PHARMACEUTICAL SCIENCES
Year:2009 | Volume:15 | Issue:2|Papers Count:15

Objectives: Mucilage polysaccharides costitute a structurally diverse class of biological macromolecules which are the basis for the different applications in the broad field of pharmacy and medicine. Some examples will be given for the so-called immune-modulating antitumor polysaccharides which have been shown to be prominent candidates for an adjuvant tumor therapy. Methods: In the present research, plant mucilages, has been isolated from the leaves and bulbs of Allium chrysantherum from important bulbous plants of iran (Liliaceae). Each organ was pretreated to remove interfering substances and the extracted mucilage (by cold and hot methods) was also purified from contaminants. The chemical composition of the mucilage was studied by analysing the hydrolysates quantitatively and qualitatively by TLC and GLC of their alditol acetate derivatives. Results: Purified mucilages extracted from leaves and bulbs of Allium chrysantherum, were shown to be acidic polysaccharides, containing: glucose (65%), mannose (22%), galactose (12%) and glucoronic acid was also present in the leaf mucilage and the bulb mucilage of this species was composed of rhamnose (10%), mannose (12%) glucose (29%) and galactose was the predominant sugar (48.5%), glucoronic acid and galacturonic acid were also present. Conclusion: The findings of the present study suggest that two mucilages of the leaves and bulbs , containing acidic polysaccharide and hegsuses are the predominant sugars.

Objective: The medicinal properties attributed to Crocus sativus L. (saffron) are extensive, but saffron taken in large amounts is highly toxic. This study was performed to elucidate the possible toxic effects of total extract of Crocus sativus L. stigma on liver, kidney and some hematological parameters in normal rats. Methods: Male Wistar rats were randomly assigned into four groups of eight animals each. Group 1 was treated with ISS as control and Groups 2 to 4 were treated with total saffron extract administered daily for 2 weeks intraperitoneally in doses of 0.35, 0.70 and 1.05 g/kg, respectively. Body weight of the animals were recorded on the first, 7 and 14 of the experiment Hematological and biochemical parameters were measured on final days of the experiment. Tissue specimens of the liver and kidneys were subjected to histological examination using standard hematoxyline-eosin staining. Results: Total saffron extract caused significant reductions in the Hb and HCT levels and total RBC count, although it showed no dose-dependent effect. Total WBC count showed significant dose-dependent increases in extract treated rats. The extract treated animals, also, exhibited significant dose-dependent increased values of AST, ALT, urea, uric acid and creatinine. In the histopathological studies of liver and kidneys in extract treated rats, there were mild to severe tissue injuries supporting the biochemical analysis. Conclusion: The results of this study indicated that total extract of Crocus sativus L. stigma is toxic (in given doses), and causes hepatic and renal tissue damages along with anemia in rats.

Objectives: Naproxen is a poor water soluble non-steroidal analgesic and anti-inflammatory drug. Oral absorption and effectiveness of a drug can be improved by preparing solid dispersions and subsequent increase of dissolution rate. The aim of this study was to evaluate analgesic effect of solid dispersions of naproxen (1:1) in crosspovidone and Elaeagnus Angustifolia fruit powder by using co-grinding technique and formalin test. Methods: Study was carried out in male wistar rats weighing 180-200g (n=8 rats per each group). Formalin test was performed one hour after oral administration of drugs by intraplantar injection of formalin 2.5%. Results: Solid dispersions of naproxen in crosspovidone and Elaeagnus Angustifolia produced more (P<0.001) analgesic effect when compared with physical mixtures of naproxen with crosspovidone and Elaeagnus Angustifolia and pure naproxen powder. The analgesic effect of physical mixtures of naproxen with crosspovidone and Elaeagnus Angustifolia were not significantly different from pure naproxen powder. The analgesic effect of solid dispersion of naproxencrosspovidone was markedly (P<0.01) more than of solid dispersion of naproxen- Elaeagnus Angustifolia. Conclusion: We suggest that the analgesic effect of naproxen may be increased by preparing its solid dispersions in crosspovidone and Elaeagnus Angustifolia fruit powder.

