Vol. 25, November, 2007

viagra livraison 48h 1/25 Formulation and evaluation of secnidazole or doxycycline dento-oral gels for the treatment of periodontitis

S.E. Abd El-Hady, *M.A. El-Nabarawi and H.A. Gad

Department of Drug Technology, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt, *Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt

Local delivery of antibiotics has been shown to be effective in reducing periodontopathic microorganisms. The purpose of this study is to formulate gels containing secnidazole or doxycycline hydrochloride that could be used in the treatment of periodontitis by direct periodontal intrapocket administration. Different mucoadhesive polymers (cellulose derivatives, carbopol and Eudragit) were used as bases for the prepared gels. The prepared formulations were evaluated for their in vitro drug release, rheological behavior and mucoadhesive force. Increasing the concentration of each polymer increased the viscosity, mucoadhesion and the time required for 30%, 50% release of the original mass of each drug. Formulations that offered an appropriate balance of the above examined parameters were selected for microbiological evaluation. Microbiological studies on selected formulations showed better release of the two drugs (expressed as inhibition zones) than the commercial products of chlorhexidine gel (Elugel ®) and miconazole nitrate emulgel (Miconaz®).

 

2/25 THE PHYSIOLOGICAL STIMULATING EFFECT OF DAIDZEIN OR DAIDZIN ON AGE-RELATED BONE CHANGES IN FEMALE ALBINO RATS

N.E.M. Shaheen.

Zoology Department, Art, Science & Education, University College for Women, Ain Shams University

The present study aimed to investigate the expected effect of aging and the possibility of treatment with isoflavones (daidzein and daidzin) on several biochemicalmarkers related to the growth rate and bone turn-over. Senile female albino rats (55-60 weeks) were divided into (6) groups (10 female rats each): Control adult intact (G I), Control senile intact (G II), Senile rats treated with low dose daidzein (50 mg/100 g. b. w.) (GIII), Senile rats treated with low dose daidzin (50 mg/100 g. b. w.) (GIV), Senile rats treated with high dose daidzein (100 mg/100 g. b. w.) (GV) and senile rats treated with high dose daidzin (100 mg/100 g. b. w.) (GVI). The present results revealed that calcium, phosphorus and magnesium contents of bones declined with aging in female senile rats, but their contents were elevated in their serum and treatment with daidzein or daidzin induced a marked improvement in all above parameters. The decrease in alkaline and acid phosphatase activities, total protein and albumin contents in female senile which were ameliorated after these treatment.Parathyroid hormone (PTH) concentration increased while serum calcitonin and oestradiol hormones reduced with aging. After treatment with daidzein or daidzin a significant decrease was observed in PTH, but calcitonin and oestradiol increased significantly.

levitra bezugsquellen 3/25 HYPOGLYCEMIC AND HYPOLIPIDEMIC EFFECTS OF GINSENG IN DIABETIC RATS.

E.T. Mohamed and N.M. Fahmy

Health Rad. Res. Dept., National Center for Radiation Research and Technology (NCRRT)

Diabetes is a predominant public health concern that has increasedsteadily worldwide. Increased free radical generation and oxidative stress are hypothesized to play an important role in pathogenesis of diabetes and its late complications. Panax ginseng is one of the most popular natural tonics used in oriental countries. It exhibits a wide range of pharmacological actions such as antiaging, immunoenhancement, antistress, antitumor and antioxidant. This study was designed to examine the hypoglycemic, hypolipidemic and antioxidant defense of ginseng in streptozotocin induced diabetes in rats. Ginseng was given orally at a dose level of 10 mg/kg body wt for 5 weeks. Diabetes was induced in rats by a single intraperitonealinjection of Streptozotocin at a dose of 80 mg /kg body wt. Blood samples were collected from all groups for the determination of serum fasting blood glucose (FBG), glycated hemoglobin (HbA1c), total cholesterol (TC), high density lipoprotein (HDL), low density lipoprotein (LDL) and triglycerides (TG). Also liver thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD) and catalase (CAT) were determined. In diabetic rats there was a highly significant increase in the percentage of HbA1c and concentration of FBG, TC, TG and LDL and in liver TBARS. On the other hand, significant decrease in the activity of liver SOD and CAT was observed. Treatment of the diabetic rats with ginseng caused a significant decrease in the percentage of HbA1c and in the serum level of FBG, TC, TG, liver TBARS and significant increase in the activity of liver SOD and CAT compared to the diabetic rats. On the basis of these observations, one could conclude that ginseng showed an encouraging hypoglycemic, hypolipidemic as well as antioxidant properties and could be considered as a valuable candidate in the reversal of diabetes complications.

4/25 BIOLOGICAL ROLE OF DATES FORMULA IN PREGNANT RATS

A.I.S. Ahmed, A.A. Bakry, E.F. Sayed-Ahmed and A.M. Bayomy

Dept of Special Food & Nutr, FTRI, ARC, Giza, Egypt.

