Pub Date : 2017-06-01DOI: 10.26510/2394-0859.PBE.2017.27
S. Sahoo, S. K. Mekap
Objective: In the present work, RP-HPLC procedure is optimized to finalize a different approach for the estimation of rivaroxaban in tablet dosage form. A novel drug rivaroxaban used as anti-coagulant in the patients for the prevention of thromboembolism. Methods: The molecule is identified with the molar mass of 435.882 g/mol and molecular formula C 19 H 18 ClN 3 O 5 S. The determination was executed by C18 column (Phenomenex 250 x 4.6 mm, 5 μm maintained at 35°C) at 251 nm with a mobile phase (ACN: Water, 55:45 v/v) and flow of 1.2 ml/min. Results: The retention time found to be about 3.8minutes.The validation parameters performed as per ICH guidelines and found to be within acceptance criteria. Linearity of the method is found to be accepted across five concentration level i.e. being studied by calibration curve. Accuracy was executed at three different concentrations, the amount being recovered are close to 100%. The % RSD values obtained for repeatability, intermediate and reproducibility under precision are within acceptance criteria. Conclusions: The method was accurate, precise, robust and rapid for quantitative determination of rivaroxaban by High Performance Liquid Chromatography.
{"title":"Assay comparison of rivaroxaban by new HPLC method with an existing method in tablet dosage form","authors":"S. Sahoo, S. K. Mekap","doi":"10.26510/2394-0859.PBE.2017.27","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.27","url":null,"abstract":"Objective: In the present work, RP-HPLC procedure is optimized to finalize a different approach for the estimation of rivaroxaban in tablet dosage form. A novel drug rivaroxaban used as anti-coagulant in the patients for the prevention of thromboembolism. Methods: The molecule is identified with the molar mass of 435.882 g/mol and molecular formula C 19 H 18 ClN 3 O 5 S. The determination was executed by C18 column (Phenomenex 250 x 4.6 mm, 5 μm maintained at 35°C) at 251 nm with a mobile phase (ACN: Water, 55:45 v/v) and flow of 1.2 ml/min. Results: The retention time found to be about 3.8minutes.The validation parameters performed as per ICH guidelines and found to be within acceptance criteria. Linearity of the method is found to be accepted across five concentration level i.e. being studied by calibration curve. Accuracy was executed at three different concentrations, the amount being recovered are close to 100%. The % RSD values obtained for repeatability, intermediate and reproducibility under precision are within acceptance criteria. Conclusions: The method was accurate, precise, robust and rapid for quantitative determination of rivaroxaban by High Performance Liquid Chromatography.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86288980","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-06-01DOI: 10.26510/2394-0859.pbe.2017.20
B. Prabasheela, V. Sakithya, V. Nandhini, M. Logeshwari
Bell’s palsy is a unilateral, lower motor neuron weakness of the facial nerve. Facial dysfunction has a dramatic effect on a patient’s appearance, psychological wellbeing and quality of life. Bell’s palsy has been described in patients of all ages, and is more common in adults than in children.The causes of the paralysis still remain unknown. Establishing the correct diagnosis is imperative and choosing the correct treatment options can optimize the likelihood of recovery. Hence this review deals with etiology, signs and symptoms, diagnosis and treatment management for Bell’s palsy.