Objectives: Lindane is organochlorine compound which is widely used in agriculture and medicine for treatment of pediculosis (as shampoo) and scabies ( as lotion). Lindane is absorbed through inhalation and leads to intoxication. The purpose of this investigation is studying of the effects of Lindane in Tracheal and pulmonary cells of Rats. Methods: For this investigation, solvent (Ethyl acetate) and Lindane were intraperitoneally given at doses of 10, 20 and 40mg/kg. After 24 hours the animal were killed by Ether and The Lung and Tracheal tissues were fixed in 10% formalin. After preparation of microscopic segments, H&E (Hematoxylin & Eosin) staining for histopathologic studies and AB (Alcian Blue) and PAS (Periodic Acid Schiff) staining for cytochemistry of glycoprotein secreting cells were used. Results: The results indicated that the tissue of lung and pneumocyte cells was intact in control group. Different cellular damages including swell of cells, formation of Vacuole, reduction of staining ability in the type II pneumocytes, thickening of Alveolar walls and injury in ciliated and nonciliated cells. Lindane caused changes of epithelium from pseudostratified to simple. Cytochemically, in control group, the epithelial tissue of trachea, neutral (PAS+) and acidic (AB+) glycoprotein secreting cells were observed. In all cases intensity of damages was dose dependent. Conclusion: The results indicated that Lindane cause cellular damage in the Respiratory system cells. The mechanism of this toxic effects is unknown, but reported that Lindane is converted into intermediate substance by the action of hepatic microsomal enzymes, and this new substance can cause cellular injuries.

Objective: Dihydrotestosterone (DHT) is an endogenous hormone that is derived from testosterone in an enzymatic reaction mediated by 5-alpha reductase. The high density of androgen receptors and 5-alpha reductase enzyme have been found in the centers of learning and memory in hippocampus ,and improvement in learning and memory followed by administration of DHT to gondectomized male rats indicates androgens role in learning and memory. Methods: 80 male rats randomly divided into ten equal groups. Two Canules were implanted in CA1 of animals in all groups except control. After 1 week the experiments were started. Control group tested in Morris Water Maze. One group received 0.5 ml saline 30 min and two other groups received 0.5 ml DMSO 30 min and 24 hour before tests intrahippocampaly. Doses of 5, 10, 20 Microgram DHT were solved in 0.5 ml DMSO and in three groups were injected in CA1 30 min before test and in the other three groups 24 hours before it. Results: Our results showed that injection of DHT different doses 24 hours before tests had no meaningful effects on learning and memory retrieval in Morris Water Maze but injection of 10 mg of it, 30 min before tests decreased swimming path significantly (p<0.05) and increased traveled distance percent in target quadrant (p<0.05). Conclusion: Results showed that DHT in dose of 10 microgram can improve acquisition and retrieval in intact male rats.

Objectives: Many evidence indicated that glucocorticoids enhanced memory consolidation in a variety of tasks, but the underlying mechanism(s) are not clear. The aim of this study was to determine the role of cholinergic system in glucocorticoids-induced enhancement of memory consolidation in mice. Methods: In this experimental study were performed on 100 male albino mice (about 30 g). The animals were trained in an inhibitory avoidance task (0.5 mA shock for 3 seconds). In Experiment 1, effects of corticosterone were determined. Immediately after training, the animals received of vehicle or corticosterone (0.3 mg/kg). In Experiments 2 and 3, effects of corticosterone were examined in the presence of absence of atropine, a blocker of muscarinic cholinergic receptors, (0.5 and 2 mg/kg) or Mecamylamine, a blocker of nicotinic cholinergic receptors, (0.5 and 2 mg/kg), respectively. In all experiments, memory retention tested 48 hr later. Results: Results indicated that Corticosterone enhanced memory consolidation significantly (P<0.01). Blockade of muscarinic cholinergic receptors by atropine suppressed the glucocorticoids response dose-dependently. Blockade of nicotinic cholinergic receptors by Mecamylamine did not change the glucocorticoids response. Also both blockers alone did not change memory consolidation as compared with control group. Conclusion: Finding above showed that the memory enhancing effects of corticosterone, at least in part; may mediate via muscarinic cholinergic receptors.

