Showing papers in "Indian Journal of Pharmaceutical Sciences in 2011"
TL;DR: Gum-resin extracts of Boswellia serrata have been traditionally used in folk medicine for centuries to treat various chronic inflammatory diseases.
Abstract: The resin of Boswellia species has been used as incense in religious and cultural ceremonies and in medicines since time immemorial. Boswellia serrata (Salai/Salai guggul), is a moderate to large sized branching tree of family Burseraceae (Genus Boswellia), grows in dry mountainous regions of India, Northern Africa and Middle East. Oleo gum-resin is tapped from the incision made on the trunk of the tree and is then stored in specially made bamboo basket for removal of oil content and getting the resin solidified. After processing, the gum-resin is then graded according to its flavour, colour, shape and size. In India, the States of Andhra Pradesh, Gujarat, Madhya Pradesh, Jharkhand and Chhattisgarh are the main source of Boswellia serrata. Regionally, it is also known by different names. The oleo gum-resins contain 30-60% resin, 5-10% essential oils, which are soluble in the organic solvents, and the rest is made up of polysaccharides. Gum-resin extracts of Boswellia serrata have been traditionally used in folk medicine for centuries to treat various chronic inflammatory diseases. The resinous part of Boswellia serrata possesses monoterpenes, diterpenes, triterpenes, tetracyclic triterpenic acids and four major pentacyclic triterpenic acids i.e. β-boswellic acid, acetyl-β-boswellic acid, 11-keto-β-boswellic acid and acetyl-11-keto-β-boswellic acid, responsible for inhibition of pro-inflammatory enzymes. Out of these four boswellic acids, acetyl-11-keto-β-boswellic acid is the most potent inhibitor of 5-lipoxygenase, an enzyme responsible for inflammation.
247 citations
TL;DR: Findings show that the polyphenolic constituents in the extracts are responsible for free radical scavenging capacity.
Abstract: The powder samples and methanol extract of 11 medicinal plants were subjected to analysis of proximate composition and measurement of antioxidant activity. Different parameters studied include phenolic contents, moisture, ash, crude fiber, fats and waxes. The assays employed were ferric reducing antioxidant power, trolox equivalent antioxidant capacity and scavenging effect on the 1,1-diphenyl-2-picrylhydrazyl free radical. Results obtained indicate that the antioxidant potential varied significantly from plant to plant. The total phenolic contents were determined spectrophotometrically using Folin-Ciocalteu reagent. Significant correlation is observed between ferric reducing antioxidant power and phenolic contents (R(2) = 0.96). These findings show that the polyphenolic constituents in the extracts are responsible for free radical scavenging capacity.
178 citations
TL;DR: Actaea spicata Linn.
Abstract: Actaea spicata Linn. (Ranunculaceae) has been traditionally used for the treatment of various ailments such as rheumatism, inflammation, nerve diseases, lumbago, scrofula and chorea, but no systematic phytochemical and pharmacological work has ever been carried out on this potential plant. Preliminary phytochemical screening showed presence of phenols and flavonoids in A. spicata. Thus, the present investigation was undertaken to estimate total phenols and flavonoids in methanol extract of A. spicata roots, and its ethyl acetate fraction. In vitro antioxidant activity was also evaluated in the methanol extract and ethyl acetate fraction using DPPH method. Ethyl acetate fraction was found to contain twice the content of flavonoids and phenols in comparison to methanolic extract, whereas phenolic content in methanol extract was approximately similar to ethyl acetate fraction. A significant antioxidant activity, i.e., mean percentage inhibition of DPPH radical was observed in methanol extract and ethyl acetate fraction at the concentration of 10 μg/ml and 5 μg/ml respectively. Finally, it was suggested that polyphenols are responsible for antioxidant activity of A. spicata.
114 citations
TL;DR: The noninvasive routes which were of minor importance as parts of drug delivery in the past have assumed added importance in protein and peptide drug delivery and these include nasal, ophthalmic, buccal, vaginal, transdermal and pulmonary routes are reviewed.
Abstract: Recent advances in the field of pharmaceutical biotechnology have led to the formulation of many protein and peptide-based drugs for therapeutic and clinical application. The route of administration has a significant impact on the therapeutic outcome of a drug. The needle and syringe is a well established choice of protein and peptide delivery which has some drawback related to patient and to formulation such as pain, cost, sterility etc. Thus, the noninvasive routes which were of minor importance as parts of drug delivery in the past have assumed added importance in protein and peptide drug delivery and these include nasal, ophthalmic, buccal, vaginal, transdermal and pulmonary routes. The pharmaceutical scientists have some approaches to develop the formulations for protein and peptide delivery by noninvasive routes. But, due to the physiochemical instability and enzymatic barrier of proteins and peptides there are several hurdle to develop suitable formulation. So there is need of penetration enhancers, enzyme inhibitors and suitable vehicles for noninvasive delivery to increase the bioavailability. In this review, the aim is to focus on the approaches to formulation of protein and peptide based drug administration by noninvasive route.
