The radioactive agents used in the nuclear medical field are called radiopharmaceuticals and are required to exhibit high and specific localization of radioactivity into target tissue. Among radionuclides used in radiopharmaceuticals 99mTc plays an important role in widespread applications. The preeminence of 99mTc is attributable to its optimal nuclear properties of a short half-life and a gamma photon emission of 140 keV, which is suitable for high-efficiency detection and which results in low radiation exposure to the patient. Radionuclides in nuclear medicine are all synthetic and fall into four categories namely, generator produced, thermal neutron reactor produced, cyclotron produced and pile produced. Radiopharmaceuticals undergo a very lengthy and expensive regulatory process as well as extensive chemical and physical testing (pH, isotonicity and chemical parameters) to insure that the final product is sterile, pyrogen free, safe for human use and is efficacious. These include both animal and human studies prior to release of the product for sale. Clinical application of radioactive diagnostic and therapeutic agents constitutes one of the great advances in nuclear medicine. Various radiopharmaceuticals have been applied clinically in the diagnosis of various malignant and benign conditions. This article highlights the preparation, evaluation and applications of radiopharmaceutical preparations; which contain such useful radio atoms.

Smoking can be ranked as the most serious risk factor in terms of its impact on the well being of an individual and society. Factors such as withdrawal symptoms, abstinence levels achieved, quit failures associated with particular nicotine. replacement product decides success of any smoking cessation therapy. Often, individual preferences play a crucial role in selecting particular intervention program. Today, several dosage forms of nicotine (gum, inhaler, patch, spray) are available in the market, which claim to meet varied clinical demands of smokers in terms of nicotine intake during treatment. There is a strong scientific rationale behind development of these products, and each product aims to reinforce the treatment. However, there is a clear need for new dosage forms and more effective therapy so as to persuade a large number of smokers for treatment, thereby enhancing cessation rates and improving public health. The present manuscript is a compilation of products available for smoking cessation program and discusses their usefulness, advantages and limitations.

The ethanol extract of the dried leaves of Desrnodium triquetrum was studied for wound healing effect using incision, excision and dead space wound models in rats. Significant Increase in wound contraction rate, skin breaking strength, granuloma strength and dry granuloma weight and significant decrease in epithelization period was observed. The prohealing actions seemed to be due to increased collagen deposition as well as better alignment and maturation.

The title compounds were synthesized by the intramolecular cyclisation of thiosemicarbazides generated by the action of hydrazides 3a-d on carbon disulfide in the presence of potassium hydroxide in good yield. All the compounds have been characterized by elemental analysis and spectral data. All the synthesized compounds were screened for their antibacterial, antifungal, anticonvulsant, antiinflammatory and diuretic activities.

Quantitative structure activity relationship analysis of 41 amide and ester derivatives of indomethacin using Hansch's extra thermodynamic multi-parameter approach and receptor surface analysis has been performed to determine the factors required for selective inhibition of second isoform of cyclooxygenase enzyme by these derivatives. The substrate's conformation was abstracted from Cambridge crystallographic data bank. For the Hansch approach, special emphasis was laid on various electronic, spatial and thermodynamic descriptors at the minimum energy conformation. Receptor surface analysis was performed taking most selective molecule as a reference compound. Statistical analysis was performed using multiple regression analysis for simple quantitative structure activity relationship analysis and genetic function approximation for receptor surface analysis. The quantitative structure activity relationship analysis model derived from receptor surface analysis was found to be significant as compared to those produced from using conventional physico-chemical descriptors. These results provide the tools for predicting the affinity of related compounds and for guiding the design and synthesis of new selective cyclooxygenase-2 inhibitors with predetermined affinity.

This work is an attempt to develop a generalized upgradable bench top level technology for nanocapsulation of antineoplastic drug substances. Methotrexate was selected as a model drug and calcium alginate was used as a coating material. A nebulizer head was so designed as to atomize a drug-polymer microemulsion directly into calcium chloride cross linker media. Nanocapsules thus formed were compared with those produced by in situ gelling technique. Control of various process parameters resulted in the development of superior drug nanocapsules by pneumatic nebulization technique with good yield.

