSol; Swelling ratio; Mechanical strength","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91423769","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02024
Prashant Khemariya, Sachin Mishra, A. Shukla, Mohit Bhargava, S. Singhai, S. Goswami
The rationale of this research was to prepare a gastroretentive drug delivery system of Ranitidine HCL. Floating Drug delivery system used to target drug release in the stomach or to the upper part of the intestine. The oral delivery of Ranitidine is tested by preparing a non-disintegrating floating dosage form, which increase its absorption in the stomach by increasing the drug’s gastric residence time. The polymer PVC and Sodium bicarbonate was used as the gas–generating agents. Sodium bicarbonate causes the tablets to floats for more then 24hr. The prepared tablets were evaluated on their physicochemical properties and drug release characters. In-vitro release studies indicate that the Ranitidine release form the floating dosage form was uniform followed zero order release. A combination of sodium bicarbonate (70mg) and citric acid (15mg) was found to achieve Optimum in vitro buoyancy. The tablets with methocel K100 were found to float for longer duration of time as compared to formulations containing methocel K15M. The drug release from the tablets was sufficiently sustained. Keywords: Ranitidine; Floating tablets; Methocel
{"title":"An Emerging Trend in Tablet Technology:- Floating Tablets of Ranitidine HCl","authors":"Prashant Khemariya, Sachin Mishra, A. Shukla, Mohit Bhargava, S. Singhai, S. Goswami","doi":"10.5138/IJDD.2010.0975.0215.02024","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02024","url":null,"abstract":"The rationale of this research was to prepare a gastroretentive drug delivery system of Ranitidine HCL. Floating Drug delivery system used to target drug release in the stomach or to the upper part of the intestine. The oral delivery of Ranitidine is tested by preparing a non-disintegrating floating dosage form, which increase its absorption in the stomach by increasing the drug’s gastric residence time. The polymer PVC and Sodium bicarbonate was used as the gas–generating agents. Sodium bicarbonate causes the tablets to floats for more then 24hr. The prepared tablets were evaluated on their physicochemical properties and drug release characters. In-vitro release studies indicate that the Ranitidine release form the floating dosage form was uniform followed zero order release. A combination of sodium bicarbonate (70mg) and citric acid (15mg) was found to achieve Optimum in vitro buoyancy. The tablets with methocel K100 were found to float for longer duration of time as compared to formulations containing methocel K15M. The drug release from the tablets was sufficiently sustained. Keywords: Ranitidine; Floating tablets; Methocel","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89365303","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02018
M. Wagh, D. Kothawade, K. Salunkhe, N. V. Chavan, Vandana R. Daga
Formulation of a convenient dosage form for administration, by considering swallowing difficulty and poor patient compliance, leads to development of orally disintegrating tablets. This are also called as orodisperse, mouth dissolving, rapidly disintegrating, and fast melt system. This disintegrates in the mouth in seconds without chewing and the need of water which is advantageous mainly for pediatrics, geriatrics and patients having difficulty in swallowing tablets and capsules. Conventional preparation methods are spray drying, freeze drying, direct compression, Molding, and sublimation while new technologies have been developed for the production of orodispersible tablets. This review depicts conventional and recent technologies that are used to prepare orodispersible tablets in detail. Keywords: Orally disintegrating tablet; Superdisintegrant; Patented technologies; Orodispersible tablets
{"title":"Techniques used in orally disintegrating drug delivery system","authors":"M. Wagh, D. Kothawade, K. Salunkhe, N. V. Chavan, Vandana R. Daga","doi":"10.5138/IJDD.2010.0975.0215.02018","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02018","url":null,"abstract":"Formulation of a convenient dosage form for administration, by considering swallowing difficulty and poor patient compliance, leads to development of orally disintegrating tablets. This are also called as orodisperse, mouth dissolving, rapidly disintegrating, and fast melt system. This disintegrates in the mouth in seconds without chewing and the need of water which is advantageous mainly for pediatrics, geriatrics and patients having difficulty in swallowing tablets and capsules. Conventional preparation methods are spray drying, freeze drying, direct compression, Molding, and sublimation while new technologies have been developed for the production of orodispersible tablets. This review depicts conventional and recent technologies that are used to prepare orodispersible tablets in detail. Keywords: Orally disintegrating tablet; Superdisintegrant; Patented technologies; Orodispersible tablets","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74720860","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02026
