Vol. 24, July, 2007.

1/24 PREPARATION AND EVALUATION OF TOPICAL DIBUCAINE EMULSION GELS

S. Mansour

Department of Pharmaceutics, Faculty of Pharmacy, Ain Shams University,

Cairo, Egypt

Emulsion gels are vehicles of potential for delivery of many drugs. The purpose of this work was to formulate the local anesthetic dibucaine into topical emulsion gel dosage form with optimum rheological properties, drug release rate and stability. Dibucaine emulsion gels formulations were prepared using either Carbopol 934 or hydroxypropylmethyl cellulose (HPMC) as gelling agents; liquid paraffin, jojoba oil or isopropyl myristate as oil phase; and blends of either (Span 40/Tween 40) or (Span 40/Brij 58) as emulsifying agents. The prepared emulsion gels were evaluated for their physical appearance, rheological properties, drug release, physical stability and in vivo local anesthetic activity using pin-prick test. All the prepared emulsion gels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability and pH values. They exhibited non-Newtonian shear thinning-behavior with thixotropy. The viscosity and the drug release rate were affected by the type of gelling agent, the type of oil used and the surfactant blend. Emulsion gels formulations prepared using jojoba oil showed the highest drug release rate. The drug release from all formulations was found to follow diffusion-controlled mechanism. Physical shelf stability study indicated that all the prepared dibucaine emulsion gels formulations were stable except some formulations have shown separation of oil droplets after one year of shelf storage. In conclusion, dibucaine base emulsion gels formulations composed of either (Carbopol 934 /jojoba oil/ Span 40/Tween 40) or (HPMC /jojoba oil/ Span 40/Tween 40) were the formulae of choice since they showed superior drug release rate, rheological characteristics, shelf stability over one year of storage with promising local anesthetic effect compared to the commercial Neocaine® cream.

2/24 THE EFFECT OF HIGH AND LOW DOSES OF GARLIC INTAKE ON ANTIOXIDANT, HAEMATOLOGICAL, AND HISTOPATHOLOGICAL PROFILES IN ALBINO RATS

F.E. Agha, *M.M. Ali, *S.Y. Mostafa, *S.E. Gawish

Department of Forensic Medicine and Toxicology, Faculty of Medicine for Girls, El-Azhar University,Cairo, Egypt.

*Department of Biochemistry, Division of Genetic Engineering and Biotechnology, National Research Centre, Cairo, Egypt.

The effects of subchronic garlic intake on various endogenous antioxidant enzymes and lipid peroxidation on the liver and kidneys of albino rats were investigated. Male albino rats were fed with fresh garlic homogenate daily by gavage in two different doses (250 and 1000 mg/kg/day) for 30 days. After this period, rats were sacrificed and blood, liver, and kidneys were harvested for biochemical estimation. In comparison to saline-treated rats, the 250 mg/kg/day dose significantly reduced thiobarbituric acid reactive substances (TBARS) as indication to depletion of lipid peroxidation with significant increase in superoxide dismutase (SOD), glutathione peroxidase (Gpx) activities, and reduced glutathione (GSH) level, while there was insignificant increase in catalase (CAT) activity, with no histopathological changes in both organs or in the blood picture profile. In contrast, treated with high dose of garlic (1000 mg/kg/day) significantly reduced endogenous antioxidants (CAT and SOD) with increase in TBARS levels. Also, there was decrease in liver and kidney GSH, while there was no change in the activity of Gpx in both liver and kidney. The high dose of garlic also caused marked histopathological and haematological changes. The liver showed focal and diffuse necrosis, focal fatty changes with congested central vein while focal cloudy degeneration of renal convoluted tubules was observed in kidney. These changes were accompanied with increase in all kidney and liver function tests except ALP which revealed significant decrease in activity. Moreover erythrocytic count, haemoglobin concentration and haematocrite value were significantly decreased at the high dose. The results suggest that garlic in low doses has the potential to enhance the endogenous antioxidant status, although at higher doses a reversal of these effects is observed. The present study also highlights the potential ability of a high dose of garlic to induce morphological changes in the liver and kidney, indicating that garlic may not be safe if taken in excess.