105 citations
TL;DR: This review focuses on the preparation, characterization of chitosan microspheres and their role in novel drug delivery systems.
Abstract: The main aim in the drug therapy of any disease is to attain the desired therapeutic concentration of the drug in plasma or at the site of action and maintain it for the entire duration of treatment. A drug on being used in conventional dosage forms leads to unavoidable fluctuations in the drug concentration leading to under medication or overmedication and increased frequency of dose administration as well as poor patient compliance. To minimize drug degradation and loss, to prevent harmful side effects and to increase drug bioavailability various drug delivery and drug targeting systems are currently under development. Handling the treatment of severe disease conditions has necessitated the development of innovative ideas to modify drug delivery techniques. Drug targeting means delivery of the drug-loaded system to the site of interest. Drug carrier systems include polymers, micelles, microcapsules, liposomes and lipoproteins to name some. Different polymer carriers exert different effects on drug delivery. Synthetic polymers are usually non-biocompatible, non-biodegradable and expensive. Natural polymers such as chitin and chitosan are devoid of such problems. Chitosan comes from the deacetylation of chitin, a natural biopolymer originating from crustacean shells. Chitosan is a biocompatible, biodegradable, and nontoxic natural polymer with excellent film-forming ability. Being of cationic character, chitosan is able to react with polyanions giving rise to polyelectrolyte complexes. Hence chitosan has become a promising natural polymer for the preparation of microspheres/nanospheres and microcapsules. The techniques employed to microencapsulate with chitosan include ionotropic gelation, spray drying, emulsion phase separation, simple and complex coacervation. This review focuses on the preparation, characterization of chitosan microspheres and their role in novel drug delivery systems.
96 citations
TL;DR: A number of new in vitro techniques have been devised which help to decrease the use as well as the number of animals in biomedical research, but such alternatives cannot eliminate the need for animals in research completely.
Abstract: The preclinical studies for drug screening involve the use of animals which is very time consuming and expensive and at times leads to suffering of the used organism. Animal right activists around the world are increasingly opposing the use of animals. This has forced the researchers to find ways to not only decrease the time involved in drug screening procedures but also decrease the number of animals used and also increase the humane care of animals. To fulfill this goal a number of new in vitro techniques have been devised which are called 'Alternatives' or 'Substitutes' for use of animals in research involving drugs. These 'Alternatives' are defined as the adjuncts which help to decrease the use as well as the number of animals in biomedical research. Russell and Burch have defined these alternatives by three R's - Reduction, Refinement and Replacement. These alternative strategies include physico-chemical methods and techniques utilizing tissue culture, microbiological system, stem cells, DNA chips, micro fluidics, computer analysis models, epidemiological surveys and plant-tissue based materials. The advantages of these alternatives include the decrease in the number of animals used, ability to obtain the results quickly, reduction in the costs and flexibility to control the variables of the experiment. However these techniques are not glittering gold and have their own shortcomings. The disadvantages include the lack of an appropriate alternative to study the whole animal's metabolic response, inability to study transplant models and idiosyncratic responses and inability to study the body's handling of drugs and its subsequent metabolites. None-the-less these aalternative methods to certain extent help to reduce the number of animals required for research. But such alternatives cannot eliminate the need for animals in research completely. Even though no animal model is a complete set of replica for a process within a human body, the intact animal does provide a better model of the complex interaction of the physiological processes.
78 citations
TL;DR: An up-to-date and comprehensive review on O. indicum covering its traditional and folk medicinal uses, phytochemistry and pharmacology, and its antiinflammatory, antiulcer, hepatoprotective and immunostimulant properties are compiled.
Abstract: Oroxylum indicum Vent. (O. indicum) is a tree commonly called Indian trumpet tree found in tropical countries, such as India, Japan, China, Sri Lanka, Malaysia. The chemical constituents obtained from different parts of plant include baicalein-7-O-diglucoside (Oroxylin B), baicalein-7-O-glucoside, chrysin, apegenin, prunetin, sitosterol, oroxindin, biochanin-A, ellagic acid, baicalein and its 6- and 7-glucuronides, scutellarein, tetuin, antraquinone and aloe-emodin. Various parts of the plant are used in Ayurveda and folk medicine for the treatment of different ailments such as cancer, diarrhea, fever, ulcer and jaundice. Recent in vivo and in vitro studies have indicated its antiinflammatory, antiulcer, hepatoprotective, anticancer, antioxidant, photocytotoxic, antiproliferative, antiarthritic, antimicrobial, antimutagenic and immunostimulant properties. Exhaustive literature survey reveals that there are some activities which are still not proven scientifically. This article is an attempt to compile an up-to-date and comprehensive review on O. indicum covering its traditional and folk medicinal uses, phytochemistry and pharmacology.
64 citations
TL;DR: The alcohol and aqueous extract of bark of Tamarindus indica exhibited significant anthelmintic activity as evidenced by decreased paralyzing time and death time, which support the use ofTamarindu indica as an anthel minting agent.