P. Muthuraman, S. Ravikumar, J. Vikramathithan, G. Nirmalkumar, K. Srikumar
Dietary phytohormones may influence the metabolic processes in animal cells. To determine the effect of the plant growth regulators 28-homobrassinolide, gibberellic acid and kinetin on the tissue hexokinase and some blood components in male rats. Methods: 50μg 28-bomobrassinolide, gibberellic acid and kinetin (Normal saline served as control) was injected intradermally. Hexokinase activity in several tissues and blood level of glucose, hemoglobin and cholesterol were determined 2 h after injection. 28-homobrassinolide increased hexokinase activity in all tissues studied, and reduced blood glucose level but increased hemoglobin and cholesterol level. Gibberellic acid increased hexokinase activity in liver, but decreased it in other tissues and increased significantly blood cholesterol and slightly glucose and hemoglobin levels. Kinetin decreased hexokinase activity significantly in liver and kidney, but not significantly in other tissues, and reduced slightly glucose and hemoglobin levels and reduced significantly serum cholesterol level. This study indicated that treatment of rat with 28-homobrassinolide significantly increased hexokinase activity in liver, heart and kidney whereas gibberellic acid increased hexokinase activity only in the liver, and Kinetin decreased hexokinase activity in most tissues. Decreased hexokinase activity was observed due to kinetin and gibberellic acid treatment, except for gibberellic acid in the liver tissue, and was indicative of the fact that kinetin and gibberellic acid acted as negative modulators of this enzyme in the rat tissues. Thus, three different phytohormones possessed different degrees of effect in the animal cells. Keywords: Hexokinase; Hemoglobin; Gibberellic acid; 28-homobrassinolide; Kinetin.
{"title":"Effect of phytohormones on tissue hexokinase and on some blood components in wistar rats","authors":"P. Muthuraman, S. Ravikumar, J. Vikramathithan, G. Nirmalkumar, K. Srikumar","doi":"10.5138/IJDD.2010.0975.0215.02026","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02026","url":null,"abstract":"Dietary phytohormones may influence the metabolic processes in animal cells. To determine the effect of the plant growth regulators 28-homobrassinolide, gibberellic acid and kinetin on the tissue hexokinase and some blood components in male rats. Methods: 50μg 28-bomobrassinolide, gibberellic acid and kinetin (Normal saline served as control) was injected intradermally. Hexokinase activity in several tissues and blood level of glucose, hemoglobin and cholesterol were determined 2 h after injection. 28-homobrassinolide increased hexokinase activity in all tissues studied, and reduced blood glucose level but increased hemoglobin and cholesterol level. Gibberellic acid increased hexokinase activity in liver, but decreased it in other tissues and increased significantly blood cholesterol and slightly glucose and hemoglobin levels. Kinetin decreased hexokinase activity significantly in liver and kidney, but not significantly in other tissues, and reduced slightly glucose and hemoglobin levels and reduced significantly serum cholesterol level. This study indicated that treatment of rat with 28-homobrassinolide significantly increased hexokinase activity in liver, heart and kidney whereas gibberellic acid increased hexokinase activity only in the liver, and Kinetin decreased hexokinase activity in most tissues. Decreased hexokinase activity was observed due to kinetin and gibberellic acid treatment, except for gibberellic acid in the liver tissue, and was indicative of the fact that kinetin and gibberellic acid acted as negative modulators of this enzyme in the rat tissues. Thus, three different phytohormones possessed different degrees of effect in the animal cells. Keywords: Hexokinase; Hemoglobin; Gibberellic acid; 28-homobrassinolide; Kinetin.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81924356","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02021
Dhirendra Kumar, Vivek Dave, S. Lewis, Brajesh Parmar, K. R. Gajbhiye, S. Paliwal
