International Journal of Pharmaceutical Sciences and Drug Research

88-96

Authors: Izhar Ahmed Syed, E. Pavani

The “Liquisolid” technique is a novel and capable addition towards such an aims for solubility enhancement and dissolution improvement, thereby it increases the bioavailability. It contains liquid medications in powdered form. This technique is an efficient method for formulating water insoluble and water soluble drugs. This technique is based upon the admixture of drug loaded solutions with appropriate carrier and coating materials. The use of non-volatile solvent causes improved wettability and ensures molecular dispersion of drug in the formulation and leads to enhance solubility. By using hydrophobic carriers (non-volatile solvents) one can modify release (sustained release) of drugs by this technique. Liquisolid system is characterized by flow behavior, wettability, powder bed hydrophilicity, saturation solubility, drug content, differential scanning calorimetry, Fourier transform infra red spectroscopy, powder X-ray diffraction, scanning electron microscopy, in-vitro release and in-vivo evaluation. By using this technique, solubility and dissolution rate can be improved, sustained drug delivery systems be developed for the water soluble drugs.

105-109

Authors: Nikhil Omer1, Ankur Rohilla1*, Seema Rohilla2, Ashok Kushnoor1

Nitric oxide (NO), a free radical, possesses various modulatory effects on biological systems. NO is synthesized from L-arginine by converting it to L-citrulline via nitric oxide synthase (NOS) enzymes. Moreover, various precursors of NO have been reported that include arginine, citruline, arginine alphaketoglutarate (A-AKG) and arginineketoisocaproate (A-KIC). NO possess various direct and indirect effects that broadly affect various tissues and organ systems inside the body. The present review article aims to discuss about the pharmacology, physiological roles and effects of NO.

115-122

Authors: Yaswanth Allamneni1*, B V V K Reddy2, P Dayananda Chary1, Venkata Balakrishna Rao N1, S Chaitanya Kumar1, Arun Kumar Kalekar1

The objective of the present investigation was to design mucoadhesive microspheres to achieve a substantial increase in length of stay of the drug in the GI tract of glipizide for treatment of type 2 diabetes mellitus. Glipizide is a second-generation sulfonylurea derivative used for the treatment of type II diabetes. Its short biological half-life (0.3 ± 0.7 h) necessitates the need to be administered in two or three doses of 2.5-10 mg per day. Mucoadhesive microsphere exhibit a prolonged residence time at the site of application and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved or better therapeutic performance of drug. It would, therefore be advantageous to have means for providing an intimate contact of the drug delivery system with the absorbing membranes. In the present study, alginate based mucoadhesive microspheres of were prepared by ionotropic external gelation technique utilizing calcium chloride (CaCl2) as a cross linking agent, to take the advantage of swelling and mucoadhesive property of alginate beads for improving the oral delivery of glipizide. Interaction studies performed using FTIR spectroscopy and DSC revealed that there was no drug to polymer interactions. The prepared microspheres are discrete, spherical and free flowing which was characterized by entrapment efficiency, particle size, micromeritic properties, in-vitro release behavior, scanning electron microscopy (SEM), in-vitro wash off test etc. Depending upon the variability in the concentration of sodium alginate, time of cross linking agent, the factors like particle size, and incorporation efficiency and release rate and mucoadhesion properties of microspheres varies. It was observed that increasing the polymer concentration along with the cross-linking time given the better affect on microspheres characteristic and percentage release of drug. Formulation F8 containing 5% w/v sodium alginate was selected as best formulation by considering its better % drug entrapment [84.31%] and flow properties [Carr’s index (8.204), angle of repose (31.15)].

126-129

Authors: Sashank Srivastava*, P. H. Pathak

Garlic is an ayurvedic herb that has been extensively used as medication and as the taste enhancer of the food. The present investigation was undertaken to provide data on the efficacy of garlic (Allium sativum Linn.) extract on glycogen deposition and protein metabolism in female albino rats that may further explore medicinal potential of garlic. The rats were divided into four groups A, B, C and D, keeping group A as a healthy control. The garlic extract was tried in three different doses, 1ml, 2ml and 4ml/ kg body weight as low, medium and high dose respectively and given orally for the period of 7, 14, 21 and 28 days daily to the rats of group B, C and D as stated above. The significant (P<0.01 & P<0.05) increase in glycogen and protein level was observed when rats were fed with low and medium dose but when rats were fed with high dose of garlic extract there was significant (P<0.01) decrease in glycogen level and a not significant decrease in protein level was observed.