Abstract: The aim of the present study was to evaluate the anthelmintic activity of ethanolic and aqueous extract of leaves and bark of Tamarindus indica Linn using Pheretima posthuma and Tubifex tubifex as test worms. The time of paralysis and time of death were studied and the activity was compared with piperazine citrate as reference standard. The alcohol and aqueous extract of bark of Tamarindus indica exhibited significant anthelmintic activity as evidenced by decreased paralyzing time and death time. The results thus support the use of Tamarindus indica as an anthelmintic agent.
55 citations
TL;DR: The in vitro release of clotrimazole from its solid dispersions and inclusion complexes incorporated suppositories was markedly improved when compared to the intact drug incorporated suppository, and polyvinyl pyrrolidone solid dispersion incorporated supp repositories were found to possess excellent antifungal activity.
Abstract: Solid dispersions of a slightly water-soluble drug, clotrimazole, were prepared in different weight ratios using polyethyleneglycol 4000 and different molecular weight polyvinyl pyrrolidones as carriers. Moreover, binary and ternary β-cyclodextrin complexes were prepared in different molar ratios. Both solid dispersions and β-cyclodextrin complexes were prepared by solvent evaporation technique. A phase solubility method was used to evaluate the effect of the tested carriers on the aqueous solubility of clotrimazole. The dissolution of all the preparations was tested using the USP paddle method. The selected solid dispersions and inclusion complexes were characterized by differential scanning calorimetry and X-ray powder diffractometry studies, and results clarified the role of the tested carriers in decreasing the crystallinity of clotrimazole and complexing abilities. Based on physical characters and in vitro drug release pattern, polyvinylpyrrolidone solid dispersions (1:1 weight ratio) and ternary cyclodextrin complexes (clotrimazole-β-cyclodextrin complexes with either polymer, 1:1 molar ratio) were selected as ideal batches for suppositories. Suppocire AM/50 mg carbopol 940, was chosen as a suppository base and the suppositories were prepared by molding technique. The prepared suppositories were characterized for weight variation, softening time and drug content. All these properties were found to be ideal. The in vitro drug release pattern was determined in citrate buffer (pH 4.5) containing 1% sodium lauryl sulfate. The in vitro release of clotrimazole from its solid dispersions and inclusion complexes incorporated suppositories was markedly improved when compared to the intact drug incorporated suppositories. Polyvinyl pyrrolidone solid dispersions incorporated suppositories were found to possess excellent antifungal activity.
52 citations
TL;DR: Investigation in normal and alloxan-induced diabetic rats demonstrated that ethanol extract of Plectranthus amboinicus leaves possesses hypoglycemic and antihyperlipidemic effects mediated through the restoration of the functions of pancreatic tissues and insulinotropic effect.
Abstract: The present study was undertaken to investigate the antihyperglycemic and antihyperlipidemic effects of ethanol extract of Plectranthus amboinicus in normal and alloxan-induced diabetic rats. Diabetes was induced in Wistar rats by single intraperitoneal administration of alloxan monohydrate (150 mg/kg). Normal as well as diabetic rats were divided into groups (n=6) receiving different treatments. Graded doses (200 mg/kg and 400 mg/kg) of ethanol extract of Plectranthus amboinicus were studied in both normal and alloxan-induced diabetic rats for a period of 15 days. Glibenclamide (600 μg/kg) was used as a reference drug. Oral administration with graded doses of ethanol extract of Plectranthus amboinicus exhibited hypoglycemic effect in normal rats and significantly reduced the peak glucose levels after 120 min of glucose loading. In alloxan-induced diabetic rats, the daily oral treatment with ethanol extract of Plectranthus amboinicus showed a significant reduction in blood glucose. Besides, administration of ethanol extract of Plectranthus amboinicus for 15 days significantly decreased serum contents of total cholesterol, triglycerides whereas HDL-cholesterol, total proteins and calcium were effectively increased. Furthermore, effect of ethanol extract of Plectranthus amboinicus showed profound elevation of serum amylase and reduction of serum lipase. Histology examination showed ethanol extract of Plectranthus amboinicus exhibited almost normalization of damaged pancreatic architecture in rats with diabetes mellitus. Studies clearly demonstrated that ethanol extract of Plectranthus amboinicus leaves possesses hypoglycemic and antihyperlipidemic
50 citations
TL;DR: Out of the 30 actinobacterial cultures screened for antimicrobial activity, 28 cultures were found to produce active products against various pathogenic microorganisms using a modified cross streak method, and Streptomyces sp.
Abstract: Out of the 30 actinobacterial cultures screened for antimicrobial activity, 28 cultures were found to produce active products against various pathogenic microorganisms such as Gram-negative, Gram-positive bacteria and yeast, using a modified cross streak method. The modified method helped in easy quantification of results and also in ruling out probable mutual antibiosis. The actinobacterial strains that showed the ability to produce antimicrobial compounds belonged to Streptomyces (53%), Micromonospora (13%) and Actinomadura (10%) genera. Streptomyces sp. strain MMA-5 showed the highest multispecific antibiosis efficiency score value. Broad antibiotic spectrum activity was exhibited by Streptomyces sp. strain MMA-2 and Micromonospora sp. strain MMA-8. The multidrug resistant human pathogenic yeast strain Candida albicans was inhibited by 18 actinobacterial strains.
