PHARMACEUTICAL SCIENCES
Year:2007 | Volume:- | Issue:4|Papers Count:11

Objectives: Nausea and vomiting are common complaints of pregnancy mainly throughout the first trimester and various herbal and synthetic drugs were used in the treatment of it. The aim of this study was to compare the effect of metoclopramide with ginger in treatment of pregnant women’s nausea and vomiting.Methods: Women with Nausea & vomiting in pregnancy, with single fetus < 20 weeks gestation, were invited to participate in this study. During a 6 months period, 60 eligible women gave consent and were randomized in a double- blind design to receive either oral ginger 1g per day or oral metoclopramide 10 mg 3 times daily. Subjects graded the severity of their nausea using visual analog scale and recorded the number of vomiting episodes in the previous 24 hours before treatment and again during 4 consecutive days while taking treatment.Results: 60 women remained in study (30 per each group). There were no significant differences between the groups with respect to maternal age / gravidity / parity and gestational age. The visual analog scores of post therapy minus baseline nausea and vomiting episodes decreased significantly in 4th day in both groups (p<0.01). Likert scale showed that 90% in ginger group and 63.4% in metoclopramide group had improved in nausea & vomiting of pregnancy. (p=0.04).Conclusion: Ginger is more effective than metoclopramide in relieving the severity of nausea & vomiting of pregnancy.

Objectives: Approaches to increase the gastric residence time (GRT) include: floating drug delivery systems (FDDS), swellingexpanding forms, bio (muco) adhesive forms, modified shape and high density systems. Diltiazem HCl (DTZ), a model drug for this study, is a calcium antagonist used in the treatment of chronic heart diseases such as angina and hypertension. It has elimination half-life of 3.5 hours and hence is a suitable model candidate for gastro-retentive formulation. The major objectives of this study were to develop a single unit FDDS of DTZ and to study the effect of formulation and processing parameters on the floating and drug release of the system.Methods: DTZ matrix tablets (120 mg) containing HPMC (K4M, Colorcon, UK), Carbomer (934P, B.F. Goodrich, USA), Na CMC (Merck, Germany), Guar gum (Hercules, USA) and Xanthan gum (Arthur Branwell, UK) were prepared by direct compression method. All tablets contained an effervescent base consisting of sodium bicarbonate and citric acid. The tablets were evaluated for in vitro floating ability (floating lag time and duration of floating time), bioadhesiveness and drug release. Bioadhesion was measured by a method based on shearing tensile strength existing between tablets and a mucosal layer. The drug release studies were carried out using a dissolution apparatus (Erweka, Type DT700, Germany) basket method (100 rpm) in 900 ml of 0.1 N HCl buffer solution (pH = 1.2, 37oC). At appropriate time intervals, samples were withdrawn and assayed spectrophotometrically at 237.8 nm with suitable dilutions.Results: In vitro floating test showed that tablets containing 12% effervescent base had a floating lag time of 30-120 seconds. The duration of floating was 19-24 hours for all the formulations and the hardness of tablets had no significant effects on the floating time. The more carbomer content of the tablets, the more in the bioadhesive properties. Drug release data was fitted on both Higuchi and first order kinetic models. The mechanism of drug release showed a non Fickian (anomalous) behavior based on Korsmeyer- Peppas equation.Conclusion: We concluded that the proposed tablets with 12% effervescent base, 30% HPMC and 10% Na CMC showed good floating, bioadhesion and drug release properties in vitro and seems to be considered as FDDS for DTZ.

Objectives: The Smyrnium cordifolium Boiss, is a biannual plant belongs to Umbeliferae familiy that growing wildly in West and South West mountains of Iran and have nutrient and medicinal usages in these regions.Methods: This plant was collected in post-flowering stage from mountains of Khoramabad. The antibacterial effects of essential oil and aqueous, methanolic, ethanolic and etheric extracts of different parts of studied plants against Staphyllococcus aureus, Shigella flexneri, Salemonella typhi, Staphyllococcus epidermidis, Staphyllococcus saprophiticus, Psuedomonas aeruginosa and E. coli bacteria were studied by digging hole and measuring diameter of grows inhibiting ring. In this study the relevant dissolver were used as control and gentamicine antibiotic was used for comparision.Results: The results showed that aqueous extracts except extract from leaves of Smyrnium which has clear effect on Shigella. In other cases didn’t show remarkable antibacterial effects while ethanolic and etheric extracts showed desirable antibacterial activity in the most of study microorganisms.Conclusion: In general, the antibacterial activity of essential oil and different extracts tested were more pronounced of S. cordifolium against of Gram-positive bacteria than against Gram-negative bacteria. This generally higher resistance among Gram-negative bacteria could be ascribed to the presence of their outer phospholipidic membrane, almost impermeable to lipophilic compounds. Antibacterial activity of the essential oil of this plant was probably attributed to large content of oxygenated sesquiterpens especially Curzerene and Curzerenone.

