A simple, specific, accurate and stability indicating reversed phase high performance liquid chromatographic method was developed for the simultaneous determination of atorvastatin calcium and amlodipine besylate in tablet dosage forms. A phenomenex Gemini C-18, 5 mm column having 250´4.6 mm i.d. in isocratic mode, with mobile phase containing 0.02 M potassium dihydrogen phosphate:acetonitrile:methanol (30:10:60, v/v/v) adjusted to pH 4 using ortho phosphoric acid was used. The flow rate was 1.0 ml/min and effluents were monitored at 240 nm. The retention times of atorvastatin calcium and amlodipine besylate were 11.6 min and 4.5 min, respectively. The calibration curves were linear in the concentration range of 0.08-20 µg/ml for atorvastatin calcium and 0.1-20 µg/ml for amlodipine besylate. Atorvastatin calcium and amlodipine besylate stock solutions were subjected to acid and alkali hydrolysis, chemical oxidation and dry heat degradation. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. The proposed method was validated and successfully applied to the estimation of atorvastatin calcium and amlodipine besylate in combined tablet dosage forms.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

A dry process induced phase transited, non disintegrating, controlled release, in situ formed asymmetric membrane capsular system for poorly water soluble drug, ketoprofen, was developed and evaluated both in vitro and in vivo for osmotic and controlled release of the drug. In situ formed asymmetric membrane capsules were prepared using fabricated glass capsule holders via dry, phase inversion process. Effect of varying osmotic pressure of the dissolution medium on drug release was studied. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores and an inner porous region for the prepared asymmetric membrane. In vitro release studies and statistical test for all the prepared and marketed formulation were done at P >0.05. The drug release was found to be independent of the pH, but dependent on the osmotic pressure of the dissolution medium. In vivo pharmacokinetic studies showed a level A correlation (R ² >0.99) with 39.24 % relative bioavailability compared to immediate release tablet of ketoprofen. Excellent correlation achieved suggested that the in vivo performance of the phase transited in situ formed AMCs could be accurately predicted from their in vitro release profiles and could a means for controlled delivery of drugs with varying solubility.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

The antimicrobial activity of alcoholic, butanolic and chloroform extracts of leaves and roots of the plant Acanthus ilicifolius ware studied. Ampicillin and clotrimazole were used as standard antibacterial and antifungal agents respectively. The result of the study revealed that the alcoholic extract and chloroform extract of leaves exhibited strong inhibitory action against Bacillus subtilis, Staphylococcus aureus, Candida albicans, Aspergillus fumigatus and Aspergillus niger and moderate inhibitory action against Pseudomonas aeruginosa and Proteus vulgaris. The rest of the extracts showed moderate activity.

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A simple sensitive spectrofluorimetric method was developed for the analysis of total coumarins calculated as scopoletin in the plants Evolvulus alsinoides and Convulvulus pluricaulis . The fluorescent nature of scopoletin proved to be of immense value in the development of the spectrofluorimetric method. The excitation and emission wavelengths for scopoletin were 430 nm and 460 nm respectively and the instrument was Shimadzu RF 5301 PC spectrofluorophotometer. The method was validated in terms of linearity, accuracy and precision. The proposed spectrofluorimetric method provides a faster and cost effective qualitative and quantitative control for routine analysis of scopoletin in Evolvulus alsinoides and Convulvulus pluricaulis and their formulations.

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A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the estimation of sumatriptan in tablet dosage forms. The stationary phase used was precoated silica gel 60F254. The mobile phase used was a mixture of methanol:water:glacial acetic acid (4.0:8.0:0.1, v/v/v). The detection of spots was carried out at 230 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 200 to 800 ng/spot. The limit of detection and the limit of quantification for the sumatriptan were found to be 63.87 and 193.54 ng/spot, respectively. The proposed method can be successfully used to determine the drug content of marketed formulation.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

Reactive oxygen species are implicated in various inflammatory disorders. Vitex negundo is mentioned in Ayurveda as useful in treating arthritic disorders. The present work was undertaken to evaluate the antioxidant potential and anti-inflammatory activity of the plant. The total methanol extract of the plant was standardized in terms of total polyphenols. The standardized extract in a dose of 100 mg/kg caused a comparable reduction in edema with that of diclofenac sodium (25 mg/kg) when evaluated for antiinflammatory activity by carrageenan-induced rat paw edema method. The extract also exhibited a strong free radical scavenging activity by 1,1-diphenyl-2-picrylhydrazyl method and caused a significant reduction in the formation of thiobarbituric acid reacting substances when evaluated for its lipid peroxidation inhibitory activity. The results strongly suggest that radical quenching may be one of the mechanisms responsible for its antiinflammatory activity.