TL;DR: It is confirmed that a high degree of malnutrition was prevalent in patients on hemodialysis, as shown by anthropometric assessment, biochemical markers of malnutrition and Subjective Global Assessment-Dialysis Malnutrition Score.
Abstract: Malnutrition is widely prevalent among patients on hemodialysis. Malnutrition can be estimated using a fully quantitative scoring system Subjective Global Assessment-Dialysis Malnutrition Score which is simple, reliable and dynamic. The primary objective of the study was to assess the severity of malnutrition in patients with end stage renal disease and undergoing hemodialysis in a tertiary care teaching hospital in Chennai, using Subjective Global Asses sment-Dialysis Malnutrition Score and correlate it with standard indicators of malnutrition like anthropometric and biochemical parameters of the study population by Pearson's correlation. Anthropometric assessment included height, body weight, triceps skin fold thickness, mid arm circumference, mid arm muscle circumference % and biochemical parameters included serum albumin, transferrin, ferritin, total protein, total cholesterol, blood urea nitrogen and creatinine. Based on the scores, of the 66 patients, 91% were moderately malnourished. There was a significant negative correlation between modified Subjective Global Assessment-Dialysis Malnutrition Score and anthropometric measures such as triceps skin fold thickness, mid arm circumference, mid arm muscle circumference; biochemical markers such as albumin, transferrin and ferritin. The data obtained from this study confirm that a high degree of malnutrition was prevalent in patients on hemodialysis, as shown by anthropometric assessment, biochemical markers of malnutrition and Subjective Global Assessment-Dialysis Malnutrition Score. Nutritional status as determined by Subjective Global Assessment-Dialysis Malnutrition Score is a useful and reliable index for identifying patients at risk for malnutrition and it correlates well with anthropometric and biochemical assessment. may be integrated in regular assessment of malnutrition in patients on maintenance hemodialysis.
TL;DR: The niosomal vaccine did not alter but rather enhanced the immunogenicity of the Newcastle disease vaccine, which showed a 71% increment in immune response over that of the marketed La Sota® vaccine.
Abstract: Span 20-based niosome was prepared by lipid film hydration technique and loaded with Newcastle disease vaccine. Three batches with Span 20, cholesterol and dicetyl phosphate in micro molar ratios of 10:10:1; 15:15:1 and 20:20:1 were prepared and evaluated for encapsulation efficiency using haemagglutination test. The morphology of the vesicles was studied by means of transmission electron microscopy. Particle size, zeta potential and polydispersity index were determined by photon correlation spectroscopy using a nanosizer. Adjuvanticity was assessed using haemagglutination inhibition test. The vesicles of Span 20-based niosomes were distinct, near spherical large unilamellar vesicles. The vesicles were of varied sizes (<1000 nm) with the entrapped Newcastle disease vaccine in the core of the vaccine. The zeta potential had a peak at -50 mV. The polydispersity index was 0.68. Haemagglutination inhibition test showed a 71% increment in immune response over that of the marketed La Sota® vaccine which had a 60% increment in immune response. The niosomal vaccine did not alter but rather enhanced the immunogenicity of the Newcastle disease vaccine.
TL;DR: The high recovery and low relative standard deviation confirm the suitability of the method for routine determination of aspirin, atorvastatin calcium and clopidogrel bisulphate in bulk drug and capsule dosage form.
Abstract: A simple, accurate, rapid and precise isocratic reversed-phase high-performance liquid chromatographic method has been developed and validated for simultaneous determination of aspirin, atorvastatin calcium and clopidogrel bisulphate in capsules. The chromatographic separation was carried out on an Inertsil ODS analytical column (150×4.6 mm; 5 μm) with a mixture of acetonitrile:phosphate buffer pH 3.0 adjusted with o-phosphoric acid (50:50, v/v) as mobile phase; at a flow rate of 1.2 ml/min. UV detection was performed at 235 nm. The retention times were 1.89, 6.6 and 19.8 min. for aspirin, atorvastatin calcium and clopidogrel bisulphate, respectively. Calibration plots were linear (r(2)>0.998) over the concentration range 5-30 μg/ml for atorvastatin calcium and 30-105 μg/ml for aspirin and clopidogrel bisulphate. The method was validated for accuracy, precision, specificity, linearity, and sensitivity. The proposed method was successfully used for quantitative analysis of capsules. No interference from any component of pharmaceutical dosage form was observed. Validation studies revealed that method is specific, rapid, reliable, and reproducible. The high recovery and low relative standard deviation confirm the suitability of the method for routine determination of aspirin, atorvastatin calcium and clopidogrel bisulphate in bulk drug and capsule dosage form.
