JOURNAL OF PHARMACOLOGY AND BIOMEDICINE

ISSN NUMBER: 2456-8244

JOURNAL OF PHARMACOLOGY AND BIOMEDICINE

ISSN NUMBER: 2456-8244

JOURNAL OF PHARMACOLOGY AND BIOMEDICINE

ISSN NUMBER: 2456-8244

Current Issue

Synthesis of 1,8-Napthyridine derivatives and their evaluation as possible antiepileptic agents

Brijeshkunvar Mishra

ABSTRACT Aminopropyloxy derivatives of 1,8-naphthyridines have been synthesized using the principle of Conrad-Limpach synthesis of quinolines. The hydroxy group at 2- position of the naphthyridine ring was converted to the corresponding epoxypropane ether derivative by etherification with epichlorhydrin. The epoxy ether was then aminated in presence of KOH with the corresponding amines to obtain the aminopropyloxy derivatives. The compounds were tested for anti convulsant action at dose of 150mg/Kg relative to diazepam (5mg/Kg) by prevention of PTZ-induced seizures in mice.

Volume : 1, Issue:1, Page No. 1-8


Validated RP-HPLC method for estimation of Etoricoxib & Paracetamol and its applications in analysis of formulations

Prakash Sahu and Shweta Singh

ABSTRACT The current paper describes a reversed phase high performance liquid chromatographic method for the simultaneous estimation of Etoricoxib and Paracetamol in formulations. The separation was achieved on the LUNA C18 column 5µ (250 x 4.6 mm id), using methanol - water in the ratio 63 - 37 as the mobile phase at 1 ml/min flow rate and 237 nm as detection wavelength. The retention time of Etoricoxib and Paracetamol were 1.6 and 2.9 min respectively. The method was validated in terms of linearity, accuracy, precision, as per ICH Guidelines. The calibration curve was linear in the concentration range from 10-60 µg/ml for etoricoxib and 100-600 µg/ml for paracetamol. Percentage recovery obtained for etoricoxib and paracetamol were 99.60 % and 99.04 % respectively.

Volume : 1, Issue:1, Page No. 9-14


RECENT TECHNOLOGICAL APPROACHES ON FLOATING DRUG DELIVERY SYSTEM

Surendra Dangi*, Anup K. Chakraborty, Neeraj Upmanyu, Sanjay K. Dwivedi, Bhaskar Gupta

ABSTRACT Latest technological processes has been committed to the improvement of managed launch (CR) dosage forms transport structures to triumph over physiological troubles along with unpredictable gastric emptying times (GRT) and less gastric house instances (GRT). Floating drug delivery device are of specific attraction for deliver pills this is regionally active and have limited absorption window within the stomach and upper part of small gut, displaying low solubility at high pH and drug that is risky in the intestinal or colonic environment. Floating drug shipping systems (FDDS) are substances that go with the flow immediately upon touch with gastric fluids gift within the belly and by using floating drug shipping systems for reinforcing the bioavailability of medicine. The concept of gastric retention comes from the need to localize tablets at a selected target a part of gastrointestinal tract (GIT) which include the belly inside the body. The promising methods, methodologies and technique used within the improvement of FDDS by formulating both effervescent and non-effervescent floating tablets based totally on buoyancy mechanism. By using above suitable promising methods it is viable to supply tablets that have slender therapeutic window at specific area. Keywords: Gastric residence time, Bioavailability, absorption window, swell able polymers

Volume : 1, Issue:1, Page No. 44-60


DESIGN AND OPTIMIZATION OF LAMIVUDINE FLOATING MICROSPHERES

Pandey G.K., Pandey D., Jain D., Joshi A., Dubey B.K.

The present study was focused to develop floating microspheres of Lamivudine in order to achieve an extended retention in the upper gastrointestinal tract, which may result in enhanced absorption and thereby improved bioavailability. The present study involves preparation and evaluation of floating microspheres using Lamivudine as a model drug for prolongation of the gastric retention time. As Lamivudine is mainly absorbed from stomach, thus using floating microspheres as a mode of drug delivery helps in increasing its residence time and hence increasing the bioavailability of drug. The microspheres were prepared by the Ionic gelation method. The average diameter and surface morphology of the prepared microspheres were characterized by optical microscope and scanning electron microscopic methods respectively. The prepared microspheres were evaluated for particle size, micromeritic study, drug entrapment efficiency, in vitro buoyancy, swelling index and in vitro release. The effect of various formulation variables on the size and drug release was also investigated. All the formulated microspheres were found to possess good flow properties. Scanning electron microscopy confirmed spherical structure of the prepared microspheres. The best formulation F3 drug release kinetics were evaluated using Zero order, First order, Higuchi model, Korsmeyer - Peppas model. After the interpretation of data that was based on the value of a resulting regression coefficient, it was observed that the Korsmeyer- Peppas model has a highest regression coefficient values indicating that the drug release was based on the erosion of polymeric chain matrix system.