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Ethanol extract of leaves of Clerodendron phlomoidis L. subjected to preliminary qualitative phytochemical investigations showed the presence of alkaloids, phytosterols, glycosides, saponins, phenolic compounds, proteins and flavonoids. The extract was screened for hypoglycemic activity in alloxan-induced diabetic rats (120 mg/kg, i.p.) at two dose levels, viz., 100 and 200 mg/kg. The ethanol extract at 200 mg/kg dose level exhibited significant ( p <0.05) hypoglycemic activity and also correction of altered biochemical parameters viz., cholesterol and triglycerides ( p <0.05).

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

Simple, specific, accurate and precise method, namely, reverse phase high performance liquid chromatography was developed for estimation of duloxetine HCl in pharmaceutical formulations. For the high performance liquid chromatography method, Phenomenox C-18, 5 µm column consisting of 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.01M 5.5 pH phosphate buffer: acetonitrile (60:40 v/v) and final pH adjust to 5.5±0.02 with phosphoric acid was used. The flow rate was 1.2 ml/min and effluent was monitored at 231 nm. The retention time was 5.61 min. The method was validated in terms of linearity, accuracy and precision. The linearity curve was found to be linear over 0.25-4 µg/ml. The limit of detection and limit of quantification were found to be 0.10 and 0.25 µg/ml respectively. The proposed method was successfully used to determine the drug content of marketed formulations.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

In the present work, fast dissolving tablets of clonazepam were prepared by direct compression method with a view to enhance patient compliance. Three super-disintegrants, viz., crospovidone, croscarmellose sodium and sodium starch glycolate in different ratios with microcrystalline cellulose (Avicel PH-102) along with directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on in vitro dispersion time (approximately 13 s), three formulations were tested for the in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40º/75% relative humidity for 6 mo) and drug-excipient interaction (IR spectroscopy). Among the three promising formulations, the formulation prepared by using 10% w/w of crospovidone and 35% w/w of microcrystalline cellulose emerged as the overall best formulation (t _50% 1.8 min) based on the in vitro drug release characteristics compared to conventional commercial tablet formulation (t _50% 16.4 min). Short-term stability studies on the formulations indicated that there were no significant changes in drug content and in vitro dispersion time ( P <0.05).

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Seventy five patients with oral lesions attending the different departments of Rajah Muthiah Medical College and Hospital, Annamalai University were screened for Candida . Forty six (61.3%) Candida strains were isolated from the oral lesions. Of the 46 Candida strains, Candida albicans accounted for 35 (76.08%), Candida glabrata for 5 (10.86%), Candida tropicalis and Candida krusei for 2 (4.34%) each and Candida parapsilosis and Candida guilliermondii for one (2.17%) each. Antifungal activity of ethanol extracts of five plant species that included Syzygium jambolanum, Cassia siamea, Odina wodier, Momordica charantia and Melia azedarach and two algal species, Sargassum wightii and Caulerpa scalpelliformis were tested against 25 isolated strains by disc diffusion method. Antifungal activity was observed at 100 mg/ml for Syzygium jambolanum, Cassia siamea and Caulerpa scalpelliformis and at 10 mg/ml for Sargassum wightii .

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The present study was carried out with the water-soluble portion of the ethanol extracts of flowers, barks, seeds and leaves of Nyctanthes arbortristis Linn. to confirm their CNS depressant activity. The ethanol extracts of the plant parts were obtained by soxhlet extraction. After performing the gross behavioral study, the CNS depressant activity was evaluated by observing the prolongation of sleeping time induced by pentobarbital sodium in mice. Attempts have been made to explore the possible mechanism behind this activity by determining their effect on brain monoamine neurotransmitters like dopamine and serotonin. The gross behavioral study showed that ethanol extracts of the leaves, flowers and seeds possess significant CNS depressant activity. The leaves, flowers, seeds and barks (600 mg/kg) showed significant and dose-dependent prolongation of onset and duration of sleep and so found to cause decrease dopamine and increase serotonin level. From which it can be concluded that the CNS depressant activity of the ethanol extracts of seeds, leaves and flowers may be due to the decrease in dopamine and increase in serotonin level.