Objectives: Acetazolamide, a carbonic anhydrase inhibitor, is most efficient and beneficial in the treatment of glaucoma when used as a sustained release form. In the present work some sustained release matrices of the drug were formulated.Methods: Tragacanth and acacia gums matrices containing 500 mg of acetazolamide with ratios of gum to drug (RG/D) between 0.1-1 were formulated and the release study was conducted in buffer solution (pH=7.4) using USP dissolution apparatus I for 480 min.Results: The drug release was affected by the kind of the gum as well as the RG/D values. In order to assess the efficiency of the gums, percent of drug dissolved up to any time was plotted against RG/D. The plot was named as gum efficiency curve which contained ascending and descending parts indicating two opposite effects of the gums on drug release i.e release increasing effect up to a certain RG/D and then at higher RG/Ds releases decreasing effect. The corresponding turning points from ascending to descending part were 0.45 for tragacanth and 0.55 for acacia gum. Beyond these values both gums decreased the release with different efficiency. From release decreasing point of view tragacanth was much more efficient than acacia gum as it was evident from steeper slopes of its descending efficiency curves. The most suitable kinetic model for tragacanth release was zero order one with rate constant of 0.0007 - 0.0011 fraction/min whereas Weibull and log probability models were applicable for acacia matrices.Conclusion: Because of zero order kinetic as well as stronger release retardation efficiency the tragacanth matrices were superior to acacia matrices.

Objectives: Atherosclerosis is a disease of the vascular system that produces a gradual deposition of lipids in large and medium arteries. This disease is the most common cause of death in the world. The increase in cholesterol is an important factor in development of atherosclerosis. Epidemiological studies have shown significant and positive affinity between total cholesterol and LDL cholesterol of serum by the formation of these diseases, but this affinity is negative about HDL cholesterol. It is reported that plant extracts contain flavonoids which are effective for the reduction of serum cholesterol. Silybum marianum of Asteracea family and fumaria vaillantii of fumariacea family contain flavonoid compounds. In this study we have evaluated the effect of hydroalcoholic extract of these plants on the level of serum cholesterol.Methods: 20 male rabbits were randomly divided in four experimental groups. Through 45 days, 4 groups were fed with standard food, hypercholesterolic food, hypercholesterolic food with Silybum marianum extract and hypercolesterolic food with fumaria vaillantii extract respectively. Then total cholesterol (TC), LDL cholesterol, HDL cholesterol and triglycerides (TG) were measured before and after experimental periods of 1 and 2 months of. The aorta was removed for assessment of atherosclerosis plaques.Results: The results indicate that in the third and fourth group the extracts of both plants reduce the amount of TC, LDL and TG but the amount of HDL augment.Conclusion: Therefore the extracts of Silybum marianum and fumaria vaillantii can be effective inhibited the development of atherosclerosis.

Objectives: Several studies indicate that central serotonergic neurons have important role in morphine analgesia and tolerance. The aim of this study was to investigate possible role of 5-HT1A receptors by chronic administration of buspirone (partial agonist of 5- HT1A receptors) in producing analgesic effect and on development of tolerance to analgesic effect of morphine using hot plate test.Methods: Experiments were performed on adult male mice weighing between 20 and 25 g. The control mice (n=8) had daily i.p. injection of morphine (5mg/kg/day). In the vehicle and test groups before injection of morphine (5mg/kg/day, i.p.), we injected vehicle of buspirone (saline normal: 0.5 ml/kg/day, i.p.) and buspirone (5, 7.5 and 10 mg/kg/day, i.p.) respectively and the hot-plate test just before and 30 minutes after the morphine injection performed once every 5 days. Experiments were continued for 5 days after the attainment of tolerance to analgesic effect of morphine. In the another three groups, we injected only buspirone (5, 7.5 and 10 mg/kg/day, i.p.) and the hot-plate test just before and 30 minutes after the buspirone injection performed once every 5 days for the evaluation of the analgesic effect of buspirone in chronic uses.Results: Chronic injection of buspirone (5, 7.5 and 10 mg/kg/day, i.p.) significantly delayed tolerance to morphine analgesia (p<0.05). In addition, chronic administration of buspirone (5, 7.5 and 10 mg/kg/day, i.p.) produce significant analgesic effect (p<0.05).Conclusion: The results confirmed the important role of 5-HT1A receptors in analgesia and the development of tolerance to morphine and may dissolve clinical problems due to long duration of opioides administration. However, the exact mechanism of interaction between serotonergic and opioidergic systems is not clear and remains to be elucidated.

Objectives: Considering nitric oxide (NO) as one of important molecular regulators in genital organs, we examined its effects on histo-morphologic changes in the rat ovary.Methods: 40 rats were divided in 5 groups of 8 upon observing vaginal plaque that has been considered as day zero of pregnancy. Control group, normal saline, L-NAME, L-Arginine and L-NAME + L-Arginine groups. Except the control group the remaining groups received normal saline (2 ml / kg / ip), L-NAME (20 mg / kg / ip), LArginine (200 mg / kg / ip) and a mixture of the same doses of L NAME + L- Arginine, respectively on the 3rd, 4th and 5th days of pregnancy. On the 18th day of pregnancy the rats were anesthetized by diethyl ether and then paralyzed by cutting the spinal cord.After laparotomy the ovaries were fixed in 10% formalin and after tissue sample preparation, general (H + E) and specific (PAS) staining was performed. The histo-morphological changes were observed by optical microscopy and the necessary photographs were taken.Results: Degenerative changes and dissemination were observed in most parts of ovaries of L- Arginine group as well as reduction in growth and weight of the rats. Ovarian volume and number of corpus Luteum were also reduced in this group.Conclusion: It seems that NO induces inhibition of cell growth in the pregnancy period and can interfere with normal functions of the ovary.