Pharmaceutical Sciences
Volume:17 Issue: 1, 2011

One of the modification methods of flowability and compressibility of excipients for using in direct compression is changing in particles shape with crystallization using quasi-emulsion solvent diffusion. The aim of this research is to identify of effectiveness of quasi emulsion solvent diffusion (QESD) method in modification of mannitol compressibility. Firstly, mannitol was dissolved in distilled water at 80°C. The solution was then kept cool until 55°C. After that, ethanol was gradually added to the solution. The precipitated crystals were collected by drying. Floweability, SEM, DSC and X-ray powder diffraction of precipitated crystals was measured. Finally an equal amount of naproxen and excipients was prepared as direct compression tablets and then hardness, tensile strength and friability of tablets were measured. Flowability of mannitol was almost treated by QESD method. Bulk and tapped density of mannitol decreased; meanwhile increase in particle size was observed. The results of SEM demonstrated that primary particles of mannitol were broken in this method and were stuck together to produce very big particles that are not spherical. Tablets produced from treated mannitol had higher hardness and tensile strength than primary mannitol and they were measured 5.1 Kg± 0.72 and 0.16 Kg/mm2 ±0.0001, respectively. Spherical crystallization via QESD was useful method for changing compressibility mannitol characteristics so that tablets had suitable tensile strength. However this method had a few effect on flowability.

Epilepsy is one of the most common neurological conditions. Though there are many therapeutic strategies for epilepsy but most of these treatment modalities have been relatively successful in suppressing seizures. Ghrelin, a gastric peptide with key action on food intake, has been recently recognized as a potential anticonvulsant agent. In the present study, we investigated the effect of acute and chronic injection of ghrelin on pentylenetetrazole (PTZ)-induced seizure in rats. Forty male Wistar rats were bilaterally microinjected with saline or one of the different doses of ghrelin (0.3, 1.5, and 3.0 nmol/μl/side). Ghrelin was administered into dorsal hippocampus thirty minutes before intraperitoneal injection of PTZ. The effect of chronic administration of ghrelin into dorsal hippocampus was investigated in twenty male wistar rats. The rats were bilaterally microinjected with saline (1 μl/side) or ghrelin with effective dose (0.3 nmol/μl/side) for ten- day. In tenth day, thirty minutes after saline or ghrelin microinjection, PTZ was injected intraperitoneally. Ghrelin, at a dose of 0. nmol/μl, significantly (p<0.001) decreased the duration and seizure severity. Chronic microinjection of ghrelin significantly (p<0.001) attenuated the duration and severity of the seizure induced by PTZ. The present study provides evidences that the intrahippocampal microinjection of ghrelin has an inhibitory effect against PTZ-induced seizure.

Ibuprofen is a problematic drug in tableting due to its high cohaesivity and viscoelastic properties. In this study coprecipitation of ibuprofen with varying concentration of gelatin to optimize properties of Ibuprofen was carried out. Optical microscopy and differential scanning calorimetry (DSC) were used to investigate the physical characteristics of the co-precipitates. The dissolution behavior, flowability and compaction properties of various batches were also studied. Co-presipitation of drug with gelatin led to a change in habit from needle to plate shape crystals. The co-presipitates showed improved flow properties, while no change in dissolution rate of them was observed compared with ibuprofen alone. All of the obtained co presipitates exhibited significantly improved tableting behavior compared with drug crystals alone. Due to the fact that the polymer covering the drug particles increases and changes the nature of the surface area available for interparticulate bonds between particles. DSC experiment showed that drug particles, in co-presipitates samples, did not undergo structural modifications. The study highlights the influence of polymeric additives on crystallization process leading to modified performance.

Rutin (3, 3, 4, 5, 7-pentahydrohyflavone-3-rhamnoglucoside) is a nutrient, classified as a bioflavonoid. This study was carried out to determine the potential protective effect of rutin on acetaminophen and carbon tetrachloride (CCL4) induced liver injury. For ccl4, adult male Wistar rats were divided into 5 groups (n=7/group). Group 1 was treated by 1 mg/kg ccl4, twice a week. Group 2 received olive oil. Experimental groups (groups 3-5) received rutin at the doses of 10, 20 and 40 mg/kg respectively (i.p.) once a day plus ccl4. For the acetaminophen study, another 5 groups (n=7/group) were assessed. Group 1 treated by 300 mg/kg acetaminophen, twice a week. Group 2 received saline. Experimental groups (groups 3-5) received rutin at the doses of 10, 20 and 40 mg/kg respectively (i.p.) once a day plus acetaminophen. After 8 weeks, liver functions were assessed by serum biochemistry of alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Liver sections were stained with H&E for histopathological assessment. Serum levels of ALT and AST were reduced significantly after 8 weeks treatment by rutin at the doses of 20 and 40 mg/kg (p<0.05). Reduction was more prominent at the dose of 20 mg/kg. Histopathological assessment was shown a reduction in liver damage at the doses of 20 and 40 mg/kg of rutin for acetaminophen and 20 mg/kg for ccl4. Results suggest a potential hepatoprotective activity for rutin. Antioxidant and free radical scavenging properties, which has been shown by previous studies, may account for most of the protective effect of rutin.

