Showing papers in "Indian Journal of Pharmaceutical Sciences in 2009"
TL;DR: A broad treatment of solid lipid nanoparticles is presented discussing their advantages, limitations and their possible remedies, as well as different types of nanocarriers which were based on solid lipid like solid cholesterol nanoparticles, nanostructured lipid carriers, lipid drug conjugates are discussed.
Abstract: Solid lipid nanoparticles are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery, clinical medicine and research, as well as in other varied sciences. Due to their unique size-dependent properties, lipid nanoparticles offer the possibility to develop new therapeutics. The ability to incorporate drugs into nanocarriers offers a new prototype in drug delivery that could be used for secondary and tertiary levels of drug targeting. Hence, solid lipid nanoparticles hold great promise for reaching the goal of controlled and site specific drug delivery and hence have attracted wide attention of researchers. This review presents a broad treatment of solid lipid nanoparticles discussing their advantages, limitations and their possible remedies. The different types of nanocarriers which were based on solid lipid like solid lipid nanoparticles, nanostructured lipid carriers, lipid drug conjugates are discussed with their structural differences. Different production methods which are suitable for large scale production and applications of solid lipid nanoparticles are described. Appropriate analytical techniques for characterization of solid lipid nanoparticles like photon correlation spectroscopy, scanning electron microscopy, differential scanning calorimetry are highlighted. Aspects of solid lipid nanoparticles route of administration and their biodistribution are also incorporated. If appropriately investigated, solid lipid nanoparticles may open new vistas in therapy of complex diseases.
624 citations
TL;DR: The present review emphasizes on the applicability of polyelectrolyte complexes in drug delivery technology.
Abstract: Over the past several years, great advances have been made towards novel drug delivery systems. The phenomena of interpolymer interactions and formation of polyelectrolyte complexes have been the focus of intensive fundamental and applied research. Interpolyelectrolyte complexes combine unique physicochemical properties with high biocompatibility. Studies have been carried out on many different polymer blends and types. Such combinations may possess unique properties that are different from those of individual component. The present review emphasizes on the applicability of polyelectrolyte complexes in drug delivery technology.
235 citations
TL;DR: This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co,crystals, methods of preparation of co -crystals and application of co.crystals to modify physicochemical characteristics of active pharmaceutical ingredients along with the case studies.
Abstract: Crystal form can be crucial to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as low aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first-pass metabolism. The nature of the physical form and formulation tends to exhibit the greatest effect on bioavailability parameters of water insoluble compounds that need to be given orally in high doses. An alternative approach available for the enhancement of drug solubility, dissolution and bioavailability is through the application of crystal engineering of co-crystals. The physicochemical properties of the active pharmaceutical ingredients and the bulk material properties can be modified, whilst maintaining the intrinsic activity of the drug molecule. This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co-crystals, methods of preparation of co-crystals and application of co-crystals to modify physicochemical characteristics of active pharmaceutical ingredients along with the case studies. The intellectual property implications of creating co-crystals are also highly relevant.
187 citations
TL;DR: The porous carriers are used to improve the oral bioavailability of poorly water soluble drugs, to increase the dissolution of relatively insoluble powders and conversion of crystalline state to amorphous state.
Abstract: Considerable research efforts have been directed in recent years towards the development of porous carriers as controlled drug delivery matrices because of possessing several features such as stable uniform porous structure, high surface area, tunable pore size and well-defined surface properties. Owing to wide range of useful properties porous carriers have been used in pharmaceuticals for many purposes including development of floating drug delivery systems, sustained drug delivery systems. Various types of pores like open, closed, transport and blind pores in the porous solid allow them to adsorb drugs and release them in a more reproducible and predictable manner. Pharmaceutically exploited porous adsorbents includes, silica (mesoporous), ethylene vinyl acetate (macroporous), polypropylene foam powder (microporous), titanium dioxide (nanoporous). When porous polymeric drug delivery system is placed in contact with appropriate dissolution medium, release of drug to medium must be preceded by the drug dissolution in the water filled pores or from surface and by diffusion through the water filled channels. The porous carriers are used to improve the oral bioavailability of poorly water soluble drugs, to increase the dissolution of relatively insoluble powders and conversion of crystalline state to amorphous state.
141 citations
TL;DR: Various aspects relating to drug use during pregnancy, including the teratogenic risk of drugs, are focused on.