Dates (D) are preferable to be added to the pregnant diet, hence the scientific performance of pregnancy was improved and the metabolic system as well. A modest amount of this food component (D) at level of 25% was capable to control the physiological complications such as elevation in blood cholesterol, glucose and triglycerides. The overall data have got the assumption that productivity and healthy offspring were reached when a special plant protein source with a unique antioxidant structure (AC) was incorporated at a level of 20%. The other food component of the best diet that met the highest productivity and healthy both mothers and kids were the skimmed milk (SM) of 10% plus another source for CHO such as sweet potatoes (SP) at a high ratio of 35%. In addition, liver function as well as organs such as liver, heart and kidney histology was kept at most acceptable or optimal parameters. Seemingly, controlling glycemia is the most important role of dieting. Gestational diabetes, however, is associated withsignificant pregnancy complications such as macrosomia, perinatal mortality and prematurity. It seems that little higher ratio of proteins, i.e. 18%, most of which are plant, with plenty amount of vegetable CHO and less than 10% fat in oily form with an adequate amount of minerals and vitamins. That are particularly found in D and SP, are important food toleration for pregnancy. Obesity, which occurred with delivery, in connection with blood parameter was examined. Fortunately, the diet of choice according to the above mentioned role gave also the optimal body weight (BW) measurement. In fact, pregnancy is a special physiological case with a specific metabolic hormonal balance. More investigation is needed to observe the role of food additives used to support this kind of hormonal status.

mr ledoux viagra 5/25 INTERRELATION BETWEEN ADIPONECTIN LEVEL AND INSULIN SENSITIVITY IN OBESE SUBJECTS

S.T. Melek**, T.M. Khairy*, M.R. El-Sharkawy** and G.A. Amin***

Biochemistry Dept.* and Basic Medical Science Dept. **NODCAR. Cairo;

Int. Med. Dept., Med. Res. Inst. ***, Alex. Egypt.

Insulin resistance is associated with increased risk of type-2-diabetes, which is also strongly accompanied with obesity. It is important to understand the link between obesity and lack of insulin sensitivity. Adiponectin is a member of the adipocytokines family of fat-cell secreted proteins, which exclusively expressed in adipose tissue. It may turn out to be a promising insulin sensitizing agent. Thirty obese subjects (BMI>30kg/m2) and 10 normal, apparently healthy individuals (BMI<20kg/m2) were participated in this study. The fasting plasma glucose and insulin levels in obese subjects were significantly higher than that in normal subjects, while plasma adiponectin was significantly decreased in obese subjects in comparison to the control group. Also, it was found that plasma adiponectin was negatively correlated with fasting insulin, plasma glucose, plasma triglycerides, body mass index, waist and hip circumferences, and positively correlated with HDL-cholesterol. From the recorded results, it was found that adiponectin level was decreased in obese subjects, at the same time insulin also appeared to suppress adiponectin secretion. These findings suggested that adiponectin level could play a physiological role in insulin sensitivity.

vardenafil france 6/25 FORMULATION AND EVALUATION OF FLOATING SYSTEMS OF METRONIDAZOLE

A.A. Kassem, M.A. Marzouk and D.A. Attia

Pharmaceutics Department, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.

A strategy is proposed for the treatment of Helicobacter pylori associated gastric ulcers using floating systems loaded with metronidazole, to prolong its gastric retention time for 6 hours. The design of this delivery system was based on the development of non-effervescent single unit floating system of metronidazole (floating capsules) and multiple-unit system (floating hollow microspheres or microballoons). The in-vitro drug release of capsule preparations was controlled using different polymers like, HPMC 15000, HPMC 4000, and pectin in different drug: polymer ratios. For comparison purpose, immediate release reference capsules were used. While Eudragit S100 polymer was used for microballoon preparations in different drug: polymer ratios by using a modified emulsion solvent evaporation method. The prepared capsules were evaluated for their kinetic analysis of metronidazole release, as well as their uniformity of drug content. The prepared microspheres were physically evaluated for their micromeretic, particle size and morphology characteristics.

cialis et myelome 7/25 PREVALENCE OF FUNGAL INFECTIONS AMONG PATIENTS WITH CHRONIC RESISTANCE ASTHMATIC BRONCHITIS

A. Farghaly*, I.M. El-Kholy** and L.M. Yousef***

Air Forces Hospital*   Ain Shams Specialized Hospital** and Sohag University***

Fungal infections among asthmatics were described to be in the ratio of 10-30%. However, the true incidence among difficult to treat asthmatics has not been studied enough. Difficult to treat asthma has many causes among them is fungal colonization, specially the development of Allergic broncho-pulmonary aspergillosis (ABPA). Fortypatients with difficult to treat asthma have been included in this study. They were subjected to skin prick test, Determination of IgE level, fungal culture, tests for pathogenecity, beside   routine examination and pulmonary function testing. Clincal specimens were used for fungal culturing and serum samples were used for serological tests. Among the 40 patients included in our study, 14 (35%) proved to have fungus retrieved from there sputum cultures. These included 4 cases viagra et tylenol A. fumigatus, 3 cases cialis generique pharmacie paris A. niger, 3 cases cialis quel site A. flavus, 1 case c'est quoi le cialis A. nidulans, 1 case test achat viagra A. terreus and 2 cases showed mixed species of Aspergillus colonization (A.niger and A.flavus). Positive serology was evident in 5 cases, with proven Computed Tomography changes path gnomonic of   Allergic broncho-pulmonary aspergillosis in 4 cases.

