Vol. 11 No. 2 (2011)
Articles
Abstract: Background: Inflammatory bowel disease (IBD) refers to idiopathic inflammatory diseases of the intestine, principally ulcerative colitis and Crohn’s disease. IBD is characterized by chronic inflammation in the mucosal membrane of large intestine. 5- ASA is the gold standard for the treatment of IBD and when searched for a better 5- ASA prodrug, a novel mutual azo prodrug was designed and synthesized. Methods: A mutual prodrug was synthesized by coupling p-phenetidine with salicylic acid. The stability of this prodrug in HCl buffer, in phosphate buffer and in rat fecal matter were monitored. Results: The chemical structure of mutual prodrug was characterized by physical and spectroscopic techniques using FTIR, UV/Visible, 1H-NMR and 13C-NMR spectra. In vitro kinetic studies in HCl buffer (pH 1.2) showed negligible release of 5-ASA and p-phenetidine, whereas in phosphate buffer (pH 7.4) only (22.04 %) release was observed over a period of (6 hr.). In rat fecal matter, the hydrolysis of mutual prodrug was almost complete (77.96 %), with a half-life of 182.67 min, following zero order kinetics. Conclusion: The mutual prodrug was split in colon by the action of bacterial azoreductase into 5-ASA and p-phenetidine that constitute two anti-inflammatory compounds with different mechanisms of action. Therefore, this mutual prodrug is a promising colon specific prodrug for IBD and worthy of further study.
Abstract: Objective: Carcinoembryonic antigen (CEA) is a protein found in many types of cells associated with tumors and the developing fetus. The main use of CEA is as a tumor marker, especially with intestinal cancer. This study was designed to evaluate the effect of surgery and chemotherapy on the level of CEA. Patients and methods: The study was carried out in Al-Jamhoory Teaching Hospital in Mosul from January to July 2010. Thirty patients with colorectal carcinoma were treated by surgical removal of the cancer and chemotherapy. Blood samples were taken from the patients one week before surgery and other blood samples were taken one week after surgery. Third blood samples were taken after one week of the first cycle of chemotherapy. Serum carcinoembryonic antigen, ALP (alkaline phosphatase), ALT (alanine aminotransferase), total serum bilirubin (TSB), and albumin were estimated from the samples. Results: After surgery serum CEA and WBCs were decreased significantly (P < 0.001). Serum ALP was also decreased significantly (P < 0.05), while serum ALT, TSB, and albumin were not changed significantly after surgery compared with the results before surgery. After chemotherapy, serum CEA and WBCs decreased significantly (P < 0.001) compared with the results after surgery. At the same time, serum ALP, ALT, TSB, and albumin did not change significantly after chemotherapy. Conclusion: Surgical removal of tumor decreased CEA level, but it did not normalize. Serum CEA can be used as a marker for the effectiveness of the chemotherapy on colorectal cancer.
Abstract: Background: Diltiazem HCl is a calcium channel blocker drug used in the treatment of angina pectoris and hypertension. Objective: To prepare a sustained release diltiazem HCl capsule by complexation with polystyrene sulfonate strong cation exchange resin (dowex®50wx4) as a complexing and retarding agent. Methods: The effect of stirring time and drug: resin ratio on diltiazem HCl loading on dowex®50wx4 was studied. Drug resin complexes were characterized by Fourier Transform Infrared (FT-IR) spectroscopy. The release of drug from the complexes was examined in pH 1.2 and pH 6.8 separately in comparison with pure drug and with commercially available sustained release products Tildia® 120mg capsule and BITildiem ® 120mg tablets Results and conclusion: Most efficient loading was obtained using 1:2 and 1:2.5 drug:resin ratio with stirring time of 60 and 30 minutes respectively. The resultant complexes only retard the release of diltiazem HCl when compared with pure drug while the sustained release product was obtained by coating the complex with carnauba wax and the retardation increased as a function of wax concentration. 20% of wax coated complex gave the release profile approximately similar to the marketed sustained release product of diltiazem HCl, Bi-Tildiem® (Sanofi-France) 120 mg tablets.