Abstract: Pregnancy is a special physiological condition where drug treatment presents a special concern because the physiology of pregnancy affects the pharmacokinetics of medications used and certain medications can reach the fetus and cause harm. Total avoidance of pharmacological treatment in pregnancy is not possible and may be dangerous because some women enter pregnancy with medical conditions that require ongoing and episodic treatment (e.g. asthma, epilepsy, hypertension). Also during pregnancy new medical problems can develop and old ones can be exacerbated (e.g. migraine, headache) requiring pharmacological therapy. The fact that certain drugs given during pregnancy may prove harmful to the unborn child is one of the classical problems in medical treatment. In 1960's pregnant ladies who ingested thalidomide gave birth to children with phocomalia. Various other examples of teratogenic effects of drugs are known. It has been documented that congenital abnormalities caused by human teratogenic drugs account for less than 1% of total congenital abnormalities. Hence in 1979, Food and Drug Administration developed a system that determines the teratogenic risk of drugs by considering the quality of data from animal and human studies. FDA classifies various drugs used in pregnancy into five categories, categories A, B, C, D and X. Category A is considered the safest category and category X is absolutely contraindicated in pregnancy. This provides therapeutic guidance for the clinician. This article focuses on various aspects relating to drug use during pregnancy.
139 citations
TL;DR: Among the plants screened, W. tomentosa leaf and fruit showed the best antibacterial activity and the Gram-positive bacteria were more susceptible than Gram-negative bacteria.
Abstract: Many plants used in Saurashtra folk medicine have been reported to exhibit high antibacterial and antioxidant activities. In the present study, some parts of five plants, Guazuma ulmifolia L., Manilkara zapota L., Melia azedarach L., Syzygium cumini L. and Wrightia tomentosa R.& S., were evaluated for their antibacterial activity, total phenol content, flavonoid content, 2,2-diphenyl-1-picrylhydrazyl free radical scavenging activity and phytochemical analysis, using successive extraction by cold percolation method with petroleum ether, ethyl acetate, methanol and water. In vitro antibacterial activity was evaluated against five bacterial strains viz. Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa, Salmonella typhimurium and Enterobacter aerogenes by agar well diffusion method. Among the plants screened, W. tomentosa leaf and fruit showed the best antibacterial activity. The Gram-positive bacteria were more susceptible than Gram-negative bacteria. Methanol extract of M. zapota showed the best 2,2-diphenyl-1-picrylhydrazyl free radical scavenging activity. Highest total phenol content was shown by M. zapota and S. cumini in methanol extract, while highest flavonoid content was shown by W. tomentosa stem in petroleum ether extract and ethyl acetate extract. In all the plants, cardiac glycosides and triterpenes were more as compared to other phytoconstituents.
139 citations
TL;DR: The in situ gel forming polymeric formulations offer several advantages like sustained and prolonged action in comparison to conventional drug delivery systems, which reduces the investment and manufacturing cost from a manufacturing point of view.
Abstract: In situ forming polymeric formulations are drug delivery systems that are in sol form before administration in the body, but once administered, undergo gelation in situ, to form a gel. The formation of gels depends on factors like temperature modulation, pH change, presence of ions and ultra violet irradiation, from which the drug gets released in a sustained and controlled manner. Various polymers that are used for the formulation of in situ gels include gellan gum, alginic acid, xyloglucan, pectin, chitosan, poly(DL-lactic acid), poly(DL-lactide-co-glycolide) and poly-caprolactone. The choice of solvents like water, dimethylsulphoxide, N-methyl pyrrolidone, triacetin and 2-pyrrolidone for these formulations depends on the solubility of polymer used. Mainly in situ gels are administered by oral, ocular, rectal, vaginal, injectable and intraperitoneal routes. The in situ gel forming polymeric formulations offer several advantages like sustained and prolonged action in comparison to conventional drug delivery systems. The article presents a detailed review of these types of polymeric systems, their evaluation, advancements and their commercial formulations. From a manufacturing point of view, the production of such devices is less complex and thus lowers the investment and manufacturing cost.
137 citations
TL;DR: An actinomycete strain, Streptomyces hygroscopicus subsp.