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Sleep deprivation disrupts significantly sleep pattern and cause poor quality of sleep. The aim the present study was to explore role of Withania somniferra root extract in sleep-disturbed rats. Male wistar rats (n=5-6/group) were sleep deprived for 24 h using grid suspended over water method. Withania somniferra extract (100 mg/kg) was administered intraperitoneally (i.p.) 30 min before actual recording (EEG and EMG) recording and electrophysiological recordings are further classified as- sleep latency, slow wave sleep, paradoxical sleep, total sleep, wakefulness. One day (24 h) sleep deprivation delayed latency sleep, reduced duration of slow wave sleep, rapid eye movement sleep, total sleep time and increased total waking as compared to animals placed on saw dust (P<0.05). Pretreatment with Withania somniferra extract (100 mg/kg) and diazepam (0.5 mg/kg) significantly improved electrophysiological parameters, which was further reversed by picrotoxin (2 mg/kg) and potentiated by muscimol (0.05 mg/kg). Flumazenil (2 mg/kg) did not produce any significant effect on the sleep parameters of Withania somnifera root extract. Present study suggests the involvement of GABAergic mechanism in the sleep promoting effect of Withania somniferra in sleep-disturbed state.

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The objective of the present work was to develop a metered dose spray formulation for transdermal delivery of oxybutynin and to carry out the in vitro characterization of the optimized formulation. Oxybutynin release from a series of ethanol/acetone/methylal based formulations was assessed in vitro and the developed formulation was used for delivery from a metered dose spray. Various qualitative and quantitative parameters like spray pattern, particle size distribution, pH, evaporation time, pump seal efficiency test, average weight per metered dose, content per spray and content uniformity were evaluated. The different film forming agents were assessed and carbopol (0.5%) and lutrol (0.1%) were found to give good clarity of solution, evaporation rate, spray pattern and tackiness of the film. Diffusion studies of the optimized formulations through the semipermeable membrane showed the release of drug to the extent of almost 50% over a period of 24 h. Stability studies were conducted as per ICH guidelines and indicated that formulations were stable. Skin irritation studies were performed using rabbit as an animal model. The results obtained show that the metered dose transdermal spray formulation can be a promising and innovative therapeutic system for the transdermal administration of oxybutynin.

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In the present investigation, pharmacological evaluation of apigenin, a bioactive principle of Turnera aphrodisiaca Ward (Turneraceae) was carried out. Apigenin was evaluated for antianxiety activity at a dose of 2 mg/kg using well established models of anxiety, the hole board test, light/dark test and mirrored chamber test. Apigenin significantly increased head dipping in hole board test. Further, apigenin increased latency to leave light zone and the time spent in light compartment of light/dark model of anxiety. Apigenin also decreased the latency time to enter the mirrored chamber, and increased the total time spent/number of entries in the mirrored chamber with respect to control. All these observations confirmed the anxiolytic activity of apigenin. At a higher dose (about 12 fold the anxiolytic dose), apigenin showed mild sedative activity in actophotometer as it decreased activity scores. It (2, 5 or 10 mg/kg) was found to be devoid of anticonvulsant, antidepressant and antistress activity in MES-induced convulsion test, despair swim test and cold swimming endurance test, respectively. In tail immersion test for six hours, apigenin exhibited excellent dose dependent analgesic activity, which was comparable to that of morphine sulphate (5 mg/kg). Maximum activity was observed 30 min after the administration of 10 mg/kg dose of apigenin.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

Lovastatin is a potent hypercholesterolemic drug used for lowering blood cholesterol. Lovastatin acts by competitively inhibiting the enzyme, 3-hydroxy-3-methylglutaryl coenzyme A reductase involved in the biosynthesis of cholesterol. Commercially lovastatin is produced by a variety of filamentous fungi including Penicillium species, Monascus ruber and Aspergillus terreus as a secondary metabolite. Production of lovastatin by fermentation decreases the production cost compared to costs of chemical synthesis. In recent years, lovastatin has also been reported as a potential therapeutic agent for the treatment of various types of tumors and also play a tremendous role in the regulation of the inflammatory and immune response, coagulation process, bone turnover, neovascularization, vascular tone, and arterial pressure. This review deals with the structure, biosynthesis, various modes of fermentation and applications of lovastatin.