8/25 VOLATILES, LIPOIDS AND BIOACTIVITY OF THE FLOWERS OF OENOTHERA SPECIOSA NUTT. CULTIVATED IN EGYPT

H. H. Eid and A.A. Sleem*

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Egypt.

* Pharmacology Department, National Research Center, Giza, Egypt.

The volatile constituents of the fresh flowers of Oenothera speciosa Nutt. (Onagraceae) cultivated in Egypt, obtained by two methods (hydro-distilled and absolute volatiles) were comparatively investigated as regards composition and antimicrobial activities. The hydro-distilled floral volatiles (HV) and floral absolute volatiles (FAV) were identified and quantitated by GC/MS analysis. Fifty two and thirty seven components were identified under the experimental conditions, accounting for 97.85% and 83.53% of their total chemical composition, respectively. Aliphatic hydrocarbons were found predominant in HV (amounting to 76. 54 %), the major being tricosane, pentacosane and eicosane (29.36%, 23.17% and 21.97%, respectively). Meanwhile, FAV showed a higher percentage of oxygenated compounds than HV reaching up to 69.83% and 19.8%, respectively and being dominated by esters (43.33% and 10.28%, represented by 6 and 10 components), among which 9, 12, 15 octadecatrienoic acid, methyl ester was the major (41.53% and 7.68%, respectively). On the other hand, the unsaponifiable matter (USM) and fatty acids methyl esters (FAME) of the hexane concrete were identified and estimated by GC/MS analysis. Hydrocarbons dominated the identified constituents in the USM, reaching 77.41% with pentacosane (55.89%) as the major and followed by eicosane (17.29%).The unsaturated fatty acids reached up to 48.06% and were dominated by 9,12,15 Octadecatrienoic acid (α-linolenic acid , ω-3, 45.41%), while the saturated ones constituted about   44.12%, being mainly composed of hexadecanoic acid ( 30.41%). The antimicrobial screening revealed that FAV exhibited broad spectrum activity; meanwhile, HV showed a weak effect on Escherichia coli, Bacillus subtilis and a moderate action against Mycobacterium phlei and the tested fungal strains. The minimum inhibitory concentrations (MIC) for HV were also determined. However, the hexane concrete exerted a weak activity against Bacillus subtilis, powerful activity against Mycobacterium phlei comparable to that of Ofloxacin and a marked antifungal effect. Moreover, the hexane concrete of the flowers showed significant anti-inflammatory,analgesic and anti-hypercholesterolemic actions, as well as, moderate antipyretic and anti-ulcer effects.

9/25 EFFECT OF CERTAIN EXCIPIENTS ON THE BIOAVAILABILITY OF RANITIDINE HYDROCHLORIDE.

B.M. El-Houssieny*, N.A. Soliman* and M. Elrais**

*Department of Pharmaceutics and **Department of Chemistry, National Organization of Drug Control and Research (NODCAR )

A critical issue in the processing of drug physical and coground mixture is to elucidate the microstructure of the resulting product. Differential Thermal Analysis (DTA) was used as screening technique for assessing the compatibility of ranitidine Hcl with some excipients currently employed in certain pharmaceutical formulations namely, CaCl2, NaNO3, Na2 So4, Zn So4 and Silica Gel in both physical and Coground mixture in ratios of 1:1, 1: 2 and 1: 3 of drug to excipients respectively,aiming for overcoming its hygroscopic nature. The resulting best formula, namely sodium sulphate – ranitidine hydrochloride mixture in ratio 1:1 in both physical and coground mixtures were undergo pharmacokinetic study on rabbits in comparison with the commercial product. Statistical analysis of the pharmacokinetics data revealed that coground mixture gave more relative bioavailability than the physical mixture and commercial product.