{"title":"Understanding Bell's palsy –a review","authors":"B. Prabasheela, V. Sakithya, V. Nandhini, M. Logeshwari","doi":"10.26510/2394-0859.pbe.2017.20","DOIUrl":"https://doi.org/10.26510/2394-0859.pbe.2017.20","url":null,"abstract":"Bell’s palsy is a unilateral, lower motor neuron weakness of the facial nerve. Facial dysfunction has a dramatic effect on a patient’s appearance, psychological wellbeing and quality of life. Bell’s palsy has been described in patients of all ages, and is more common in adults than in children.The causes of the paralysis still remain unknown. Establishing the correct diagnosis is imperative and choosing the correct treatment options can optimize the likelihood of recovery. Hence this review deals with etiology, signs and symptoms, diagnosis and treatment management for Bell’s palsy.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77613104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-06-01DOI: 10.26510/2394-0859.PBE.2017.22
S. Chandra, M. Srivastav, N. Chauhan
The article reviewed various therapies other than dopamine treatment like A2a antagonists: antiparkinson medication reducing the over reactivity of substantia nigra due to loss of dopamine; Levodopa/Carbidopa Intestinal Gel: an aqueous gel containing levodopa and carbidopa; stem-cell therapies like embryonic and adult stem cell can be act through several mechanism; acupuncture: reduced the motor symptoms and other disease related factors; various antiparkinson medications like IPX066 and ND0611 are sustained release and transdermal patches which are transported to GIT through high nutrients and patches are found to be useful in increasing the concentration, half-life of levodopa, thus downs the threatening risk of PD. The future treatment for PD should be considered as they have less side-effect and better results than other treatment as they not only decrease the symptoms but also the incidences of PD. If the symptoms are diagnosed early patient should go for genetic therapy to relieve from the disease which not only reduce the progressive increase of symptoms and disease. Considering all therapies, future treatments shows the weightage in reducing the progressive increase of PD in patient. Though these treatments are proven to be effective in treatment but still more targeted tools and techniques are required which can specifically target the cause and thus lowers the graph and rating scale of PD.
{"title":"Recent advances in Parkinson disease","authors":"S. Chandra, M. Srivastav, N. Chauhan","doi":"10.26510/2394-0859.PBE.2017.22","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.22","url":null,"abstract":"The article reviewed various therapies other than dopamine treatment like A2a antagonists: antiparkinson medication reducing the over reactivity of substantia nigra due to loss of dopamine; Levodopa/Carbidopa Intestinal Gel: an aqueous gel containing levodopa and carbidopa; stem-cell therapies like embryonic and adult stem cell can be act through several mechanism; acupuncture: reduced the motor symptoms and other disease related factors; various antiparkinson medications like IPX066 and ND0611 are sustained release and transdermal patches which are transported to GIT through high nutrients and patches are found to be useful in increasing the concentration, half-life of levodopa, thus downs the threatening risk of PD. The future treatment for PD should be considered as they have less side-effect and better results than other treatment as they not only decrease the symptoms but also the incidences of PD. If the symptoms are diagnosed early patient should go for genetic therapy to relieve from the disease which not only reduce the progressive increase of symptoms and disease. Considering all therapies, future treatments shows the weightage in reducing the progressive increase of PD in patient. Though these treatments are proven to be effective in treatment but still more targeted tools and techniques are required which can specifically target the cause and thus lowers the graph and rating scale of PD.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77936796","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-06-01DOI: 10.26510/2394-0859.PBE.2017.21
A. Mohan, M. Khan, S. Chandra
Alopecia is characterized by hair loss mainly on scalp some time on other resign of the body that has negative psychological and social impact on patients. Androgenetic alopecia and alopecia areata are common disorders. Androgenetic alopecia is the sensitivity of scalp follicles to dihydrotestosterone and alopecia areata is an autoimmune disorder. Current studies have explained the efficacy of corticosteroid therapy or the combination of ultraviolet A therapy and systemic corticosteroids for severe AA. Finasteride opens up new possibilities for the treatment of androgenetic alopecia. Current drug treatment approaches use regrowth stimulators such as minoxidil and finasteride for androgenetic alopecia, as well as corticosteroids, PUVA therapy for alopecia areata. Targeted delivery to the Hair follicle units helps faster targeting to cells that accelerate drug action by faster availability of drug, novel combination treatments combinations like tretinoin with minoxidil shows better results, gene therapy are new approaches that are under developing stage and giving satisfactory results on animal as well as humans.