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A series of novel isatine-sulphonamide derivatives have been synthesized by combining isatin derivatives with sulphonamides. The structure of the synthesized compounds were elucidated by spectral analysis (IR, NMR and Mass). Investigation of anti-HIV activity was done against HIV-1(IIIB) in MT-4 cells and HIV integrase inhibitory activity. 4-(1-acetyl-5-methyl-2-oxoindolin-3-ylideneamino)-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide (SPIII-5ME-AC) inhibits the HIV Integrase enzymatic activity as both over all and strand transfer reaction and 4-(1-benzoyl-5-chloro-2-oxoindolin-3-ylideneamino)-N-(4,6-dimethylpyrimidin-2-yl)benzene sulfonamide (SPIII-5Cl-BZ) exhibits 36 percent maximum protection against HIV-1 at sub toxic concentration.

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Previous studies have demonstrated that pharmacokinetic behavior of several drugs such as paracetamol, theophylline, and aminoglycosides are significantly altered in spinal cord injured patients. No pharmacokinetic study of amitriptyline has been performed in patients and experimental models of spinal cord injury. Pharmacokinetic parameters of amitriptyline in orally treated rabbits subjected to laminectomy and spinal cord injury compared with those underwent laminectomy alone. Among twenty four male rabbits were included in this study, nine of them subjected to spinal cord injury at the 8 ^th thoracic level by knife severance method and six rabbits underwent laminectomy alone (sham group) and nine rabbits treated as control. All received a single oral dose of amitriptyline (20 mg/kg) 24 h after injury. Blood sampling were done at predetermined times to 36 h after drug administration. Amitriptyline concentration in serum samples was determined by high-performance liquid chromatography. Pharmacokinetic parameters including maximum concentration (C _max ), time to reach maximum concentration (T _max ), half life, and the area under the curve to last detectable concentration time point (AUC _0-t ) were directly determined from the concentration-time curve. Maximum concentration was observed at 6.5 h after administration in sham group with a concentration of 439.6 ng/ml, whereas in SCI group T _max was at 2.7 h with a concentration of 2763.9 ng/ml. In control group it was 3.3 h and 396 ng/ml, respectively. In SCI group, AUC was 9465.6 ng.h/ml and half life was 6 h and for control group it was 2817.4 ng.h/ml and 6.4 h, respectively. Statistical analysis of data showed that SCI didn't induce significant changes in amitriptyline pharmacokinetic parameters.

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A simple, sensitive, rapid, accurate and precise spectrophotometric method has been developed for the estimation of bicalutamide in bulk and pharmaceutical dosage forms. Bicalutamide shows maximum absorbance at 272 nm with molar absorptivity of 2.3399×10 ⁴ l/mol/cm. Beer's law was obeyed in the concentration range of 1.5-18 µg/ml. The limit of detection and limit of quantification were found to be 0.1 and 0.4 µg/ml, respectively. Results of analysis were validated statistically and by recovery studies.

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In the present study aceclofenac-gelatin micropellets were prepared by the cross linking technique using gluteraldehyde as cross linking agent and characterized by X-ray diffractometry, differential scanning calorimetry and scanning electron microscopy. The effect of drug: polymer ratio, temperature of oil phase, amount of gluteraldehyde and stirring time was studied with respect to entrapment efficiency, micropellet size and drug release characteristics. Spherical micropellets having an entrapment efficiency of 57% to 97% were obtained. Differential scanning calorimetric analysis confirmed the absence of any drug-polymer interaction. The micromeritic studies of micropellets show improved flow property. The entrapment efficiency, micropellet size and drug release profile was altered significantly by changing various processing parameters.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

HPTLC fingerprinting profile of the alcohol and aqueous extracts of Drosera burmannii is described. Seven components have been detected in the alcohol extract. Further, plumbagin, an useful antifertility agent, was also detected by comparison with the reference standard. The aqueous extract revealed two spots with no spot corresponding to plumbagin.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

A reverse phase HPLC method with UV detection has been developed and validated in order to quantify plumbagin, the bioactive marker of the roots of P. indica and P. zeylanica . A quantitative HPTLC method was also developed using hexane: ethyl acetate (8:2) as the mobile phase. The plumbagin content in the roots were determined using both the methods. P. indica was found to contain significantly higher amount of plumbagin than P. zeylanica . The HPLC and HPTLC methods described here are simple, rapid, accurate and sensitive.