Volume : 1, Issue:1, Page No. 15-29


Pharmacological Appraisal of Herbal Medicines in treating Hepatic Diseases with Recent Advances: A review

Amit Kaushik, Ajay Kumar and Dewasya Pratap Singh

Liver is the most vital organ of the. body, which perform fundamental role in the regulation of diverse processes, such as metabolism, secretion, storage, and detoxification of endogenous and exogenous substances. Due to these functions, hepatic diseases continue to arise as main problem for mankind worldwide. Despite advances in modern medicine, there are no completely effective drugs that stimulate hepatic function, that offer complete protection of the organ, or that help to regenerate hepatic cells. The use of natural remedies for the treatement of liver disease has a long history, starting with the Ayurvedic treatement. Among several novel approaches, probiotics, development of a human recombinant single chain antibody and bone marrow transplant based therapy could also be a hope for the treatement of liver diseases in future.

Volume : 1, Issue:1, Page No. 61-70


Total phenolic content, flavonoid concentration, antimicrobial and insecticidal screening of aqueous extracts of Annona squamosa (seeds), Azadirachta indica (leaves) and Lavandula angustifolia (flower)

Purva Tiwari, Amit Joshi, B. K. Dubey

The present study describes the total phenolic content, flavonoid concentration, antimicrobial and insecticidal screening of aqueous extracts of Annona squamosa (seeds), Azadirachta indica (leaves) and Lavandula angustifolia (flower). The total phenolic content in the extracts was determined using Folin-Ciocalteu reagent and their amounts were found to be 0.045, 0.052 and 0.56 mg GA (gallic acid)/mg. The concentrations of flavonoids were found to be 0.98, 1.25 and 1.12 mg Qu (quercetin)/mg. The extract exhibited dose dependent inhibition of test bacteria. Search for natural insecticides, which are easily degradable and do not have any ill effects on the non-target population, remains one of the top priority issues for many countries. In this study, the aqueous extract have exhibited potent insecticidal activity. This finding suggests that Annona squamosa, Azadirachta indica and Lavandula angustifolia may be considered as a natural source of antioxidants and antimicrobial agents.

Volume : 1, Issue:1, Page No. 30-43


An Evaluation of Phytochemicals in Maceration and Infusion Extracts of Cyperusrotundus Linn.Leaves in Two Different Solvents

Neelam Singh and Madhulika Singh

CyperusrotundusLinn.,is a perennial plant also known as purple nutsedge or nutgrass. It is being used as sedative, carminative, stimulant, tonic, aphrodisiac, diuretic, stomachic, anthelmintic, colic remedy and to remove renal calculi. It is reported to beanalgesic, alternative, astringent, antispasmodic, antimicrobial, carminative, contraceptive, demulcent, emmenagogue, emollient, febrifuge, immunostimulant, laxative, stimulative, tonic, and vermifugeproperties. The present work is aimed at extraction and analysis of phytochemicals from the leaves of Cyperusrotundus Linn. in two different methods of phytochemical extraction name maceration and infusion. Differences were observed not only in the yield of extraction but also in the presence of different phytochemical groups.Yield of extraction for acetonic maceration is 0.83%, while that of ethanolic infusion is reported to be 3.27%.Ethanolic extract were found to be rich in carbohydrates, alkaloids, tennins, phenols, flavonoids and saponins. On the other hand the acetonic extracts were rich in presence of alkaloidal group only. Since there has been little work was reported in the phytochemical of leave or areal parts of C. rotundusL., so the present investigation adds the piece of information in phytochemical study of the selected plant for methods and solvents used.