Abstract: Aim: To assess serum level of malondialdehyde (MDA) and total antioxidant status (TAS) as a representative of oxidative stress in patients with generalized epilepsy and to evaluate the therapeutic effect of the antioxidant (vitamin E and vitamin C) on the levels of MDA,TAS and frequency of seizures attacks after two months therapy. for a period of two months as a supplementation therapy. Subjects and Methods: The study was conducted in Iben-seena Hospital in Mosul city-Iraq. Fifty three patients with generalized epilepsy were included in this study (32 male and 21 female). The study included 40 apparently healthy subjects, age and sex matched as a control group. Initially from both the patients and controls, blood samples were taken. Another blood samples were taken from the patients 2 months after vitamin E and vitamin C treatment, blood samples were analysed for serum MDA and serum TAS. Result: Serum MDA was found to be significantly higher ( P
Abstract: Objectives: The purpose of this study was to investigate the histopathological changes in Swiss albino rats liver and lung tissues resulted from the oral administration of the antituberculous drugs rifampicin and isoniazid. Materials and Methods: The study was conducted on 24 adult rats aged 2.5-3 months weighing 200-250 g randomly distributed into four groups(6 animals for each), the first group served as a control group while the remaining three as test groups. The rifampicin group was treated with 50 mg/kg B.W. once per day for 60 days, the isoniazid group was treated with 25 mg/kg B.W. once per day for 60 days, the rifampicin and isoniazid groups were treated with 50, 25 mg/kg B.W. respectively once per day for 60 days. Results: Giving rifampicin alone orally once daily for 60 days caused fatty degenerative and necrotic changes in the liver in addition to proliferative lesions and emphysema in the lung. Rats receiving isoniazid alone orally once daily for 60 days showed similar degenerative and necrotic changes in liver and lung but of lower intensity. Whereas those receiving rifampicin and isoniazid combination for 60 days showed pathological changes similar to those induced when each of the two types of antituberculosis drugs was given alone but of more intensity. Conclusion: Rifampicin and isoniazid showed clear histopathological changes in the rat's liver and lung tissues when given separately ; however, changes where more intense when givenin combination.
Abstract: Objective: To evaluate the effect of oral estrogen replacement therapy (ERT) in healthy postmenopausal women on lipid profile, body mass index (BMI), blood pressure, and blood glucose; and on postmenopausal symptoms. Subjects and Methods: This prospective cohort research was carried out over a period of eight months, from Jun 2007 to February of 2008. Fifty six postmenopausal women (mean SD age of 53.3±3 years; mean menopausal period, 5 years); previously diagnosed by gynecologist were involved in this study. Thirty six postmenopausal women were treated with oral conjugated equine estrogen (CEE) (premarin®) 0.625 mg daily for two months. Twenty postmenopausal women were served as control and received daily dose of placebo. Results: In postmenopausal women treated with conjugated equine estrogen, serum total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) were decreased significantly as compared with placebo, while there was no significant change in the serum level of high-density lipoprotein cholesterol(HDL-c). In both groups, estrogen induced changes in plasma triglyceride and reduced the size of LDL particles. These observations suggest that the plasma TG increase may reduce the size of LDL particle. CEE lowered blood pressure, decreased fasting blood sugar and increased BMI of postmenopausal women . Significant positive correlation was found between the BMI and total blood cholesterol whereas significantly negative correlation was found between the BMI and LDL of treated postmenopausal women. CEE effectively alleviated bothersome symptoms of postmenopausal women such as hot flushes, night sweat and vaginal dryness. Whereas, it has no detectable effects in attenuating bone pain. Conclusion: CEE causes change in lipid profile, BMI, blood pressure and attenuates bothersome symptoms in postmenopausal women.
Abstract: Objective: The purpose of this study was to synthesize three new derivatives of metoclopramide by diazotization and replacement reactions and then to quantify in vitro their protection effects on blood cholinesterases using chlorpyrifos as a potent inhibitor. methods: The three new metoclopramide derivatives were synthesized via Sandmeyer reaction, the chemical structures of these derivatives were identified by physico-chemical and spectroscopic (U.V. and FTIR) techniques. Results and conclusion: The results of in vitro evaluation of their human cholinesterases inhibition and protection against chlorpyrifos indicated that the (OH) functional group binds to cholinesterase (ChE) at the same organophosphorous (OP) binding site and shows some competition and protection ability but not to a significant degree, while the (Cl and I) functional groups bind to the ChE at site differs from OP binding site, as well as the (I) functional group has more selectivity for enzyme moiety and binds more strongly than the (Cl) group, so that shows more ChE inhibiting ability
Abstract: Objective: To assess the changes of cerebrospinal fluid (CSF) acetyl cholinesterase (AChE) activity in children with acute bacterial meningitis in comparison to healthy age and sex matched controls. Patients and methods: Out of 41 cases admitted to Alkhansaa pediatric and dilivery hospital (Mosul city) between January 2010 and July 2010, 28 cases proved to be a case of Haemophilus influenzae meningitis, 13 child proved lack from any type of meningitis with age and sex matched subjects taken as a control group. Initially from all of the studied children (patients and controls) about 5 ml CSF samples were taken and assayed for appearance, leucocytes, red blood cells, sugar, protein and AChE activities by spectrophotometric method. Results: There were a significant increase in CSF WBCs count, RBCs count, protein levels, AChE activity with a decrease in CSF glucose level for children with acute bacterial meningitis in comparison to the control group. Conclusion: There is an important value for measurement of CSF AChE activity for confidential diagnosis of children with acute bacterial meningitis specially for those with equivocal decision by using the traditional parameters.