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An HPTLC densitometric method has been developed to estimate apigenin in Turnera aphrodisiaca aerial and its segregated parts (leaves, stems, flowers and fruits) so that plant can be standardized on the basis of its bioactive marker. The apigenin content in methanol extract of T. aphrodisiaca aerial parts was found to be about fourteen times less than acid hydrolyzed methanol extract of the plant indicating the presence of most of apigenin in glycosidic form. Amongst different plant parts, flowers possessed maximum content of apigenin followed by leaves. The apigenin content was also determined in three marketed formulations of T. aphrodisiaca viz., NLK, DWSG and SBL. DWSG contained higher content of apigenin. Aerial parts of the plant were collected at bimonthly intervals over a period of one year in the months of January, March, May, July, September and November. The plant material collected in September showed maximum content of apigenin.

[ABSTRACT]  [FULL TEXT]  [PDF] [CITATIONS]  [PubMed]

The synthesis of a cyclic heptapeptide, delavayin-C, cyclo(gly-tyr-tyr-tyr-pro-val-pro) is described. The structure of this compound was established on the basis of analytical IR, ¹ H NMR and FAB mass spectral data. The antibacterial and antifungal activities of this peptide are also described.

[ABSTRACT]  [FULL TEXT]  [PDF]  [PubMed]

In the present investigation, the poorly water-soluble drug, salicylic acid has been solubilized using 0.5 M ibuprofen sodium and 2.0 M sodium salicylate solution as hydrotropic agents for the titrimetric analysis precluding the use of organic solvents. Both hydrotropes are economic and pollution-free. The mean percent estimation of salicylic acid estimated in bulk sample by Indian Pharmacopoeial method is 98.78%. The mean percent estimation by ibuprofen sodium method and sodium salicylate method are 99.25% and 98.82%, respectively. The results of analysis by the proposed method are very close to the results of analysis by the standard method. This confirms the accuracy of the proposed method. The proposed method was validated statistically by low values of statistical parameters viz. standard deviation, percent coefficient of variation and standard error. The proposed method is new, accurate, simple and economic.

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During the process of screening for a potent antimicrobial compound, a new strain was isolated from the soil sample of Thalaikunda village in Ooty, Tamil Nadu. That organism was name as NK ₂ . It was found to be antagonistic to both bacterial and fungal test organisms. Production of antibiotic was more in a newly formulated broth. Antibiotic production reached maximum at the end of the 70 h of fermentation by stirred flask culture. The antimicrobial compound was extracted in n -butanol, ethyl acetate and methanol. Antimicrobial compound, which was produced by the soil isolate NK ₂ did not showed cytotoxic activity on Vero cell lines.

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Gravity flow characteristics of various pharmaceutical granules through static conical hoppers of different cone angles were studied. Mass flow rate depends on properties of granules and cone angles when environmental conditions such as temperature and relative humidity are kept within a fixed range. The granules were made with active pharmaceutical ingredients as per Indian pharmacopoeia with other additives like binders and diluents. Lubricants were added with the granules to observe their effects on mass flow rate. Magnesium stearate and colloidal silicon dioxide of different proportions were used as lubricants after granulation. A new dimensionally analyzed equation was developed to predict flow rate of the granules. The developed equation agreed well with the experimental data with a percentage deviation of ±10%.

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The antiinflammatory activity of the polyherbal formulation Entox^® was investigated in rats for acute and sub acute models of inflammation using carrageenan-induced rat paw edema and cotton pellet granuloma methods respectively at a dose of 300 mg/kg and 600 mg/kg administered orally. The formulation in doses of 300 mg/kg and 600 mg/kg showed 51.61% and 54.84% inhibition of paw edema, respectively at the end of 3 h. The percent inhibition of granuloma by cotton pellet method was 27.92% and 53.17%, respectively. The formulation showed a significant antiinflammatory activity in both the experimental models and the activity was comparable to that of the standard drug, indomethacin.