Tamoxifen is an nonsteroid drug which is used for treatment of breast cancer ‚CNS tumours‚stimulation of ovulation in infertility protocoles. Regarding to the affinity of tamoxifen to estrogen receptors and the possible role of estrogen on follicular differentiation, the aim of the present study is to investigate fertility of the mice that their mother had received tamoxifen during pregnancy. In this study‚ 30 adultfemale mice and 15 adult male mice are used. The mice were mated and the pregnant mice received 100μg/kg tamoxifen on 13th day of pregnancy as IP. The mice in control group only received the solvent. After delivery ‚the female pups were kept under standard condition and reached adulthood. For evalution of fertilitey‚ the mice superovulated using hMG and hCG‚ and the oocytes were collected by flashing. The collected oocytes were transferred to culture medium and sperms were added. 48 hours post insemination the number of fertilized oocytes were determined. The results from IVF showed that the role of fertilization in oocytes from experimental group was significently lower than those in control group (P<0/01). The results indicate that maternal exposure to Tamoxifen during pregnancy‚ causes that the involved embryos to show‚ disordered reduced fertility‚ after reaching adulthood.

The hippocampus has been implicated in many learning and memory processes including spatial memory. Ghrelin is a peptide hormone secreted by stomach and brain structures. Some studies have suggested that ghrelin may affect learning and memory. The goal of this study was to investigate the effect of intrahippocampal injection of different doses of ghrelin on spatial memory formation in normal rats. Fifty maleWistar rats were divided into 5 groups including: control, saline and different doses of ghrelin (0.3, 1.5 or 3 nmol). Saline or ghrelin was injected into hippocampus. All groups were trained in Morris water maze for two consecutive days. Learning parameters including escape latency and distance traveled were compared among groups. ghrelin with dose of 0.3 didnt alter Learning parameters compared to saline (p< 0.05) but ghrelin with doses of 1.5 or 3 nmol significantly improved spatial memory compared to saline in normal rats(p< 0.05). The findings indicated that ghrelin has positive effect on memory processes.

Perianesthetic aspiration is a threating side effect, that severity of it depends on pH and volume of aspirated gastric juice. Because of the loss of consciousness while anesthesia the protective reflexes disappear and make the person in risk of aspiration. Pharmacological attempts, have been made to eliminate the risk of pulmonary aspiration. The aim of this study was Comparison of oral pantaprazol and famotidine on gastric volume and pH in elective surgeries. In a double-blind, randomized clinical trial, 120 patients candidates of elective surgery were randomized in 3 groups (control or D, pantoprnzol or P and famotidine or F groups). The patients in group D  p and f were given placebo pantaprazole 40mg and famotidine 40mg orally at 11 pm a night before surgery respectively. After induction of anesthesia, gastric contents were aspirated and analyzed for the pH and volume. PH values were 2.87±0.92 in group D, 4.53±1.29 in group P and 3.79±1.97 in group F. There was statistical difference between groups D, P and F (pv<0.05). The results showed a considerable decrease in the gastric volume in groups P and F comparing to group D. (p<0.05). We concluded that oral pantaprazole is effective in reducing gastric pH comparing to famotidine and placeboand famotidine is effective in reducing gastric volume comparing to pantaprazol.

Chalcones, a class of natural products, have different biological activities. The aim of this research was synthesis and evaluation of antimicrobial effects of three chalcones bearing allyloxy moiety similar to some natural flavanoids. Chalcones (3a-c) were prepared in two steps. First, vanillin, isovanillin and salicylaldehyde were reacted with allyl bromide to afford allyloxy aldehydes. Then, allyloxy aldehydes were reacted with 2- hydroxyacetophenone in the alkaline media to afford final products. Standard disc diffusion and Agar dilution methods were used for analyzing antimicrobial activities on three gram-positive and two gram-negative bacterial species and also three fungi species. Antioxidant activity of the compounds was determined by DPPH using brand- Williams method. Chalcones 3a-c were synthesized as yellow-orange crystals in 60 70% yield. Chalcone 3c with concentration about 4 mg/disc had 11.7 mm inhibition zone on P. aeruginosa and Chalcone 3b with MIC value about 0.5 mg/ml, exhibited 8.8 and 16.5 mm inhibition zone in 2 and 4 mg/disc for S. epidermidis, respectively. Mean while MIC value of the Chalcones 3a and 3c was more than 2 mg/ml. Chalcones 3a-c had no antifungal activities. Antioxidant activities of chalcones 3a, 3b and 3c were determined to be 31, 28 and 27 percent respectively. Chalcones 3a-c were synthesized in two steps. Their antimicrobial and antioxidant activities were evaluated. The two 3b and 3c regioisomers showed selective and weak antibacterial activities. Chalcone 3b and 3c affected on gram positive and gram negative bacteria, respectively. Chalcone 3a did not show any antibacterial activity.