TL;DR: The overall objective of this study was to develop an oral sustained release metformin hydrochloride tablet by using hydrophilic Eudragit RSPO alone or its combination with hydrophobic natural polymers Gum copal and gum damar as rate controlling factor.
Abstract: Metformin hydrochloride has relatively short plasma half-life, low absolute bioavailability. The need for the administration two to three times a day when larger doses are required can decrease patient compliance. Sustained release formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of metformin. Sustained release products are needed for metformin to prolong its duration of action and to improve patient compliances. The overall objective of this study was to develop an oral sustained release metformin hydrochloride tablet by using hydrophilic Eudragit RSPO alone or its combination with hydrophobic natural polymers Gum copal and gum damar as rate controlling factor. The tablets were prepared by wet granulation method. The in vitro dissolution study was carried out using USP 22 apparatus I, paddle method and the data was analysed using zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The drug release study revealed that Eudragit RSPO alone was unable to sustain the drug release. Combining Eudragit with gum Copal and gum Damar sustained the drug release for more than 12 h. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release.
TL;DR: Results of the present study reveal that extracts of W. somnifera showing great antimicrobial potential against test microorganisms may be exploited for future antimicrobial drugs.
Abstract: In the present study antimicrobial activity of Withania somnifera L. Dunal (Solanaceae) has been evaluated against selected pathogens. Free and bound flavonoids of different parts (root, stem, leaf and fruit) of W. somnifera have been studied for their antimicrobial activity using disc diffusion assay against three Gram negative bacteria (Escherichia coli MTCC 46, Proteus mirabilis MTCC 3310 and Pseudomonas aeruginosa MTCC 1934), one Gram positive bacteria (Staphylococcus aureus MTCC 3160) and three fungi (Candida albicans MTCC 183, Aspergillus flavus MTCC 277 and Aspergillus niger MTCC 282). Minimum inhibitory concentration (MIC) of the extracts was evaluated through micro broth dilution method, while minimum bactericidal/fungicidal concentration was determined by sub culturing the relevant samples. C. albicans was found to be the most susceptible organism followed by S. aureus, P. mirabilis, E. coli and P. aeruginosa. Out of the tested organisms, A flavus and A. niger were observed to be resistant as none of the tested extracts showed activity against them. Total activity (TA) of extracts (ml/g) against each sensitive pathogens was also evaluated. Bound flavonoid extract of root showed best activity against C. albicans (IZ 30, MIC 0.039, MFC 0.039, respectively). However all the microorganisms were found to be sensitive against the extracts tested. Total activity of bound flavonoid extract of root was found to be same for E.coli, P. mirabilis, S. aureus and C. albicans (153.84 ml/g). Results of the present study reveal that extracts of W. somnifera showing great antimicrobial potential against test microorganisms may be exploited for future antimicrobial drugs.
TL;DR: The management of the disease involves replacement therapy, non-replacement therapy and other therapies that include antifibrinolytics and topical agents.
Abstract: Most commonly inherited bleeding disorder, first described in Aland Islands by Erik von Willebrand. It occurs as a result of decrease in plasma levels or defect in von Willebrand factor which is a large multimeric glycoprotein. Monomers of this glycoprotein undergo N-glycosylation to form dimers which get arranged to give multimers. Binding with plasma proteins (especially factor VIII) is the main function of von Willebrand factor. The disease is of two forms: Inherited and acquired forms. Inherited forms are of three major types. They are type 1, type 2, and type 3; in which type 2 is sub-divided into 2A, 2B, 2M, 2N. Type 1 is more prevalent than all other types. Mucocutaneous bleeding is mild in type 1 whereas it is mild to moderate in types 2A, 2B, and 2M. Type 2N has similar symptoms of haemophilia. The pathophysiology of each type depends on the qualitative or quantitative defects in von Willebrand factor. The diagnosis is based on von Willebrand factor antigen, von Willebrand factor activity assay, FVIII coagulant activity and some other additional tests. Results should be analyzed within the context of blood group. von Willebrand factor multimer analysis is essential for typing and sub typing the disease. The management of the disease involves replacement therapy, non-replacement therapy and other therapies that include antifibrinolytics and topical agents.
TL;DR: Eugenol microcapsules possessed good flow properties, thus improved handling, and the percent oil loading and encapsulation efficiency increased with increase in core: coat ratio whereas treatment with dehydrating agent resulted in reduction in loading and percent encapsulated efficiency.
Abstract: Present study describes microencapsulation of eugenol using gelatin-sodium alginate complex coacervation. The effects of core to coat ratio and drying method on properties of the eugenol microcapsules were investigated. The eugenol microcapsules were evaluated for surface characteristics, micromeritic properties, oil loading and encapsulation efficiency. Eugenol microcapsules possessed good flow properties, thus improved handling. The scanning electron photomicrographs showed globular surface of microcapsules prepared with core: coat ratio1:1.The treatment with dehydrating agent isopropanol lead to shrinking of microcapsule wall with cracks on it. The percent oil loading and encapsulation efficiency increased with increase in core: coat ratio whereas treatment with dehydrating agent resulted in reduction in loading and percent encapsulation efficiency of eugenol microcapsules.
