Volume 2 (2011) - Issue 10, October
Nanoemulsions are submicron sized emulsions that are under investigation as drug carriers for improving the delivery of therapeutic agents. These are the thermodynamically stable isotropic system in which two immiscible liquids are mixed to form a single phase by means of appropriate surfactant and cosurfactant. Nanoemulsion droplet sizes fall typically in the range of 20-200nm and shows narrow si...
G protein-coupled receptors (GPCRs), also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), comprise a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. GPCRs are involved in a wide ...
Most of the drugs in the developmental pipeline are emerging from the High-Throughput Screening methodology resulting in increased molecular weights and thus consequential bioavailability problems. The bioavailability issue can be due to insufficient solubility of permeability. Most compounds face the solubility problems. Hence, with the advancement of chemical science, the need of development of ...
The control of cancer, the second largest cause of death in the world, may benefit from the potential that resides in alternative therapies. The primary carcinogens stem from a variety of agricultural, industrial, and dietary factors. A number of natural products have been implicated as anticancer agents. Many anticancer molecules such as vincristine, vinblastine, combretastatins, taxol, podophyll...
ROLE OF BIOINFORMATICS, CHEMOINFORMATICS AND PROTEOMIC IN BIOMARKER IDENTIFICATION AND DRUG TARGET VALIDATION IN DRUG DISCOVERY PROCESSES
Novel biomarker identification and drug target validation are highly complex and resource-intensive processes, requiring an integral use of various tools, approaches and information. The recently developed proteomic technology features high-throughput parallel analysis of thousands of proteins in individual patients and amount populations and thus opens up the possibility of providing more details...
Bi-layer tablets have been developed to achieve controlled delivery of different drugs with pre-defined release profiles. In the last decade, interest in developing a combination of two or more Active Pharmaceutical Ingredients (API) in a single dosage form (bilayer tablet) has increased in the pharmaceutical industry, promoting patient convenience and compliance. Bilayer tablets can be a primary ...
Now a days, various routes of administration have been explored for the effective delivery of the drug to the target site. The oral route is considered to be most convenient for the administration of drugs to patients. But it has a serious drawback in conditions where localized delivery of the drug in the colon is required. Colon target aimed mainly because of less enzymatic activity, longer tra...
A number of 2-amino-4-(2', 5'-dimethyl-3'-furyl)-6-(aryl)-pyrimidines 4(a-n) have been synthesized by treating the 1-(2', 5'-dimethyl-3'-furyl)-3-(aryl)-2-propen-1-one (3a-n) with guanidine hydrochloride in presence of potassium hydroxide and ethanol. All these compounds were characterized by means of their IR, 1H NMR spectroscopic data and microanalyses. When these compounds were evaluated for an...
HECKEL AND KAWAKITA ANALYSES OF GRANULES OF THE CRUDE LEAVES EXTRACT OF VERNONIA GALAMENSIS PREPARED USING GELATIN AS BINDER
The powdered leaf of Vernonia galamensis (Asteraceae) is a herbal drug used in the treatment of diabetes mellitus in folk medicine in northern Nigeria. The crude aqueous extract of the leaves is deliquescent and usually stored in airtight desiccators. Efforts to use common diluents such as lactose, starch, and magnesium carbonate for tablet formulation of the extract produced tablets with defects ...
There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, anti-inflammatory, anti platelet, anti malarial, antimicrobial, anti-mycobacterial, anti-tumoral, vasodilator, anti-viral and anti-chistosomiasis activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development....
The present study was conducted to assess the anti-inflammatory, analgesic and cytotoxic properties of 50% ethanol extract of the stem bark of Terminalia arjuna plant on laboratory animal. In vitro cytotoxicity test was studied by Brine Shrimp Lethality Bioassay and results illustrated significant (p<0.05) cytotoxicity against A. salina, that were expressed as LC50. Terminalia arjuna et...
ANTI-ULCER PROPERTIES OF ALKALOIDS ISOLATED FROM THE FRUIT PULP OF CUCUMIS METULIFEROUS (CURCURBITACEAE)
Anti-ulcer properties of the alkaloids isolated from the fruit of Cucumis metuliferous was investigated in mice. Ethanol-induced gastric lesion was used to assess the anti-ulcer activity. In this study, there was a significant (p<0.05) decrease in haemorrhages and ulcerations of the gastric mucosa at 500 and 1000 mg/kg of the alkaloid compared with control. The activity of the extract is compar...
NOVEL METHODS FOR THE VISIBLE SPECTROPHOTOMETRIC DETERMINATION OF PIPAZETHATE HCl AND CHLORPHENOXAMINE HCl IN PURE AND TABLET DOSAGE FORMS
Three rapid, simple, precise and sensitive visible spectrophotometric methods (A-C) have been developed for the determination of pipazethate hydrochloride (PZ-HCl) and Chlorphenoxamine hydrochloride (CPA-HCl) in pure and Tablet Dosage Forms. Both methods (A-C) involves the formation of intense yellow ion-association complex between drug(s) and either of picric acid (PA) or phenol red (PR) or chlor...