Abstract: An actinomycete strain, Streptomyces hygroscopicus subsp. ossamyceticus (strain D10) was isolated from Thar Desert soil, Rajasthan during the year 2006 and found to produce a yellow color pigment with antibiotic activity. Crude pigment was produced from strain D10 by solid state fermentation using wheat bran medium followed by extraction with ethyl acetate. The antimicrobial activity of the crude pigment was evaluated against drug resistant pathogens such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant Staphylococcus aureus, extended spectrum beta-lactamase producing cultures of Escherichia coli, Pseudomonas aeruginosa and Klebsiella sp. About 420 mg of crude pigment was produced per 10 g of wheat bran medium. In the disc diffusion method the crude ethyl acetate extract showed a minimum of 10 mm inhibition against Klebsiella sp. and maximum of 19 mm of inhibition against Escherichia coli. The crude pigment was partially purified using thin layer chromatography with the solvent system chloroform:methanol (30:70) and the Rf value was calculated as 0.768. Antimicrobial activity of the partially purified compound from thin layer chromatography was determined using the bioautography method. The purified pigment showed minimum of 15 mm inhibition against Klebsiella sp. and a maximum of 23 mm of inhibition against vancomycin-resistant Staphylococcus aureus in the disc diffusion method. Based on the results of chemical screening, the pigment was tentatively identified as group of sugar containing molecules.
119 citations
TL;DR: The results support the folkloric use of these plants in the treatment of urinary tract infections by the tribals of Mahakoshal region of central India.
Abstract: Seventeen Indian folklore medicinal plants were investigated to evaluate antibacterial activity of aqueous, ethanol and acetone extracts against 66 multidrug resistant isolates of major urinary tract pathogens (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Enterococcus faecalis) by disc diffusion method. Ethanol extract of Zingiber officinale and Punica granatum showed strong antibacterial activity against Escherichia coli. Ethanol extracts of Terminalia chebula and Ocimum sanctum exhibited antibacterial activity against Klebsiella pneumoniae. Ethanol extract of Cinnamomum cassia showed maximum antibacterial activity against Pseudomonas aeruginosa while ethanol extract of Azadirachta indica and Ocimum sanctum exhibited antibacterial activity against Enterococcus faecalis. The results support the folkloric use of these plants in the treatment of urinary tract infections by the tribals of Mahakoshal region of central India.
105 citations
TL;DR: The main objective is to formulate and evaluate in situ oral topical gels of clotrimazole based on the concept of pH triggered and ion activated systems and found that increase in calcium ions produced stronger gels.
Abstract: increase in calcium ions produced stronger gels. The drug content, clarity, and pH of the formulation were found to be satisfactory. The viscosity was found to be in the range 5 to 85 centipoise for the sol, whereas for the gels it was up to 16000 centipoise. The formulation showed pseudoplastic flow with thixotrophy. The maximum gel strength (using texture analyzer) and bioadhesion was found to be up to 6.5 g and 4 g, respectively. The optimized formulations were able to release the drug up to 6 h. The formulation containing gellan gum showed better sustained release compared to carbopol based gels.
87 citations
TL;DR: Essential oil extracted from Cymbopogon martini showed the highest activity against both gram positive and gram negative bacteria among the tested essential oils.
Abstract: Essential oils extracted from flower petals of palmarosa (Cymbopogon martini), evening primrose (Primula rosea), lavender (Lavandula angustifolia) and tuberose (Polianthus tuberosa) were tested for their antibacterial activities against gram-positive and gram-negative bacteria. Different concentrations of each essential oil ranging from 10-100% were tested. Both gram-positive and gram-negative bacteria were found susceptible to the studied flower essential oils. With increase in concentration of essential oil, increase in zone of inhibition was observed thus dose-dependent response was clear for each essential oil. Essential oil extracted from Cymbopogon martini showed the highest activity against both gram positive and gram negative bacteria among the tested essential oils.
TL;DR: Ethanol extract of the aerial part of Andrographis paniculata is potent in inhibiting bacterial growth of both Gram-negative and Gram positive bacteria.
Abstract: In the present study the ethanol extract of the aerial part of Andrographis paniculata was prepared and evaluated for antimicrobial activity against eleven bacterial strains by determining minimum inhibitory concentration and zone of inhibition. Minimum inhibitory concentration values were compared with control and zone of inhibition values were compared with standard ciprofloxacin in concentration 100 and 200 μg/ml. The results revealed that, the ethanol extract is potent in inhibiting bacterial growth of both Gram-negative and Gram positive bacteria.
TL;DR: Viscometric, turbidity and coacervate dry yield investigations were used to investigate optimum conditions for complex coac conservation and showed that optimum coacervation occurred at 25% sodium alginate fraction at pH 3.5.