10/25 FEFFECT OF FORMULATION ADDITIVES ON THE DISSOLUTION OF MELOXICAM FROM LIQUISOLID TABLETS

S.A. El-Gizawy

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Tanta, Tanta, Egypt

The purpose of this research is to enhance in vitro dissolution of meloxicam using the liquisolid technique.For poorly soluble, highly permeable (class II) drugs, such as meloxicam, the rate of oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Different formulations of liquisolid tablets were prepared by applying a 3 x 22 full factorial design to investigate the influences of three independent variables on the in vitro drug dissolution: type of vehicle (A), drug/ vehicle ratio (B) and type of disintegrant (C). In all formulations, the ratio of microcrystalline cellulose (carrier) to silica (coating material) was 20:1. The dissolution behavior of meloxicam from liquisolid tablets and reference tablets was studied at different pH values (1.0 and 6.8). The time required for 50% drug dissolution (T50) was selected as a dependent variable. The results of multiple linear regression analysis revealed that the type and nature of vehicle was the most significant variable (P<0.001) affecting T50 of drug dissolution as indicated by its high coefficient values in both dissolution media. Liquisolid formulations containing propylene glycol and polyethylene glycol-400 showed significantly (P<0.05) decreased drug dissolution whereas those containing Tween-80 showed significantly (P<0.05) increased drug dissolution compared with the reference product. Factor B showed significant effect (P<0.05) on drug dissolution in pH 6.8 only. Factor C showed no significant effects on drug dissolution in both media. The optimized formulation delivered meloxicam in a Higuchi pattern at dissolution rates of 0.143 and4.172 mg min-1/2 in pH 1.0 and 6.8, respectively. This formulation contained Tween 80 as a vehicle, a drug/vehicle ratio of 1:4   and sodium starch glycolate as a disintegrant. In conclusion, the liquisolid technique could be a promising alternative tool to increase the dissolution of poorly water-soluble drugs.

11/25 THE PUTATIVE EFFLUX TRANSPORTER GENE YCCS OF ESCHERICHIA COLI: CLONING, EXPRESSION AND FUNCTIONAL ANALYSIS.

M.M.M. Aboulwafa

Department of Microbiology and Immunology, Faculty of Pharmacy,

Ain-Shams University

The study was conducted to clone and overexpress the yccS gene and to analyze some phenotypic characters of E. coli strains lacking or containing single or multicopies of the gene. The respective gene was amplified by PCR from E. coli chromosomal DNA and cloned into the expression plasmid pBAD24. Then, transformed into E. coli DH5a for recombinant plasmid propagation. The recombinant plasmid with an insert displaying the yccS sequence was introduced into E. coli BW25113 to give the recombinant strain BW25113-pBAD24-yccS.Functional analysis of yccS gene was conducted using two approaches. The first depended on the use of two E. coli strains, one containing a single copy of chromosomal yccS (wild type BW25113) and the other is devoid of that gene (BW25113 D yccS). Testing the susceptibilities of both strains to several carboxylic acids, parabens, and some phenols in Luria Bertani (LB) broth showed that the most active agents against the tested strains were p-nitrophenol (MIC 1.56 mM) and butyl paraben (MIC 3.9 mM). The MIC values of the different tested agents against the wild strain BW25113 were either similar to or higher by a factor not exceeding two fold than those recorded against the knock out mutant BW25113   D yccS. In M9 medium, the lowest MIC values (less 1 mM) were recorded with 2,3,4 trihydroxybenzoic acid, 2,3 dihydroxybenzaldehyde, 2,5 dihydroxybenzaldehyde. The relative resistance of both tested strains to 2,4 dihydroxybenzoic was nearly unaffected by change of growth medium pH. The second approach used for testing the role of yccS gene in resistance to different agents relied upon the overexpression of this gene using a multicopy expression plasmid (pBAD24). In most cases the MIC values for the overexpression strain were approximately similar to those obtained using the knockout mutant strain. With all the tested agents, both the overexpression strain and the control strain exhibited similar MIC values or they differed by a factor not more than 2 fold. Measuring the expression of yccS gene revealed a basal constant level of yccS expression as determined by reverse transcriptase-PCR under the tested conditions. No evidence was found showing that yccS gene is involved in resistance to the different tested agents. Accordingly, the substrate specificity of the yccS gene may be verynarrow. The significance and biological relevance of this gene is still need more studies. The apparent nonessential nature of yccS gene could opens the way for constructing a reduced strain, which will provide a clean background for functional genomics studies and a more efficient background for use in biotechnology applications.

12/25 PHARMACEUTICAL STUDY ON BIPHENYL DIMETHYL DICARBOXYLATE SOLID DISPERSION.

B.M.E. Yousef

National organization for Drug Control and Research.

Solid dispersion of biphenyl dimethyl dicorboxylate (BDDS) with polyethylene glycol 6000 in ratios 1:1, 1:2 and 1:3 (drug: carrier, w/w), were prepared by both fusion (I) and solvent evaporation method (II). BDDS of 1:1 w/w prepared by solvent evaporation method (II) display the best solubility and dissolution results of the tested ratios. The incorporation of different surfactants namely, polysorbate 80, Brij 52, sodium lauryl sulphate (SLS), cremophore EL and RH in (1&2%) to the previous BDDS (II) revealed that an almost instant and complete dissolution was obtained with dispersion incorporating SLS (2%). Differential thermal analysis (DTA) study indicate the role of the selected carrier and surfactant in decreasing the crystallinity of BDD and complexability. Furthermore, the bioavailability of BDDS (II) in comparison to commercial product was investigated. The extent of absorption of BDDS as reflected by AUC0-6 and AUC0- was significantly different following the administration of BDDSII compared to commercial product.