TL;DR: The results of the present study indicate that bacoside-A protects the brain from oxidative stress induced by morphine.
Abstract: In the present study, we investigated the protective effect of bacoside-A the active principle isolated from the plant Bacopa monniera against oxidative damage induced by morphine in rat brain. Morphine intoxicated rats received 10- 160 mg/kg b.w. of morphine hydrochloride intraperitoneally for 21 days. Bacoside-A pretreated rats were administered with bacoside-A (10 mg/kg b.w/day) orally, 2 h before the injection of morphine for 21 days. Pretreatment with bacoside-A has shown to possess a significant protective role against morphine induced brain oxidative damage in the antioxidant status (total reduced glutathione, superoxide dismutase, catalase, glutathione peroxidase and lipid peroxidation) and membrane bound ATP-ases(Na+/K+ ATPase. Ca2+ and Mg2+ ATPases) activities in rat. The results of the present study indicate that bacoside-A protects the brain from oxidative stress induced by morphine.
TL;DR: The methanolic extract of the seeds and 2,3,4-trihydroxytoluene showed antifungal activity against Aspergillus flavus, Candida albicans and Penicillium citrinium.
Abstract: Phytochemical investigation of the ethanolic extracts of the seeds of Carica papaya L. (Caricaceae) led to the isolation of 2,3,4-trihydroxytoluene (caricaphenyl triol) and glyceryl-1-(2',3',4'-trihydroxybenzoyl)-2,3-dioleate (papayaglyceride) as the new phytoconstituents along with the known components glyceryl-1-oleiyl-2,3-dilinoleiate, glyceryl-1-oleiyl-2,3-diarachidate, glyceryl-1-linoleiyl-2,3-distearate, carpaine, glyceryl-1,2-dipalmitate, glyceryl trimyristate, glyceryl tristearate, glyceryl-1,2-dipalmityl-3-myristate, glyceryl-1-oleiyl-2,3-dimyristate, β-sitosterol glucoside, glyceryl-1-oleiyl-3-phosphate, glyceryl-1-oleiyl-2-lauryl-3-phosphate and glyceryl-1,2-distearyl-3-phosphate. The structures of all these compounds have been elucidated by spectral data analysis and chemical reactions. The methanolic extract of the seeds and 2,3,4-trihydroxytoluene (200 μg/ml) showed antifungal activity against Aspergillus flavus, Candida albicans and Penicillium citrinium.
TL;DR: Season has significant effect on quality and quantity of thyme oil, as indicated by results of investigation of essential oil content and composition in different seasons.
Abstract: Thymus serpyllum L. grown in Kumaon region of Western Himalaya was investigated for essential oil content and composition in different seasons. The oils of fresh samples were obtained by hydrodistillation. The yield of essential oil (% v/w) during different seasons varied from 0.07 to 0.28% with the highest in summer season, at vegetative stage. The oils were analyzed by GC and GC-MS. Major components of all the samples were thymol (19.4-60.1%), γ-terpinene (0.3-13.8%) and p-cymene (3.5-10.4%). The results clearly indicated that season has significant effect on quality and quantity of thyme oil.
TL;DR: This study reveals that the ulcer preventive efficacy of andrographolide may probably due to its antioxidant, cytoprotective and antiacid secretory effects.
Abstract: The major objective of the study was to evaluate the gastroprotective property of andrographolide, a chief component of the leaves of Andrographis paniculata in terms of the ulcer preventive effect in rats. An acute toxicity test was conducted with different concentrations of andrographolide to determine the LD50 value. The dose responsive study was conducted in rats pretreated with andrographolide (1, 3 and 5 mg/kg) for a period of 30 days, prior to ulcer induction by administering ethanol, aspirin or by pyloric ligation. The ulcer protective efficacy was tested by determining the ulcer score, pH, pepsin, titrable acidity, gastric mucin, lipid peroxides, reduced glutathione, and enzymatic antioxidants superoxide dismutase, catalase and glutathione peroxidase in gastric tissue. The activities of H+-K+ ATPase and myeloperoxidase were also determined in gastric tissue. The LD50 value was found to be 48 mg/kg b. wt and the effective dose was found to be 3 mg/kg. We have observed a significant reduction in the ulcer score in rats pretreated with 3 mg of andrographolide/kg body weight. A favourable increase in the pH and decrease in titrable acidity were observed in the gastric fluid of rats pretreated with the test drug. The gastric tissue H+-K+ ATPase and myeloperoxidase activities were elevated in ulcer-induced animals. The elevation in the enzyme activity was significantly minimized in the andrographolide received animals. The antioxidants and mucin levels were significantly maintained in the gastric tissue of drug-pretreated animals. Andrographolide did not produce any toxic effects in normal rats. This study reveals that the ulcer preventive efficacy of andrographolide may probably due to its antioxidant, cytoprotective and antiacid secretory effects.
