Pub Date : 2020-09-17DOI: 10.33974/ijrpst.v2i1.231
B. Gowthami, S. Krishna, D. Rao
Oral administration is considered as major, convenient route among all other routes of delivery, owing to several benefits. But, the poor solubility or enzymatic/metabolic activity are the major concerns in developing a successful formulation. About 40% of approved drugs which are in the current market and 90% of new drug molecules in the developmental pipeline are hydrophobic in nature. The challenge to formulate insoluble drugs has met with various approaches to overcome the problems related to solubility, application of nanotechnology is one amongst them. The present review deals with various nanocarriers and technologies that are proven to be effective in enhancing the bioavilability of poorly soluble drugs.
{"title":"Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs","authors":"B. Gowthami, S. Krishna, D. Rao","doi":"10.33974/ijrpst.v2i1.231","DOIUrl":"https://doi.org/10.33974/ijrpst.v2i1.231","url":null,"abstract":"Oral administration is considered as major, convenient route among all other routes of delivery, owing to several benefits. But, the poor solubility or enzymatic/metabolic activity are the major concerns in developing a successful formulation. About 40% of approved drugs which are in the current market and 90% of new drug molecules in the developmental pipeline are hydrophobic in nature. The challenge to formulate insoluble drugs has met with various approaches to overcome the problems related to solubility, application of nanotechnology is one amongst them. The present review deals with various nanocarriers and technologies that are proven to be effective in enhancing the bioavilability of poorly soluble drugs.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"106 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75958733","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-02-18DOI: 10.33974/ijrpst.v1i3.161
V. Viswanath, P. Tulasi
The revolution in nanotechnology has lead to the development of various dosage forms such as vesicular drug delivery and in particular liposomes, niosomes, proniosomes, aquasomes, bilosomes etc. The disad-vantages exhibited by the liposomes, niosomes can be overcome through introduction of proniosomes which are compact liquid crystalline structures and convert to niosomes upon hydration. The investigation is focused on development and optimization of Betaxolol proniosomes using three square factorial design technique with the aid of design expert 11.0 ® trial version. The optimization technique prefers choles-terol and span 60 as independent variables and drug content, vesicular size, and entrapment efficacy as dependent variables. The design generated total 13 formulations among which F10 exhibited 98.1% drug content and 97.3% of entrapment efficacy. In view of other parameters, F10 exhibits 6.5 pH, 3.8 ve-sicular size and follows diffusion mechanism with anomalous drug transport. Hence, the obtained results specify that F10 is optimized and can be opted for commercialization.
{"title":"Formulation, optimization and characterization of Betaxolol hydrochloride proniosomes using 3-2 factorial design","authors":"V. Viswanath, P. Tulasi","doi":"10.33974/ijrpst.v1i3.161","DOIUrl":"https://doi.org/10.33974/ijrpst.v1i3.161","url":null,"abstract":"The revolution in nanotechnology has lead to the development of various dosage forms such as vesicular drug delivery and in particular liposomes, niosomes, proniosomes, aquasomes, bilosomes etc. The disad-vantages exhibited by the liposomes, niosomes can be overcome through introduction of proniosomes which are compact liquid crystalline structures and convert to niosomes upon hydration. The investigation is focused on development and optimization of Betaxolol proniosomes using three square factorial design technique with the aid of design expert 11.0 ® trial version. The optimization technique prefers choles-terol and span 60 as independent variables and drug content, vesicular size, and entrapment efficacy as dependent variables. The design generated total 13 formulations among which F10 exhibited 98.1% drug content and 97.3% of entrapment efficacy. In view of other parameters, F10 exhibits 6.5 pH, 3.8 ve-sicular size and follows diffusion mechanism with anomalous drug transport. Hence, the obtained results specify that F10 is optimized and can be opted for commercialization.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79919262","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.33974/ijrpst.v1i3.151
Samreen Sulthana, M. Aruna, S. Rasheed