In the present study a series of chalcone- semicarbazones was synthesized and evaluated for their antibacterial activity by paper disk diffusion method. Based on the results of an antibacterial study, compound 28 was the most active compound against gram negative bacteria. Synthesized compounds were inactive against gram positive bacteria. It was found that chloro- substitution in the aldehydic mo...
ASSESSMENT OF CYTOTOXICITY AND ANTIBACTERIAL ACTIVITIES OF ETHANOLIC EXTRACTS OF KALANCHOE PINNATA LINN. (FAMILY: CRASSULACEAE) LEAVES AND STEMS
Objective: In the present work, the leaves and stems of Kalanchoe pinnata Linn. (Family: Crassulaceae) have been investigated for screening phytochemicals, cytotoxicity and antibacterial activities. Materials and methods: Brine shrimp lethality (BSL) bioassay was used as a pre-screening method for cytotoxic effect. Ethanolic extract of the plant was tested by using this method. The agar disc di...
Five Indian Brands (coded as A,B,C,D,E) of 100 mg Nimesulide tablets were evaluated for various In vitro parameters, i.e. size and shape, uniformity of weight, hardness, friability, content, disintegration time and dissolution profile. All the products met the requirements of British Pharmacopoeia for tablet formulation. The hardness of all the brands was found to be in the range of 4.2-4.4 kg, wh...
Primary spinal cord presentation of Primitive neuroectodermal tumors (PNET) is a rare occurrence and carries poor prognosis. A 13-year-old boy presented with pain in neck region, bilateral upper and lower limb weakness and bladder and bowel dysfunction. Neurological examination revealed the marked paresis with hyporeflexia of both the upper and lower extremities. Preoperative MRI of spine revealed...
The free radical scavenging potential of blue green algae spirulina platensis (Oscillatoriaceae) was studied by different antioxidant models. Free radicals are implicated for more than 80 diseases including Diabetes mellitus, arthritis, cancer, ageing etc. In the treatment of theses diseases, antioxidant therapy has gained an utmost importance. Current research is directed towards finding naturall...
SYNTHESIS, EXPERIMENTAL STUDIES OF THE ANTIMICROBIAL POTENTIAL OF SOME NOVEL 1, 5- BENZO THIAZEPINE DERIVATIVES
Optically active 1, 5- benzothiazepines belong to the well known benzothiazepine type substances. Some of them possess important bioactivities. In this article, optically active 2, 3-dihydro-1, 5-benzothiazepine derivatives are synthesized by the reaction of new α-β unsaturated carbonyl compounds with 2-aminothiophenol under mild conditions in the presence of silver sulphate in acetonitrile in s...
The purpose of the study was to improve the physicochemical properties of Mesalamine like solubility and dissolution rate by forming solid dispersions with sodium lauryl sulphate (SLS) and Urea (UR) as water-soluble carriers. The solid dispersion of Mesalamine by kneading method were prepared using 1:1, 1:2 and 1:3 ratios of drug to polymer using methanol as solvent. Characterization of Mesalamine...
DEVELOPMENT OF INTEGRATED INDUSTRIAL PROCESS LAYOUT DESIGN FOR THE PRODUCTION AND QUALITY CONTROL FACILITY OF VARIOUS PHARMACEUTICAL FORMULATIONS
Objectives: To develop an integrated industrial production and quality control layout which facilitates the pharmaceutical industries for manufacturing, controlling quality of various types of pharmaceutical formulations in a single production unit. Methods: For designing the integrated process layout for the production and quality control, different operations and their sequences involved in t...
Caesalpinia pulcherrima (Linn.) Popularly known as Peacock flower in India belongs to family Caesalpiniace. The objective of the present work was to evaluate the in-vitro antimicrobial potency of the ethanolic and aqueous extract of Caesalpinia pulcherrima (Linn.) flower (CPF) using agar plate disk diffusion method against Escherichia coli, bacillus subtilis and streptococcus aureus. Cephalosporin...
Plants have traditionally provided a source of hope for novel drug compounds, as plant herbal mixtures have made large contributions to human health and well-being. We report in this work for the first time, the potent antibacterial activity of Punica granatum and its wild form daru. Ethanol, petroleum ether and distilled water extract of fruit’s white membrane were screened for in vitro activit...
The objective of present study is to evaluate the anti ulcer activity of ethanol extract of leaves of Heliotropium indicum. The ethanol extract of H. indicum was investigated for its anti ulcer activity against Aspirin plus pylorus ligation induced gastric ulcer in rats, HCl –Ethanol induced ulcer in mice and water immersion stress induced ulcer in rats. The antiulcer activity was assessed by de...