TL;DR: A new strategy for the synthesis of curcuminoids is described involving the reaction of acetylacetone difluroboronites with an aromatic aldehyde in the presence of n-butylamine as catalyst, resulting in new intermediate products that are stable and can be isolated and hydrolysed with aq.
Abstract: A new strategy for the synthesis of curcuminoids is described involving the reaction of acetylacetone difluroboronite with an aromatic aldehyde in the presence of n-butylamine as catalyst. The new intermediate products, curcuminoid difluroboronites, of symmetrically substituted curcuminoids like curcumin and bisdemethoxycurcumin are stable, can be isolated and hydrolysed with aq. methanol at pH 5.8 to get the curcuminoids of high purity. The method is applicable for unsymmetrical curcuminoids like demethoxycurcumin also with some modification involving column chromatography. The intermediate curcuminoid difluroboronites, as also the natural β-diketone pongamol difluroboronite, prepared for the first time were characterized on the basis of physical and chemical properties and spectroscopic data. The advantage of using borontrifluoride to protect the enol group in acetylacetone over the generally used boric oxide is brought out. The importance of conducting biological activity studies using pure curcuminoids is explained.
TL;DR: Pectin based in situ gels can be successfully used to prolong the duration of action of azithromycin and were proved to be safe and non irritant on rabbit eyes.
Abstract: Gelation of pectin caused by divalent cations especially calcium ions has been applied to develop an ophthalmic formulation of azithromycin in the present study. Rapid elimination of drug on instillation into cul de sac would be minimal with in situ gelling ophthalmic solution leading to increased precorneal contact time and prolonged drug delivery. In the formulation development studies pectin was used in different concentrations (1-5% w/v) and different proportions of the hydrocolloids hydroxypropyl methylcellulose and sodium carboxymethyl cellulose of different grades of viscosity were used. The primary criteria for formulation optimization were gelling capacity and rheological behaviour. In addition, formulations were evaluated for pH, and antimicrobial efficacy and drug release. The clarity, pH, gelation in simulated tear fluid and rheological properties of the optimized formulations were satisfactory. The formulations inhibited the growth of Staphylococcus aureus effectively in cup–plate method and were proved to be safe and non irritant on rabbit eyes. The results indicate that pectin based in situ gels can be successfully used to prolong the duration of action of azithromycin.
TL;DR: Concepts of vulnerable populations, therapeutic misconception and post trial access hold special importance in ethical conduct of research, especially in developing countries like India, where most of the research participants are uneducated and economically backward.
Abstract: Ethics in clinical research focuses largely on identifying and implementing the acceptable conditions for exposure of some individuals to risks and burdens for the benefit of society at large. Ethical guidelines for clinical research were formulated only after discovery of inhumane behaviour with participants during research experiments. The Nuremberg Code was the first international code laying ethical principles for clinical research. With increasing research all over, World Health Organization formulated guidelines in the form of Declaration of Helsinki in 1964. The US laid down its guidelines for ethical principles in the Belmont Report after discovery of the Tuskegee's Syphilis study. The Indian Council of Medical Research has laid down the 'Ethical Guidelines for Biomedical Research on Human Subjects' in the year 2000 which were revised in 2006. It gives twelve general principles to be followed by all biomedical researchers working in the country. The Ethics Committee stands as the bridge between the researcher and the ethical guidelines of the country. The basic responsibility of the Ethics Committee is to ensure an independent, competent and timely review of all ethical aspects of the project proposals received in order to safeguard the dignity, rights, safety and well-being of all actual or potential research participants. A well-documented informed consent process is the hallmark of any ethical research work. Informed consent respects individual's autonomy, to participate or not to participate in research. Concepts of vulnerable populations, therapeutic misconception and post trial access hold special importance in ethical conduct of research, especially in developing countries like India, where most of the research participants are uneducated and economically backward.
TL;DR: It was concluded that the concept of mixed hydrotropic solid dispersion is novel, safe and cost-effective technique for enhancing bioavailability of poorly water-soluble drugs by dissolving drug in nonionized form.
Abstract: Conventional furosemide tablets are practically insoluble in water, have slow onset of action (45-60 min) and poor bioavailability (39-53%), and therefore cannot be given in emergency clinical situations like hypertension or pulmonary edema. So purpose of research was to provide a fast dissolving oral dosage form of furosemide, which can provide quick onset of action by using concept of mixed hydrotropy. Initially solubility of furosemide was determined individually in 4 hydrotropic agents namely urea, sodium acetate, sodium benzoate, sodium citrate at concentration of 10, 20, 30 and 40% w/v solutions using purified water as solvent. Highest solubility was obtained in 40% sodium benzoate solution. Then different combinations of 2, 3 and 4 hydrotropic agents in different ratios were used to determine solubility, so that total concentration of hydrotropic agents was always 40%. Highest solubility was obtained in solution of urea+sodium benzoate+sodium citrate at optimum ratio of 15:20:5. This optimized combination was utilized in preparing solid dispersions by common solvent technique using distilled water as solvent. Solid dispersions were evaluated for flow properties, XRD, DSC, SEM and were also compressed to form tablets. Dissolution studies of conventional and prepared tablets were done using USP Type II apparatus. It was concluded that the concept of mixed hydrotropic solid dispersion is novel, safe and cost-effective technique for enhancing bioavailability of poorly water-soluble drugs by dissolving drug in nonionized form. The magical enhancement in solubility of furosemide is clear indication of its potential to be used in future for other poorly water-soluble drugs in which low bioavailability is major concern.