134-136

Authors: G B Talagadadeevi, B R Vancha, S Anusuri, M. Rao. Jampani*

The process for the preparation of antibacterial compound 4-amino-N-(5-methyl-1, 3, 4-thiadiazol-2-yl)benzenesulfonamide (Sulfamethizole) 4 involves the reaction of 2-amino-5-methyl-1, 3, 4-thiadiazole 1 with 4-acetamidobenzenesulfonyl chloride 2 followed by alkaline hydrolysis of the intermediate N-{4-[(5-methyl-1, 3, 4-thiadiazol-2-yl)sulfamoyl]phenyl}acetamide 3. The HPLC analysis of sulfamethizole showed the formation of an impurity which was isolated and identified as N-[4-({4-[(5-methyl-1, 3, 4-thiadiazol-2-yl) sulfamoyl] phenyl} sulfamoyl) phenyl] amine 6. This impurity is the result of the reaction of unreacted sulfonyl chloride 2 with sulfamethizole to form N-[4-({4-[(5-methyl-1, 3, 4-thiadiazol-2-yl)sulfamoyl]phenyl}sulfamoyl)phenyl]acetamide 5 followed by alkaline hydrolysis of the acetamido group. The structure was further confirmed by independent synthesis.

140-142

Authors: Krishna Kumar HN*, Rakshitha HR, Navyashree SN, Jyoti Bala Chauhan

In the present study, antioxidant activities of aqueous and methanolic fruit extracts of Pritchardia arecina were investigated. The antioxidant properties of the extracts were assessed using 1, 1,-diphenyl-2-picryl-hydrazyl (DPPH) assay and reducing power assay. Both the extracts exhibited significant reducing power which was dose dependent. The IC50 value in DPPH assay was found to be 18 and 27µg/ml for methanolic and aqueous extract respectively. Phytochemical analysis revealed the presence of tannins, steroids, amino acids and carbohydrates. The total phenolic content observed for aqueous and methanolic extracts were 25 and 40 mg gallic acid equivalent per gram of extract respectively.

147-149

Authors: Shilpa K, Harish Chandra R*, Krishnaveni B

Crinum defixum Ker-Gawl is a bulbous herb which has a wide geographical distribution in India. It is commonly called Bon-naharu (meaning wild garlic) in Assam. Traditionally the bulb has been reported to have nauseant, emetic, emollient, diaphoretic properties and it is also used in various inflammatory conditions. The anti-inflammatory activity of the bulbs of the plants has been investigated in the present study in order to establish its traditional claims. The ethyl acetate, chloroform and ethanol extracts of bulbs of Crinum defixum were screened for anti-inflammatory activity by using carrageenan induced rat paw edema method. The study revealed that the ethyl acetate extract of the plant had significant anti-inflammatory activity than the chloroform and ethanol extracts. The study supports the ethanomedicinal use of this plant for inflammatory conditions.

154-156

Authors: Vaisakh M N*, Pandey A

The aim of the study was to evaluate the effect of different permeation enhancers in the transdermal permeation of flavonoids. A weed plant named Chromolaena odorata have been employed as the flavonoid source. Six different cream formulations have been prepared with the Chromolaena extract using different permeation enhancers such as ethanol, dimethyl sulphoxide, surfactants and occlusive agents. The amount of flavonoids penetrated during a time period of four hours was noted. The highest amount of penetration was obtained with the formulation no 6 which contained a combination of different permeation enhancers. The result suggests that a synergistic combination of different permeation enhancers can be adopted for enhancement of permeation of flavonoids in topical drug delivery systems.

160-163

Authors: M. T. Harde*, S. B. Jadhav, D. L. Dharam, P. D. Chaudhari

Development and validation of two simple, accurate, precise and economical UV Spectrophotometric methods for simultaneous estimation of Thiocolchicoside and Dexketoprofen in bulk and in tablet dosage form. The methods employed were Method-1 Absorbance correction method and Method-2 First order derivative spectroscopic method. In method-1 Absorbance is measured at two wavelengths 370nm at which Dexketoprofen has no absorbance and 255nm at which both the drug have considerable absorbance. In method-2, two wavelengths 232nm for Thiocolchicoside (zero cross for Dexketoprofen) and 242nm for Dexketoprofen (zero cross for Thiocolchicoside) were selected. The beers law obeyed in the concentration range 4-40µg/ml and 5-50µg/ml for Thiocolchicoside and Dexketoprofen respectively in methanol. The suggested method is validated by using ICH validation parameters like accuracy, precision, linearity, LOD and LOQ respectively. Recovery study values of Thiocolchicoside and Dexketoprofen was found 99.8% and 100.2% respectively for both the methods. Standard deviation and RSD for intra-day and inter-day precision studies was found to be less than ± 2. The linearity coefficient was found 0.9996 at 242nm and 0.999 at 255 nm for Dexketoprofen and 0.9997 at both 232nm and 370nm for Thiocolchicoside. The LOD and LOQ for Method-1 were found to be 0.0067μg/ml and 0.020μg/ml for Thiocolchicoside, 0.043μg/ml and 0.132μg/ml for Dexketoprofen and for Method-2 were found to be 0.0093μg/ml and 0.028μg/ml for Thiocolchicoside, 0.055μg/ml and 0.168μg/ml for Dexketoprofen respectively. The developed methods were successfully applied to estimate the amount of Thiocolchicoside and Dexketoprofen in bulk and tablet dosage form.