In the past few decades, considerable attention has been focused on the development of new drug delivery system (NDDS). The NDDS should ideally fulfill two prerequisites. Firstly, it should deliver the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it should channel the active entity to the site of action. Conventional dosage forms including prolonged release dosage forms are unable to meet none of these. At present, no available drug delivery system behaves ideally, but sincere attempts have been made to achieve them through various novel approaches in drug delivery. The aim of present work is to develop a niosomal drug delivery system of aceclofenac. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. 8 niosomal formulations are prepared by the thin film hydration method using the cholesterol as the phospholipid. Prepared niosomal formulations were characterized by vesicle size, shape, surface charge, entrapment efficiency, drug content and invitro drug release studies. The vesicle size, size distribution and zeta potential of the optimized formulation (F5) was found to be 65.6 nm and zeta potential was found to be -1.5mV. Size distribution curve confirms the normal size distribution of the vesicles. The % entrapment efficiency of niosomal vesicles formulations were found to be in the range of 54.18±0.59 to 92.71±0.56 and optimized formulation was found to be 92.71±0.56 and drug content of niosomes formulations (F1to F8) were determined to be in the range of 94.6 -97.8%. The pH of all topical niosomal gels were found to be in the range of 7.4±0.02 to 7.4±0.08.The best fit with higher correlation (r2> 0.99) was found with the Zero Order Release and follows Korsemeyer peppas equation for all the formulations, which means that release of Aceclofenac from the lipid bilayer vesicles were due to diffusion. The stability studies were carried out and there was no significant change found in the formulations.
{"title":"Formulation and in-vitro evaluation of niosomal drug delivery system for aceclofenac.","authors":"Samreen Sulthana, M. Aruna, S. Rasheed","doi":"10.33974/ijrpst.v1i3.151","DOIUrl":"https://doi.org/10.33974/ijrpst.v1i3.151","url":null,"abstract":"In the past few decades, considerable attention has been focused on the development of new drug delivery system (NDDS). The NDDS should ideally fulfill two prerequisites. Firstly, it should deliver the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it should channel the active entity to the site of action. Conventional dosage forms including prolonged release dosage forms are unable to meet none of these. At present, no available drug delivery system behaves ideally, but sincere attempts have been made to achieve them through various novel approaches in drug delivery. The aim of present work is to develop a niosomal drug delivery system of aceclofenac. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. 8 niosomal formulations are prepared by the thin film hydration method using the cholesterol as the phospholipid. Prepared niosomal formulations were characterized by vesicle size, shape, surface charge, entrapment efficiency, drug content and invitro drug release studies. The vesicle size, size distribution and zeta potential of the optimized formulation (F5) was found to be 65.6 nm and zeta potential was found to be -1.5mV. Size distribution curve confirms the normal size distribution of the vesicles. The % entrapment efficiency of niosomal vesicles formulations were found to be in the range of 54.18±0.59 to 92.71±0.56 and optimized formulation was found to be 92.71±0.56 and drug content of niosomes formulations (F1to F8) were determined to be in the range of 94.6 -97.8%. The pH of all topical niosomal gels were found to be in the range of 7.4±0.02 to 7.4±0.08.The best fit with higher correlation (r2> 0.99) was found with the Zero Order Release and follows Korsemeyer peppas equation for all the formulations, which means that release of Aceclofenac from the lipid bilayer vesicles were due to diffusion. The stability studies were carried out and there was no significant change found in the formulations.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"54 2","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72618049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-10-12DOI: 10.33974/ijrpst.v1i2.150
M. Aruna, Samreen Sultana, S. Rasheed
The aim of present work is to develop a fast disintegrating solid oral dosage form of Metoprolol succinate. The concept of fast dissolving drug delivery system emerged from the desire to provide patient with more conventional means of taking their medication. Problems associated with conventional tablets can be resolved by means of fast dissolving tablets when put on tongue these tablets disintegrate and dissolve rapidly in saliva without need of drinking water. The faster the drug disintegrates in to solution, the quicker the absorption and onset of clinical effect. Preformulation results reveal that the flow properties of the active pharmaceutical ingredient were found to be excellent as per IP limits. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. Eight formulations were prepared with varying super disintegrating agent ratios and were found that as the level of super disintegrating agent decreased the drug release rates were found to be increased. Amongst all the formulations, formulation containing CCS (F4) as super disintegrant is fulfilling all the parameters satisfactorily. It has shown excellent in-vitro disintegration, in-vitro dissolution compared to other formulations. The prepared tablets disintegrate within few minutes without need of water; thereby enhance the absorption leading to its increased bioavailability. It was concluded that Fast Disintegrating tablets of Metoprolol can be prepared successfully as it satisfies all the criteria as a dispersible tablet and would be alternative to the currently available conventional tablets. Prepared formulations were stable during 90 days storage period at controlled 40°C and 75%RH.
