Antidiabetic antihyperlipidemic and hepato-protective effect of Gluconorm-5: A polyherbal formulation in steptozotocin induced hyperglycemic rats.

Background: The antidiabetic, antihyperlipidemic, and hepato-protective effect of Gluconorm-5, was studied in steptozotocin (STZ) induced hyperglycemic rats.

Materials And Methods: The hypoglycemic effect of single dose of Gluconorm-5 (150, 300 and 600 mg/kg body weight) made up of five plants namely Camellia sinensis, Punica granatum, Macrotyloma uniflorum, Foeniculum vulgare and Trigonella foenum-graecum was studied in normal, glucose loaded normal and diabetes-induced rats. The extent of antihyperlipidemic and liver-protective effect was studied by estimating the lipid profile, and the liver marker enzymes.

Influence of alpha lipoic acid on antioxidant status in D-galactosamine-induced hepatic injury.

D-Galactosamine (GalN)-induced liver injury is associated with reactive oxygen species and oxidative stress. In the present study, we evaluated the effect of alpha lipoic acid (ALA) supplementation on acute GalN-induced oxidative liver injury. Hepatotoxicity induced by single intraperitoneal injection of GalN (500 mg/kg body wt) was evident from increase in lipid peroxidation and serum marker enzymes (asparate transaminase, alanine transaminase, alkaline phosphatase, and lactate dehydrogenase).

Synthesis and pharmacological evaluation of 1-(1-((substituted)methyl)-5-methyl-2-oxoindolin-3-ylidene)-4-(substituted pyridin-2-yl)thiosemicarbazide.

Some novel Mannich base isatin derivatives were synthesized by reacting 1-(5-methyl-2-oxoindolin-3-ylidene)-4-(substitutedpyridin-2-yl)thiosemicarbazide with formaldehyde and several secondary amines. Their chemical structure was elucidated by means of spectral (FT-IR, (1)H- and (13)C-NMR and mass) analysis. Investigation of anti-inflammatory activity of synthesized compounds was done by carrageenan induced paw oedema method using diclofenac sodium as standard drug and analgesic activity was done by acetic acid induced writhing method.

Immune Augmentation of Single Contact Hepatitis B Vaccine by Using PLGA Microspheres as an Adjuvant.

The present study was aimed to replace the alum type adjuvant for hepatitis B vaccine. The hepatitis B vaccine was encapsulated in poly (DL-lactide-co-glycolide) microspheres by solvent evaporation technique. The formulated microspheres were characterized in terms of morphology, particle size analysis, in vitro release study and in vivo immune response in male Wistar rats.

Mitigation of azathioprine-induced oxidative hepatic injury by the flavonoid quercetin in wistar rats.

ABSTRACT Azathioprine (AZA), one of the widely prescribed immunosuppressant drugs in organ transplantation and autoimmune diseases, could cause hepatotoxicity in the course of therapy. The current work was designed to assess the protective role of the dietary flavonoid, quercetin (QE), in oxidative hepatic damage induced by AZA. Adult male Wistar rats were divided into four treatment groups.

Antitumor and cytotoxic effects of Phyllanthus polyphyllus on Ehrlich ascites carcinoma and human cancer cell lines.

To evaluate the antitumor and cytotoxic activity of methanol extract of Phyllanthus polyphyllus (MPP) in mice and human cancer cell lines, the antitumor activity of MPP was evaluated against an Ehrlich ascites carcinoma (EAC) tumor model. The activity was assessed using survival time, hematological studies, lipid peroxidation (LPO), antioxidant enzymes such as superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx), glutathione S-transferase (GST), solid tumor mass, and short-term in vitro cytotoxicity. The cytotoxic activity of MPP was evaluated using human breast cancer (MCF7), colon cancer (HT29), and liver cancer (HepG2) cell lines Oral administration of MPP (200 and 300 mg/kg) increased the survival time and significantly reduced the solid tumor volume in a dose-dependent manner.

Characterization of polymeric poly(epsilon-caprolactone) injectable implant delivery system for the controlled delivery of contraceptive steroids.