Durva ghrita is herbal formulation containing Cynodon dactylon and Cow's ghee as its main constituents. In the present study Durva ghrita was evaluated for its wound healing property by incision and excision wound models in male Wistar rats. Treatment with Durva ghrita alone promoted wound contraction and reduced the time for closure showing healing potential comparable to framycetin sulphate cream 1% w/w. Histopathological studies shows proliferation of epithelial tissue, angiogenesis and fibrosis due to treatment with Durva ghrita. The present study demonstrates wound healing potential of the test formulation.

The effect of aspirin, ibuprofen, and nimesulide the three nonsteroidal anti inflammatory drugs on cell growth of MCF-7 human malignant breast tumour cells was investigated. The results demonstrated that the drugs exerted a preferential cytotoxic effect on actively proliferating cells but to different extents. The inhibitory effect of aspirin i.e. acetyl salicylic acid was around two to four times more pronounced than those produced by the ibuprofen and nimesulide. The IC50 obtained with aspirin was 5 μg/ml whereas those of ibuprofen and nimesulide were 13.5 μg/ml and 28 μg/ml respectively. Further the inhibitory effects were dose and time dependent. These effect of acetyl salicylic acid appeared to arise from a clear antiproliferative shift towards a reduced percentage of cells at the S and G2/M phases, together with an increased percentage of cells at the G1 phase. Aspirin could be more effective on MCF-7 than K-562 erythroleukemic cells and also as an lnclusion compound with the advantage of oral administration and a greater bioavailability of the compound. Using the Chick chorioallantoic membrane model, the aspirin loaded pellets release sufficient acetyl salicylic acid to produce vascular regression and inhibitionof angiogenesis.

Menadione sodium bisulphate was determined calorimetrically with chloranilic acid. It forms instantaneous purple charge transfer complex with chloranilic acid in ethanol-dioxan mixture, which had λmax at 510 nm. The complexation was maximum at room temperature and at 30 min after mixing the reactants. The molar absorptivity and association constant for the complex were determined to be 147.4 I/mol/cm and 1.32 l/mol, respectively. The standard free energy change for the complex was calculated to be 6.85 kcal/mol. The percentage recovery for the assay of the tablets was 97.6% while the experiment was obtainable at the concentration range of 0.2-1.1 mg% menadione sodium bisulphate.

A new method of preparation of sintered matrix tablets of rifampicin with ethylene-vinyl acetate copolymer is developed for controlling its release rate. This method is very simple. Drug and polymer powder (ethylene-vinyl acetate copolymer) were mixed and compressed at room ternperature. The compressed fluffy matrices were kept at 60o, 70o and 80o for 1.5,3 and 4.5 h for sintering. The sintered tablets were characterized for their physical characteristics and evaluated for in vitro dissolution studies. The sintering time markedly affected the drug release properties from the matrices. The release rate of rifampicin from EVA 1408 matrices was inversely related to the time of sintering due to the increase in the extent and firmness of sintering which compacts the mass further so that the drug release is affected. The drug release followed diffusive mechanism with first-order release kinetics.

Bovine serum albumin microspheres of diclofenac sodium were prepared by emulsion polymerization technique and the gelatin microspheres were prepared by gelation and dehydration technique. These microspheres were prepared for targeting of diclofenac sodium to inflammation site. The silicone coated magnetite particles were prepared and used for-the preparation of magnetic microspheres. Effect of different formulation and process variables was studied on particle size, drug entrapment, in vitro release rate, magnetic responsiveness, biodistribution and stability of the microspheres.

In the present investigation we prepared drug free polymeric films of ethyl cellulose (EC), to explore their suitability for transdermal application as the rate controlling membrane. Castor oil, glycerol was incorporated at a concentration of 30%w/w, 40%w/w of dry polymer, as plasticizer. The dry free films were evaluated for various physicochemical characters. The permeability characteristics of free films was studied using nifedipine as model drug. Drug was incorporated in 4% hydroxy propylmethylcellulose gel. The backing membrane was a non permeable aluminium foil laminated with polyethylene. Skin irritation study for the transdermal patches were assessed and were found to be free of irritation. An enhancement technique for drug permeation and in vivo pharmacological studies were also carried out. From this study it was concluded that faster release was observed from ethyl cellulose patches containing glycerol as plasticizer.