{"title":"Advance approaches in alopecia","authors":"A. Mohan, M. Khan, S. Chandra","doi":"10.26510/2394-0859.PBE.2017.21","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.21","url":null,"abstract":"Alopecia is characterized by hair loss mainly on scalp some time on other resign of the body that has negative psychological and social impact on patients. Androgenetic alopecia and alopecia areata are common disorders. Androgenetic alopecia is the sensitivity of scalp follicles to dihydrotestosterone and alopecia areata is an autoimmune disorder. Current studies have explained the efficacy of corticosteroid therapy or the combination of ultraviolet A therapy and systemic corticosteroids for severe AA. Finasteride opens up new possibilities for the treatment of androgenetic alopecia. Current drug treatment approaches use regrowth stimulators such as minoxidil and finasteride for androgenetic alopecia, as well as corticosteroids, PUVA therapy for alopecia areata. Targeted delivery to the Hair follicle units helps faster targeting to cells that accelerate drug action by faster availability of drug, novel combination treatments combinations like tretinoin with minoxidil shows better results, gene therapy are new approaches that are under developing stage and giving satisfactory results on animal as well as humans.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88220493","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-06-01DOI: 10.26510/2394-0859.PBE.2017.24
Eze Cj, I. Iroha, S. C. Eluu, P. C. Ejikeugwu, C. Iroha, M. Ajah, E. Nwakaeze, E. Ugwu
Objective: This study investigated the antibacterial activity of the acetone, methanol, and ethanol leaf extracts of Azadirachta indica and Psidium guajava against methicillin resistant Staphylococcus aureus ( MRSA) and vancomycin resistant Staphylococcus aureus (VRSA) strains as well as the antimicrobial activity of some conventional antibiotics on these multidrug resistant organisms. Methods: MRSA and VRSA strains were obtained from the culture collection unit of a tertiary hospital in Ebonyi State, Nigeria. The test organisms and the plant extracts were processed using standard microbiology techniques. Kirby-Bauer disk diffusion technique was used to determine the antimicrobial susceptibility profile of the MRSA and VRSA strains to some conventionally used antibiotics; and the antibacterial activity of the plant extracts was evaluated using agar well diffusion technique with three solvents: ethanol, methanol and acetone. Results: It was revealed in this study that the extracts of A. indica and P. guajava demonstrated some level of antimicrobial activity against the test organism at concentrations of 100 mg/ml and 50 mg/ml. Compared to the conventional antibiotics used, the antibiotics showed better antimicrobial activity against the test organisms than the plant extracts which was least active against the MRSA and VRSA strains. Conclusions: Though the A. indica and P. guajava extracts showed some appreciable antimicrobial activity against the MRSA and VRSA strains, the conventional antibiotics produced better antimicrobial action against these multidrug resistant bacteria. The search for novel compounds with putative antimicrobial activity should be stepped up since plants holds the potential for discovering novel drugs.
{"title":"Comparative studies on the antibacterial activities of leaf extracts of Azadirachta indica and Psidium guajava and antibiotics on methicillin and vancomycin resistant Staphylococcus aureus","authors":"Eze Cj, I. Iroha, S. C. Eluu, P. C. Ejikeugwu, C. Iroha, M. Ajah, E. Nwakaeze, E. Ugwu","doi":"10.26510/2394-0859.PBE.2017.24","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.24","url":null,"abstract":"Objective: This study investigated the antibacterial activity of the acetone, methanol, and ethanol leaf extracts of Azadirachta indica and Psidium guajava against methicillin resistant Staphylococcus aureus ( MRSA) and vancomycin resistant Staphylococcus aureus (VRSA) strains as well as the antimicrobial activity of some conventional antibiotics on these multidrug resistant organisms. Methods: MRSA and VRSA strains were obtained from the culture collection unit of a tertiary hospital in Ebonyi State, Nigeria. The test organisms and the plant extracts were processed using standard microbiology techniques. Kirby-Bauer disk diffusion technique was used to determine the antimicrobial susceptibility profile of the MRSA and VRSA strains to some conventionally used antibiotics; and the antibacterial activity of the plant extracts was evaluated using agar well diffusion technique with three solvents: ethanol, methanol and acetone. Results: It was revealed in this study that the extracts of A. indica and P. guajava demonstrated some level of antimicrobial activity against the test organism at concentrations of 100 mg/ml and 50 mg/ml. Compared to the conventional antibiotics used, the antibiotics showed better antimicrobial activity against the test organisms than the plant extracts which was least active against the MRSA and VRSA strains. Conclusions: Though the A. indica and P. guajava extracts showed some appreciable antimicrobial activity against the MRSA and VRSA strains, the conventional antibiotics produced better antimicrobial action against these multidrug resistant bacteria. The search for novel compounds with putative antimicrobial activity should be stepped up since plants holds the potential for discovering novel drugs.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89146132","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-06-01DOI: 10.26510/2394-0859.pbe.2017.25
