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
Derivatization of Gallic Acid with amino acids for accentuation of its antioxidant potential
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 , Neelima Mishra, Prabhat Jain and Brijeshkunvar Mishra
DRUG DISCOVERY TOOLS: COMPUTER AIDED MOLECULAR DESIGN AND CHEMO-INFORMATICS
The article reviews the different approaches used in computer aided molecular design. It also reviews current achievements in the field of chemo-informatics and their impact on modern drug discovery processes. The main data mining approaches used in chemo-informatics such as structural similarity matrices, and classification algorithms, are also outlined. In the conclusion, future prospects of chemo-informatics are also mentioned.
Volume : 1, Issue:4, Page No. 103-114 , Richa Mishra and Brijeshkunvar Mishra
MICROWAVE-ASSISTED SYNTHESIS OF PYRIMIDINETHIONE DERIVATIVES
The application of microwave irradiation (MWI) to organic synthesis has been the focus of considerable attention in recent years and is becoming an increasingly popular technology. The salient features of the microwave approach are rapid reaction rates, cleaner reaction conditions and enhancements in chemical yields. Under the framework of “green chemistry” we have developed an environmentally benign synthesis of pyrimidinethiones.
Volume : 1, Issue:4, Page No. 115-118 , Meenakshi Jaiswal
Comparative 2D QSAR Studies of 1,8-Naphthyridine against Tumor Cell Lines
In a persevering effort to develop better anticancer drugs, a quantitative structure activity relationship analysis using a set of 2-D descriptors was performed on a series of 1,8-naphthyridine derivatives acting by the inhibition of tubulin polymerization. QSAR models that were derived from the study were found to be statistically significant with a good predicting ability. The results obtained from the study justify the use of 2-D descriptors for exploring the requirements of binding of 1,8-naphthyridines to the heterodimer, tubulin. Attempt has been made to explore the structural and/or physicochemical requirements of the compounds, responsible for the action against tumor cells. The physicochemical descriptors and indicator variables were correlated with the biological activity
Volume : 1, Issue:5, Page No. 119-128 , Brijeshkunvar Mishra and Richa Mishra
Dissolution Enhancement of Cefprozil by Solid Dispersion Technique
Oral route is the most preferred route of drug delivery for most of the drugs but it presents a considerable challenge for water insoluble drugs. In the present work solid dispersions of cefprozil were prepared in order to improve the water solubility and thereby its bioavailabilty. The solid dispersions were prepared using mannitol and PEG-6000 as the solubility enhancing agent. The solid dispersion was formulated as tablet and the disintegration and dissolution study were performed. The result revealed increased dissolution of cefprozil and improved bioavailability.
Volume : 1, Issue:5, Page No. 129-133 , Rahul Giri Goswami, Brijeshkunvar Mishra and Richa Mishra