13/25 FORMULATION AND IN-VITRO AND IN-VIVO EVALUATION OF METRONIDAZOLE SUSTAINED RELEASE FLOATING TABLETS

E.E. Zein El-Deen, S.A. El-Gizawyand N.M. Borg

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Tanta, Tanta, Egypt

The purpose of this study is to design oral metronidazole hydrodynamically balanced tablets with sustained release characteristics for the treatment of Helicobacter pylori associated gastric ulcers. This is to prolong the gastric residence time and to maintain high local drug concentrations for a long duration. Matrix tablets were prepared by direct compression using the hydrocolloid hydroxypropyl methylcellulose. The formulated tablets were optimized to maximize drug content while maintaining buoyancy and a pharmaceutically accepted hardness range. The optimized formula contained 150 mg metronidazole, had a bulk density less than 1.0 gm/cm3 and a hardness range of 5-6 Kg, showed immediate floating, and remained float until complete dissolution. The optimized tablets were evaluated in vitro and in vivo in comparison with conventional tablets of the same dose strength. The drug release profile in 0.1N hydrochloric acid was found to follow Higuchi’s equation from both floating and conventional tablets. Floating tablets exhibited significantly retarded release as compared with conventional tablets. The results showed that sustained-delivery of metronidazole was achieved while the tablet remained float for more than 6 hours. Single dose oral pharmacokinetic study revealed that floating tablets significantly improved the bioavailability of metronidazole in healthy volunteers as compared with conventional tablets. The average relative drug bioavailability from floating tablets in relation to conventional tablets was 1.22. Floating tablets showed a significant increase in the MRT of metronidazole reflecting in vivo sustained drug delivery.

14/25 PHYSIOLOGICAL CHARACTERIZATION OF E. COLI STRAINS LACKING AND HARBORING THE PUTATIVE EFFLUX TRANSPORTER GENE YDHK

M.M.M. Aboulwafa

Department of Microbiology and Immunology, Faculty of Pharmacy,

Ain Shams University

The study aimed to clone, overexpress and characterize the E. coli putative efflux transporter gene ydhK. This gene was amplified by PCR and ligated into the pBAD24 expression vector plasmid. The recombinant E. coli strains BW25113-pBAD24-ydhK and BW25113 D acrAB, emrAB, emrD-pBAD24-ydhK were then generated and physiologically characterized. Two E. coli strains, BW25113 having one copy of ydhK gene and its knock out mutant BW25113 D ydhK were also included in this study. Using Phenotype Microarray (PM) plates, the tested strains BW25113 and BW25113 D ydhK could well utilize 71 out of 190 carbon sources, 40 out of 95 of nitrogen sources, 49 out of 59 phosphorous sources and 35 tested sulfur sources. In all cases no pronounced difference in the utilization pattern was observed between the two tested strains. The susceptibility of E. coli strains BW25113 and its mutant W25113 D ydhK was determined against certain antibiotics, basic dyes and aromatic carboxylic acids. Among the tested antibiotics, clinafloxacin proved to be the most active where its MIC did not exceed 0.03 mg/ml for both strains. Among the tested aromatic carboxylic acids, the dihydroorotic acid with MIC of ≤ 0.02 mM showed the highest antimicrobial activity with both strains. The antimicrobial activity of the tested acids followed the order dihydroorotic acid > fusaric acid > gallic acid. All the tested dyes exhibited MIC values not exceeding 5 mM. For all the tested agents it was found that in most cases both the wild type strain and the ydhK mutant exhibited similar MIC values and in few cases the values for both strains differed by a factor not exceeding 2. The susceptibility of the E. coli strains BW25113-pBAD24 and BW25113-pBAD24-ydhK to certain antimicrobial agents, mineral salts, carboxylic acids and other tested compounds was determined. For all the tested agents it was found that both strains exhibited either similar MIC values (most cases) or they differed by a factor not exceeding 2 (few cases). Introduction and expression of the recombinant plasmid pBAD24-ydhK into the E. coli strain BW25113 D acrAB, emrAB, emrD did not change its susceptibility to two carboxylic acids, gibberellic and fusaric acids. Accordingly, it can be concluded that the E. coli ydhK gene is nearly not involved in the utilization of several carbon, nitrogen, phosphorous and sulfur sources. Also, this gene has minor effect on the resistance phenotypes of ydhK gene-harbouring strains to multiple agents. Constructing ydhK gene deficient strains can be advantageous as a background for research studies and in biotechnology applications.