Abstract: A gelatin and sodium alginate complex coacervation system was studied and an effect of pH and colloid mixing ratios on coacervation was investigated. A colloid mixing ratio at which optimum coacervation occurred varied with the coacervation pH. Viscometric, turbidity and coacervate dry yield investigations were used to investigate optimum conditions for complex coacervation. Optimum coacervation occurred at pH 3.5 at a gelatin sodium alginate ratio 4:1. Coacervate and equilibrium fluid was analyzed for gelatin and sodium alginate contents and yields calculated on the basis of chemical analysis showed that optimum coacervation occurred at 25% sodium alginate fraction at pH 3.5.
TL;DR: A simple, accurate, economical and reproducible HPLC method has been developed for quantitative estimation of metformin hydrochloride from tablet dosage form and formulated microspheres and the linearity was observed in concentration range of 0-25 μg/ml.
Abstract: A simple, accurate, economical and reproducible HPLC method has been developed for quantitative estimation of metformin hydrochloride from tablet dosage form and formulated microspheres. The developed HPLC method is a reverse phase chromatographic method using phenomenex C(18) column and acetonitrile:phosphate buffer (65:35) pH adjusted to 5.75 with o-phosphoric acid as mobile phase and glipizide as internal standard. The linearity was observed in concentration range of 0-25 mug/ml for metformin hydrochloride. Results of analysis were validated statistically and by recovery studies.
TL;DR: The rapid high performance liquid chromatographic method has been developed and validated and is found to be robust and can be successfully used to determine the drug content of marketed formulations.
Abstract: A rapid high performance liquid chromatographic method has been developed and validated for the estimation of ramipril and telmisartan simultaneously in combined dosage form. A Genesis C18 column having dimensions of 4.6x250 mm and particle size of 5 mum in isocratic mode, with mobile phase containing a mixture of 0.01 M potassium dihydrogen phosphate buffer (adjusted to pH 3.4 using orthophosphoric acid): methanol:acetonitrile (15:15:70 v/v/v) was used. The mobile phase was pumped at a flow rate of 1.0 ml/min and the eluents were monitored at 210 nm. The selected chromatographic conditions were found to effectively separate ramipril (R(t): 3.68 min) and telmisartan (R(t): 4.98 min) having a resolution of 3.84. The method was validated in terms of linearity, accuracy, precision, specificity, limit of detection and limit of quantitation. Linearity for ramipril and telmisartan were found in the range of 3.5-6.5 mug/ml and 28.0-52.0 mug/ml, respectively. The percentage recoveries for ramipril and telmisartan ranged from 99.09-101.64% and 99.45-100.99%, respectively. The limit of detection and the limit of quantitation for ramipril was found to be 0.5 mug/ml and 1.5 mug/ml respectively and for telmisartan was found to be 1.5 mug/ml and 3.0 mug/ml, respectively. The method was found to be robust and can be successfully used to determine the drug content of marketed formulations.
TL;DR: The results obtained in the present study indicated that ginger oil has a protective action against gastric ulcers induced by aspirin plus pylorus ligation in Wistar rats.
Abstract: The present investigation was performed in aspirin and pylorus ligation-induced ulcer model in Wistar rats, in which ability of ginger oil to provide gastric protection was studied at two different doses, 0.5 and 1 g/kg po. Gastric protection was evaluated by measuring the ulcer index, serum gamma-GTP levels, total acidity of gastric juice and gastric wall mucus thickness. The results obtained in the present study indicated that ginger oil has a protective action against gastric ulcers induced by aspirin plus pylorus ligation in Wistar rats.
TL;DR: Results of the present study suggest that the aqueous extracts of H. indicus, F. bengalensis and P. marspium roxb has significant antibacterial activity against pathogenic bacteria.
Abstract: The antimicrobial activity of Hemidesmus indicus, Ficus bengalensis and Pterocarpus marsupium roxb was evaluated against pathogenic bacteria Stahylococcus aureus, Pseudomonas aeruginosa and Klebsiella pneumonia in an in vitro condition. Aqueous extracts from roots of H. indicus and barks of F. bengalensis and P. marspium roxb were tested for antimicrobial activity using the zone of inhibition method and also screened for phytochemicals. The aqueous extract of P. marsupium roxb inhibited growth of bacteria with the minimal inhibitory concentration ranging from 0.04 mg to 0.08 mg and extracts of F. bengalensis and H. indicus showed inhibition at the range of 0.04 mg to 0.1 mg against the bacteria tested. The susceptibility of bacterial pathogens was in the order of S. aureus, K. pneumoniae and P. aeruginosa. The antimicrobial activity of plant extracts was synergistic with antibiotics tested. Results of the present study suggest that the aqueous extracts of H. indicus, F. bengalensis and P. marspium roxb has significant antibacterial activity against pathogenic bacteria.