 

 

3/24 FORMULATION, IN VITRO AND IN VIVO EVALUATION OF OCULAR POLOXAMER-BASED CIPROFLOXACIN HYDROCHLORIDE IN SITU FORMING GELS

M. Mansour, S. Mansour, N.D. Mortada and *S.S. Abd ElHady

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

The purpose of this study was to develop poloxamer-based in situ gelling formulations of ciprofloxacin hydrochloride aiming at prolonging corneal contact time, controlling drug release, enhancing ocular bioavailability and increasing patient compliance. The in situ forming gels were prepared using different concentrations of poloxamer 407 (P407) and poloxamer 188 (P188). Mucoadhesives such as hydroxypropylmethyl cellulose (HPMC) or hydroxyethyl cellulose (HEC) were added to the formulations to enhance the gel bioadhesion properties. The prepared formulations were evaluated for their in vitro drug release, sol-gel transition temperature, rheological behavior and mucoadhesion force. The in vivo antimicrobial efficacy of selected ciprofloxacin hydrochloride in situ gelling formulations were studied on infected rabbit's eyes and compared with that of the marketed conventional eye drops. The gelation temperature of the prepared formulations ranged between 28.00 and 34.03C. Increasing the concentrations of P407, HPMC and HEC increased the viscosity and mucoadhesion force of the preparations and decreased the in vitro drug release. Ciprofloxacin hydrochloride in situ forming gel formulae composed of P407/P188/HPMC (18/13/1.5 % w/w) and P407/P188/HEC (18/13/0.5 % w/w) showed optimum release and mucoadhesion properties, improved ocular bioavailability as evidenced by an enhanced therapeutic response compared to the marketed conventional eye drops.

 


4/24 BIOEQUIVALENCE STUDY OF ORALLY DISINTEGRATING TABLETS OF DICLOFENAC POTASSIUM

A.A. Ammar

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy for Girls, Al-Azhar University, Nasr City, Cairo, Egypt.

Orally disintegrating tablets of diclofenac potassium(DP) were prepared using direct compression after incorporating a superdisintegrant such as Pharmaburst B2 (diluents, disintegrant), avicel PH102 (disintegrant)aspartame, saccharin (sweeteners), magnesium stearate , and purified talc (lubricant). The tablets were evaluated for various physical parameters, oral disintegration time and in vitro drug release. In vivo study were performed to study the DP orally disintegrating tablets as test formulation and Cataflam 25mg tablets, as reference formulation from the market to 6 healthy volunteers. After an overnight fast, the volunteers received a single oral dose (25 mg) of each formulation, following an open, randomized, two-period crossover design, with a fourteen-day washout interval between doses. Blood samples were obtained over a 24-h interval post-dosing, and were analyzed for their DP content by HPLC-UV. No adverse effect was reported for any of the administered formulations. Various pharmacokinetic parameters (ie, Cmax, Tmax, area under the curve [AUC0-24], and mean residence time MRT) and relative bioavailability were determined. The prepared DP orally disintegrating tablets were within the USP limits for weight variation and friability limit, determined tablets hardness was found to be 3kg ± 0.37. The tablets disintegration time and dissolution rate are suitable for its site of administration. The oral bioavailability study revealed DP orally disintegrating tablet was absorbed at twice as fast as reference Cataflam tablet (Tmax 0.5 and 1hr) respectively, with 87% relative bioavailability.

 

 

5/24 TRITERPENE ACIDS FROM THE STEM EXUDATEOF SCHINUS MOLLE L.

E. Abdel-Sattar, A.E. Khaleel* and F.M.H. Harraz

Department of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Kingdom of Saudi Arabia.

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

A new triterpene acid, (13α,14β,20R,24Z)-3-oxo-26-hydroxyolanosta-8,24-dien-21-oic acid (mollinoic acid) (3) along with isomasticadienonalic acid (1), an epimeric aldehydes mixture of (13α,14β,17α,20R,24Z)-3α-hydroxy-21-oxolanosta-8,24-dien-26-oic acid (2) and its 20S epimer (2a), 3-epi-isomasticadienolic (4) and masticadienonic acids (5) were isolated from the chloroformic extract of the exudate from the stem and stem branches of Schinus molle L.   (F. Anacardiaceae) cultivated in Saudi Arabia. The structures of the isolated compounds were elucidated by analysis of their 1H-NMR, 13C-NMR, 1H-1H-COSY, HMQC, HMBC, NOE, NOESY and mass spectra.

 


6/24 Overview of antifungal and anti-toxigenic activities of various teas and coffee extracts

E.M. El-Taher

Regional Center for Mycology and Biotechnology, Al-Azhar University,

Cairo, Egypt.

This study aimed to overview the activity of green tea, black tea and coffee extracts against the fungal growth and aflatoxins production by Aspergillus parasiticus strain. Different concentrations of the extracts (0.3 1.0, and 3.0%) were tested for their ability to inhibit the fungal growth and the aflatoxin production. The three extracts were found to have an inhibition action on the growth of the tested fungi genera (Alternaria alternata, Penicillium sp, Trichoderma sp, Candida albicans, Saccharomyces cerevisiae and Aspergillus parasiticus) as well as their effects to inhibit the aflatoxin production by A. parasiticus. These effects were in dose dependent manner. It could be concluded that these extracts may be useful as antifungal and anti-mycotoxins production although green tea was the most effective extract in this respect.

