Journal of Chemical and Pharmaceutical Research

ABSTRACT: 4-Aminopyrimidine-5-carbaldehyde 1 underwent facile condensation with various aromatic ketone derivatives in the presence of K2CO3 and small catalytic amount of KI in acetone was afforded corresponding 7-Substituted pyrido[2,3-d]pyrimidine derivatives 3a-j. Their chemical structures were characterized using IR, H1 NMR and Mass spectral studies. All the above compounds were screened for anti-microbial activity, anti-oxidant activity and their bioassay showed them to possess significant antimicrobial activity and anti-oxidant activity. Introduction :   For small organic molecules, simple nitrogen-containing heterocycles receive a large amount of attention in the literature, of these heterocycles, the synthesis, reactions and biological activities of pyridine containing molecules stands as an ever expanding area of research in hetero aromatic chemistry. pyrido[2,3-d]pyrimidine heterocycles have received much less attention in the literature, in spite of their ...

ABSTRACT: The present work focuses on the development of hydrodynamically balanced delivery system of loratadine as a single unit floating capsules. Sustained release floating capsules for loratadine were fabricated using drug:polymer ratio of 1:4. The hydrocolloids were used in different proportions using 32 full factorial design and formulations were prepared. These formulations were optimized on the basis of buoyancy, matrix integrity, duration of floating and in vitro drug release. All the nine formulations showed good buoyancy and matrix integrity. The duration of floating was more than 12 h for all formulations. In vitro drug release study of these formulations indicated controlled release of loratadine and about 90 percent drug was released at the end of 12 h. Further details @ http://www.jocpr.com/ For more details @ http://www.jocpr.com/articles/formulation-and-invitro-evaluation-of-floating-capsules-ofloratadine.pdf

ABSTRACT: Two innovative, new, simple and low cost UV-spectrophotometric and first order derivative methods were developed and validated for estimation of Galantamine Hydrobromide in bulk drug and tablet dosage form. Galantamine Hydrobromide was estimated at 289 nm in Distilled Water. In first order derivative, it showed amplitude at 284.8 nm and λminima = 290.4 nm with 286.4 nm as zero crossing point (ZCP). In both the methods linearity was found to be in the range of 20-100 µg/ml; for UV spectrophotometric method (y = 0.007x - 0.002, r² = 0.999) and for first order derivative spectrophotometric method (Y=0.0012 x+0.00045; r2=0.999), respectively. These methods were analyzed and validated for various validation parameters according to USP guidelines. The quantitation limits were found to be 0.50 and 1.54 µg/ml, for UV-Spectrophotometric method and 3.3 and 10 µg/ml for the 1st order derivative method. The proposed methods were successfully applied for the determination of Galant...

ABSTRACT: In the present study, the wound-healing activity of some substituted hydroxytriazenes was investigated. Excision, resutured incision and dead space wound models were used to evaluate the wound-healing activity of substituted hydroxytriazenes. In excision wound model, treatment was continued till the complete healing of the wound, in incision and dead space wound models the treatment was continued for 10 days. For topical application, 5% w/w ointment of hydroxytriazenes was prepared in 2% sodium alginate and for oral administration hydroxytriazenes dissolved in DMSO, at dose 5 mg/kg were used. In excision and incision wound models, the control group of animals was left untreated and in dead space wound models the animals were treated with DMSO (1ml/kg). The healing of the wound was assessed by the rate of wound contraction, period of epithelialisation, skin breaking strength, granulation strength, dry granulation tissue weight and hydroxyproline estimation. Except the p...

ABSTRACT: To study describe the actions of antipsychotics or neuroleptics on the behavioral effects elicited by ketamine on open-field, rota rod and tail suspension tests in mice. A series of novel analogs of 2-[3-{4-(3-chlorophenyl)-1-piperazinyl} propyl]-1,2,4-triazolo [4,3-a] pyridine-3- (2H)-one hydrochloride, a potential psychoactive drug of the piperazine and triazolopyridine chemical classes that has antidepressant, anxiolytic, and hypnotic properties were synthesized. Male swiss albino mice (25–30g) were used for the study and compounds were administered alone (0.1 or 0.2 mg/kg) or thirty minutes before ketamine (10 mg/Kg, ip). ketamine increased (63.3 ± 4.2) the locomotor activity compared to control, while neuroleptics decreased it (25.5 ± 4.2). Pretreatment with neuroleptics, in both doses, blocked hyperlocomotion caused by ketmine. Further details @ http://www.jocpr.com/ For more details @ http://www.jocpr.com/articles/studies-of-antipsychotic-drugs-as-pote...