Objectives: Ribes biebersteinii fruit is used for treatment of hypertension in folk medicine of Azarbaijan. However it's mechanism of action is not studied. This work was aimed to examine the vasorelaxant effect of the Ribes biebersteinii fruit total extract (RBE) and role of endothelium in rat isolated aorta. Methods: Rings of aorta (3-5 mm length) were prepared and equilibrated in Krebs' solution under 2 g tension. Rings with or without endothelium were contracted by phenylephrine (PHE, 0.1mM) or PGF2a(8 mM) and then exposed to cumulative doses of RBE. In order to asses the role of endothelium in the vasorelaxant effect of RBE, tissues were studied by incubation for 20 min by (L-NAME, 100mM) or (Methylene blue, 10mM) before contraction by PHE. Results: RBE induced relaxation in rat aortic rings pre-contracted with PHE or PGF2α dose–dependently in both intact and endothelium-denuded aortic rings. The differences between the relaxant response of intact and endothelium–denuded rings were not significant (p>0.05). L-NAME and Methylene blue did not affect the RBE-induced relaxant response in rat aortic rings. Conclusion: the results indicate that RBE induces relaxation dose-dependently in rat aortic rings precontracted with PHE by a mechanism independent of endothelium function or its productions.

Objectives: Synergistic effects between UV absorbers can produce many advantages in sunscreen products such as: decreasing topical irritation, allergic reactions and skin absorption of sunscreen agents. Methods: six currently used UV filters of Eusolex® series (232, 6007, HMS, OS, 4360 and 9020) were studied. Various concentrations from each sunscreen were prepared in isopropyl alcohol and UV spectrums of them were taken in 290-400nm with reference concentration of each UV filters. Six commonly used solvents were used and the best solvent was selected. The best AUC for all sunscreens were obtained from their solutions in isopropyl alcohol as solvent. Single solutions and all probable binary mixtures of them were prepared and compared with another. Synergistic effects of two sunscreen agents in binary systems were compared based on AUCs and their absorption intensity in 310nm. Results: Maximum synergistic effects in UVB wavelengths was related to Eusolex® 9020-Eusolex® 4360 combination with 10%-90% ratio (about 64% in AUC and 65.7% in 310nm absorption intensity). Combination of Eusolex® 9020 and UVB filters with low weight retios also significantly improved AUC of Eusolex® 9020 in UVA wavelengths (up to 61% in combination with Eusolex® 6007). Eusolex® HMS and Eusolex® OS also showed markedly synergistic effect in combination with Eusolex® 4360 with low ratios (47% and 18.9% respectively). Conclusion: these results demonstrated that exactly choosing the type and ratios of UV filters in sunscreens can greatly improve efficiency and decrease effective concentration of formulation active ingredients.

Objectives: One of the most popular oral drug delivery systems is the multiparticulate tablets such as compacted pellets which their benefits over single unit dosage forms have been widely studied. One challenge in the production of such tablets is maintaining the desired drug release after compaction, as the application of compaction force can damage the pellets and alter the drug release. The aim of this study was to design diclofenac sodium multiparticulate tablets which upon oral ingestion rapidly disintegrate into comprising pellets. Methods: In the present work pellet formulations containing 10, 20, and 30% diclofenac sodium and 20, 40 and 60% of Eudragit RS PO:RL PO (1:1) were studied and manufactured based on full factorial design and using the extrusion-spheronization. Detailed consideration was given to the effect of formulation variables on the physical and release properties of pellets. The effect of curing on the pellet properties also was studied. Results: Increase in amount of drug in both uncured and cured pellets led to decrease in MDT, whereas increasing amount of eudragit in uncured pellets had no considerable effect on drug release but in cured pellets, specially at lower amounts of drug, led to increase in MDT or decrease in drug release rate. Tablets containing 60% pellets and 40% filler blend with acceptable hardness and disintegration time have been produced. Conclusion: Results showed that no apparent damage to the pellets has occurred as a result of the compaction process. Intact pellets were rapidly released from single unit dosage form upon contact with dissolution medium.