TL;DR: The proposed method can be successfully used to determine the drug content of marketed tablet formulation.
Abstract: A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the estimation of emtricitabine and tenofovir simultaneously in combined dosage form. The stationary phase used was precoated silica gel 60F 254.The mobile phase used was a mixture of chloroform: methanol (9:1 v/v). The detection of spots was carried out at 265 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 200 to 1000 ng with regression coefficient of 0.9995.The proposed method can be successfully used to determine the drug content of marketed tablet formulation.
TL;DR: Ionic surfactants were found to be much better solubilizing agents than non-ionic surfactant and cetyltrimethylammonium bromide amongst ionic Surfactants, solubility was finding to be very high in anionic Surfactant, sodium dodecylsulphate as compared to the cationic surfacts.
Abstract: Solubility enhancement of antimicrobial drug enrofloxacin has been studied using a series of co-solvents and surfactants. Aqueous solubility of enrofloxacin could be increased up to 26 times. Co-solvents alone produced only small increase in solubility. However, the combined effect of co-solvents and buffer was synergistic and a large increase in solubility could be attained. Ionic surfactants were found to be much better solubilizing agents than non-ionic surfactant. Amongst ionic surfactants, solubility was found to be very high in anionic surfactant, sodium dodecylsulphate as compared to the cationic surfactant, cetyltrimethylammonium bromide. Up to 3.8 mg/ml of enrofloxacin could be dissolved in sodium dodecylsulphate. Mechanism of solubilization has been proposed and surfactant solubilization parameters have been calculated.
TL;DR: The developed protocol can be utilized for mass production of true to type planting material on large scale independent of season, i.e. external environmental conditions.
Abstract: Stevia rebaudiana Bertoni that conventionally propagated by seed or by cuttings or clump division which has a limitation of quality and quantity seed material. In present study, callus culture technique was tried to achieve rapid plant multiplication for quality seed material. Callus induction and multiplication medium was standardized from nodal as well as leaf sagments. It is possible to maintain callus on Murashige and Skoog medium supplemented with 6-benzyl amino purine and naphthalene acetic acid. Maximum callus induction was obtained on Murashige and Skoog medium incorporated with 6-benzyl amino purine (2.0-3.0 mg/l) and naphthalene acetic acid (2.0 mg/l) treatments. However, Murashige and Skoog medium containing 2.0 mg/l 6-benzyl amino purine+2.0 mg/l naphthalene acetic acid was found to be the best for callus induction. Higher regeneration frequency was noticed with Murashige and Skoog medium supplemented with 2.0 mg/l 6-benzyl amino purine+0.2 mg/l naphthalene acetic acid. Regenerated plants were rooted better on ¼ Murashige and Skoog strength supplemented with 0.1 mg/l indole-3-butyric acid. The rooted plantlets were hardened successfully in tera care medium with 63 per cent survival rate. The developed protocol can be utilized for mass production of true to type planting material on large scale independent of season, i.e. external environmental conditions.
TL;DR: A sensitive and accurate UV spectrophotometric method with multivariate calibration technique for the determination of metformin hydrochloride in bulk drug and different pharmaceutical formulations has been described and was found highly accurate, precise and reproducible.
Abstract: A sensitive and accurate UV spectrophotometric method with multivariate calibration technique for the determination of metformin hydrochloride in bulk drug and different pharmaceutical formulations has been described. This technique is based on the use of the linear regression equations by using relationship between concentration and absorbance at five different wavelength. The results were treated statistically and were found highly accurate, precise and reproducible. The method is accurate, precise (% recovery 102.500.063, CV≤0.56, r =0.997) and linear within the range 1-10 mg/ml. There was no interference from the excipients i.e Povidone K 30, magnesium stearate, lactose and hydroxypropylmethylcellulose. This statistical approach gives optimum results for the eliminating fluctuations coming from instrumental or experimental conditions.
TL;DR: In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by direct compression method and the formulation prepared by using 8% w/w of Plantago ovata mucilage and 60% of microcrystalline cellulose emerged as the overall best formulation.