ABSTRACT: A simple sensitive spectrophotometric method in UV region has been developed for the determination of Ceftazidime in bulk dosage form. The solution of ceftazidime in 0.1N HCl shows maximum absorbance at 261nm, beer’s law was obeyed in the concentration range of 2-10 µg ml-1. The absorbance was found to increase linearly with increasing concentration of ceftazidime, which is corroborated by the calculated correlation coefficient value of 0.9981. The slope and intercept of the equation of the regression line are 0.0465 and 0.0007 respectively. The analysis were validated statistically and its recovery studies result of percentage shows that the method was not affected by the presence of excepients which proves suitability of the developed method for the routine estimation of ceftazidime bulk and solid dosage form. This method were extended to pharmaceutical formulations and there no interference from excepients and diluents. The proposed methods are economical and sensit...

ABSTRACT: In the present study, Adapalene gels were prepared using CMC Na, HPMC, HPC, Carbomer and combinations of cellulose derivatives; as base and PluronicPE-6200 as penetration enhancer for the treatment of Acne. The gels were evaluated for drug content, viscosity determination, in vitro permeation (Nylone-66) and stability studies. The drug content of the gels was found to range from 98-105.7 %. The viscosity of the gels ranged between 7100-83144 cps. . In-vitro diffusion profile of Adapalene gel (optimized formula F-22) obtained in ethanol with water (80:20) indicate that 40.33% drug release found within 6 hrs. while 35.22% of marketed preparation. Although the difference is insignificant, the percentage release of drug was found to increase in the following order of the polymer composition: Carbopol-980> Carbopol-940> Carbopol-934> HPC > SODIUM CMC> HPC+SODIUM CMC > METHYL CELLULOSE > HPMC > HPC+HPMC. Further the formulation F-22 was found to be st...

ABSTRACT: Metal chelates of biologically important Schiff bases namely 4-methyl-2-{[(5'-methyl-3'- isoxazolyl)imino] methyl} phenol(MEMIIMP) and 5-methoxy-2--{[(5'-methyl-3'- isoxazolyl)imino] methyl} phenol(MMIIMP) with Cu(II), Ni(II), Co(II), Zn(II) and VO(IV) have been synthesized. The metal chelates have been characterized by elemental analysis molar conductivity data TG, DTA, spectral (IR, 1H-NMR, Mass, ESR and electronic) and magnetic moments. The dissociation constants of Schiff bases and stability constants of Cu(II), Ni(II), Co(II) and Zn(II) complexes have been determined potentiometrically in aquo organic medium at 30±1oC and at 0.1 M KNO3 ionic strength. Antimicrobial activities of Schiff bases and their complexes were screened against bacteria & fungi are discussed. Introduction :   Studies on a new kind of chemotherapeutic Schiff bases are now attracting the attention of biochemists. Schiff base complexes derived from 4-hydroxy salicylal...

ABSTRACT: Sustained release dosage forms are designed to release a drug at a predetermined rate by maintaining a constant drug level for a specific period of time with minimum side effects. In the recent years, focus on the development of controlled release drug delivery systems has increased. The basic rationale of controlled release drug delivery system optimises the biopharmaceutical, pharmacokinetic, and pharmacodynamic properties of a drug in such a way that its utility is maximized, side-effects are reduced and cure or control of the condition is achieved, in the shortest possible time by using smallest quantity of drug administered by the most suitable route. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance due to less frequent drug administration, reduction of fluctuation in steady-state drug levels, maximum utilisation of the drug, increased safety margin of potent drug, reduction in healthca...

ABSTRACT: Seven new chalcones and flavones containing substitued naphthalene nucleus in their structure were synthesized and the structures of these compounds were confirmed by spectral data. The newly synthesized compounds were screened for antibacterial activity against Escherichia coli and Stahylococcus aureus. Introduction:   The flavoniods have been reported to possess a wide range of biological activites such as antimicrobial, anticancer, antioxidant, antinocicepative, anti-inflammatory, antihypertensive and antifeedant. In view of these observations and in continuation of our work on biologically active chalcones and their heterocycles, we have been planned to synthesize the some new flavones (IIa-h) from chalcones (Ia-h) and also studied their antibacterial activity against Escherichia coli (E. coli) and Stahylococcus aureus (S. aureus) using Tetracycline as a standard drug. Further details @ http://www.jocpr.com/ For more details @ http://www.jocpr...