The aim of the present study was to formulate once daily sustained release matrix tablets of Stavudine to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance. The sustained release tablets were prepared by direct compression and formulated using different drug: polymer ratios, formulations such as F1to F15. Hydrophilic polymers like Hydroxy propyl methyl cellulose (HPMC), Carboxymethyl cellulose (CMC) and Starch 1500 were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with pharmacopoeial standards. Formulation containing Stavudine:HPMCK15: Na-CMC (1:2:0.5) with hardness 10-11kg/cm2 showed the desired release profile which matched the theoretical release profile. SEM studies of the formulations were carried out for the confirmation of mechanism of drug release. The in vitro drug release characteristics were studied in both simulated gastric and intestinal fluids for a period of 24 hr using USP Type 2 dissolution apparatus. Mathematical analysis of the release kinetics indicated a coupling of diffusion and erosion mechanisms. The study proves that the developed sustained release tablet is capable of releasing the drug in a sustained manner for 24 hr. Keywords: Sustained release; Matrix tablets; Hydroxy propyl methylcellulose; Stavudine
{"title":"Design and evaluation of sustained-release matrix once daily formulation of stavudine","authors":"Dhirendra Kumar, Vivek Dave, S. Lewis, Brajesh Parmar, K. R. Gajbhiye, S. Paliwal","doi":"10.5138/IJDD.2010.0975.0215.02021","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02021","url":null,"abstract":"The aim of the present study was to formulate once daily sustained release matrix tablets of Stavudine to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance. The sustained release tablets were prepared by direct compression and formulated using different drug: polymer ratios, formulations such as F1to F15. Hydrophilic polymers like Hydroxy propyl methyl cellulose (HPMC), Carboxymethyl cellulose (CMC) and Starch 1500 were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with pharmacopoeial standards. Formulation containing Stavudine:HPMCK15: Na-CMC (1:2:0.5) with hardness 10-11kg/cm2 showed the desired release profile which matched the theoretical release profile. SEM studies of the formulations were carried out for the confirmation of mechanism of drug release. The in vitro drug release characteristics were studied in both simulated gastric and intestinal fluids for a period of 24 hr using USP Type 2 dissolution apparatus. Mathematical analysis of the release kinetics indicated a coupling of diffusion and erosion mechanisms. The study proves that the developed sustained release tablet is capable of releasing the drug in a sustained manner for 24 hr. Keywords: Sustained release; Matrix tablets; Hydroxy propyl methylcellulose; Stavudine","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80062704","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 : 2010-07-23DOI: 10.5138/IJDD.2010.0975.0215.02023
R. Patel, B. Dadhani, R. Ladani, A. Baria, J. Patel
The present investigation deals with the formulation, optimization and evaluation of sodium alginate based In situ gel of Clarithromycin and Metronidazole Benzoate. Sodium alginate used as a polymer and CaCO3 was used as a cross-linking agent. The In situ formulation exhibited well, viscosity, drug content and sustained drug release; this study reports that oral administration of aqueous solutions containing sodium alginate results in formation of In situ gel, such formulations are homogenous liquid when administered orally and become gel at the contact site. The results of a 32 full factorial design revealed that the concentration of sodium alginate and concentration of CaCO3 significantly affected the dependent variables Q1, Q12 and T80. These In situ gels are, thus, suitable for oral sustained release of Clarithromycin and Metronidazole Benzoate. Keywords: In situ gel; Stomach specific; Gastric residence time.
{"title":"Formulation, evaluation and optimization of stomach specific in situ gel of clarithromycin and metronidazole benzoate","authors":"R. Patel, B. Dadhani, R. Ladani, A. Baria, J. Patel","doi":"10.5138/IJDD.2010.0975.0215.02023","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02023","url":null,"abstract":"The present investigation deals with the formulation, optimization and evaluation of sodium alginate based In situ gel of Clarithromycin and Metronidazole Benzoate. Sodium alginate used as a polymer and CaCO3 was used as a cross-linking agent. The In situ formulation exhibited well, viscosity, drug content and sustained drug release; this study reports that oral administration of aqueous solutions containing sodium alginate results in formation of In situ gel, such formulations are homogenous liquid when administered orally and become gel at the contact site. The results of a 32 full factorial design revealed that the concentration of sodium alginate and concentration of CaCO3 significantly affected the dependent variables Q1, Q12 and T80. These In situ gels are, thus, suitable for oral sustained release of Clarithromycin and Metronidazole Benzoate. Keywords: In situ gel; Stomach specific; Gastric residence time.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90677457","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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