Pub Date : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02040
M. Abdulkarim, G. Z. Abdullah, Mallikarjun Chitneni, E. S. Mahdi, M. Yam, A. Faisal, I. M. Salman, O. Ameer, M. Sahib, Munavvar Zubaid Abdulsattar, M. Basri, A. M. Noor
Palm oil esters are high molecular weight esters oil that has been newly synthesized by University Putra Malaysia researchers. It has received a lot of attention for its pharmaceutical and chemical application. Piroxicam is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity. It has low solubility in water as well as in oil with Log P value of 1.8. Generally, drugs with Log P value of more than 0.5 are needed to be formulated into a modified dosage form. One of these formulations is nano sized cream. Hence, the ability of formulating of these tricky drugs into dispersed system is questionable. The aim of this study is to investigate the ability of palm oil esters to be the oil phase for formulation of piroxicam into O/W nano-cream. Three points were selected from prepared pseudoternary diagram of palm oil esters and different Tween and Span mixtures. Piroxicam solubility and partition coefficient in oil and external phase was detected. Rheological properties, droplet size, structural properties and zeta potential of the dispersion system containing piroxicam were measured. O/W cream was formed with droplet size measurement by TEM of less than 100 nm. It could be concluded that palm oil esters is suitable oil for the formulation of suitable nano-cream containing piroxicam. Keywords: Palm oil esters; Piroxicam Solubility; partition coefficient; Rheology; Surface activity.
{"title":"Formulation and characterization of palm oil esters based nano- cream for topical delivery of piroxicam","authors":"M. Abdulkarim, G. Z. Abdullah, Mallikarjun Chitneni, E. S. Mahdi, M. Yam, A. Faisal, I. M. Salman, O. Ameer, M. Sahib, Munavvar Zubaid Abdulsattar, M. Basri, A. M. Noor","doi":"10.5138/IJDD.2010.0975.0215.02040","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02040","url":null,"abstract":"Palm oil esters are high molecular weight esters oil that has been newly synthesized by University Putra Malaysia researchers. It has received a lot of attention for its pharmaceutical and chemical application. Piroxicam is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity. It has low solubility in water as well as in oil with Log P value of 1.8. Generally, drugs with Log P value of more than 0.5 are needed to be formulated into a modified dosage form. One of these formulations is nano sized cream. Hence, the ability of formulating of these tricky drugs into dispersed system is questionable. The aim of this study is to investigate the ability of palm oil esters to be the oil phase for formulation of piroxicam into O/W nano-cream. Three points were selected from prepared pseudoternary diagram of palm oil esters and different Tween and Span mixtures. Piroxicam solubility and partition coefficient in oil and external phase was detected. Rheological properties, droplet size, structural properties and zeta potential of the dispersion system containing piroxicam were measured. O/W cream was formed with droplet size measurement by TEM of less than 100 nm. It could be concluded that palm oil esters is suitable oil for the formulation of suitable nano-cream containing piroxicam. Keywords: Palm oil esters; Piroxicam Solubility; partition coefficient; Rheology; Surface activity.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78638138","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02043
M. A. Attia, Heba Y. El Badawy
Oral mucositis is one of the main complications of non-surgical cancer treatments. The present work focuses on the treatment or reduction of oral mucositis by using combined mechanism by formation of physical barrier by forming a film to cover the oral ulcer and use of therapeutic agents, such as diclofenac sodium and ofloxacin separately or in combination. The selected polymers for film forming gel formulations are Hydroxypropylcellulose (HPC), hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (Na CMC) and carbopol 940 (CP). The residence time in simulated buccal saliva was between 5.5 to 6 hours for all formulations. The in-vitro release data of the investigated drugs from the prepared formulations followed zero-order and diffusion mechanism. The permeability studies data revealed that diclofenac sodium showed higher permeability from Na CMC/CP (2:0.3%) than from HPMC 4%, while in case of ofloxacin higher permeability was shown from Na CMC/CP (2:0.3%) than from HPMC/HPC (2:3%). The permeation parameters for diclofenac sodium and ofloxacin in their combination do not depend on either viscosity or pH, they depend on the type of polymers used. Keywords: Mucositis; Film-forming gel; Rheology; In vitro studies.