A SIMPLE UV SPECTROPHOTOMETRIC METHOD FOR THE DETERMINATION OF FEBUXOSTAT IN BULK AND PHARMACEUTICAL FORMULATIONS
A simple and cost effective spectrophotometric method is described for the determination of febuxostat in pure form and in pharmaceutical formulations. The drug was highly soluble in methanol so it was selected as the solvent system for the drug. This ensured adequate drug solubility and maximum assay sensitivity. The linearity range for febuxostat at its wavelength of detection of 315 nm was obta...
PROTECTIVE EFFECT OF COCCINIA INDICA LEAF EXTRACT AGAINST ALCOHOL COMBINED WITH CARBON TETRACHLORIDE AND PARACETAMOL INDUCED LIVER DAMAGE IN RATS
Liver is a major metabolic organ affected by various toxins and chemicals. So the potential therapeutic agent is needed for the treatment of liver diseases. Natural products are the best source of remedies for the treatment of all diseases.The aim of our study was to investigate the effect of leaf extract of Coccinia indica against Alcohol combines with CCl4 and Paracetamol induced hepatotox...
Eclipta prostrata Linn. (Asteraceae) popularly known as "Bhringaraj" is a very useful medicinal plant in India. The aim of the present study is to evaluate the anti-inflammatory activity of ethanolic extract of leaves of Eclipta prostrata. The anti-inflammatory effects were investigated by employing acute inflammatory model; Carrageenan induced paw edema and Sub-acute inflammatory model; formalin ...
Zidovudine is the first approved compound for the treatment of HIV; however the main limitation to therapeutic effectiveness of Zidovudine is its dose dependent toxicity, short biological half-life and poor bioavailability. Thus, to overcome the problem the gastroretentive floating drug delivery system is developed. Floating drug delivery system is a low density system which have capacity to remai...
CHOLESTEROL ESTERASE ENZYME INHIBITORY AND ANTIOXIDANT ACTIVITIES OF LEAVES OF CAMELLIA SINENSIS (L.) KUNTZE. USING IN VITRO MODELS
The present study was to evaluate the in vitro cholesterol esterase enzyme inhibitory and in vitro antioxidant activity of the methanol extract of the leaves of Camellia sinensis (L.). Phytochemical screening of the extract shows the presence of flavonoids, phenolics and terpenoids. The extract shows ability to inhibit the enzyme with IC50 (82.46±0.74µg/ml) whereas that of standard, Orlistat (...
AN APPROACH FOR ENHANCEMENT OF DISSOLUTION RATE OF PIOGLITAZONE HCL BY SOLID DISPERSION TECHNIQUE USING PEG 6000
Pioglitazone hydrochloride is a novel antidiabetic drug in thiazolidinediones group and it improves insulin sensitivity in insulin resistant patients. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. The present study is an approach to enhance the dissolution rate of pioglitazone HCl by preparing...
In order to have a good coordination between the quality of raw materials, in process materials and the final products, it has become essential to develop reliable, specific and sensitive quality control methods using a combination of classical and modern instrumental method of analysis. Standardization is an essential measurement for ensuring the quality control of the herbal drugs. “Standard...
Chonemorpha grandiflora, (Roth) M.R. and S.M. Almeida syn C. fragrans (Moon), Alston (Apocynaceae) has been included in the list of an endangered medicinal plants. It is used in medicinal preparations like kumaryasavam and sudarsanasavum used as tonic3. Entire plant, roots and root bark are used for fever and stomach disorders. The plant is useful in treatment of skin diseases and inflammations....
Context: The leaves of Nyctanthes arbor-trisitis (Linn.) are used in Traditional System of Medicine for the treatment of stomachic, carminative, intestinal astringent, expectorant, biliousness piles, hair tonic and wound healing. Objective: To evaluate wound healing activity of Nyctanthes arbor-trisitis (Linn.) Material & Methods: Extracts from the dried leaves of Nyctanthes arbor-trisitis ...
INVESTIGATION ON REGIONAL VARIATION IN TOTAL PHENOLIC, ALKALOID CONTENT AND IN-VITRO ANTIOXIDANT ACTIVITY OF LEUCAS ASPERA
In this study, we investigated and compared the total phenolic, alkaloid content and in-vitro antioxidant activity of Leucas aspera collected from four different regions; Tirupathi (Southern zone), Lam (Krishna river region), Jagityala (Northern Telangana) and Hyderabad (Southern Telangana) of Andhra Pradesh, India. Quantitative regional variation was observed in total phenolic content, and alka...