Volume : 1, Issue:2, Page No. 77-84


ESTIMATION OF DIACEREIN USING HYDROTROPIC AGENT AND DYE DRUG REACTION

Kailashpati Pandey, Prabhat Jain and Brijeshkunvar Mishra

This study was designed to develop and validate hydrotropic agent and dye drug reaction methods for estimation of diacerein in capsule formulation. Hydrotropic solubilization is a technique used to increase the aqueous solubility of poorly water-soluble drugs and the present study was aimed at developing a hydrotropic technique to increase the solubility of diacerein. The analysis of tablets indicated good correlation between the amounts estimated and label claim. The study results indicate good sensitivity of the proposed method. The results of analysis were validated statistically and by recovery studies. The developed methods were validated according to ICH guidelines and values of accuracy, precision and other statistical analysis were found to be in good accordance with the prescribed values. Thus the proposed method was found to be simple, environmentally friendly, accurate and cost effective and can be successfully employed in routine analysis of diacerein in capsule.

Volume : 1, Issue:2, Page No. 85-93


Hepatoprotective effect of ethanolic extract of Curcuma caesia rhizomes in rats on paracetamol induced liver cirrhosis

Rizwan Arif and Sanjay Kumar Dwivedi

The objective of the study to evaluate the hepatoprotective effect of ethanolic extract of Curcuma caesia rhizomes in Wistar rats on paracetamol induced liver. Albino wistar rats were separated into five groups (n=6). Ethanolic extract of Curcuma caesia rhizomes was prepared and evaluated for its hepatoprotective efficacy against paracetamol (PCM) (2g/kg p.o.) induced hepatotoxicity in rats. Silymarin (100mg/kg p.o.) was used as standard. Levels of Serum glutamic pyruvate transaminase (SGPT), Serum glutamic oxaloacetic transaminase (SGOT), alkaline phosphatase (ALP), and total protein was evaluated along with histopathological investigation in various experimental groups of rats. Present study suggested thatthe protective effect of ethanolic extract of Curcuma caesia against paracetamol induced hepatic damage.

Volume : 1, Issue:2, Page No. 71-76


Derivatization of Gallic Acid with amino acids for accentuation of its antioxidant potential

Neelima Mishra, Prabhat Jain and Brijeshkunvar Mishra

Phenolics like gallic acid have been known for their anti oxidant activity since long time. Many attempts for increasing antioxidant potency of phenolics have been made utilizing synthetic and drug discovery tools. In an attempt to improve the antioxidant potential of gallic acid, it was decided to introduce a few amino acids into the structure of gallic acid and evaluate their antioxidant potential in vitro. The amino acid derivatized gallic acid molecules were confirmed for their formation by spectral studies and the in vitro antioxidant potential was evaluated using DPPH free radical scavenging protocol and hydrogen peroxide free radical scavenging assay method. The results revealed that presence of cysteine residues in the amino acids were particularly beneficial for the antioxidant potential.

Volume : 1, Issue:3, Page No. 94-102


Archive

Synthesis of 1,8-Napthyridine derivatives and their evaluation as possible antiepileptic agents

ABSTRACT Aminopropyloxy derivatives of 1,8-naphthyridines have been synthesized using the principle of Conrad-Limpach synthesis of quinolines. The hydroxy group at 2- position of the naphthyridine ring was converted to the corresponding epoxypropane ether derivative by etherification with epichlorhydrin. The epoxy ether was then aminated in presence of KOH with the corresponding amines to obtain the aminopropyloxy derivatives. The compounds were tested for anti convulsant action at dose of 150mg/Kg relative to diazepam (5mg/Kg) by prevention of PTZ-induced seizures in mice.

Volume : 1, Issue:1,Page No. 1-8 , Brijeshkunvar Mishra


Validated RP-HPLC method for estimation of Etoricoxib & Paracetamol and its applications in analysis of formulations

ABSTRACT The current paper describes a reversed phase high performance liquid chromatographic method for the simultaneous estimation of Etoricoxib and Paracetamol in formulations. The separation was achieved on the LUNA C18 column 5µ (250 x 4.6 mm id), using methanol - water in the ratio 63 - 37 as the mobile phase at 1 ml/min flow rate and 237 nm as detection wavelength. The retention time of Etoricoxib and Paracetamol were 1.6 and 2.9 min respectively. The method was validated in terms of linearity, accuracy, precision, as per ICH Guidelines. The calibration curve was linear in the concentration range from 10-60 µg/ml for etoricoxib and 100-600 µg/ml for paracetamol. Percentage recovery obtained for etoricoxib and paracetamol were 99.60 % and 99.04 % respectively.