{"title":"Film forming gel for treatment of oral mucositis: In vitro studies","authors":"M. A. Attia, Heba Y. El Badawy","doi":"10.5138/IJDD.2010.0975.0215.02043","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02043","url":null,"abstract":"Oral mucositis is one of the main complications of non-surgical cancer treatments. The present work focuses on the treatment or reduction of oral mucositis by using combined mechanism by formation of physical barrier by forming a film to cover the oral ulcer and use of therapeutic agents, such as diclofenac sodium and ofloxacin separately or in combination. The selected polymers for film forming gel formulations are Hydroxypropylcellulose (HPC), hydroxypropyl methylcellulose (HPMC), sodium carboxymethylcellulose (Na CMC) and carbopol 940 (CP). The residence time in simulated buccal saliva was between 5.5 to 6 hours for all formulations. The in-vitro release data of the investigated drugs from the prepared formulations followed zero-order and diffusion mechanism. The permeability studies data revealed that diclofenac sodium showed higher permeability from Na CMC/CP (2:0.3%) than from HPMC 4%, while in case of ofloxacin higher permeability was shown from Na CMC/CP (2:0.3%) than from HPMC/HPC (2:3%). The permeation parameters for diclofenac sodium and ofloxacin in their combination do not depend on either viscosity or pH, they depend on the type of polymers used. Keywords: Mucositis; Film-forming gel; Rheology; In vitro studies.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78362745","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02047
B. Zadeh, Taybeh Jamei, F. Rahim, Mohammd Reza Abbaspur
The aim of this study was prepare and evaluate floating granules of sodium diclofenac with lipid excipient for prolonged gastric residence and reduced dose regimen. Floating granules prepared by extruder-spheronization technique. Compritol and gelucire as lipid excipient, HPMC as retardant and tween 80 as emulsifier were used. The effect of drug/lipid, drug/HPMC, drug amount, percentage of tween and type of lipid on floating ability, morphology and dissolution parameters were evaluated by factorial design. Results showed floating ability of granules was influenced by proportion of drug/lipid, drug/HPMC and percentage of tween. Floating property of Compritol was more than gelucire and provided good floating particles. Compritol granules provided suitable sustained release pattern in the manner that increase in D/L reduced D8 and MDT and increase in %T increased MDT. Higuchi model was the best fitted for dissolution data of granules prepared by Compritol and gelucire. In conclusion, Compritol provided more suitable floating ability and sustained release property. Keywords: Sodium diclofenac; Floating granules; Gastric residence time; Extruder-spheronization
{"title":"Multiple unite sustained released floating of sodium diclofenac: Formulation and evaluation using factorial design","authors":"B. Zadeh, Taybeh Jamei, F. Rahim, Mohammd Reza Abbaspur","doi":"10.5138/IJDD.2010.0975.0215.02047","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02047","url":null,"abstract":"The aim of this study was prepare and evaluate floating granules of sodium diclofenac with lipid excipient for prolonged gastric residence and reduced dose regimen. Floating granules prepared by extruder-spheronization technique. Compritol and gelucire as lipid excipient, HPMC as retardant and tween 80 as emulsifier were used. The effect of drug/lipid, drug/HPMC, drug amount, percentage of tween and type of lipid on floating ability, morphology and dissolution parameters were evaluated by factorial design. Results showed floating ability of granules was influenced by proportion of drug/lipid, drug/HPMC and percentage of tween. Floating property of Compritol was more than gelucire and provided good floating particles. Compritol granules provided suitable sustained release pattern in the manner that increase in D/L reduced D8 and MDT and increase in %T increased MDT. Higuchi model was the best fitted for dissolution data of granules prepared by Compritol and gelucire. In conclusion, Compritol provided more suitable floating ability and sustained release property. Keywords: Sodium diclofenac; Floating granules; Gastric residence time; Extruder-spheronization","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79694709","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02045