Abstract: In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by direct compression method. In this method mucilage of Plantago ovata and crospovidone were used as superdisintegrants (2-8% w/w) along with microcrystalline cellulose (20-60% w/w) and 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 8 s), the two 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 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation prepared by using 8% w/w of Plantago ovata mucilage and 60% w/w of microcrystalline cellulose emerged as the overall best formulation (t 50% 3.3 min) based on the in vitro drug release characteristics compared to conventional commercial tablets formulation (t 50% 17.4 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).
TL;DR: Melastoma malabathricum water extract treated mice showed significant reduction in the fecal output and protected them from castor oil-induced diarrhoea and reduced the intestinal fluid secretion induced by magnesium sulphate and gastrointestinal motility after charcoal meal administration in the mice.
Abstract: The antidiarrhoeal effect of the water extract of Melastoma malabathricum Linn (Melastomataceae) leaves were investigated by employing four experimental models of diarrhea in Swiss mice Melastoma malabathricum water extract treated mice showed significant reduction in the fecal output and protected them from castor oil-induced diarrhoea The extract also reduced the intestinal fluid secretion induced by magnesium sulphate and gastrointestinal motility after charcoal meal administration in the mice No mortality and visible signs of general weakness was observed in the mice following the test extract administration up to 2000 mg/kg dose
TL;DR: A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated and can be successfully used to determine the drug content of marketed formulation.
Abstract: A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed and validated for the simultaneous estimation of valsartan and hydrochlorothiazide in combined dosage forms. The stationary phase used was precoated silica gel 60F 254 . The mobile phase used was a mixture of chloroform: methanol: toluene: glacial acetic acid (6:2:1:0.1 v/v/v/v). The detection of spots were carried out at 260 nm. The method was validated in terms of linearity, accuracy, precision and specificity. The calibration curve was found to be linear between 300 to 800 ng/spot for valsartan and 100 to 600 ng/spot for hydrochlorothiazide. The limit of detection and the limit of quantification for the valsartan were found to be 100 and 300 ng/spot respectively and for hydrochlorothiazide 30 and 100 ng/spot respectively. The proposed method can be successfully used to determine the drug content of marketed formulation.
TL;DR: 1,8-cineole had weak antimicrobial activity against all of the tested microorganisms, Hence the use of P. abrotanoides oil could be useful in fighting secondary infections in leishmaniasis especially against S. aureus.
Abstract: In Iranian folk medicine, Perovskia abrotanoides is used for treatment of leishmaniasis. These patients may develop secondary infections with opportunistic microorganisms. Therefore, the antimicrobial activity of essential oil from aerial part of P. abrotanoides and its main components was evaluated against different microorganisms. Disc diffusion and broth micro dilution assays were used for in vitro antimicrobial screening. The antibacterial activity of this oil and main components on viability of S. aureus was determined. The oil showed antimicrobial activity against Candida albicans and Gram positive bacteria especially Staphylococcus aureus with zone inhibitions and minimal inhibitory concentration values in the range of 7.6 to 29 mm and 2 to 8 mul/ml respectively, whereas the least susceptible were Aspergillus niger and Gram negative bacteria. In viability test, the results showed that the antimicrobial activity of 1,8-cineole was more than that of alpha-pinene and camphor but after 60 min this effect gradually decreased only for 1,8-cineole and ultimately the antibacterial activity of camphor was more than that of alpha-pinene. 1,8-cineole had weak antimicrobial activity against all of the tested microorganisms. Hence the use of P. abrotanoides oil could be useful in fighting secondary infections in leishmaniasis especially against S. aureus.
TL;DR: The synthesized heterocycles were characterized on the basis of physical, chemical tests and spectroscopic data and tested for the acute antiinflammatory activity and antibacterial activity using carrageenan-induced rat paw edema method and cup-plate method, respectively.
Abstract: Chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in ethanolic KOH solution. These chalcones were immediately reacted with hydroxylamine hydrochloride in presence of glacial acetic acid as reagent to obtain the corresponding isoxazole derivatives. The synthesized heterocycles were characterized on the basis of physical, chemical tests and spectroscopic data. These compounds were tested for the acute antiinflammatory activity and antibacterial activity using carrageenan-induced rat paw edema method and cup-plate method, respectively.
TL;DR: The proposed method was found to be accurate and precise for routine estimation of metformin hydrochloride in bulk and from tablet dosage forms.