{"title":"Formulation and evaluation of fast disintegrating tablets of metoprolol succinate using various superdisintegrants","authors":"M. Aruna, Samreen Sultana, S. Rasheed","doi":"10.33974/ijrpst.v1i2.150","DOIUrl":"https://doi.org/10.33974/ijrpst.v1i2.150","url":null,"abstract":"The aim of present work is to develop a fast disintegrating solid oral dosage form of Metoprolol succinate. The concept of fast dissolving drug delivery system emerged from the desire to provide patient with more conventional means of taking their medication. Problems associated with conventional tablets can be resolved by means of fast dissolving tablets when put on tongue these tablets disintegrate and dissolve rapidly in saliva without need of drinking water. The faster the drug disintegrates in to solution, the quicker the absorption and onset of clinical effect. Preformulation results reveal that the flow properties of the active pharmaceutical ingredient were found to be excellent as per IP limits. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. Eight formulations were prepared with varying super disintegrating agent ratios and were found that as the level of super disintegrating agent decreased the drug release rates were found to be increased. Amongst all the formulations, formulation containing CCS (F4) as super disintegrant is fulfilling all the parameters satisfactorily. It has shown excellent in-vitro disintegration, in-vitro dissolution compared to other formulations. The prepared tablets disintegrate within few minutes without need of water; thereby enhance the absorption leading to its increased bioavailability. It was concluded that Fast Disintegrating tablets of Metoprolol can be prepared successfully as it satisfies all the criteria as a dispersible tablet and would be alternative to the currently available conventional tablets. Prepared formulations were stable during 90 days storage period at controlled 40°C and 75%RH.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87602239","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-26DOI: 10.33974/ijrpst.v1i2.148
B. Salman, Mirza Abdul Hannan Baig
Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.
{"title":"Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method","authors":"B. Salman, Mirza Abdul Hannan Baig","doi":"10.33974/ijrpst.v1i2.148","DOIUrl":"https://doi.org/10.33974/ijrpst.v1i2.148","url":null,"abstract":"Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79814071","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-08-15DOI: 10.33974/IJRPST.V1I2.132
Thamrook s Shajahan, Shaiju S. Dharan, M. Mohan
Human saliva is a clear, slightly acidic biological fluid containing a mixture of secretions from multiple salivary glands, including the parotid, sublingual gland other minor glands beneath the oral mucosa as well as gingival crevice fluid. Salivary diagnostics has evolved into a sophisticated science and serves as a subset of the larger field of molecular diagnostics, now recognized as a central player in a wide variety of biomedical basic and clinical areas. Saliva biomarkers are source of indicators for local, systemic, and infectious disorders. The saliva based microbial, immunologic, and molecular biomarkers offers unique opportunities to bypass the painful invasive procedures such as biopsies and repeated blood draws by utilizing oral fluids to evaluate the condition of diseased individuals. Accurate and reliable early stage disease detection is the benefit of salivary biomarkers. Salivary biomarkers represent a promising non-invasive approach for oral cancer detection also. This review explains about the salivary biomarkers and their diagnostic approaches