M. Abdulkarim, G. Z. Abdullah, Mallikarjun Chitneni, E. S. Mahdi, M. Yam, A. Faisal, I. M. Salman, O. Ameer, M. Sahib, Munavvar Zubaid Abdulsattar, M. Basri, A. M. Noor
The aim of this study is to study the stability of the nano-cream formula containing the newly synthesized palm oil esters when stored for reasonable storage duration. The prepared 0.5% piroxicam nano-cream formula contained phosphate buffer as external phase, palm oil esters as the oil phase and a combination of (80:20) of Tween 80 and Span 20 as emulsifier at a ratio of 37:25:38, respectively. Piroxicam is a hydro-lipophobic drug. Stability on storage is an important aspect which ensures the dosage form can exert the effects it is supposed to exert for the duration of storage. Droplets size, electrical conductivity, drug content, pH and rheological parameters are the parameters that have been assessed under different temperature to evaluate the stability of nano-cream preparation. Thus, experiments which measure the above parameters were conducted at storage temperatures of 4, 25 and 40οC.The data obtained from the stability study conducted on nano-cream formula showed that this formulation was stable for the whole 3 months period of the study when stored at tested several temperatures. Keywords: Palm oil esters; Nonionic surfactant; Piroxicam; Nano-cream
{"title":"Stability studies of nano-cream containing piroxicam","authors":"M. Abdulkarim, G. Z. Abdullah, Mallikarjun Chitneni, E. S. Mahdi, M. Yam, A. Faisal, I. M. Salman, O. Ameer, M. Sahib, Munavvar Zubaid Abdulsattar, M. Basri, A. M. Noor","doi":"10.5138/IJDD.2010.0975.0215.02045","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02045","url":null,"abstract":"The aim of this study is to study the stability of the nano-cream formula containing the newly synthesized palm oil esters when stored for reasonable storage duration. The prepared 0.5% piroxicam nano-cream formula contained phosphate buffer as external phase, palm oil esters as the oil phase and a combination of (80:20) of Tween 80 and Span 20 as emulsifier at a ratio of 37:25:38, respectively. Piroxicam is a hydro-lipophobic drug. Stability on storage is an important aspect which ensures the dosage form can exert the effects it is supposed to exert for the duration of storage. Droplets size, electrical conductivity, drug content, pH and rheological parameters are the parameters that have been assessed under different temperature to evaluate the stability of nano-cream preparation. Thus, experiments which measure the above parameters were conducted at storage temperatures of 4, 25 and 40οC.The data obtained from the stability study conducted on nano-cream formula showed that this formulation was stable for the whole 3 months period of the study when stored at tested several temperatures. Keywords: Palm oil esters; Nonionic surfactant; Piroxicam; Nano-cream","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79593022","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02039
O. Mashinchian, R. Salehi, G. Dehghan, Ayoub Aganejad, S. Davaran, Y. Omidi
The purpose of this research was to synthesize polymer based smart nanosystems for delivery of important bioactive natural products such as sesquiterpene coumarin derivatives of ferula szowitsiana, farnesiferol C as a potent anticancer. To this aim, polymeric micelles were prepared using Nisopropylacrylamide (NIPAAM), vinyl pyrrolidone (VP) and methacrylate (MAA) as monomers which were cross-linked with N, N-methylene bisacrylamide (MBA). The molar ratio of the PNIPAAm: VP: MAA group was 75.7:9.5:14.8. These micelles were further characterized upon their physicochemical properties using particle size analyzer, FT-IR, H-/C-NMR, HPLC. Particle size analyzer resulted in ~500 nm micelles with ~95% drug entrapments. Drug release from the polymeric micelles after 300 hours at 37°C and 40°C were 60 and 98 %, respectively. Upon these findings, it is proposed that the P (N-isopropylacrylamide-co-Methacrylic acid-coVinylpyrrolidone) micelles may be considered as thermosensitive delivery nanosystem.
