PHARMACEUTICAL SCIENCES
Year:2007 | Volume:- | Issue:2|Papers Count:9

Objective: Propranolol hydrochloride is a widely used beta blocker agent which is administered 3 times daily due to its short half life. The aim of this study was to design and evaluate polymeric film of propranolol hydrochloride using psyllium seed’s mucilage as a natural occurring substance in order to deliver the active agent in a controlled manner. Methods: In this study matrix polymeric films of propranolol hydrochloride using psyllium as a natural polymer and Eudragit RSPO, RLPO was designed and prepared by solvent evaporation technique. The dissolution behavior of the prepared films was evaluated using USP apparatus No. P with some modifications including a disk which hold the patch at the bottom of the vessel. All the experiments were performed automatically and the dissolution tester was matched with a UV spectrophotometer. The results were compared with that of Eudragit. Some other characteristics such as film thickness, drug content, and release rate, kinetics of drug release and Dissolution Efficiency (DE) were also investigated. All calculations were done using Excel 2003 software. Results: Kinetic analysis of the drug release from polymeric films indicated that release was predominantly attributable to the Peppas model and the in vitro release behavior of this new polymeric film prepared using natural polymer is comparable to that of semi synthetic polymer such as Eudragit with the advantage of low cost, ease of preparation and low skin irritability potential. Conclusion: The Results of this study indicated that the formulation prepared with 400 mg of psyllium could retard drug release rate significantly.

Objectives: Statins have been proven to possess anti-inflammatory activities unrelated to cholesterol lowering actions. Here we compared the anti-inflammatory and anti-leukocyte accumulation effects of atorvastatin, simvastatin and lovastatin. Methods: Carrageenan-induced rat paw edema and mouse air-pouch as acute and local inflammatory models were used in this study. Animals were received 1, 5, and 10 mg/kg of drugs orally 20, 12, 6, and 1h prior to inflammation induction by injection of carrageenan into either rat paw or the pouch. Results: We found that all three statins reduced both the maximal edema response attained during 4h and neutrophils infiltration in inflammation zone. Lovastatin had the lowest and atorvastatin had the greatest effects. The effect of simvastatin was between lovastatin and atorvastatin. Dِuring this time statins did not alter serum cholesterol and triglycerides. Atorvastatin (10 mg/kg) caused the most potent inhibition of the carrageenan-induced inflammation (70% reduction; p<0.0001) and leukocyte accumulation (80% reduction; p<0.0001). Atorvastatin was comparable to indomethacin in this model. Also, in the mouse air-pouch model atorvastatin treatment produced a very significant (p<0.0001) reduction in carrageenan-induced pouch leukocyte recruitment and exudates production. Co-administration of mevalonate reversed the effect of atorvastatin on leukocyte recruitment and the exudates production. Conclusion: The result of this study shows that the anti-inflammatory potency of statins is according to their inhibitory potency on hydroxy-methyl-glutaryl CoA reductase but unrelated to lipid reduction.

Objectives: Mineral waters and some extract of plants contain some elements and components such as flavonoids that are therapeutic. In this study the effect of the total extract of Hypericum Scabrum and calcic and magnesic sulfate mineral water on lipid profile of in hypercholesterolemic rats were compared. Methods: 48 male SD rats (100-150 g) were selected. They were divided to 8 groups of 6 rats and seven groups received cholesterol rich diet and one group received normal diet as control for the first 60 days. Then the diet of rats was changed for the second 60 days.:Group1: normal diet, City water, DMSO (ip), Group2: normal diet, Mineral water, DMSO (ip), Group3: normal diet, City water, Atorvastatin (0.5mg/kg, ip), Group4: hypercholesterolemic diet, City water, normal saline (ip),Group5: hypercholesterolemic diet, City water, DMSO (ip), Group6: hypercholesterolemic diet, Mineral water, DMSO (ip),Group7: normal diet, City water, Scabrum (4mg/kg, ip), Group8: normal diet, City water, Scabrum (12mg/kg, ip) and again at the end of the second period the blood sample was taken from rats, eyes. Results: the results of tests showed that the difference in lipid profile were significant for all groups in comparison with high cholesterol control group (P<0.001) the difference in serum magnesium level by Mineral water was not significant in comparison with other groups (P>0.05). Conclusions: According to the results of this study it seems that the study about hypocholesterolemic effects of Hypericum Scabrum and mineral water in human kind may be useful.

Objectives: Diabetes is one the most common endocrine disorders, obesity, improper nutrition, and inactivity was considered as proposing factors. Historically plant extracts are used for diabetes control. This study was implemented to determine the effect of total and different fraction of Iranian black orthodox tea on weight, food intake and blood sugar in type I diabetic rats. Methods: This study was conducted on 56 rats which were randomly divided in to 8 groups (7 rats in each group). The weight of rats was 200 – 250 gr. Group 1 and 2 was non-diabetic, groups 3 – 8 were diabetic, and diabetes was induced with intraperitoneal injection of streptozotocin 60mg/kg. Group 1 to 8 received carrier, total extract, carrier, total extract, methanol fractions of 20%, 40%, 60% and 80% plus 100% respectively. Blood sugar was measured beginning and end of intervention, weight and food intake was measured each week during intervention (5 times). Data was analyzed by using one and two ways ANOVA, repeated measure and nested variance. Results: Food intake and weight was reduced, in 40% fraction received group, significantly more than other groups (p=0.000).also total extract decreased food intake significantly (p=0.000). There were no significant differences between other groups. Change in Mean blood sugar between groups during intervention was not found statistically significant. Conclusion: It can be concluded that injection of total extract and 40% fraction of black tea had positive effect on decreasing of food intake in diabetic rats and prevention of obesity. Therefore consumption of black tea might prevent from diabetes and its complications.

