International Journal of Pharmaceutical Sciences and Drug Research

80-83

Authors: K. P. R. Chowdary*, Veeraiah Enturi

The objective of the study is to prepare, characterize and evaluate starch phosphate, a new modified starch as a carrier in solid dispersions for enhancing the dissolution rate of Efavirenz. The feasibility of formulating solid dispersions of Efavirenz in starch phosphate into compressed tablets with enhanced dissolution rate was also investigated. Starch phosphate was prepared by reacting starch with di-sodium hydrogen orthophosphate anhydrous at elevated temperatures. It was insoluble in water and has good swelling (400%) property without pasting or gelling when heated in water. Solid dispersions of Efavirenz in starch phosphate were prepared by solvent evaporation method employing various weight ratios of drug: starch phosphate such as 2:1(SD-1), 1:1(SD-2), 1:2(SD-3), 1:3(SD-4) and 1:9(SD-5) and were evaluated for dissolution rate and efficiency. All the solid dispersions prepared gave rapid and higher dissolution of Efavirenz when compared to pure drug. Dissolution followed first order kinetics. A 13.98 and 31.37 fold increase in the dissolution rate (K1) of Efavirenz was observed with solid dispersions SD-4 and SD-5 respectively. The DE30 was also increased from 10.66% in the case of Efavirenz pure drug to 51.13% and 71.51% in the case of these solid dispersions. Efavirenz (50 mg) tablets were prepared employing Efavirenz alone and its solid dispersions SD-3 and SD-4 by wet granulation method and were evaluated. Efavirenz tablets formulated employing its solid dispersions in starch phosphate gave rapid and higher dissolution rate and DE30 when compared to plain and commercial tablets. A 16.71 and 31.04 fold increase in the dissolution rate (K1) was observed with tablet formulations containing solid dispersions SD-3 and SD-4 respectively when compared to plain tablets.

89-96

Authors: Hanan M. Hassan1*, Amal M. El-Gayar1, Tarek M. Ibrahim2, Mohammed M. H. Al-Gayyar1

The aim of this study is to investigate the anti-inflammatory effects of simvastatin alone and in combination with aspirin, the most widely used analgesic, antipyretic and anti-inflammatory agent, and to evaluate the effect of using them in combination which may produce synergistic effect and lower the dose required for each agent. 72 Male Wistar albino rats suffering from air pouch granuloma were used. They were divided into 12 groups each comprising 6 rats, they received either simvastatin (20 mg/kg/day) or aspirin (25 mg/kg/day) or combined therapy (simvastatin & aspirin) for either 3 or 6 executive days. The control groups received the solvents only for the same periods. Biochemical markers of inflammation as serum tumor necrosis factor-α, interleukin-6 and interleukin-4 were measured by an Elisa method. Antioxidant activity was calorimetrically assessed by measuring serum nitric oxide concentration. Results indicated that treatment with simvastatin alone had no significant difference from treatment with aspirin alone which give solid ground for the predicted anti-inflammatory effects of simvastatin. Furthermore, our study demonstrated that treatment with the combined therapy reduced the extent of inflammation as compared to treatment with simvastatin alone or aspirin alone indicating that aspirin-simvastatin combination represents a synergistic combination concerning the immune response to the inflammatory challenge. The combination treatment with agents that inhibit different aspects of the signal transduction pathways will be transformational and have better efficacy with fewer side effects.

101-103

Authors: Dhaneshwar Shep1, Asmita Nimkar2, Rajen Shah2, Vijaya Jaiswal1*

The aim was to assess the comparative bioavailability of two formulations (200 mg tablet) of sodium valproate in healthy subjects. This open label randomized, two periods, two treatments, two sequence, 2-way crossover design study was conducted in 18 healthy Indian adult subjects. Subjects received sodium valproate 200 mg of either test or reference formulation with a washout period of 7 days. After study drug administration, serial blood samples were collected over a period of 60 hours. Plasma concentrations of Valproic acid were measured by pre-validated LC-MS-MS method. Pharmacokinetic (PK) parameters Cmax, Tmax, t1/2, AUC0-t, AUC 0-∞, and kel were determined for the 2 sodium valproate formulations. Cmax, AUC0-t, and AUC0-∞ were used to test for bioequivalence after log-transformation of plasma data. The formulations were to be considered bioequivalent if the log-transformed ratios of Cmax, AUC0-t, and AUC0-∞ were within the predetermined bioequivalence range of 80% to 125%. A total of 18 healthy subjects were enrolled. No significant differences were found based on analysis of variance, with mean values and 90% confidence intervals of test/reference ratios for these parameters as follows: Cmax, 15.64 versus 15.20μg/ml (90.79 to 115.45); AUC0-t, 72.71 versus 66.95μg.h/ml (96.03 to 124.87); and AUC0-∞, 105.65 versus 98.11μg.h/ml (94.61 to 124.75). In these healthy Indian subjects, results from the PK analysis suggested that the test and reference formulations of sodium valproate 200 mg tablets were bioequivalent. Both the formulations were well tolerated.