Abstract: A simple and sensitive spectrophotometric method has been developed and validated for the estimation of metformin hydrochloride in bulk and in tablet formulation. The primary amino group of metformin hydrochloride reacts with ninhydrin in alkaline medium to form a violet colour chromogen, which is determined spectrophotometrically at 570 nm. It obeyed Beer's law in the range of 8-18 µg/ml. Percentage recovery of the drug for the proposed method ranged from 97-100% indicating no interference of the tablet excipients. The proposed method was found to be accurate and precise for routine estimation of metformin hydrochloride in bulk and from tablet dosage forms.
TL;DR: In the present study a new dissolution medium was developed, as there is no validated dissolution method available in the literature, and it was revealed that addition of surfactant may be suitable as a dissolution medium.
Abstract: Curcumin is a phytoconstituent with wide range of biological activity. It is poorly soluble in water. In the present study a new dissolution medium was developed, as there is no validated dissolution method available in the literature. The composition of the dissolution medium was selected on the basis of solubility data at 37°. Solubility data revealed that addition of surfactant may be suitable as a dissolution medium. The suitability of dissolution medium (0.5% sodium lauryl sulphate in water) relative to the other dissolution medium was evaluated. The selected dissolution media was used for the evaluation of curcumin tablets.
TL;DR: Two UV Spectrophotometric and one reverse phase high performance liquid chromatography methods have been developed for the simultaneous estimation of amlodipine besilate and olmesartan medoxomil in tablet dosage form and all the validation parameters are met.
Abstract: Two UV Spectrophotometric and one reverse phase high performance liquid chromatography methods have been developed for the simultaneous estimation of amlodipine besilate and olmesartan medoxomil in tablet dosage form. First UV spectrophotometric method was a determination using the simultaneous equation method at 237.5 nm and 255.5 nm over the concentration range 10-50 μg/ml and 10-50 μg/ml, for amlodipine besilate and olmesartan medoxomil with accuracy 100.09%, and 100.22% respectively. Second UV spectrophotometric method was a determination using the area under curve method at 242.5-232.5 nm and 260.5-250.5 nm over the concentration range of 10-50 μg/ml and 10-50 μg/ml, for amlodipine besilate and olmesartan medoxomil with accuracy 100.10%, and 100.48%, respectively. In reverse phase high performance liquid chromatography analysis carried out using 0.05M potassuim dihydrogen phosphate buffer:acetonitrile (50:50 v/v) as the mobile phase and Kromasil C18 (4.6 mm i.d.Χ250 mm) column as the stationery phase with detection wavelength of 238 nm. Flow rate was 1.0 ml/min. Retention time for amlodipine besilate and olmesartan medoxomil were 3.69 and 5.36 min, respectively. Linearity was obtained in the concentration range of 4-20 μg/ml and 10-50 μg/ml for amlodipine besilate and olmesartan medoxomil, respectively. Proposed methods can be used for the estimation of amlodipine besilate and olmesartan medoxomil in tablet dosage form provided all the validation parameters are met.
TL;DR: This study examined the protective effects of quercetin on chronic ethanol-induced liver injury and found that the changes in enzyme activities as well as levels of lipid peroxidation products were reversed to a certain extent by quercETin.
Abstract: This study examined the protective effects of quercetin on chronic ethanol-induced liver injury. Rats were treated with ethanol at a dose of 4 g/100 g/day for 90 days. After ethanol intoxication, levels of serum amino transferases were significantly elevated. Decreased activity of superoxide dismutase, catalase, glutathione peroxidase and glutathione reductase was also observed on ethanol administration. Increased amounts of lipid peroxidation products viz. hydroperoxides, conjugated dienes and malodialdehyde were observed on ethanol intoxication. Ethanol administration resulted in significant decrease in liver glutathione content. After 90 days, the control animals were divided into two groups, the control group and the control+quercetin group. Ethanol-treated group was divided into two groups, abstention group and quercetin-supplemented group. After 30 days, the animals were sacrificed and various biochemical parameters were analyzed. The changes in enzyme activities as well as levels of lipid peroxidation products were reversed to a certain extent by quercetin. Quercetin supplementation resulted in increase of glutathione content to a significant level compared to normal abstention group. Quercetin supplemented group showed a faster recovery than abstention group. This shows the protective effect of quercetin against chronic ethanol induced hepatotoxicity. Histopathological study is also in line with these results.