D. Patel, K. Patel, P. Bharadia
Objective: The objective of present research work was to develop formulation of orodispersible tablets of Ivabradine HCl and evaluate it for different evaluation parameters. Methods: The tablets were prepared by direct compression method. The formulation of the tablets were evaluated before compression for characterization of flow properties and after compression for different parameters of orodispersible tablet formulation. Results: Ivabradine hydrochloride orodispersible tablets were developed with considerable increase in drug release as compared to marketed formulations; nine formulations were developed and studied. The difference in drug release values was found to be 100.88 ± 0.10 respectively. The drug was characterized according to different compendial methods, on the basis of identification by HPLC, pH, organoleptic properties and other tests. Parameters evaluated were within prescribed limits and indicated good free flowing properties. The F6 batch with disintegration time 21 ± 3.0 and dissolution 99.29% was selected as optimized formulation. This was compared with conventional marketed formulation and was found superior. Batch F6 was also subjected to stability studies for two months and was tested for its hardness, wetting time, disintegration time, drug contents and dissolution behaviour monthly. Conclusions: By appropriate selection of excipients, it was possible to develop orodispersible tablets of Ivabradine HCl.
{"title":"Formulation and evaluation of orodispersible tablet of ivabradine hydrochloride","authors":"D. Patel, K. Patel, P. Bharadia","doi":"10.26510/2394-0859.pbe.2017.25","DOIUrl":"https://doi.org/10.26510/2394-0859.pbe.2017.25","url":null,"abstract":"Objective: The objective of present research work was to develop formulation of orodispersible tablets of Ivabradine HCl and evaluate it for different evaluation parameters. Methods: The tablets were prepared by direct compression method. The formulation of the tablets were evaluated before compression for characterization of flow properties and after compression for different parameters of orodispersible tablet formulation. Results: Ivabradine hydrochloride orodispersible tablets were developed with considerable increase in drug release as compared to marketed formulations; nine formulations were developed and studied. The difference in drug release values was found to be 100.88 ± 0.10 respectively. The drug was characterized according to different compendial methods, on the basis of identification by HPLC, pH, organoleptic properties and other tests. Parameters evaluated were within prescribed limits and indicated good free flowing properties. The F6 batch with disintegration time 21 ± 3.0 and dissolution 99.29% was selected as optimized formulation. This was compared with conventional marketed formulation and was found superior. Batch F6 was also subjected to stability studies for two months and was tested for its hardness, wetting time, disintegration time, drug contents and dissolution behaviour monthly. Conclusions: By appropriate selection of excipients, it was possible to develop orodispersible tablets of Ivabradine HCl.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78490506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-06-01DOI: 10.26510/2394-0859.PBE.2017.23
N. Panda, S. Bhoi, R. Rawal, M. K. Raval
Objective: Lysin specific demethylase 1 (LSD1) inhibits the tumor suppressor activity of p53 and facilitates the progress of tumor. In order to check the tumor growth, the activity of LSD1 enzyme is to be blunted. Methods: Phytochemicals from naturally occurring plant-based anti-cancer compound-activity-target (NPACT) database are screened with LSD1 as target applying genetic algorithm (GA) method to study best ligand poses and free energy of binding using Argus Lab. The prediction of drug-likeness and oral toxicity of the ligands are performed by the online tools Molsoft and ProTox respectively. Results: Calyxin H shows optimum binding affinity to both the substrate and FAD binding sites of LSD1. The LD 50 value (median lethal dose) of calyxin H is more than 1000 mg/kg body weight and the toxicity class is 4. Conclusions: Calyxin H is the inhibitor of choice against target LSD1. The lead molecule may be the future potential herbal drug for cancer treatment.