ABSTRACT: Allium cepa is highly valued for its therapeutic properties. It has been used as a food remedy from time immemorial.Research shows that onions may help guard against many chronic diseases. That's probably because onions contain generous amounts of the flavonoid quercetin. Studies have shown that quercetin protects against cataracts, cardiovascular disease, and cancer. In addition, onions contain a variety of other naturally occurring chemicals known as organosulfur com-pounds that have been linked to lowering blood pressure and cholesterol levels.Although rarely used specifically as a medicinal herb, the onion has a wide range of beneficial actions on the body and when eaten (especially raw) on a regular basis will promote the general health of the body. The bulb is anthelmintic, anti-inflammatory, antiseptic, antispasmodic, carminative, diuretic, expectorant, febrifuge, hypoglycaemic, hypotensive, lithontripic, stomachic and tonic. When used regularly in the diet ...

ABSTRACT: Nimesulide is a second generation non–steroidal anti–inflammatory agent, which is widely used in the long term therapy of rheumatoid arthritis, in alleviating pain and inflammation. But its short half-life (only 3–4hrs.), so its causes more fluctuation. After oral administration Nimesulide causes to produces heart burn, nausea, loose motions, pruritus, etc. The present study based on the preparation of bioadhesive topical gel of Nimesulide, so as to avoid all gastric side effects. For the preparation of bioadhesive topical gel natural polymer aegel marmelos (plant Bale) was used. Bioadhesive polymers are the agents which increases the contact between the formulation and biological membrane, so as to avoid the fluctuation of formulation and behave as a sustained release formulation. In the present study, prepared bioadhesive topical gel was evaluated with the help of different parameters like drug content, spreadability, extrudability, swelling index study, in–vitro dru...

ABSTRACT: A differential pulse polarographic (DPP) method for the determination of Flumetralin is described based on the reduction of a nitro group at a dropping mercury electrode (DME) in Briton-Robinson buffers of pH 2.0 to 12.0 using 25% acetone-water mixture as a solvent. Also a cyclic voltammetric (CV) technique has been used to study the behaviour of Flumetralin at a hanging mercury drop electrode (HMDE). The DPP method described here has been applied to the analysis of Flumetralin in formulations, grains, soils and spiked water samples. Both standard addtion and calibration methods were used for the analytical measurements. The lower detection limit was found to be 1.87x10-8 M. Introduction : Pesticides containing nitro substituents are extensively used in agriculture throughout the world. Flumetralin is one of the dinitroaniline pesticide families and is an economically important class of agricultural compound used to prevent the growth of grasses and weeds in cu...

ABSTRACT: Vasaka is a well-known herb in indigenous systems of medicine for its beneficial effects, particularly in bronchitis.Vasaka leaves, bark, the root bark, the fruit and flowers are useful in the removal of intestinal parasites. Vasaka herb is used for treating cold, cough, chronic bronchitis and asthma. The decoction of its root and bark in doses of 30 grams twice or thrice a day for 3 days can be given for this purpose. The juice of its fresh leaves can also be used in doses of a teaspoon thrice a day for days. In acute stages of bronchitis, vasaka gives unfailing relief, especially where the sputum is thick and sticky. It liquefies the sputum so that it is brought up more easily. For relief in asthma, the dried leaves should be smoked. In Ayurveda, a preparation made from vasaka flowers, known as gulkand is used to treat tuberculosis. The juice from its leaves should be given in doses of 2 to 4 grams in treating diarrhea and dysentery.A few fresh petals of vasaka flowe...

ABSTRACT: Carvedilol is a poorly water soluble oral antihypertensive agent, with problems of variable bioavailability and bioequivalence related to its poor water solubility. Carvedilol is a nonselective beta adrenergic blocking agent with alpha-1 blocking activity and is indicated for the treatment of hypertension and mild to moderate heart failure of ischematic or cardiomyopathic origin In the present work solubility was enhanced by using β- cyclodextrin as a complexing agent. Sweeteners and flavors were used to enhance the organoleptic properties of tablet. Solubility studies were performed to investigate the drug carrier interaction. I.R. and D.S.C studies carried out to investigate any interaction and stability of formulation. Tablets were prepared by direct compression technique. Prepared tablets were evaluated for thickness, uniformity of weight, hardness, friability, wetting time, in-vitro disintegration time, drug content and in vitro drug release. All the formulations ...