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Leptospirosis is now acknowledged as the most widespread zoonoses in the world. Hundreds of cases occur in India every year accounting for considerable morbidity and sizable mortality. Several studies have delineated the epidemiology, pathology and variable clinical features of this condition. The present study comprises the importance and utilization of traditional based medicines to overcome the adverse reaction by conventional drugs and standardize the technology. The antileptospiral activity of Eclipta alba L. was well studied by both tube dilution and micro dilution techniques and the result showed better inhibitory action against various serogroups of Leptospira interrogans. L. australis, L. autumnalis and L. grippotyphosa are inhibited by both water and ethanol extract by tube dilution technique. The MIC level observed are 50 µg and 100 µg respectively. Similarly acetone extract, Icterohaemorrhagiae was responded to 200 µg/ml as MIC whereas in petroleum ether extract, no inhibition was observed. In the case of micro dilution technique, the entire inhibition rates are supported to the tube dilution technique. It showed that the micro dilution technique is the best method where we obtained the results within 30 minutes; at the same time tube dilution technique takes minimum of 7 days to provide the result.

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The present study was taken up to investigate the effect of petroleum ether extract of Tinospora cordifolia (Wild.) Miers, on depression in mice. The extract (50, 100 and 200 mg/kg, p.o.) was administered for 14 successive days to Swiss young albino mice (either sex) and evaluated for antidepressant-like activity using tail suspension test and forced swim test. Petroleum ether extract at all three doses produced significant antidepressant-like effect in tail suspension test as well as in forced swim test and their efficacies were found to be comparable to imipramine (15 mg/kg, p.o.) and sertraline (20 mg/kg, p.o.). The extract at a dose of 50 mg/kg showed most potent effect and did not show any significant change in locomotor functions of mice as compared to control. The antidepressant-like effect of the extract was significantly reversed by pretreatment of animals with prazosin (a α₁ -adrenoceptor antagonist), sulpiride (a selective dopamine D ₂ -receptor antagonist), p-CPA (a serotonin synthesis inhibitor) and baclofen (GABA-B agonist), when tested in tail suspension test. Moreover, petroleum ether extract also reduced the mouse whole brain monoamine oxidase (MAO-A and MAO-B) activities as compared to control, resulting in increase in the levels of brain monoamines. Therefore, the extract may have potential therapeutic value for the management of depressive disorders.

[ABSTRACT]  [FULL TEXT]  [PDF]  [PubMed]

Non-steroidal antiinflammatory drugs are routinely prescribed for the patients with rheumatic disease and such patients are at increased risk of serious gastrointestinal complications, when non-steroidal antiinflammatory drugs administered by oral route. The aim of the present study was to develop and characterized a vesicular drug carrier system (proliposome) for topical delivery of aceclofenac to overcome the problems related with oral route. Aceclofenac proliposome were prepared by the film-deposition on carriers method and characterized for size and surface morphology, drug content in both proliposomes and liposomal system, percent yield, in vitro drug release studies and drug permeation studies. The prepared system was also characterized for drug-excipients interaction by Fourier transform infrared spectrophotometer and stability studies. The size and surface morphology were studied using optical microscopy, scanning electron microscopy and transmission electron microscopy. A spherical shape of reconstituted aceclofenac liposome with an average vesicular size of about 500 nm was observed in photomicrographs. The maximum entrapment efficiency of reconstituted liposomes was 80.31% whereas the drug content in proliposomes was found to be more than 90%. In vitro release of drug was significantly retarded indicating sustained release of aceclofenac from proliposomes. Stability study was performed at various temperatures indicating that aceclofenac proliposomes are stable at lower temperature.

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A pH mediated in situ gelling system was developed using prilocaine hydrochloride for periodontal anesthesia using combination of chitosan and hydroxypropylmethylcellulose. The gel so developed can be used as anaesthetic in lengthy dental surgery. The gel was evaluated for many parameters like gelation pH, viscosity, physicochemical properties, in vitro release, sterility and stability. Gel with chitosan (0.25% w/v) and hydroxypropylmethylcellulose (0.25% w/v) was found to have good gelation near pH 7.4 (pH of mucous) with prolonged action.