{"title":"Novel thermosensitive poly (N-isopropylacrylamide-co-vinylpyrrolidone-co-methacrylic acid) nanosystems for delivery of natural products","authors":"O. Mashinchian, R. Salehi, G. Dehghan, Ayoub Aganejad, S. Davaran, Y. Omidi","doi":"10.5138/IJDD.2010.0975.0215.02039","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02039","url":null,"abstract":"The purpose of this research was to synthesize polymer based smart nanosystems for delivery of important bioactive natural products such as sesquiterpene coumarin derivatives of ferula szowitsiana, farnesiferol C as a potent anticancer. To this aim, polymeric micelles were prepared using Nisopropylacrylamide (NIPAAM), vinyl pyrrolidone (VP) and methacrylate (MAA) as monomers which were cross-linked with N, N-methylene bisacrylamide (MBA). The molar ratio of the PNIPAAm: VP: MAA group was 75.7:9.5:14.8. These micelles were further characterized upon their physicochemical properties using particle size analyzer, FT-IR, H-/C-NMR, HPLC. Particle size analyzer resulted in ~500 nm micelles with ~95% drug entrapments. Drug release from the polymeric micelles after 300 hours at 37°C and 40°C were 60 and 98 %, respectively. Upon these findings, it is proposed that the P (N-isopropylacrylamide-co-Methacrylic acid-coVinylpyrrolidone) micelles may be considered as thermosensitive delivery nanosystem.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81308941","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02044
V. Shukla, F. Manvi
Oral route of administration have wide acceptance up to 50-60% to total drug forms. Fast disintegrating drug delivery system has number of advantage such as faster onset of action, attractive elegance, ease of administration. In this study, an attempt has been made to study direct compression method, for formulation of fast disintegrating tablets of Isoniazid and Rifampicin, an anti-tubercular drug in view of enhancing bioavailability. These formulations have sufficient hardness and can be manufactured by commonly used equipment. Prior to formulation the pre-compression parameters were characterized for flow properties and prepared formulations were evaluated for physico-chemical parameters, X-ray powder crystallography, SEM and in-vivo bioavailability. All four formulations possessed good disintegration properties with total disintegration time of 25 to 40 seconds. The effects of different superdisintegrants and process variables on drug release profile and disintegration property were evaluated and results revealed the better drug release with different superdisintegrants such as Ac-di sol and Polyplastadone XL. All formulations are rapidly disintegrated in oral cavity as well as all formulations possess good anti-tubercular properties. SEM Showed the mechanical strength of the formulations affected the morphological changes after compression. Hence, it is evident from this study that fast dispersible tablets could be a promising delivery system for Isoniazid, Rifampicin and their combination with good mouth feel and improved drug availability with better patient compliance. Keywords: Isoniazid; Rifampicin; Superdisintegrants; Direct compression method; Bioavailability.
{"title":"Effect of two different superdisintegrants on combinaion dispersible tablets of isoniazid and rifampicin for oral treatment of tuberculosis","authors":"V. Shukla, F. Manvi","doi":"10.5138/IJDD.2010.0975.0215.02044","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02044","url":null,"abstract":"Oral route of administration have wide acceptance up to 50-60% to total drug forms. Fast disintegrating drug delivery system has number of advantage such as faster onset of action, attractive elegance, ease of administration. In this study, an attempt has been made to study direct compression method, for formulation of fast disintegrating tablets of Isoniazid and Rifampicin, an anti-tubercular drug in view of enhancing bioavailability. These formulations have sufficient hardness and can be manufactured by commonly used equipment. Prior to formulation the pre-compression parameters were characterized for flow properties and prepared formulations were evaluated for physico-chemical parameters, X-ray powder crystallography, SEM and in-vivo bioavailability. All four formulations possessed good disintegration properties with total disintegration time of 25 to 40 seconds. The effects of different superdisintegrants and process variables on drug release profile and disintegration property were evaluated and results revealed the better drug release with different superdisintegrants such as Ac-di sol and Polyplastadone XL. All formulations are rapidly disintegrated in oral cavity as well as all formulations possess good anti-tubercular properties. SEM Showed the mechanical strength of the formulations affected the morphological changes after compression. Hence, it is evident from this study that fast dispersible tablets could be a promising delivery system for Isoniazid, Rifampicin and their combination with good mouth feel and improved drug availability with better patient compliance. Keywords: Isoniazid; Rifampicin; Superdisintegrants; Direct compression method; Bioavailability.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81293083","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02041
S. U. Zate, P. Kothawade, Mohan N. Rathi, Mohan H. Shitole, Chetan Yewale, Vinayak S. Gawande
The present study was undertaken with an aim to formulation development and evaluation of gastroretentive mucoadhesive sustained release tablet of Venlafaxine hydrochloride which releases the drug in a sustained manner over a period of 12 hours, by using Carbopol 971P in combination with eudragit RS-PO and ethyl cellulose as a mucoadhesive and release retardant respectively. Preformulation study was done initially and results directed for the further course of formulation. Based on Preformulation studies different batches of Venlafaxine hydrochloride were prepared using Carbopol 971P, Eudragit RS-PO and ethyl cellulose chosen for their different hydrophilic properties to calculate the sustained release properties. Sustained release tablets were prepared by direct compression and were evaluated for bioadhesion time, swelling index and matrix erosion, and in vitro drug release. The tablets of batch F3 and F6 had high swelling behaviors but release of drug is very less. And batch F2 having considerable swelling index and in vitro drug release (99.85%). Batch F2 can be taken as an ideal or optimized formulation of sustained release tablets for 12 hour release as it fulfills all the requirements for sustained release tablet. From the discussion it is concluded that use of carbopol as a release retardant and adhesive polymer is very effective; and also it act as strong release retardant in combination with hydrophobic polymers. Keywords: Gastroretentive; Mucoadhesive; Venlafaxine hydrochloride; Tablet.