Volume : 1, Issue:1,Page No. 9-14 , Prakash Sahu and Shweta Singh


RECENT TECHNOLOGICAL APPROACHES ON FLOATING DRUG DELIVERY SYSTEM

ABSTRACT Latest technological processes has been committed to the improvement of managed launch (CR) dosage forms transport structures to triumph over physiological troubles along with unpredictable gastric emptying times (GRT) and less gastric house instances (GRT). Floating drug delivery device are of specific attraction for deliver pills this is regionally active and have limited absorption window within the stomach and upper part of small gut, displaying low solubility at high pH and drug that is risky in the intestinal or colonic environment. Floating drug shipping systems (FDDS) are substances that go with the flow immediately upon touch with gastric fluids gift within the belly and by using floating drug shipping systems for reinforcing the bioavailability of medicine. The concept of gastric retention comes from the need to localize tablets at a selected target a part of gastrointestinal tract (GIT) which include the belly inside the body. The promising methods, methodologies and technique used within the improvement of FDDS by formulating both effervescent and non-effervescent floating tablets based totally on buoyancy mechanism. By using above suitable promising methods it is viable to supply tablets that have slender therapeutic window at specific area. Keywords: Gastric residence time, Bioavailability, absorption window, swell able polymers

Volume : 1, Issue:1,Page No. 44-60 , Surendra Dangi*, Anup K. Chakraborty, Neeraj Upmanyu, Sanjay K. Dwivedi, Bhaskar Gupta


DESIGN AND OPTIMIZATION OF LAMIVUDINE FLOATING MICROSPHERES

The present study was focused to develop floating microspheres of Lamivudine in order to achieve an extended retention in the upper gastrointestinal tract, which may result in enhanced absorption and thereby improved bioavailability. The present study involves preparation and evaluation of floating microspheres using Lamivudine as a model drug for prolongation of the gastric retention time. As Lamivudine is mainly absorbed from stomach, thus using floating microspheres as a mode of drug delivery helps in increasing its residence time and hence increasing the bioavailability of drug. The microspheres were prepared by the Ionic gelation method. The average diameter and surface morphology of the prepared microspheres were characterized by optical microscope and scanning electron microscopic methods respectively. The prepared microspheres were evaluated for particle size, micromeritic study, drug entrapment efficiency, in vitro buoyancy, swelling index and in vitro release. The effect of various formulation variables on the size and drug release was also investigated. All the formulated microspheres were found to possess good flow properties. Scanning electron microscopy confirmed spherical structure of the prepared microspheres. The best formulation F3 drug release kinetics were evaluated using Zero order, First order, Higuchi model, Korsmeyer - Peppas model. After the interpretation of data that was based on the value of a resulting regression coefficient, it was observed that the Korsmeyer- Peppas model has a highest regression coefficient values indicating that the drug release was based on the erosion of polymeric chain matrix system.

Volume : 1, Issue:1,Page No. 15-29 , Pandey G.K., Pandey D., Jain D., Joshi A., Dubey B.K.


Pharmacological Appraisal of Herbal Medicines in treating Hepatic Diseases with Recent Advances: A review

Liver is the most vital organ of the. body, which perform fundamental role in the regulation of diverse processes, such as metabolism, secretion, storage, and detoxification of endogenous and exogenous substances. Due to these functions, hepatic diseases continue to arise as main problem for mankind worldwide. Despite advances in modern medicine, there are no completely effective drugs that stimulate hepatic function, that offer complete protection of the organ, or that help to regenerate hepatic cells. The use of natural remedies for the treatement of liver disease has a long history, starting with the Ayurvedic treatement. Among several novel approaches, probiotics, development of a human recombinant single chain antibody and bone marrow transplant based therapy could also be a hope for the treatement of liver diseases in future.

Volume : 1, Issue:1,Page No. 61-70 , Amit Kaushik, Ajay Kumar and Dewasya Pratap Singh


Total phenolic content, flavonoid concentration, antimicrobial and insecticidal screening of aqueous extracts of Annona squamosa (seeds), Azadirachta indica (leaves) and Lavandula angustifolia (flower)

The present study describes the total phenolic content, flavonoid concentration, antimicrobial and insecticidal screening of aqueous extracts of Annona squamosa (seeds), Azadirachta indica (leaves) and Lavandula angustifolia (flower). The total phenolic content in the extracts was determined using Folin-Ciocalteu reagent and their amounts were found to be 0.045, 0.052 and 0.56 mg GA (gallic acid)/mg. The concentrations of flavonoids were found to be 0.98, 1.25 and 1.12 mg Qu (quercetin)/mg. The extract exhibited dose dependent inhibition of test bacteria. Search for natural insecticides, which are easily degradable and do not have any ill effects on the non-target population, remains one of the top priority issues for many countries. In this study, the aqueous extract have exhibited potent insecticidal activity. This finding suggests that Annona squamosa, Azadirachta indica and Lavandula angustifolia may be considered as a natural source of antioxidants and antimicrobial agents.