{"title":"Lysine specific demethylase 1 as therapeutic target of cancer","authors":"N. Panda, S. Bhoi, R. Rawal, M. K. Raval","doi":"10.26510/2394-0859.PBE.2017.23","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.23","url":null,"abstract":"Objective: Lysin specific demethylase 1 (LSD1) inhibits the tumor suppressor activity of p53 and facilitates the progress of tumor. In order to check the tumor growth, the activity of LSD1 enzyme is to be blunted. Methods: Phytochemicals from naturally occurring plant-based anti-cancer compound-activity-target (NPACT) database are screened with LSD1 as target applying genetic algorithm (GA) method to study best ligand poses and free energy of binding using Argus Lab. The prediction of drug-likeness and oral toxicity of the ligands are performed by the online tools Molsoft and ProTox respectively. Results: Calyxin H shows optimum binding affinity to both the substrate and FAD binding sites of LSD1. The LD 50 value (median lethal dose) of calyxin H is more than 1000 mg/kg body weight and the toxicity class is 4. Conclusions: Calyxin H is the inhibitor of choice against target LSD1. The lead molecule may be the future potential herbal drug for cancer treatment.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86056125","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-04-02DOI: 10.26510/2394-0859.PBE.2017.14
E. K. Kporou, C. Ibourahema, A. J. Ackah, S. Ouattara
Objective: The present study was undertaken to evaluate antifungal potential of improved crude extracts of Mitracarpus scaber Zucc., an ivorian traditional medicinal plant against two species of clinical yeast isolates: Candida parapsilosis and Candida guilliermondii . Methods : For evaluation of antifungal activity, double dilution method in slope tubes was used. Crude extracts of M . scaber were prepared by extracting with a blender in aqueous and hydroalcohol. In first; Aqueous (X Aq ) and Hydroalcoholic (X 0 ) extracts were evaluated, and secondary the crude extract X 0 was improved by partition in mixture of aqueous and hexanic solvent 50:50 v/v. Each dried phase was also examined. A phytochemical screening has been performed on most active extracts. Results : In vitro antifungal activity showed that crude extract X 0 was the most active with MIC = 6.25 mg/ml. Among the extracts obtained by partition from extract X 0 , extract X 11 (Hexanic phase) was the better with lowest antifungal parameters MIC and MFC range between 1.562 mg/ml and 0.781 mg/ml and IC 50 range between 0.73 mg/ml to 0.598 mg/ml. In addition, the most active extract contained only terpens and steroids. Conclusions : Antifungal activity of M . scaber was improved by partition of an hydroalcoholic extract (X 0 ) in mixture hexane-water 50:50 v/v. Hexanic phase (X 11 ) was more active against C . parapsilosis and C . guilliermondii .