{"title":"Development and characterization of gastroretentive mucoadhesive tablets of venlafaxine hydrochloride","authors":"S. U. Zate, P. Kothawade, Mohan N. Rathi, Mohan H. Shitole, Chetan Yewale, Vinayak S. Gawande","doi":"10.5138/IJDD.2010.0975.0215.02041","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02041","url":null,"abstract":"The present study was undertaken with an aim to formulation development and evaluation of gastroretentive mucoadhesive sustained release tablet of Venlafaxine hydrochloride which releases the drug in a sustained manner over a period of 12 hours, by using Carbopol 971P in combination with eudragit RS-PO and ethyl cellulose as a mucoadhesive and release retardant respectively. Preformulation study was done initially and results directed for the further course of formulation. Based on Preformulation studies different batches of Venlafaxine hydrochloride were prepared using Carbopol 971P, Eudragit RS-PO and ethyl cellulose chosen for their different hydrophilic properties to calculate the sustained release properties. Sustained release tablets were prepared by direct compression and were evaluated for bioadhesion time, swelling index and matrix erosion, and in vitro drug release. The tablets of batch F3 and F6 had high swelling behaviors but release of drug is very less. And batch F2 having considerable swelling index and in vitro drug release (99.85%). Batch F2 can be taken as an ideal or optimized formulation of sustained release tablets for 12 hour release as it fulfills all the requirements for sustained release tablet. From the discussion it is concluded that use of carbopol as a release retardant and adhesive polymer is very effective; and also it act as strong release retardant in combination with hydrophobic polymers. Keywords: Gastroretentive; Mucoadhesive; Venlafaxine hydrochloride; Tablet.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88749633","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02048
V. Muthuviveganandavel, P. Muthuraman, S. Muthu, K. Srikumar
Methyl 2-benzimidazole carbamate (carbendazim) is one of the synthetic fungicides that controlled organisms that caused plant diseases of different types. It is widely used as a preservative in leather, paint, textile, fruits and papermaking industry. It is also used as an anticancer drug in chemical medicine. In the present study low concentrations of carbendazim was administered at 5, 10, 25 and 50mM doses intradermally to male albino rats. At the end of 6 hr, 12hr and 24hr duration, blood samples were collected from the animal for the analysis of biochemical and haematological parameters. Carbendazim caused an increase of cholesterol, uric acid, glucose and creatinine while serum phosphorous content was decreased. However, mean hemoglobin, WBC, E, and platelet counts increased and total RBC, N and L counts decreased. These results indicated that low dose level carbendazim contributed to toxicological effects in the rat tissues. Keywords: Methyl 2-benzimidazole carbamate; Fungicide; Rat tissues
{"title":"Biochemical evaluation of low dose methyl 2-benzimidazole carbamate fungicide on male albino rats","authors":"V. Muthuviveganandavel, P. Muthuraman, S. Muthu, K. Srikumar","doi":"10.5138/IJDD.2010.0975.0215.02048","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02048","url":null,"abstract":"Methyl 2-benzimidazole carbamate (carbendazim) is one of the synthetic fungicides that controlled organisms that caused plant diseases of different types. It is widely used as a preservative in leather, paint, textile, fruits and papermaking industry. It is also used as an anticancer drug in chemical medicine. In the present study low concentrations of carbendazim was administered at 5, 10, 25 and 50mM doses intradermally to male albino rats. At the end of 6 hr, 12hr and 24hr duration, blood samples were collected from the animal for the analysis of biochemical and haematological parameters. Carbendazim caused an increase of cholesterol, uric acid, glucose and creatinine while serum phosphorous content was decreased. However, mean hemoglobin, WBC, E, and platelet counts increased and total RBC, N and L counts decreased. These results indicated that low dose level carbendazim contributed to toxicological effects in the rat tissues. Keywords: Methyl 2-benzimidazole carbamate; Fungicide; Rat tissues","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74477364","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02046
S. U. Zate, P. Kothawade, Jitendra W Gajbe, Anantwar S. Pramod, S. Boraste
A simple, precise and economical spectrophotometric method for the estimation of Itopride hydrochloride in pharmaceutical bulk and tablet dosage form was developed and validated. Identification was carried out using a UV-visible double beam spectrophotometer detector with working wavelength at 258nm in 0.1N HCl medium. The method was validated with respect to its specificity, linearity range, accuracy, and precision in analytical media. Itopride hydrochloride show the maximum absorbance (λmax) at 258 nm, Regression analysis showed good correlation in the concentration range 5-100 mcg/ml and 96.80 to 106.84% recovery with relative standard deviation 0.293 to 3.98%. Statistical treatment of data reflects that the proposed method is precise, accurate and easily applicable for determination of Itopride hydrochloride in bulk and pharmaceutical preparation. Keywords: Spectrophotometric; Itopride hydrochloride; Validation.