Trigonella foenum graecum, (Fenugreek) (Family: Leguminosae) is used as a traditional medicine for anti-inflammatory, antiseptic, antidiabetic and antilipidemic. Hydroalcoholic extract of its seeds were subjected for in vitro antioxidant activity by different methods viz, 1- diphenylpicryl- hydrazyl radical (DPPH), hydroxyl, and ABTS radical cation assay. Total antioxidant capacity, Total phen...
A new, simple, safe, accurate and reproducible spectrophotometric analytical method was developed for the quantitative estimation of gatifloxacin in solid dosage form by mixed hydrotropic agents. The enhancement of solubility of drug gatifloxacin was more than 15 fold in mixed hydrotropic solution (20% N,N dimethyl urea and 20% sodium citrate solution) as compared to solubility in distilled wate...
Aim of the study: Now a days due to the hammering of movies and fashion most of the people specifically age group between 18 to 30 years, are diverted more to have the protein supplements in excess for getting good physique and well toned body shape. The people suppose to eat more calcium, vitamins and some steroids with intension that they will get done the things too fast. Without been having go...
BIOEQUIVALENCE STUDY OF FIXED DOSE COMBINATION TABLET CONTAINING LORNOXICAM AND THIOCOLCHICOSIDE IN HEALTHY SUBJECTS
The study was designed to determine the relative bioavailability of two sustained release Fixed dose combination (FDC) products of two manufacturers containing Lornoxicam [CAS No. 70374-39-9] 8mg and Thiocolchicoside [CAS No. 602-41-5] 8mg in 24 healthy male volunteers. The pharmacokinetics of Lornoxicam and Thiocolchicoside individually after oral administration of tablet formulation has been ext...
Zymodyne Syrup is poly herbal formulation made by Ayrulab Herbals Pvt. Ltd., as an appetite enhancer. This formulation contains various 17 plant extract from these 6 plants namely Cyperus rotundus, Bacopa monnieri, Glycyrrhiza glabra, Phyllanthus amarus, Asparagus racemosus, and Tribulus terrestris contains Quercetin flavonoid as a chemical constitute and it can be determined by HPTLC method. Th...
To determine the anticonvulsant activity of the leaf extract of Erythrina Indica in mice and rats, and in order to verify the traditional use of the plant in the treatment of epilepsy. The pentyleneterazole (PTZ) and the maximal electroshock seizure (MES) models were used for assessing the anticonvulsant effects of the chloroform leaf extract in mice and rats. The chloroform extract (500 mg/kg p.o...
The present study was undertaken to determine the anti-ulcer potential of Calamintha officinalis Moench, a standardized oil of Calamintha officinalis Moench, commonly known as Calamint. Effect of various doses (0.4ml/kg and 0.8ml/kg,) of Calamintha officinalis Moench. oil was studied on gastric ulcers in pylorus ligation, Diclofenac sodium induced gastric mucosal injury in rats. Anti-ulcer activit...
Aim: Primary urinary bladder adenocarcinoma is a rare entity. This is a clinical case presentation with review of the literature on this topic. Primary adenocarcinoma of the urinary bladder has shown a poor response to radiation or chemotherapy individually. Therefore, combination chemotherapy with radical EBRT is the effective therapeutic approach for inoperable cases. Method: A 58 year o...
The aim of present study is to develop a delayed release pellets dosage form of duloxetine hydrochloride with a suitable polymer by using suspension layered method. Drug loaded nuclei was prepared using suspension layered technique in a Fluidized Bed Processor, the nuclei was coated with an acid resistant acrylic polymer (Eudragit L30-D55) and compared acid resistant properties with HPMC phthalate...
CONTROLLED RELEASE OF AN ANTI- EMETIC AGENT FROM A POLYMERIC MATRIX: FORMULATION AND IN- VITRO STUDY
The objective of the present study was to develop once daily controlled-release matrix tablets of Domperidone Maleate, an anti- emetic agent. Several formulations containing an anti- emetic agent (domperidone maleate) and hydrophilic polymers (Hydroxypropyl methylcellulose, Carbopol and Polyethylene oxide) were prepared by wet granulation methods. The tablets were subjected to thickness, diameter,...
The different extracts of the roots of Caesalpinia Bondue (Family- Fabeaccae) were tested for anti-diabetic activity, by glucose tolerance test in normal rats and alloxan induced diabetic rats. Aqueous ethanol and chloroform extracts had shown significant protection and lowered the blood glucose levels to normal in glucose tolerance test. In alloxan induced diabetic rats the maximum reduction in b...
Diabetes is a chronic metabolic disorder characterized by altered carbohydrates, fat and protein metabolism, and an increased risk of vascular complications. Swiss albino mice weighing 20-25g and albino rats (Wistar strain) weighing 170-190g of either sex were used for the studies. Mice used for toxicity and rats for anti-diabetic study. The aqueous roots extract of Murva was found to be safe at a...