Abstract: Objective: A simple, sensitive, and accurate indirect spectrophotometric method for the determination of bisacodyl in pure form and in some of its pharmaceutical preparations. Method: The method is based on the oxidation of bisacodyl by iron (III), and subsequent complexation of iron (II) with o-phenanthroline. Results: Forming a red-colored complex (ferroin) having the maximum absorbance at 510 nm. Beer’s law is obeyed in the concentration range of 0.5-5 µg/ml. The molar absorptivity and sandell’s sensitivity were 1.55×104 L.mol-1.cm-1 and 0.0233µg.cm-2 respectively. The relative standard deviation (RSD) was less than 1.5 (n=11). The limits of detection and quantitation are 0.083 and 0.25 µg.ml-1 respectively. Conclusion: The method is applied successfully for determination of bisacodyl in environmental water samples and in some pharmaceutical formulations (tablets and suppositories). A statistical comparison of these results with those of official method shows good agreement and indicates no significant difference in the precision.
Abstract: Background: Toxoplasmosis is an infection caused by the protozoan parasite Toxoplasma gondii. This parasite can be transmitted via blood transfusion. Cytomegalovirus (CMV) is a herpes virus that can cause many complications and mostly transfer via blood transfusion. The aim of this study was to evaluate the percentage of risk of infections that could occur due to blood transfusion. Subjects and methods: Ninety blood donor samples were randomly obtained from central blood bank of Mosul city and investigated for IgM of toxoplasmosis and CMV by the serological method ELISA, IgM. Results: ELISA test for Toxoplasma gondii IgM test showed 3% seropositive and for CMV showed 10% seropositive. Conclusion: The results indicate a risk of infection with toxoplasmosis and CMV via blood transfusion.
Abstract: Objective: The aim of this study was to examine the metabolism of donepezil via N – oxidation of donepezil HCl in vitro, and the kinetic studies at a temperature similar to that of the human body. Methods: Direct reaction of donepezil with hydrogen peroxide and formic acid at room temperature, the N – oxide undergoes a series of rearrangements, the reaction was followed by ultraviolet at λmax= 268 nm at 37 °C. The donepezil N- oxide was also tested as potential cholinesterase inhibitor using electrometric for cholinesterase determination. Results: According to the present work , the structure of donepzil N- oxide was elucidated using spectroscopic analysis , also , in vitro kinetic study at 37 °C using ultraviolet spectrophotometer at λmax = 268 nm showed that the reaction proceeded at a first order reaction . Biologically, the compound was found to inhibit both plasma and erythrocyte cholinesterase activities in vitro .. Conclusion: We concluded that the N- oxide of denepezil undergoes a series of rearrangements, the reaction followed first order at 37 °C. It has a potential anticholinesterase activity
Abstract: Objectives: To compare between the qualitative estimation of biochemical markers Point-of-Care testing) with the quantitative estimation of the same markers in the diagnosis of acute coronary syndrome (ACS). Design: Case-series study. Setting: This study was carried out in coronary care unit in Ibn- Sena Teaching Hospital in Mosul city from January to November, 2008. Participant: Sixty five patients with acute coronary syndrome (ACS) presented with chest pain. Main outcome measures: Three cardiac markers (Creatine kinase (CK-MB) activities (marker of necrosis), myoglobin (marker of muscle injury), and troponin I (marker of necrosis), were estimated qualitatively (near the patient= Point-of-Care testing), and quantitatively, and the results were compared. Kappa test was used for the association between the quantitative and qualitative test results. Results: The case-series study showed correlation of attributes between qualitative estimation results of troponin I, myoglobin and CK-MB and quantitative estimation results of the same parameters in (88.9%) tests. Conclusion: The early diagnosis of ACS might be facilitated by the use of qualitative point-of-care testing based on CK-MB, troponin I and myoglobin tests.
Abstract: Objective: To evaluate the effect of olanzapine therapy on serum immunoglobulin levels (IgA, IgG, IgM) in male schizophrenic patients after 2 months of treatment by olanzapine at a daily dose of 20 mg. Patients and Methods: Twenty-eight patients with schizophrenia were included in this study, assessment of each case was done by a psychiatric, also included a 30 healthy subjects as a control group. Serum immunoglobulin concentrations were determined for both patients and controls by Mancini Radial Immuno-diffusion method using immunoglobulin kits. For the patients group and after 2 months therapy with olanzapine at a fixed daily dose of 20 mg, serum immunoglobulins were determined again using the same method for the assay. Results: No significant difference was found between serum levels of immunoglobulin (IgA, IgG, IgM) in schizophrenic patients before therapy in comparison to controls. Also insignificant difference was found between serum immunoglobulin levels (IgA, IgG, IgM) in schizophrenic patients after 2 months of olanzapine therapy and the controls. By comparing serum immunoglobulin levels in patients with schizophrenia before and 2 months after starting olanzapine therapy, no statistically significant difference was found. Conclusion: Olanzapine as atypical antipsychotic may not have an influence on the humoral immune response as reflected by the immunoglobulin levels (IgA, IgG, IgM)