A simple, sensitive and accurate spectrophotometric method has been developed for the determination of betaxolol hydrochloride and metoprolol tartrate in bulk and from pharmaceutical dosage forms. This is an indirect method for the estimation of betaxolol hydrochloride and metoprolol tartrate, which involves oxidation of drug by N-bromosuccinimide and estimation of unreacted N-bromosuccinimide with metol-sulphanilamide reagent. The charge transfer complex so formed is estimated at 520 nm. Both the drugs obey Beer's law in the concentration range of 4-40 mg/ml.

A new, simple, sensitive spectrophotometric method in ultraviolet region has been developed for the determination of tizanidine hydrochloride in bulk and in dosage form. Tizanidine hydrochloride exhibited maximum absorbance at 320 nm with apparent molar absorptivity of 13.1104x103 I/mol.cm. Beer's law was obeyed in the concentration range of 5-20 μg/ml. Results of the analysis were validated statistically and by recovery studies.

The synthesis and photoprotection efficacy of a new water-soluble photoprotective agent, 1,1'-oxy bis[(4-methoxy cinnamidopropyl dimethyl ammonio) ethane] dichloride is reported. This non-irritating hydrolytically stable UV-absorber is substantive to both skin and hair due to its cationic nature. It can be easily formulated into a variety of hair and skin care formulations.

Two simple spectrophotometric methods for the determination of ornidazole and norfloxacin in pharmaceutical preparations have been developed. First method is based on simultaneous equations. In the second method, derivative spectroscopy is used to eliminate spectral interference. Both drugs obey Beer's law in the concentration range employed for the analysis. The results of analysis have been validated statistically and by recovery studies.

Ketoprofen-loaded polystyrene microparticles containing variable amount of polyvinylpyrrolidone as a copolymer were prepared by emulsion solvent evaporation method. The effect of polymer combination and initial drug loading on physical characteristics of the microparticles were studied. Although the microparticles were prepared by emulsification using different polymer combinations, the mean diameters were confined within a narrow range. However increase in initial drug loading increased the mean diameters of the microparticles. Polystyrene was found to be highly impermeable to drug release. Incorporation of polyvinylpyrrolidone easily modulated drug release. Mechanism of drug release was found to be a complex one.

A simple, efficient and reproducible method for the simultaneous determination of metformin and gliclazide from tablets has been developed using reversed phase high performance liquid chromatography. The separation was done using a mobile phase consisting of 0.025 M disodium hydrogen phosphate and acetonitrile (25:75%v/v) with pH adjusted to 3.2 with dilute ortho phosphoric acid. Column used was Shimpack CLC C8 (250x4 mm 1.d.) 5 μ with flow rate of 1 ml/min with detection at 240 nm. The external standard calibration method was employed for quantitation. An elution order was metformin (2.8 min) and gliclazide (4.3 min).The linear dynamic range was 5-500 μg/ml and 10-100 μg/rnl for metformin and gliclazide, respectively. Analytical parameters were calculated and a full statistical evaluation included.

In the present study, the bark of Machilus macrantha Nees. (Lauraceae) was investigated for antiinflammatory activity in carrageenan-induced rat paw oedema. The alcoholic and aqueous extract showed dose-dependent inhibition of rat paw oedema, at per oral doses of 100 and 200 mg/kg, when compared to control group. The activity was compared with that of the standard drug, diclofenac sodium (15 mg/kg, p. o.)

In view of the potent analgesic antiinflammatory and antimicrobial activities exhibited by quinazolin- 4(3H)-ones, a series of novel 2-phenyl-3-(substitutedmethyl amino) quinazolin-4(3H)-ones have been synthesized. When these compounds were evaluated for analgesic, antiinflammatory and antibacterial activities, compounds I and II exhibited comparable analgesic activity, while the compounds II and Ill exhibited comparable antiinflammatory activity with the standard diclofenac sodium.

Hypocholesterolemic activity was studied on normal rats for hexane, chloroform and methanol extracts of Trichilia connaroides (W. & A.) Bentilezen. The parameters studied include free cholesterol, triglycerides and high density lipoprotein levels in blood. Only hexane and methanol extracts produced a rise in high density lipoprotein level (p<0.05 at 90 mg/kg) and did not show any fall in cholesterol and triglyceride levels when compared to control group. On Triton-induced hypercholesterolemla, only cholesterol and triglyceride levels were studied for all the three extracts. Chloroform and methanol extracts produced a significant fall in cholesterol level (p<0.05) within 24 h of induction when compared to control group.