Objectives: Telomerase is a RNA dependent DNA polymerase which synthesis telomeric repeats and in most cases are molecular base of unlimited proliferation. Telomerase gene expression occurs in most tumor cells rather than normal cells. Combination of external and internal factors including Zn, Cu and Selenium are involved in breast tumor development and growth. The aim of this study was to evaluate the effect of Zinc, Selenium and Copper on telomerase gene expression in breast cancer T47D cell line. Methods: Time and dose dependent manner treatment of T47D breast cancer cell lines were carried out by adding Zn, Cu, and Selenium in tissue culture. Relative telomerase activity (RTA) of T47D cell line was measured by TRAP assay. Results: After being treated with 100 mM/L Zn So4 for 6 hours, telomerase activity of T47D cells was markedly increased (5.2 fold) but with 100 mM /L Zn So4 for 24 hours and 500 mM /L Zn So4 for 6, 24 hours, telomerase activity was 0.76, 0.39 and 0.12% respectively (control 49.2%). After being treated with 10 mM /L Cu So4 for 6 hours, telomerase activity of T47D cells 3.67 fold was increased. After being treated with 10, 30 mM /L selenium-L- methuonin, telomerase activity were markedly inhibited. Telomerase activity of T47D cells for 24 hours were 0.93, 0.60 and for 48 hours were 0.76, 0.12 respectively (control 49.2%). Conclusion: Based on obtained results, it is speculated that pharmacologic doses of Se, Zn and Cu could have an inhibitory effects on telomerase gene expression and it could be used as a target therapy in tumor cells.

Objectives: Different factors are in involved in inducing and progressing of atherosclerosis. One of these factors is endothelin-1. Since in atherosclerotic vessels obvious and certain changes with abnormality in transferring of calcium ions are seen, some researchers suggested that calcium channel blockers can slowdown the process of atherosclerosis. Methods: 36 male Newsland white rabbits were divided into four groups: The normal control group, normal group receiving amlodipine, high-cholesterol diet group and high-cholesterol diet with amlodipine group. After 8 weeks all animals anesthetized and blood and tissues samples were colleted. Results: The levels of cholesterol and triglyceride in groups of high-cholesterol diet comparison to control group increased significantly (p< 0.01). Amlodipine consumption in eight weeks reduced significantly (p< 0/01) plasma endothelin-1 levels in both of high-cholesterol diet plus amlodipine and amlodipine groups. Amlodipine consumption caused significant reduction (p<0/01) in the level of endothelin-1 in heart tissue of high-cholesterol diet plus amlodipine group but did no effect on reduction of heart tissue endothelin-1 in amlodipine group. Conclusion: High-cholesterol diet caused enhancing of plasma and renal tissue endothelin-1 and amlodipine reduced plasma and tissue endothelin-1 levels in high-cholesterol diet group. In conclusion amlodipine treatment could have positive effects in pathology of atherosclerotic renal arteries.

Objectives: Acetaminophen (Paracetamol) is a widely used antipyretic and analgesic drug, which in overdose can cause extensive hepatic damage. This study initiated to compare differential effects of therapeutic and toxic dose of acetaminophen on enzymatic and non-enzymatic antioxidant factors, plasma total antioxidant capacity, level of plasma AST and ALT and structure of liver in developing and adult rats. In this paper, histopathologic and enzymatic findings are report. Methods: 12 neonatal and 12 adult male albino Wistar rats were divided into 2 groups (neonatal and adult). In each group, the rats were randomly divided into 3 subgroups (n=4/group). Treated groups were given single low (25 mg/Kg.b.w) and high dose of APAP (450 mg/Kg.b.w), respectively. Controls received phosphate buffer salin (PBS) only as the vehicle. All animals were euthanized after 24 hours and necropsied. Tissue samples from the liver were fixed in 10% neutral buffered formalin, embedded in paraffin and sectioned at 6 microns and stained with H&E for histopathological examination. The level of plasma AST and ALT were also measured by autoanalyser. Results: Histopathologic examination revealed centrilobular necrosis, infiltration of inflammatory cells, swelling, granular degeneration, fatty change and single cell necrosis of hepatocytes in subgroups that received high dose of acetaminophen. Congestion, scattered foci of hepatocytes necrosis and inflammatory cell infiltration were observed in subgroups that received low dose of acetaminophen. The lesions were more severe in adult than neonatal rats. ALT in adult and ALT and AST levels in neonatal rats were significantly increased in high dose subgroups (p<0/05). Conclusion: The results of this study indicated that the lesions in liver were more severe in adults than neonatal rats. This can be due to inducible certain antioxidant factors and less severe induction of cytochrome P450 in neonatal rat hepatocytes than in adults.