15/25 POTENTIOMETRIC DETERMINATION OF PAROXETINE HYDROCHLORIDE IN PRESENCE OF ITS DEGRADATION PRODUCT

S.M. Riad

Analytical Chemistry Department, Faculty of Pharmacy, 6 October University

Three novel techniques for the selective determination of Paroxetine Hydrochloride (PX) in presence of its oxidative degradation product were described. The first and second techniques were the construction and electrochemical response characteristics of novel poly (vinyl chloride) matrix membrane sensors for Paroxetine cation based on the use of the ion- association complexes of this cation with tetraphenyl borate and ammonium reineckate counter anions as ion exchange sites in a plasticized PVC matrix, either as ion selective membranes or as microcoated wire sensors. The third technique was a carbon paste electrodes. All these sensors were prepared and fully characterized in terms of composition, life span, usable pH range, response time and temperature. The electrodes were applied for the potentiometric determination of (PX) in pure form, pharmaceutical preparations and in presence of its oxidative degradation product. These sensors showed a near-Nernstian slopes of 58.3, 57.9, 60.0, 58.5, 57.7 and 57.5 mv over the concentration ranges of 1.0 x 10-6-1.0 x 10-2 M, 5.0 x 10-7-1.0 x 10-2 M, 5.0 x 10-7-1.0 x 10-2 M for techniques one, two and three, respectively. The electrodes exhibit good selectivity for (PX) with respect to a large number of inorganic cations, organic cations, sugars and amino acids. The proposed electrodes offer the advantages of simplicity, accuracy and applicability to turbid and colored samples.

16/25 THE SIDE EFFECTS OF DIABETES AND THE MODULATIVE ROLE OF OCIMUM GRATISSIMUM EXTRACT ON SOME BIOMARKERS OF FEMALE ALBINO RATS

N.E. Mohamed

Zoology Department, College for Women (Art, Science & Education),

Ain Shams University.

This study was conducted to elucidate the therapeutic modulative effect of herb Ocimum on alloxan-induced diabetic female rats. Adult female rats were divided into five groups: intact group (GI), control alloxan-diabetic group (GII), hyperglycemic rats treated with 200mg/kg b.w. (low dose) of Ocimum (GIII) hyperglycemic rats treated with 400 mg/kg b.w. (high dose) of Ocimum (GIV) and female rats injected with 200 mg/kg body weight (low dose) of Ocimum only (GV). A significant increase in the serum glucose level of alloxan-diabetic rats was noticed, while after treatment with Ocimum a highly significant improvement in serum glucose level was recorded. After treatment with Ocimum a highly significant enhancement was observed in oestradiol hormone level, testosterone level, AST and ALT activities in all treated groups especially at high dose of Ocimum. Highly significant improvements were achieved in serum total cholesterol and triglycerides concentrations in all treated groups especially at high dose. Slight changes were observed in calcium, phosphorus, total protein and albumin contents in serum in all treated groups. Also HB% and hematocrite showed highly significant improvement with the two doses of Ocimum.

17/25 SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME AMINO ACID DERIVATIVES OF THIAZOLIDINE-4-CARBOXYLIC ACID.

F.S.M. Ahmed, A.M. El-Gazzar, S.A. Shedid and K.A. El-Sharkawy*

Chemistry Department, Faculty of Science, Al-Azhar University, Nasr

City, Cairo, Egypt.

*Organic Chemistry Department, Faculty of Pharmacy, M.S.A

University, El-Wahat Road, 6 October City, Giza, Egypt.

The synthesis of different N-Acetyl-thiazolidine-4-carbonyl amino acid methyl esters, corresponding amino acid hydrazides; dipeptide methyl esters and dipeptide hydrazides (2-33) are described. Some of the synthesized compounds are found to possess antimicrobial activities towards different microorganism included gram-positive, gram-negative microorganisms Bacillius subtilis, Bacillus pumilus, Pesudomonas aeruginosa and Escherichia coli and the fungi Candida utilis


18/25 ANTIWARTS ANTHRAQUINONES FROM ASPHODELUS MICROCARPUS SALZM. ET VIVI GROWING IN EGYPT

A.I. Mohammed, E.A. Genady and U.Y. Shaheen

Pharmacognosy Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

Two new anthraquinones; 10,7’-bichrysophanol (3) and chrysophanol-8-O-methyl ether (4) were isolated for the first time from the tubers of A. microcarpus, together with two known anthraquinones; chrysophanol (1) and asphodelin (2), which were isolated previously from the same plant. The structures of all isolated compounds were established on the basis of spectroscopic data. All compounds (1-4) were evaluated for antiviral activity against warts. Compound 3 appeared to be the most active.

19/25 SYNTHESIS AND IN VITRO EVALUATION OF SOME -2- CHLORO-4-(SULPHONYL AMINO ACID DERIVATIVES) BENZYLIDINE HYDANTION AS ANTIMICROBIAL AGENTS.

F.S.M. Ahmed, A.H. El-Gazzar, R.A. El-Sayed and K.A. El-Sharkawy*

Chemistry Department, Faculty of Science, Al- Azhar University, Nasr City, Cairo, Egypt and *Organic Chemistry Department, Faculty of Pharmacy, MSA University , El-Wahat Road, 6 October City, Giza, Egypt

The synthesis of different 2-choro-4-(sulphonyl-amino acid methyl esters) benzylidine hydantion, amino acid hydrazides, dipeptide methyl esters and dipepide hydrazides (2-37) are described, some of the synthesized compounds were found to possess antimicrobial activities toward different microorganisms included gram-positive, gram-negative microorganisms Bacillius subtilis, Bacillus pumilus, Pesudomonas aeruginosa and Escherichia coli and the fungi Candida utilis.