{"title":"The salivary biomarkers: future clinical investigation technique","authors":"Thamrook s Shajahan, Shaiju S. Dharan, M. Mohan","doi":"10.33974/IJRPST.V1I2.132","DOIUrl":"https://doi.org/10.33974/IJRPST.V1I2.132","url":null,"abstract":"Human saliva is a clear, slightly acidic biological fluid containing a mixture of secretions from multiple salivary glands, including the parotid, sublingual gland other minor glands beneath the oral mucosa as well as gingival crevice fluid. Salivary diagnostics has evolved into a sophisticated science and serves as a subset of the larger field of molecular diagnostics, now recognized as a central player in a wide variety of biomedical basic and clinical areas. Saliva biomarkers are source of indicators for local, systemic, and infectious disorders. The saliva based microbial, immunologic, and molecular biomarkers offers unique opportunities to bypass the painful invasive procedures such as biopsies and repeated blood draws by utilizing oral fluids to evaluate the condition of diseased individuals. Accurate and reliable early stage disease detection is the benefit of salivary biomarkers. Salivary biomarkers represent a promising non-invasive approach for oral cancer detection also. This review explains about the salivary biomarkers and their diagnostic approaches","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"50 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86624581","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}
Inflammation is a complicated problem for today’s human beings. Large numbers of people have been diagnosed with arthritis along with inflammation. This is beside the others that suffer inflammation caused by an injury. There are alternatives that can be considered as temporary or permanent treatments of chronic inflammatory diseases. Plants, as well as other biological resources, are most welcomed to the therapeutic area. Using the plants’ compounds with high potential as novel techniques are today’s bio-pharmacologist concern. Bromelain has been more attractive due to its characteristics. This review is an overview of anti-inflammatory and anti-cancer effect of bromelain as a confident treatment for all inflammatory disease.
{"title":"Bromelain as an anti-inflammatory and anti-cancer compound","authors":"Siavash Hosseinpour Chermahini","doi":"10.33974/IJRPST.V1I2.68","DOIUrl":"https://doi.org/10.33974/IJRPST.V1I2.68","url":null,"abstract":"Inflammation is a complicated problem for today’s human beings. Large numbers of people have been diagnosed with arthritis along with inflammation. This is beside the others that suffer inflammation caused by an injury. There are alternatives that can be considered as temporary or permanent treatments of chronic inflammatory diseases. Plants, as well as other biological resources, are most welcomed to the therapeutic area. Using the plants’ compounds with high potential as novel techniques are today’s bio-pharmacologist concern. Bromelain has been more attractive due to its characteristics. This review is an overview of anti-inflammatory and anti-cancer effect of bromelain as a confident treatment for all inflammatory disease.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86209871","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}
Syed mujtaba pasha, Syed Abid Ali, Omair Ahmed, Omer wasiq, Mohammed mukaram, Mohammed abdul aala, Mohammed Ali
The objective of this study is to design and evaluate a new EOP called swellable elementary osmotic pump (SEOP) of the freely water soluble drug, amitriptyline hydrochloride (1 g /mL) by adding water swellable polymers in the core. The hydrophilic polymers included in the core retard the highly water soluble drug by producing hydrogel within the core, which may restrict and delay the solvent contact with drug molecules and may increase the diffusional length of the solvent to achieve a constant release rate. Thus, this technology can be exploited to achieve constant drug release at predetermined rate especially for highly water soluble drugs.