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Fungal infections of skin are one of the most common infections in human beings. The areas which are likely to get infected include the scalp, the hands and the feet. Dermatophytes, yeasts and moulds are the three major fungi responsible for skin infections. Earlier oral antifungal agents were used for treatment of fungal infection in finger and toe nails. The disadvantages of oral antifungal agents are toxicity and longer treatment period. Now medicated nail lacquers have been developed for the treatment of fungal infections i.e. onychomycosis, which has less toxicity and shorter treatment period.

[ABSTRACT]  [FULL TEXT]  [PDF]  [PubMed]

Ethyl naphtho[2,1- b ]furan-2-carboxylate (2) on reaction with hydrazine hydrate in presence of acid catalyst in ethanol medium affords naphtho[2,1-b]furan-2-carbohydrazide (3). The reaction of substituted acetophenones (4a-c) with aromatic aldehydes (5a-e) produces chalcones (6a-o) via the Claisen condensation. The reaction of naphtho[2,1- b ]furan-2-carbohydrazide (3) with chalcones (6a-6o) in presence of acetic acid as catalyst in dioxane produces 1-(naphtho[2,1- b ]furan-2-yl-carbonyl)-3,5-disubstituted-2,3-dihydro-1H-pyrazoles (7a-o). The structures of newly synthesized compounds have been established by elemental analysis and spectral studies. The compounds 7a-o have been evaluated for their antimicrobial activity and some selected compounds evaluated for antiinflammatory, analgesic, anthelmintic, diuretic and antipyretic activities.

[ABSTRACT]  [FULL TEXT]  [PDF]  [PubMed]

Insulin loaded hydrophobic nanoparticles were prepared by solvent diffusion followed by lyophilization. Nanoparticles were characterized for mean size by dynamic laser scattering and for shape by scanning electron microscopy. Insulin encapsulation efficiency, in vitro stability of nanoparticles in presence of proteolytic enzymes and in vitro release were determined by high pressure liquid chromatography analysis. The biological activity insulin from the nanopraticles was estimated by enzyme-linked immunosorbant assay and in vivo using Wister diabetic rats. Nanoparticles ranged 0.526±0.071 µm in diameter. Insulin encapsulation efficiency was 95.7±1.2%. Insulin hydrophobic nanoparticles suppressed insulin release promoted sustained release in pH 7.4 phosphate buffer and shown to protect insulin from enzymatic degradation in vitro in presence of chymotripsin. Nanoencapsulated insulin was bioactive, demonstrated through both in vivo and in vitro.

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Formulation of insulin into a microemulsion very often presents a physicochemical instability during their preparation and storage. In order to overcome this lack of stability and facilitate the handling of these colloidal systems, stabilization of insulin in presence of hydrophobic components of a microemulsion appears as the most promising strategy. The present paper reports the use of egg yolk for stabilization of insulin in self microemulsifying dispersions. Insulin loaded egg yolk self microemulsifying dispersions were prepared by lyophilization followed by dispersion into self microemulsifying vehicle. The physicochemical characterization of selfmicroemulsifying dispersions includes such as insulin encapsulation efficiency, in vitro stability of insulin in presence of proteolytic enzymes and in vitro release. The biological activity of insulin from the dispersion was estimated by enzyme-linked immunosorbant assay and in vivo using Wistar diabetic rats. The particle size ranged 1.023±0.316 µm in diameter and insulin encapsulation efficiency was 98.2±0.9 %. Insulin hydrophobic self microemulsifying dispersions suppressed insulin release in pH 7.4 phosphate buffer and shown to protect insulin from enzymatic degradation in vitro in presence of chymotripsin. Egg yolk encapsulated insulin was bioactive, demonstrated through both in vivo and in vitro.

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In the light of escalating use of medical devices, stringent regulatory standards are required to ensure that the devices are safe, well studied and have least adverse reactions. Recently introduced guidelines and the amendment in the law will provide adequate guidance for both the manufacturers and competent authorities to manage cases efficiently and appropriately. India has emerged as one of the leaders in pharmaceutical industry. Like many other amendments in Drugs and Cosmetics Act that have boosted the global confidence in pharmaceutical industry in India, guidelines for devices will encourage the much needed research in medical devices. Pharmacy personnel can certainly play an important role in the regulation of medical devices. Safety, risks, effectiveness and performance of the medial devices need to be well established and regulated properly. It is hoped that the guidelines are implemented and regulated properly with effective outcome.

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