20/25 BIOCHEMICAL PROPERTIES AND PURIFICATION OF A SPECIAL PROTEINASE PRODUCED BY STREPTOMYCES CRATERIFER

T.M. Khairy and F.H. Ahmed*

Biochemistry Department and *Microbiology Department, NODCAR, Egypt

A purified enzyme with proteolytic activity was produced by S. craterifer, which was isolated from soil sample obtained from Abu-Rawash, Guiza. The conditions for maximum yield of the proteolytic activity were studied using a shaking culture at pH 7.5 after 6 days incubation at 30 °C. The medium which was supplemented with D-glucose as a carbon source and ammonium bromide as a nitrogen source gave the maximum proteolytic activity. Precipitation with ammonium sulphate, followed by DEAE-cellulose column chromatography and gel-filtration using sephadex column was used. These processes resulted in having a purified enzyme with specific activity 2043 u/mg protein corresponding to 9-fold purification of the crude extract. For detection of the molecular weight of purified enzyme, polyacrylamide gel electrophoresis was applied. The data showed that, the obtained proteinase has a molecular weight of 50 KDa.

21/25 INVESTIGATION OF BACTERIAL PATHOGENS ISOLATED FROM BONE AND JOINT INFECTIONS AND THEIR ANTIMICROBIAL SUSCEPTIBILITIES

H.M. Hefni*, A.M. El-Srsawy***, W.N. El Tayeb** and T.R. Mohamed*

Department of Microbiology and Immunology, Faculty of Pharmacy (Boys),

*Al-Azhar University and ** Misr International University, Egypt

***Department of the Orthopedic Surgery, El Sahel Educational Hospital, Cairo, Egypt

Bacterial infections play an important role in bone and tissue pathology. Not only they cause osteomyelitis and septic arthritis but also they play an effective role in causing osteoporesis. This study included 108 clinically diagnosed patients. 54 (50%), 35 (32.41%), 11 (10.19%), and 8 (7.41%) patients suffered from osteomyelitis, infectious arthritis, autograft, and metal implant infections, respectively. Eighty-nine of 108 (82.41%) cases were confirmed by positive bacterial culture. 49/89(55.06%), 25/89(28.09%), 9/89(10.11%), and 6/89(6.74%) microbiologically confirmed cases were suffering from Osteomyelitis, infectious arthritis, autograft, and metal implant infections, respectively. Bone and joint infections were more frequent in males (69.7%) than in females (30.3%) (P<0.001) and more frequent among cases 21->60 years (93.26%) than among cases <1-20 years (6.74%). 2/89(2.25%), 4/89(4.49%), 29/89(32.58%), 20/89(22.47%), 13/89(14.61%) were orthopedic infections in age groups <1-10 yrs, 11-20 yrs, 21-30 yrs, 31-40 yrs, 41-50 yrs, 51->60 yrs, respectively. One hundred and twenty nine bacterial isolates were recovered. One hundred and two isolates (79.07%) were aerobic-facultative anaerobes, whereas 27 isolates (20.93%) were strictly anaerobic. 19/108(17.6%), 32/108(29.63%), 57/108(52.78%) were the frequencies of cases with negative culture, positive monomicrobic culture, and positive polymicrobic cultures, respectively. Aerobic isolates were either single isolate per infection 27/102 (26.47%) or polymicrobic culture per infection 75/102 (73.53%). The predominance of polymicrobic infections containing anaerobes 22/27(81.48%) over infection with single anaerobe 5/27(18.52%) was noticed among anaerobes (P<0.0001). The frequencies of Gram +ve aerobic-facultative anaerobic isolates, as arranged in descending order, were: 41.67%, 31.25%, 20.83%, 6.25% for S. epidermidis, S. aureus, St. pyogenes and Enterococcus spp, respectively, with statistical significant differences between the frequency of S. epidermidis and each of St. pyogenes and Enterococcus spp. (P<0.05). Staphylococcal spp. the most frequently isolated (72.92%), when compared with other species (27.08%) with significant difference (P<0.0001). Gram –ve aerobic-facultative anaerobic isolates as arranged in descending frequencies, were: 40.74%, 22.2%, 14.8%, 11.11%, 5.56%, 5.56% for P. aeruginosa, E. coli, K. pneumonia, P. mirabilis, H. influenzae, and Salmonella spp, respectively, with significant differences between the frequency of Ps. aeruginosa and others (P<0.05). On the other hand, Gm-ve anaerobic isolates, arranged in descending order, were: 29.6%, 22.2%, 22.2%, 14.8%, 11.11% for B. fragilis, F. nucleatum, P. melaninogenicus, P. intermedia and E. corrodens with significant difference between B. fragilis and E. corrodens (P<0.05). Neither Gm +ve anaerobes nor yeast or molds were detected. Experimental septic arthritis was induced in mouse using a selected Ps. aeruginosa isolate. Histopathological and X ray examination of the infected area were indicative of both osteomyelitis and osteoarthritis. Antimicrobial susceptibility testing of all aerobic-facultative anaerobic and anaerobic isolates wascarried out. More than 90% of all aerobic–facultative anaerobes were sensitive to amikacin, ciprofloxacin, norfloxacin, ofloxacin, whereas 70-80% of anaerobes were sensitive to the above antimicrobial agents. In addition, 40-60% of all isolates were sensitive to cefoxitin, cefotaxime, rifamycin, clindamycin and chloramphenicol. Finally, 10-30% of all isolates were sensitive to ampicillin, erythromycin, penicillin and vancomycin.