Volume : 1, Issue:1,Page No. 30-43 , Purva Tiwari, Amit Joshi, B. K. Dubey


An Evaluation of Phytochemicals in Maceration and Infusion Extracts of Cyperusrotundus Linn.Leaves in Two Different Solvents

CyperusrotundusLinn.,is a perennial plant also known as purple nutsedge or nutgrass. It is being used as sedative, carminative, stimulant, tonic, aphrodisiac, diuretic, stomachic, anthelmintic, colic remedy and to remove renal calculi. It is reported to beanalgesic, alternative, astringent, antispasmodic, antimicrobial, carminative, contraceptive, demulcent, emmenagogue, emollient, febrifuge, immunostimulant, laxative, stimulative, tonic, and vermifugeproperties. The present work is aimed at extraction and analysis of phytochemicals from the leaves of Cyperusrotundus Linn. in two different methods of phytochemical extraction name maceration and infusion. Differences were observed not only in the yield of extraction but also in the presence of different phytochemical groups.Yield of extraction for acetonic maceration is 0.83%, while that of ethanolic infusion is reported to be 3.27%.Ethanolic extract were found to be rich in carbohydrates, alkaloids, tennins, phenols, flavonoids and saponins. On the other hand the acetonic extracts were rich in presence of alkaloidal group only. Since there has been little work was reported in the phytochemical of leave or areal parts of C. rotundusL., so the present investigation adds the piece of information in phytochemical study of the selected plant for methods and solvents used.

Volume : 1, Issue:2,Page No. 77-84 , Neelam Singh and Madhulika Singh


ESTIMATION OF DIACEREIN USING HYDROTROPIC AGENT AND DYE DRUG REACTION

This study was designed to develop and validate hydrotropic agent and dye drug reaction methods for estimation of diacerein in capsule formulation. Hydrotropic solubilization is a technique used to increase the aqueous solubility of poorly water-soluble drugs and the present study was aimed at developing a hydrotropic technique to increase the solubility of diacerein. The analysis of tablets indicated good correlation between the amounts estimated and label claim. The study results indicate good sensitivity of the proposed method. The results of analysis were validated statistically and by recovery studies. The developed methods were validated according to ICH guidelines and values of accuracy, precision and other statistical analysis were found to be in good accordance with the prescribed values. Thus the proposed method was found to be simple, environmentally friendly, accurate and cost effective and can be successfully employed in routine analysis of diacerein in capsule.

Volume : 1, Issue:2,Page No. 85-93 , Kailashpati Pandey, Prabhat Jain and Brijeshkunvar Mishra


Hepatoprotective effect of ethanolic extract of Curcuma caesia rhizomes in rats on paracetamol induced liver cirrhosis

The objective of the study to evaluate the hepatoprotective effect of ethanolic extract of Curcuma caesia rhizomes in Wistar rats on paracetamol induced liver. Albino wistar rats were separated into five groups (n=6). Ethanolic extract of Curcuma caesia rhizomes was prepared and evaluated for its hepatoprotective efficacy against paracetamol (PCM) (2g/kg p.o.) induced hepatotoxicity in rats. Silymarin (100mg/kg p.o.) was used as standard. Levels of Serum glutamic pyruvate transaminase (SGPT), Serum glutamic oxaloacetic transaminase (SGOT), alkaline phosphatase (ALP), and total protein was evaluated along with histopathological investigation in various experimental groups of rats. Present study suggested thatthe protective effect of ethanolic extract of Curcuma caesia against paracetamol induced hepatic damage.

Volume : 1, Issue:2,Page No. 71-76 , Rizwan Arif and Sanjay Kumar Dwivedi


ABOUT JOURNAL OF PHARMACOLOGY AND BIOMEDICINE

Journal of Pharmacology and Biomedicine publishes findings from quality research articles, reviews and general articles in the field of pharmacology, pharmacotherapeutics, biomedicine and drug delivery & analysis.

JPB encompasses all aspects of basic research/clinical studies related to the field of pharmacology, pharmacotherapeutics and biomedicine.

The areas of Biomedicine that are particularly significant in research and included in the journal are

  • Mechanism of Drug Action
  • Drug Discovery
  • Analytical Approaches for New Drugs
  • Extraction and Isolation of Bioactives from Plant Sources

 

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