{"title":"Spectrophotometric method development and validation of itopride hydrochloride in bulk and dosage form","authors":"S. U. Zate, P. Kothawade, Jitendra W Gajbe, Anantwar S. Pramod, S. Boraste","doi":"10.5138/IJDD.2010.0975.0215.02046","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02046","url":null,"abstract":"A simple, precise and economical spectrophotometric method for the estimation of Itopride hydrochloride in pharmaceutical bulk and tablet dosage form was developed and validated. Identification was carried out using a UV-visible double beam spectrophotometer detector with working wavelength at 258nm in 0.1N HCl medium. The method was validated with respect to its specificity, linearity range, accuracy, and precision in analytical media. Itopride hydrochloride show the maximum absorbance (λmax) at 258 nm, Regression analysis showed good correlation in the concentration range 5-100 mcg/ml and 96.80 to 106.84% recovery with relative standard deviation 0.293 to 3.98%. Statistical treatment of data reflects that the proposed method is precise, accurate and easily applicable for determination of Itopride hydrochloride in bulk and pharmaceutical preparation. Keywords: Spectrophotometric; Itopride hydrochloride; Validation.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74522663","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 : 2010-12-03DOI: 10.5138/IJDD.2010.0975.0215.02042
A. Tapas, P. Kawtikwar, D. Sakarkar
The objective of the present work was to enhance the solubility and dissolution rate of valsartan (VAL) a poorly water soluble antihypertensive, by spherically agglomerated solid dispersions using methanol, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like polyvinyl pyrrolidone, Hydroxypropyl β-cyclodextrin, Hydroxypropyl methylcellulose were used in agglomeration process. The pure drug (VAL) and its agglomerates with different polymers were characterize by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The DSC results indicated that decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility, dissolution rate and micromeritic properties (bulk density, flow property, compactability) compared with VAL. The SEM studies showed that the agglomerates posseeses a good spherical shape. Keywords: Valsartan; Spherical agglomeration; Solid dispersion; Solubility; Dissolution rate; Micromeritic properties.
{"title":"Spherically agglomerated solid dispersions of valsartan to improve solubility, dissolution rate and micromeritic properties","authors":"A. Tapas, P. Kawtikwar, D. Sakarkar","doi":"10.5138/IJDD.2010.0975.0215.02042","DOIUrl":"https://doi.org/10.5138/IJDD.2010.0975.0215.02042","url":null,"abstract":"The objective of the present work was to enhance the solubility and dissolution rate of valsartan (VAL) a poorly water soluble antihypertensive, by spherically agglomerated solid dispersions using methanol, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like polyvinyl pyrrolidone, Hydroxypropyl β-cyclodextrin, Hydroxypropyl methylcellulose were used in agglomeration process. The pure drug (VAL) and its agglomerates with different polymers were characterize by differential scanning calorimetry (DSC), X-ray diffraction (XRD), IR spectroscopic studies and scanning electron microscopy (SEM). The DSC results indicated that decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility, dissolution rate and micromeritic properties (bulk density, flow property, compactability) compared with VAL. The SEM studies showed that the agglomerates posseeses a good spherical shape. Keywords: Valsartan; Spherical agglomeration; Solid dispersion; Solubility; Dissolution rate; Micromeritic properties.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2010-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83667919","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}