ABSTRACT: Variety of 2-amino-3-cyano-4-aryl-6-(1-napthyl amino)-pyridines 3(a-h) have been synthesized by reacting 1-(1-napthyl amino)-3-aryl-2-propen-1-ones 2(a-h) with malononitrile and ammonium acetate in methanol under reflux condition. Structures of the synthesized compounds were confirmed by the spectral analysis. Furthermore, all the synthesized products were screened for their antibacterial activity. Introduction : Among the wide variety of heterocycles that have been explored developing pharmaceutically important molecules like pyridines, cyano-pyridines have played an important role in the heterocyclic chemistry. Pyridine derivatives have occupied a unique position in medicinal chemistry. The naturally occurring B6-vitamins pyridoxine, pyrodoxal, pyridoxamine, and codecarbaxylase contain a pyridine nucleus. In addition to this, many naturallly occurring and synthetic compounds containing the pyridine scaffold possess interesting pharmacological properties. Amon...

ABSTRACT: Bone marrow is the spongy tissue inside some of your bones, such as your hip and thigh bones. It contains immature cells, called stem cells. The stem cells can develop into the red blood cells that carry oxygen through your body, the white blood cells that fight infections, and the platelets that help with blood clotting. If you have a bone marrow disease, there are problems with the stem cells or how they develop. Leukemia is a cancer in which the bone marrow produces abnormal white blood cells. With aplastic anemia, the bone marrow doesn't make red blood cells. Other diseases, such as lymphoma, can spread into the bone marrow and affect the production of blood cells. Other causes of bone marrow disorders include your genetic makeup and environmental factors. The cell compression caused by an overgrowth of the supporting fibrous tissue network, resulting in abnormally shaped cells and decreased numbers of cells. One cell line that becomes predominant because the c...

ABSTRACT: The Raman Effect occurs when light impinges upon a molecule and interacts with the electron cloud and the bonds of that molecule. Raman spectroscopy is commonly used in chemistry, since vibrational information is specific to the chemical bonds and symmetry of molecules. It therefore provides a fingerprint by which the molecule can be identified.A new spectroscopy technique to uncover the precise sequence of atomic movements and structural changes that occur during complex chemical transformations. GFP involves a classic intermolecular proton transfer reaction to produce its fluorescent form. This happens on an ultra fast timescale - from 10 femtoseconds to 10 picoseconds. To perform structural measurements and determine the mechanism and pathway of any reaction occurring in this time range by using femtosecond stimulated Raman spectroscopy (FSRS). A great deal was known about the kinetics of the proton transfer reaction but little was known about the actual complexity ...

ABSTRACT: Medicinal plants are finding use as pharmaceuticals, nutraceuticals, cosmetics and food supplements. Even as traditional source of medicines and they continue to play pivotal rule. Ethanolic extract of three medicinal plants viz., Acalypha indica, Ricinus communis and Euphorbia hirta were evaluated for there therapeutic potential as antimicrobial agent against six standard organisms 3 bacteria (Klebsiela pneumoniae, Salmonella typhi, Pseudomonas aeruginosa) and 3 fungi (Aspergillus flavus, Fusarium oxysporium, Penicillium chrysogenum) by using Filter Paper Disc Method. Antimicrobial efficacy of callus cultures of E. hirta with inhibition zone of 16 mm was found to highest against F. oxysporium (Fungus) and in A. indica with inhibition zone of 27 mm was found to maximum against K. pneumoniae (Bacteria). Contrary, in in vivo analysis of antimicrobial efficacy of A. indica with inhibition zone of 15 mm were found to highest against P. chrysogenum (Fungus) and E. hirta wit...

ABSTRACT: Anti-inflammatory drug ketoprofen was encapsulated in niosome for topical application. Ketoprofen niosome were prepared by thin film hydration method technique using surfactant, cholesterol, dicetyl phosphate & drug mixture in different weight ratios. The prepared niosomes were characterized by various physicochemical parameters & evaluation of release studies of entrapped ketoprofen in niosomes were carried out by UV Visible spectrophotometric method. Introduction :   Niosomes are surfactant vesicles which are used to entrap several pharmaceutical drugs to enhance their sustainability . The present research is attempt towards development of topical application of ketoprofen niosomes. so that drug will reach to target site with enhance sustainability & stability. The novelty of research work is to provide effective and maximize drug concentrations and therapeutic value. Materials and Methods : Sorbitan Esters-20, 40, 60 & 80 & Ch...