Dental implants of tinidazole were formulated using Poly (ε-caprolactone), a biodegradable polymer and evaluated. Clinical evaluation was carried out to evaluate the usefulness in periodontal therapy. Gingival crevicular fluid concentration of the drug was found to be 4.9±13.2 μg per mg of gingival fluid which was higher than the minimum inhibitory concentration for many of the periodontal pathogens through out the period of study (40 days). Low drug concentration was found in saliva which is desirable. High concentration of drug in saliva may supress the normal commencal flora of the oral cavity and may also pose a risk of over growth of opportunistic organisms causing several adverse effects. The implants prepared were capable of releasing tinidazole and maintain effective concentration in gingival crevicular fluid for an adequate duration of time to inhibit the growth of various periodontopathic organisms which confirms the clinical efficacy of the implants prepared.

The present study has three primary objectives. Firstly, in view of the low aqueous solubility of celecoxib, solid dispersions of the drug were prepared and evaluated. Different carriers were chosen and a constant drug to carrier ratio was maintained. The solid dispersions obtained were subjected to solubility and dissolution studies including dissolution rate and efficiency. The best carrier was polyvinylpyrrolidone-vinyl acetate co-polymer, as it increased the solubility by a factor of ten. It also exhibited marked increase in the dissolution rate and efficiency. Secondly, the effect of the surfactant sodium lauryl sulphate on the dissolution rate of celecoxib was investigated. The solubility of a poorly soluble drug is one of the most important factor influencing its dissolution rate and bioavailability. Presence of a surfactant in the dissolution medium permits an experimental situation similar to in vivo conditions and hence results in meaningful in-vitro observations. Dissolution study was conducted using various concentrations of sodium lauryl sulphate employing USP dissolution rate testing apparatus 1. Ultimately, a dissolution medium, which gave reproducible results in vitro was designed. Finally, possible drug excipient interactions between celecoxib and the commonly used excipients including those used in the preparation of its solid dispersions were investigated by storing their respective mixtures at various temperatures and humidity conditions followed by evaluating them with reference to physical and chemical stability and the results were confirmed by IR and DSC spectral studies. Polyvinylpyrrolidone was found to be the most satisfactory excipient. Degradation was evident with all other excipients studied although only at elevated temperatures.

Various acylonucleoside analogs were synthesized and evaluated for antibacterial and antifungal activity. All the acyclic nucleosides exhibited good antifungal activity compared to the standard drug clotrimazole. However, none of the compounds possess broad-spectrum antibacterial activity. The structure-activity relationships of acyclic nucleosides were studied in order to develop the most potential antifungal agent for preclinical evaluation.

Aqueous extract of the seeds of Nigella sativa were tested for hepatoprotective activity on male Wistar rats against carbon tetrachtoride induced hepatotoxicity. Various biochemical parameters were studied to evaluate the hepatoprotective activity. Aqueous extract showed significant hepatoprotective activity against carbon tetrachloride-induced toxicity on the liver indicating promising hepatoprotective activity.

TLC-colourimetric method was employed for the estimation of free and combined forms of chrysophanol, emodin and physcione in lndian rhubarb. It was found that lndian rhubarb contains free chrysophanol (0.15 %), O-glycosidic chrysophanol (0.06%), C-glycosidic chrysophanol (0.21%), free emodin (0.07 %), O-glycosidic emodin (0.30 %), C-glycosidic emodin (0.08 %),free physcione (0.40 %), O-glycosidic physcione (0.18 %) and C-glycosidic physcione (0.17 %).

The roots of Jatrophe curcas were extracted successlvely with petroleum ether and methanol to investigate local antilnflammatory activity based on ethnobotanlcal lead. Methanol extract was studied against 12-O-Tetradecanoylphorbol-13-acetate, Ethyl phenylpropiolate and Arachidonic acid induced local Inflammatory response In albino mice. The methanol extract showed dose dependant local antllnflammatory activity against all these phlogestic agents. Net local antiintlammatory activity is complex mainly evident due to Inhibition of biosynthesis of prostaglandin, leukotrienes and protein kinase C and action on peripheral vascular permeability