22/25 GASTROPROTECTIVE POTENTIAL OF AN ANTIANGINAL DRUG (NICORANDIL) IN INDOMETHACIN AND ALCOHOL-INDUCED ULCERS IN RATS

M.A. El-Moselhy, *N.M. Abdel-Hamid and **S.R. Abdel-Raheim

Pharmacology and *,**Biochemistry Departments, *College of Pharmacy and **College of Medicine, Minia University, Egypt

Background: Despite the fact that dietary habits and lifestyles are incredibly advancing, gastric ulceration still a terrible complaint. Extensive use of non-steroidal anti-inflammatory drugs (NSAIDs) and alcohol, in addition to stress, are all predisposing factors for ulcers. Most of medical treatments are always time consuming, not efficient nor satisfactory to the patients. Cardiovascular patients always need NSAIDs, or mostly can’t quit alcohols, while using many cardiovascular drugs. Aim of the study: To study the possible benefit of a common nitrogen oxide donor, anti-anginal drug, nicorandil [N-(2-hydroxyethyl) nicotinamide nitrate ester], in managing acute gastric ulcers in two models. Five groups of male Wistar rats were assigned as, control, indomethacin, nicorandil plus indomethacin, ethanol and nicorandil plus ethanol groups. Mucosal content of lipid peroxidation and nitric oxide (NO) in addition to serum tumor necrosis factor – alpha (TNF-α) were determined. As well as, gastric mucosal lesions were assessed as ulcer indices and mucosal histology was studied to pursue the drug effects on the tissue level. Results: Our study revealed that both indomethacin and alcohol induced gastric ulcers occur mainly through up-regulation of gastric mucosal lipid peroxidation, local tissue inflammation, leukocytic infiltration and necrosis. Both ulcerogens significantly elevated TNF-α and decreased NO, initiating ulcer formation. Nicorandil pre-treatment depicted a higher preventive index in indomethacin (89.8 %) and alcohol-induced (77.7 %) acute ulceration. On the tissue level, it also protected the gastric mucosa combating leukocyte infiltration and tissue congestion. Nicorandil protected tissue necrosis through decreasing oxidative stress, elevating NO levels and down-regulating the ulcerogen- induced TNF-α elevation and improved sub-mucosal blood supply. We conclude that nicorandil may be a suitable bimodal treatment for cardiovascular patients who are at high risk of gastric ulcers by using variable analgesics to alleviate possible cardiac pain episodes, and probably frequent doses will offer a more established and long-lasting protection.

23/25 CEREBROPROTECTIVE CONSTITUENTS, ANTIMICROBIAL ESSENTIAL OIL AND DNA-FINGERPRINTING OF CHAMAECYPARIS LAWSONIANA (A. MURRAY) PARL. GROWN IN EGYPT

D.R. Abou-Hussein, *M.F. Schaalan and *S.M. Abdelraouf

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

*Pharmacology and Toxicology Department, Faculty of Pharmacy,

Misr International University, Cairo, Egypt.

A bioactivity-guided investigation of the different extracts of the needles of Chamaecyparis lawsoniana (A. Murray) Parl. revealed the highest antioxidant activity of the ethyl acetate-soluble fraction. The cerebroprotective activity of this fraction against ischemia/reperfusion-induced oxidative stress was, for the first time, investigated in rat brain. Pretreatment with the tested fraction (100 mg/kg b.wt., p.o./7days) was able to increase the total antioxidant capacity and reduce the cytosolic SOD activity of the ischemia/reperfused rats. The glutathione and MDA contents, as well as, LDH activity were significantly decreased and rendered to their normal levels. Column chromatographic bioactivity-guided fractionation of the ethyl acetate fraction resulted in isolation, for the first time, of three flavonols: kaempferol (I), afzelin (II) and quercetrin (III) identified via spectral analysis. HPLC quantification revealed that quercetrin was the major constituent (amounting to 19.6%). Moreover, quercetrin exhibited the highest antioxidant activity, followed by afzelin then kaempferol. The essential oil of the fresh needles of the plant under investigation, prepared by hydrodistillation (0.16% v/w), exerted a moderate antimicrobial activity; MIC of the oil against the tested microorganisms was determined. Hydrocarbons constituted the majority of the oil composition (91.72%), as revealed by GC/MS analysis, with the predominance of monoterpenes (83.06%) among which α-pinene was prevalent (69.59%). DNA of Chamaecyparis lawsoniana (A. Murray) Parl. was amplified using six decamer primers as a contribution to the characterization of the plant.

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