Objectives: Regarding to the hyperlipidemia as one of the most important risk factors for cardiovascular disease, the present study was conducted to assess the effects of flaxseed dietary supplement on serum lipid profile and malondialdehyde (MDA) in hyperlipidemic rabbits. Methods: Twenty-four New Zealand male rabbits after 2 weeks of adaptation were fed 0.5 % cholesterol that was added their diet for 1 month to induce hyperlipidemia. Then the rabbits were divided into two groups, the rabbits in control group were continued on the 0.5 % cholesterol diet and flaxseed group received 7.5 g/kg b.w/day crushed flaxseed which was added to the 0.5 % cholesterol diet, each for 2 months. The diets were isocaloric and isonitrogenous. Fasting blood samples were obtained at baseline, after hyperlipidemia, 1 month and 2 months of intervention to determine the concentrations of serum lipid profile and MDA. Results: Serum TC, LDL-C and MDA were lower in flaxseed group as compared to control group by 34 and 37% (P<0.001), 35 and 38.5% (P<0.001) and 36.3 and 38.5% (P<0.05), respectively, at the end of first and second month. There were no significant differences in HDL.C and TG concentrations (P>0.05). Conclusion: The results of the present study demonstrate that dietary flaxseed favorably decrease serum TC, LDL-C, TC/HDL.C, LDL.C/HDL.C and lipid peroxidation parameter (MDA) and may be developed as a useful therapy for hyperlipidemia.

Objectives: Chronic opiate administration induces tolerance to the analgesic effect. Several studies indicate that nitric oxide/ N-methyl D-aspartate pathway has important role on morphine induced tolerance. The main goal of this study was to evaluate the effects of systemic administration of Minocycline and Riluzole on Morphine induced tolerance in rat. Methods: Animals were divided in 8 groups (n=8) and received daily: Saline (1 ml/kg’ ip) or {Saline (1ml/kg’ ip) + Morphine (10 mg /kg’ ip)} or {Minocycline (10, 20, 40 mg/kg’ ip) + Morphine (10 mg/kg’ ip)} or Minocycline (10 mg/kg’ ip) or Tween 80 (2%) (1 ml/kg’ ip) or {Tween 80 (2%) (1ml/kg’ ip) + Morphine (10 mg /kg’ ip)} or {Riluzole (4, 8, 12 mg/kg’ ip) + Morphine (10 mg/kg’ ip)} or Riluzole (12 mg/kg’ ip). Nociception was assessed using hot-plate apparatus. The hot-plate latency was recorded when rat licked its hind paw. A baseline latency was determined daily, then drug was injected. After 30 minutes morphine was administrated and post-drug latency evaluated 30 minutes after the injection of Morphine. Results: Results showed that Minocycline (20, 40 mg/kg) and Minocycline (10 mg/kg), delayed the tolerance appearing time about 3 and 4 days respectively. Riluzole (8, 12 mg/kg) could postpone day of morphine tolerance for 5 days in comparison with control group. Conclusion: Interaction with nitric oxide system and glutamatergic pathway are the possible mechanisms of Minocycline and ability of Riluzole as a glutamate release inhibitor could be the major mechanism in attenuating the development of Morphine induced tolerance.

Objectives: Diabetes is a metabolic disorder characterised by hyperglycemia resulting from perturbation in insulin secretion, insulin action or both. Juglans regia (Juglandaceae) has been used in Iranian traditional medicine in the treatment of diabetes. In this experience the preventive effect of hydroalcoholic extract of Juglans regia leaves on activity of AST and ALT in alloxan-induced diabetic rats was investigated. Methods: In this research 18 male white Wistar rats, with body weights of 180 – 220 g were randomly allocated into three groups with six rats per group: first group(nondiabetic control); second group(diabetic control) and third group(diabetic rats treated with hydroalcoholic extract of Juglans regia leaves). In order to induce diabetes, alloxan was administered as a single dose (120 mgkg-1BW), intraperitoneally. At the initial and the end of 2 and 6 weeks of experimental period, rats were fasted for 8h, and then fasting blood samples were collected in heparinated tubes. Sampling was performed from the orbital sinus. Results: The results indicate a significant difference in AST and ALT level in the diabetic group compared with the other groups (P<0.05). Histological studies of the liver of these animals, demonstrated the same results. Conclusion: These results show that the hydroalcoholic extract of Juglans regia leaves could affects on preventive of diabetes.