112-115

Authors: Javeed Ahmed Wani1*, Rajeshwara N. Achur1, R. K. Nema2

The plant Asparagus racemosus is widely distributed in the Himalayan and sub-Himalayan regions of India. Based on preliminary reports, there is a lot of interest in using the roots of this plant for treating sexual disorders. In this study, the hydro-alcoholic and aqueous extracts of the roots of Asparagus racemosus were subjected to preliminary phytochemical screening which showed the presence of saponins, carbohydrates, glycosides and mucilages. The total extracts were tested for their aphrodisiac activity in experimental rats. The hydro-alcoholic extract of Asparagus racemosus root at higher concentration (400 mg/kg body weight) showed significant aphrodisiac activity on male wistar albino rats as evidenced by an increase in number of mounts and mating performance. On the other hand, hydro-alcoholic extract at lower dose (200 mg/kg. body weight) and aqueous extract (400 mg/kg body weight) showed moderate aphrodisiac property. Thus, in experimental rats, the results of the present study suggest that the extracts of Asparagus racemosus exert significant aphrodisiac activity. Further, detailed studies are needed to know whether in-vivo administration of the extracts is beneficial for patients suffering from sexual disorders.

123-126

Authors: R. S. Sreenivasan1*, P. Krishna Moorthy2, M. Deecaraman3

The fresh water field crab, Spiralothelphusa hydrodroma is an important human food source in parts of South India and the crab is constantly exposed to pesticides, which are used extensively to control agricultural pests. Evaluation of the toxic effect of cypermethrin on the experimental crab for the LC₅₀ value was carried out. Effect of cypermethrin on the biochemical changes in the hepatopancreas and muscle was observed. Quantitative study of biochemical changes of acid phosphatase and alkaline phosphatase were undertaken.

130-136

Authors: Elhoussine derwich1*, Rachida Chabir2, Rachid Taouil3, Omar Senhaji3

The present study was to evaluate the in vitro antioxidant activity and chemical composition of essential oil of Mentha piperita from Morocco. Mentha species from the Lamiaceae family are widely distributed in Morocco and commonly used as herbal tea, flavoring agent and medicinal plant. In this stud y, the essential oils of Mentha piperita collected in the region of Meknes (Morocco) were obtained by hydro-distillation of the leaves and analysed by gas chromatography equipped with flame ionisation detector (GC-FID) and gas chromatography coupled to mass spectrometry system (GC/MS) for their chemical composition. The antioxidant activity of essential oils against DPPH radical was determined in vitro by treated with different concentrations of essential oil and vitamin C as standard antioxidant compound. The percentages of DPPH inhibition and IC50 were recorded. Thirty compounds were identified in leaves oil representing 58.61% of the total oil composition. The yield of essential oil of Mentha piperita was 1.02% and the major compound in the leaves was: Menthone (29.01%) followed by menthol (5.58%), menthyl acetate (3.34%), menthofuran (3.01%), 1,8-cineole (2.40%), isomenthone (2.12%), limonene (2.10%), α-pinene (1.56%), germacrene-D (1.50%), β-pinene (1.25%), sabinene (1.13%) and pulegone (1.12%). The radical scavenging activity (% inhibition) of the essential oil from Mentha piperita was the highest (81.09± 1.21%) at the concentration of 150µg/ml and the IC50 values of these plant extracts were 53.67µg/ml.