本研究的目的是通过在核心中加入水可膨胀聚合物，设计并评价自由水溶性药物盐酸阿米替林(1 g /mL)的可膨胀初级渗透泵(SEOP)。核内包含的亲水性聚合物通过在核内产生水凝胶来延缓高水溶性药物，这可能限制和延迟溶剂与药物分子的接触，并可能增加溶剂的扩散长度以达到恒定的释放速率。因此，该技术可用于实现以预定速率恒定释放药物，特别是高水溶性药物。
{"title":"Osmotic drug delivery system of valsartan","authors":"Syed mujtaba pasha, Syed Abid Ali, Omair Ahmed, Omer wasiq, Mohammed mukaram, Mohammed abdul aala, Mohammed Ali","doi":"10.33974/IJRPST.V1I2.58","DOIUrl":"https://doi.org/10.33974/IJRPST.V1I2.58","url":null,"abstract":"The objective of this study is to design and evaluate a new EOP called swellable elementary osmotic pump (SEOP) of the freely water soluble drug, amitriptyline hydrochloride (1 g /mL) by adding water swellable polymers in the core. The hydrophilic polymers included in the core retard the highly water soluble drug by producing hydrogel within the core, which may restrict and delay the solvent contact with drug molecules and may increase the diffusional length of the solvent to achieve a constant release rate. Thus, this technology can be exploited to achieve constant drug release at predetermined rate especially for highly water soluble drugs.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78707678","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug. The in vitro dissolution profile showed ascendency on increasing the carrier concentration
{"title":"Enhancement of dissolution rate of Olmesartan medoxomil using urea as carrier by different solid dispersion techniques","authors":"B. Sangameswaran, M. Gomathi","doi":"10.33974/IJRPST.V1I1.35","DOIUrl":"https://doi.org/10.33974/IJRPST.V1I1.35","url":null,"abstract":"The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug. The in vitro dissolution profile showed ascendency on increasing the carrier concentration","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"89 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84229400","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}
C. Bhattacharjee, Santhosh Kumar Chinnaiyan, Neelutpal Gogoi
Parasitic roundworms (nematodes) cause substantial morbidity and mortality in livestock animals globally and considerable productivity losses to farmers. The control of these nematodes has relied largely on the use of a limited number of anthelmintics. However, resistance to many of these anthelmintics is now widespread, and, therefore, there is a need to find new drugs to ensure sustained and effective treatment and control into the future. The present study was undertaken to evaluate the anthelmintic activity of crude aqueous, Petroleum ether, chloroform and methanol extract Olea europaea leaves using Pheretima posthuma as test worms. Single concentration (5%) of extracts was tested in the bioassay, which involved the determination of the time of paralysis (P) and time of death (D) of the worms. Piperazine citrate was included as a standard reference and distilled water as a control. The results of the present study indicated that Olea europaea leaves extracts were exhibited anthelmintic activity significantly when compared with the standard (Piperazine citrate) group. Further studies are in process to isolate the active principles responsible for the activity.
{"title":"Anthelmintic activity of leaves extracts of Olea europaea on Pheretima posthuma","authors":"C. Bhattacharjee, Santhosh Kumar Chinnaiyan, Neelutpal Gogoi","doi":"10.33974/ijrpst.v1i1.34","DOIUrl":"https://doi.org/10.33974/ijrpst.v1i1.34","url":null,"abstract":"Parasitic roundworms (nematodes) cause substantial morbidity and mortality in livestock animals globally and considerable productivity losses to farmers. The control of these nematodes has relied largely on the use of a limited number of anthelmintics. However, resistance to many of these anthelmintics is now widespread, and, therefore, there is a need to find new drugs to ensure sustained and effective treatment and control into the future. The present study was undertaken to evaluate the anthelmintic activity of crude aqueous, Petroleum ether, chloroform and methanol extract Olea europaea leaves using Pheretima posthuma as test worms. Single concentration (5%) of extracts was tested in the bioassay, which involved the determination of the time of paralysis (P) and time of death (D) of the worms. Piperazine citrate was included as a standard reference and distilled water as a control. The results of the present study indicated that Olea europaea leaves extracts were exhibited anthelmintic activity significantly when compared with the standard (Piperazine citrate) group. Further studies are in process to isolate the active principles responsible for the activity.","PeriodicalId":14281,"journal":{"name":"International Journal of Research in Pharmaceutical Sciences and Technology","volume":"243 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76663494","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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