Contraceptive steroids levonorgestrel (LNG) and ethinyl estradiol (EE) have been encapsulated with poly(epsilon-caprolactone) (PCL) microspheres using a w / o /w double emulsion method. The microspheres prepared were smooth and spherical, with a mean size from 8-25 microm. In vitro release profiles of microspheres showed a trend of increasing initially at the first week, and thereafter the release was sustained.

Synthesis, anticonvulsant and antihypertensive activities of 8-substituted quinoline derivatives.

A series of 8-substituted quinolines were synthesized and tested against seizures induced by maximal electro shock (MES), pentylenetetrazole (scMet) and antihypertensive activities. Neurologic deficit was evaluated by the rotarod test. Among the newly synthesized derivatives, several compounds with a 2-hydroxypropyloxyquinoline moiety displayed excellent anticonvulsant and antihypertensive activities.

Ultrasonically controlled release and targeted delivery of diclofenac sodium via gelatin magnetic microspheres.

In the present work, an attempt was made to target diclofenac sodium to its site of action through magnetic gelatin microspheres. The gelatin magnetic microspheres loaded with 8.9% w/w of diclofenac sodium and 28.

Biopharmaceutical and pharmacodynamic studies on topically applied diclofenac gel available in Indian market.

In the present investigation, an attempt was made to study and compare, analgesic and anti-inflammatory activity produced by four marketed topical diclofenac formulations in order to justify their usefulness in the treatment of pain and inflammation. By using a diffusion cell, in vitro percutaneous permeation studies were carried out to correlate in vivo activity. The in vivo analgesic activity study was performed by tail flick method on Wistar albino rats.

Influence of manufacturing parameters on development of contraceptive steroid loaded injectable microspheres.

The main objective of this work was to develop a system consisting of polymeric microspheres loaded with steroid drugs. The drugs were encapsulated using biodegradable poly(lactide-co-glycolide) (PLG) and poly(epsilon-caprolactone) (PCL) by double emulsion solvent evaporation method. The lipophilic drugs, levonorgestrel and ethinylestradiol were made soluble by adding ethanol/water mixture.

Diclofenac sodium loaded gelatin magnetic microspheres for intra-arterial administration: formulation, characterization and in vitro release studies.

Gelatin magnetic microspheres loaded with diclofenac sodium were prepared by emulsification and crosslinking by glutaraldehyde. The microspheres were formulated with 23-30% theoretical diclofenac sodium and magnetite content. The formulated microspheres were characterized by drug loading, entrapment efficiency, encapsulation efficiency, magnetite content, FT-IR spectroscopy, particle size analysis, optical microscopy, scanning electron microscopy, and in vitro release studies.

PHARMACOGNOSTIC STUDIES ON Gisekia Pharnaceoides Linn.

Gisekia Pharnaceoides Linn is a diffuse subsucculent, glabrous herb. It is aromatic, aperient and act as powerful anthelmintic in cases of taenia. The plant possesses antibacterial, CNS depressant and anthelmintic activity.

Preparation and characterization of injectable microspheres of contraceptive hormones.

Present study describes the development of a new formulation of levonorgestrel and ethinylestradiol based on double emulsion-solvent evaporation technique using poly(epsilon-caprolactone) (PCL) as biodegradable polymer. The effect of polymer concentration on microspheres and entrapment of drug into microspheres were studied. PCL was selected because of its hydrophobicity and advantages over other biodegradable polymers.

Synthesis and anticonvulsant activity of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones.

The synthesis and pharmacological evaluation of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones (4a--l, 5a--j) as potential anticonvulsant agents are described. The compounds were tested in vivo for the anticonvulsant activity. The compound which have maximum protection against MES induced seizures is 1-[3-(2-aminophenylamino)-2-hydroxypropyl)-1,2-dihydro-pyridazine-3,6-dione 4h (ED(50)=44.

Hydroxypropyl methylcellulose based cephalexin extended release tablets: influence of tablet formulation, hardness and storage on in vitro release kinetics.

The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required theoretical release profile. The influences of HPMC, microcrystalline cellulose powder (MCCP), granulation technique, wetting agent and tablet hardness on cephalexin release from HPMC based extended release tablets were studied.