141-145

Authors: H. Saikia*, A. Lama

Dyslipidemia is major problem among population those have sedentary life style as well as in diabetics. Bougainvillea spectabilis is most commonly found in India as an ornamental plant and has got anti-diabetic action due to presence of one insulin mimicking agent D-pinitol (3-O-methyl-chiroinositol). The present investigation was undertaken to evaluate the effect of alcoholic extract of leaves of Bougainvillea spectabilis (AEBSL) on serum lipid profile in albino rats fed with high fat diet (HFD) and to compare it with a standard hypolipidaemic drug simvastatin. Thirty healthy albino rats of both sexes (100-200 g) were randomized into 5 groups of 6 animals each. The groups were treated as follows: Group A: normal diet (ND); Group B: HFD (vanaspati ghee + coconut oil mixture in ratio of 3:2 at 10 ml/kg/day); Group C: HFD+ AEBSL (100 mg/kg/day); Group D: HFD + AEBSL (200 mg/kg/day); Group E: HFD + simvastatin (1.8 mg/kg/day). Lipid profile was estimated after 8 weeks of treatment. AEBSL showed a significant (p<0.01) reduction in total cholesterol (TC), Triglyceride (TG), Low density lipoprotein (LDL), Very low density lipoprotein (VLDL) levels and significant (p<0.01) increase in high density lipoproteins (HDL) in hypercholesteromic rats (Group C and Group D). AEBSL 200 mg/kg/day found to be more effective than AEBSL 100 mg/kg/day. There is also significant improvement in atherogenic index (p<0.01) and increases the percentage of protection AEBSL treated animals. Alcoholic extract of leaves of Bougainvillea spectabilis leaves have excellent lipid lowering potentiality.

150-154

Authors: Manmohan Singhal1*, Arindam Paul2, Hemendra Pratap Singh3, Sushil Kumar Dubey1, Rajendra K. Songara1

In present study, a series of chalconesemicarbazones was synthesized and evaluated for antioxidant activity by DPPH free radical scavenging assay. Most of the compounds were found to be potent antioxidant. Free radicals play an important role in various pathological and xenotoxic effects so antioxidant may have protective role in these pathological conditions. Based on the results of an anti-oxidant study, Compound 23 was the most active compound. The highest scavenger activity observed in compound 23 is probably due to the presence of hydroxyl group in the acetophenic moiety and methoxy group in aldehydic moiety of chalcone. It was found that methoxy and hydroxyl substituted chalconesemicarbazones were potent nitric oxide scavenger and unsubstituted compound showed very less activity.

158-161

Authors: Sandeep Goyal1*, Suresh Kumar2

Pulsatilla nigricans Linn. (Ranunculaceae) has been traditionally used in the treatment of nervousness, restlessness, ovaritis, ovaralgia, pain associated with debility and due to acute inflammation, uterine affections, acute meningitis, and as taeniafuge, but no work has ever been carried out for standardizing this potential plant. The present investigation establishes histological characters, micrometric determinations and physicochemical parameters for P. nigricans. Transverse sections of stem of P. nigricans showed outermost layer consists of a single layer of tangentially elongated epidermal cells, narrow zone of sclerenchymatous cells, i.e., hypodermis followed by continuous mass of thin walled, parenchymatous cells, of cortex, collateral and closed vascular bundles, lie scattered in the ground tissue towards periphery than at the centre and followed by pith comprising parenchymatous cells with large intracellular spaces. The powdered aerial parts of P. nigricans showed presence of anomocytic stomata, unicellular covering trichomes, pericyclic fibres, lignified spiral vessels and clusters of calcium oxalate crystals. Foreign organic matter content of air dried aerial parts of P. nigricans was found to be 0.38%. Moisture content of air dried aerial parts of P. nigricans was found to be 17%. The total ash was about 15 times more than the acid insoluble ash in P. nigricans whereas water soluble ash was about 2 times less than total ash in P. nigricans. Water-soluble extractive value of P. nigricans was found to be about 18 and 2 times, respectively, in comparison to petroleum ether- and ethanol-soluble extractive value. Petroleum ether extract showed seven spots using hexane : ethyl acetate (17 : 3) as the mobile phase whereas TLC of chloroform extract showed nine spots for P. nigricans using toluene: ethyl acetate: glacial acetic acid (85:15:1) as the mobile phase, employing 0.5% anisaldehyde as the visualizing agent. Phytochemical screening of P. nigricans showed presence of steroids, flavonoids, tannins, and carbohydrates.