TL;DR: The proposed HPTLC method was found to be precise, specific and accurate for quantitative determination of L-DOPA and can be used for rapid screening of large germplasm collections of Mucuna pruriens for L- DOPA content.
Abstract: Mucuna pruriens Linn. is an important medicinal plant used for treatment of Parkinson's disease and many others in ancient Indian medical system. L-DOPA extracted from seeds of Mucuna is a constituent of more than 200 indigenous drug formulations and is more effective as drug than the synthetic counterpart. A densitometric high performance thin-layer chromatographic (HPTLC) method was developed for quantification of L-DOPA content present in the seeds extract. The method involves separation of L-DOPA on precoated silica gel 60 GF(254) HPTLC plates using a solvent system of n-butanol-acetic-acid-water (4:1:1, v/v) as the mobile phase. Quantification was done at 280 nm using absorbance reflectance mode. Linearity was found in the concentration range of 100 to 1000 ng/spot with the correlation coefficient value of 0.9980. The method was validated for accuracy, precision and repeatability. Mean recovery was 100.89%. The LOD and LOQ for L-DOPA determination were found to be 3.41 ng/spot and 10.35 ng/spot respectively. The proposed HPTLC method was found to be precise, specific and accurate for quantitative determination of L-DOPA. It can be used for rapid screening of large germplasm collections of Mucuna pruriens for L-DOPA content. The method was used to study variation in fifteen accessions of Mucuna germplasm collected from different geographical regions.
TL;DR: In this paper, an in vitro evaluation of the anti-microbial activity of medicated soaps was conducted using ditch-plate and hand washing techniques, and the most common antimicrobial active ingredients were triclosan, trichloroxylenol and trich chlorocarbanilide.
Abstract: An in vitro evaluation of the anti-microbial activity of medicated soaps was conducted using ditch-plate and hand washing techniques. Strains of reference microbes namely Candida albicans (ATCC90028), Staphylococcus aureus (ATCC25923), Pseudomonas aureginosa (ATCC27853) and Escherichia coli (ATCC25922) were tested at three different soaps' concentrations (1.0, 4.0 and 8.0 mg/ml). A total of 16 medicated soaps were assayed for their antimicrobial efficacy. Of these, 13 were medicated and 3 non-medicated soaps, which served as control. Ciprofloxacin and ketaconazole were employed as positive controls. Label disclosure for the soaps' ingredients and other relevant information were absorbed. The most common antimicrobial active ingredients were triclosan, trichloroxylenol and trichlorocarbanilide. ANOVA for means of zones of inhibition revealed variability of antimicrobial activity among the medicated soaps. Positive correlation (r=0.318; P<0.01) between zones of inhibition and soaps' concentrations was evidenced. Hand washing frequencies positively correlated with microbial counts. Roberts(®) soap exhibited the largest zone of inhibition (34 mm) on S. aureus. Candida albicans was the least susceptible microbe. Regency(®) and Dalan(®) exhibited the least zone of inhibition on the tested bacteria. Protex(®), Roberts(®), Family(®) and Protector(®) were equally effective (P<0.01) against S. aureus. In conclusion, majority of the assayed medicated soaps have satisfactory antibacterial activity; though lack antifungal effect with exception of Linda(®) liquid soap. The hand washing technique has proved to be inappropriate for evaluation of soaps' antimicrobial efficacy due to presence of the skin microflora.
TL;DR: The central core revolves around the applications of optical fibers in the medical and biomedical field and extending the use of the same in pharmaceutical industry as probes in quality control and dosage form analysis.
Abstract: The paper focuses on the introduction of fiber optics, a fusion of science and engineering and describes the materials generally used for its construction along with the procedure used to design the fibers. It gives an idea of the materials used for the construction along with the pros and cons associated with them and various factors governing the emission of ultraviolet, infrared or visible radiations. The central core revolves around the applications of optical fibers in the medical and biomedical field and extending the use of the same in pharmaceutical industry as probes in quality control and dosage form analysis.
TL;DR: Two triterpenoids, taraxerone and tricadenic acid A were isolated from the methanol extract of the outer bark of Schleichera oleosa available in Darjeeling foothills by means of chemical characterisation and IR, NMR spectral data.
Abstract: Two triterpenoids, taraxerone and tricadenic acid A were isolated from the methanol extract of the outer bark of Schleichera oleosa available in Darjeeling foothills. A preliminary study on their antimicrobial activities was also performed against some fungal and bacterial species. The structure of these compounds was determined by means of chemical characterisation and IR, NMR spectral data.