Ibuprofen-loaded ethylcellulose/polystyrene microspheres: an approach to get prolonged drug release with reduced burst effect and low ethylcellulose content.

The aim of this study was to develop ethylcellulose microspheres for prolonged drug delivery with reduced burst effect. Ethylcellulose microspheres loaded with ibuprofen were prepared with and without polystyrene, which was used to retard drug release from ethylcellulose microspheres. Ibuprofen-loaded ethylcellulose microspheres with a polystyrene content of 0-25% were prepared by the solvent evaporation technique and characterized by drug loading, infrared spectroscopy, differential scanning calorimetry and scanning electron microscopy.

Pharmacological evaluation of some new 2-substituted pyridine derivatives.

In the present study, a series of 2-substituted-pyridines were synthesized and characterized by IR, (1)H-NMR and Elemental Analysis. The compounds were assayed against seizures induced by maximal electro shock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test.

Pharmacological evaluation of some new 6-amino/methyl pyridine derivatives.

In the present study, a series of 2-substituted-pyridines were synthesized and characterized by IR, (1)H-NMR and Elemental Analysis. The compounds were assayed against seizures induced by maximal electro shock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test.

Synthesis and CNS activities of 2-methyl/5-chloro-8-(3-substituted propoxy)quinolines.

In the present study, a series of 2-methyl/5-choloro-8-(3-substituted propoxy) quinolines were synthesized. The compounds were characterized by IR, 1H-NMR and elemental analysis. The compounds were investigated for anticonvulsant and decrease in the elevated motor activity by introceptive chemical stimuli (amphetamine antagonistic activity) at the dose level of 80 and 160 mg/kg.

Formulation and in vivo evaluation of niosome-encapsulated daunorubicin hydrochloride.

The central aim of this present study was to modify the reverse evaporation process, such that an enhanced entrapment, with increased storage stability and prolonged release, could be achieved, and to translate these advantages to increased therapeutic efficacy of daunorubicin hydrochloride on Dalton's ascitic lymphoma. Niosomes prepared exhibited entrapment efficiency 20% higher than theoretically possible by the reverse evaporation process. The niosomes were found to be very stable at a storage temperature of 4 degrees C for a duration of three months.

Pharmacological evaluation of some new 1-substituted-4-hydroxy-phthalazines.

In the present study, a series of 1-substituted-4-hydroxyphthalazines were synthesized and characterized by IR, 1H-NMR and Elemental analysis. The compounds were assayed against seizures induced by maximal electroshock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test.

Eudragit NE30D based metformin/gliclazide extended release tablets: formulation, characterisation and in vitro release studies.

Metformin/Gliclazide extended release tablets were formulated with Eudragit NE30D by wet granulation technique. Two batches were prepared in order to study influence of drug polymer ratio on the tablet formation and in vitro drug release. The formulated tablets were characterized by disintegration time, hardness, friability, thickness, weight variation, and in vitro drug release.

Synthesis and pharmacological activities of 1,8-naphthyridine derivatives.

In the present study, a series of 2-substituted-4-methyl-7-amino/4,7-dimethyl-1,8-naphthyridines were synthesized and characterized by IR, 1H-NMR and elemental analysis. The compounds were investigated for anticonvulsant (125, 250 mg/kg), cardiac and antimicrobial activities. The compounds were screened for antibacterial activity against gram (+) bacteria (Staphylococcus epidermidis, Bacillus subtilis, Enterococcusfaecalis and Micrococcus luteus) and gram (-) bacteria (Proteus vulgaris, Pseudomonas aeruginosa, Escherichia coli and Salmonella typhi).

Synthesis and pharmacological activities of 2-(3'-substituted-2'-hydroxypropylamino)pyridines.

In the present study, a series of 2-(3'-substituted-2'-hydroxypropylamino)pyridines were synthesized and characterized by IR, 1H-NMR and elemental analysis. The compounds were investigated for anticonvulsant (150, 300 mg/kg) and cardiac activity. 2-(3'-Diethylamino-2'-hydroxypropylamino)pyridine 3 was found to exhibit the highest anticonvulsant activity.