{"title":"Antifungal potential of improved crude extracts of Mitracarpus scaber (Zucc) against Candida guilliermondii and Candida parapsilosis","authors":"E. K. Kporou, C. Ibourahema, A. J. Ackah, S. Ouattara","doi":"10.26510/2394-0859.PBE.2017.14","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.14","url":null,"abstract":"Objective: The present study was undertaken to evaluate antifungal potential of improved crude extracts of Mitracarpus scaber Zucc., an ivorian traditional medicinal plant against two species of clinical yeast isolates: Candida parapsilosis and Candida guilliermondii . Methods : For evaluation of antifungal activity, double dilution method in slope tubes was used. Crude extracts of M . scaber were prepared by extracting with a blender in aqueous and hydroalcohol. In first; Aqueous (X Aq ) and Hydroalcoholic (X 0 ) extracts were evaluated, and secondary the crude extract X 0 was improved by partition in mixture of aqueous and hexanic solvent 50:50 v/v. Each dried phase was also examined. A phytochemical screening has been performed on most active extracts. Results : In vitro antifungal activity showed that crude extract X 0 was the most active with MIC = 6.25 mg/ml. Among the extracts obtained by partition from extract X 0 , extract X 11 (Hexanic phase) was the better with lowest antifungal parameters MIC and MFC range between 1.562 mg/ml and 0.781 mg/ml and IC 50 range between 0.73 mg/ml to 0.598 mg/ml. In addition, the most active extract contained only terpens and steroids. Conclusions : Antifungal activity of M . scaber was improved by partition of an hydroalcoholic extract (X 0 ) in mixture hexane-water 50:50 v/v. Hexanic phase (X 11 ) was more active against C . parapsilosis and C . guilliermondii .","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76881506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-04-02DOI: 10.26510/2394-0859.pbe.2017.15
J. Rath, M. K. Raval
Objective: RmlC (dTDP-6-deoxy-D-xylo-4-hexulose 3, 5-epimerase) is a crucial enzyme for cell wall biosynthesis in Mycobacterium tuberculosis. It’s absence in human host attest it as a valid target for drug designing. In the presented study an in-silico method is employed to find out the potential phytochemical inhibitors of RmlC . Methods: AutoDock 4.2 is used to study the binding affinity of ligands in the active site of the protein. The drug-likeness and oral toxicity evaluation is done using the online tools Molsoft and ProTox respectively. Results: Chrysophanol has binding affinity of -9.24 kcal/mole to RmlC active site. PASS tool predicts chrysophanol as antitubercular compound. Its druglikeness is 0.1, and toxicity class is 5 measured by ProTox. Hence, chrysophanol emerges as a lead molecule among the phytochemicals in the database. Conclusions: Crysophanol is the lead inhibitor against RmlC target. The lead molecule may work as a successful drug in future for tuberculosis treatment.
{"title":"Structure based screening of ligands against dTDP-6-deoxy-D-xylo-4-hexulose 3, 5-epimerase (RmlC): phytochemical as drug candidate for Mycobacterium tuberculosis","authors":"J. Rath, M. K. Raval","doi":"10.26510/2394-0859.pbe.2017.15","DOIUrl":"https://doi.org/10.26510/2394-0859.pbe.2017.15","url":null,"abstract":"Objective: RmlC (dTDP-6-deoxy-D-xylo-4-hexulose 3, 5-epimerase) is a crucial enzyme for cell wall biosynthesis in Mycobacterium tuberculosis. It’s absence in human host attest it as a valid target for drug designing. In the presented study an in-silico method is employed to find out the potential phytochemical inhibitors of RmlC . Methods: AutoDock 4.2 is used to study the binding affinity of ligands in the active site of the protein. The drug-likeness and oral toxicity evaluation is done using the online tools Molsoft and ProTox respectively. Results: Chrysophanol has binding affinity of -9.24 kcal/mole to RmlC active site. PASS tool predicts chrysophanol as antitubercular compound. Its druglikeness is 0.1, and toxicity class is 5 measured by ProTox. Hence, chrysophanol emerges as a lead molecule among the phytochemicals in the database. Conclusions: Crysophanol is the lead inhibitor against RmlC target. The lead molecule may work as a successful drug in future for tuberculosis treatment.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81912906","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-04-02DOI: 10.26510/2394-0859.PBE.2017.18
V. Bakshi, .S Swapna, D. Choudhary, C. Revanth, B. Praveen, C. Praveen
Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction. Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro . The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR). Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.
{"title":"Design and characterization of metoprolol floating matrix tablet","authors":"V. Bakshi, .S Swapna, D. Choudhary, C. Revanth, B. Praveen, C. Praveen","doi":"10.26510/2394-0859.PBE.2017.18","DOIUrl":"https://doi.org/10.26510/2394-0859.PBE.2017.18","url":null,"abstract":"Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction. Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro . The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR). Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.","PeriodicalId":19998,"journal":{"name":"Pharmaceutical and Biological Evaluations","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79031872","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：