 

 

7/24 BACTERIOLOGICAL STUDY ON CAESAREAN SECTION SURGICAL SITE INFECTION

M.A. Abo-Shadi and A.O. Al-Mutrafy

Microbiology department, faculty of Science/Taibah University

(Al-Madinah Al-Munawarah, KSA)

This study was carried out on fifty-five cases suffering from SSI aftercaesarean section from a maternity and children Saudi hospital between Dec. 2006 andApril 2007 to determine the incidence of nosocomial surgical site infections after cesarean section, identify some caesarean section- specific risk factors for SSI, evaluate the use of Gram-stain for the prediction of subsequent microbiological culture results, investigate the agents responsible for this infection and to study their antimicrobial susceptibility pattern. Of the 55 specimens processed, 53 (96.4%) were stained with Gram-stain while 51 (92.7%) were culture positive. Incidence of post-caesarean SSIs was 3.3%. There were a total of 67 bacterial isolates comprising of 49 Gram-negative bacilli and 18 Gram-positive cocci (p<0.001). Organism rate per lesion was 1.3. The most common isolate was Escherichia coli followed by Klebsiella spp. and Pseudomonas aeruginosa. Our SSI cases (stained withGram-stain) had membranes ruptured prior to operation ≥12 hours (41.8%), duration of operation exceeding 60 minutes (78.2%), emergency operation in 80% and 41.8% were obese. The most effective antibiotics for S. aureus were vancomycin and cephalothin (85.7%); vancomycin for coagulas-negative Staphs (100%); norfloxacin and aztreonam for E. coli (94.7%) and norfloxacin, teinam and aztreonam For Klebsiella spp. (100%). Pseudomonas aeruginosa was most sensitive to amikacin (91.7%). 58 (86.6%) isolates showed ampicillin resistance, 44 (65.7%) showed cephalothin resistance, 43 (64.2%) showed cotrimoxazole resistance, and 29 (43.3%) showed ampicillin-clavulanic acid resistance.

 


8/24 INCIDENCE OF TOTAL AFLATOXINS AND OCHRATOXIN A IN POULTRY FEED AND FEEDSTUFFS IN EGYPT.

S.T. Moubarak

Dept. of Hygiene and Management, Fac. Veterinary Medicine, Cairo University.

Two hundreds and sixty three samples were screened for both total aflatoxins and ochratoxin A during the period from 2001 through 2006. The samples included 102 feedstuff samples and 161 poultry finished feed samples. These included 19 yellow corn, 19 soya bean meal, 7 corn gluten meal, 3 meat meal, 10 fish meal, 28 poultry concentrates and 16 bone meal samples. Finished feed samples included 104 broiler, 38 layer, and 19 broiler breeder finished feed samples. 61.9 % of the examined feedstuffs and poultry finished feed samples contained less than 5 PPB total aflatoxins. Only 28.5 % of the examined samples contained from 5 to 9 PPB and 7.6 % of the samples contained from 10 to 20 PPB total aflatoxins. Only 1.9 % (5 samples), exceeded the permissible limit of 20 PPB for total aflatoxins. 55.1 % of the examined feedstuffs and poultry finished feed samples contained less than 5 PPB ochratoxin A, 20.9 % of the examined samples contained from 5-9 PPB, and 20.5 % contained from 10-20 PPB. Nine samples (3.4 %) contained more than 20 PPB ochratoxin A . One hundred and fifty five out of 263 samples showed a mixed contamination of both total aflatoxins and ochratoxin A. The results underscored importance of ochratoxin A compared to total aflatoxins and emphasized that mycotoxins are usually found in combination.

 

 

9/24 IN -VITRO ANTIBACTERIAL ACTIVITY OF SOME SPICES COMMONLY USED IN SAUDI ARABIA

M.A. Abo-Shadi

Microbiology and Immunology Department, Faculty of Pharmacy (Girls), Al-Azhar University

Current work/ Microbiology department, faculty of Science/Taibah University (Al-Madinah Al-Munawarah, KSA)

This study was done to evaluate the antibacterial activity of 24 different spices commonly used in Saudi Arabia against five bacterial species (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacillus cereus and Staphylococcus aureus) using agar well diffusion method, compare the sensitivity of those bacterial isolates to various spice extracts and the commonly employed chemotherapeutic agent ampicillin), and also to study effect of grinding and heat treatment on the antibacterial activity of these spices. Out of 24 spice extracts tested, 20 showed antibacterial activity against one or more strains. Garlic, clove, fustet and thyme exhibited the best antibacterial effect (inhibit all the studied bacterial isolates). Black pepper, fennel, mustard and capsicum did not show any antibacterial activity. In general, Klebsiella pneumoniae & E. coli was the most susceptible. On the other hand, Staphylococcus aureus exhibited low degree of sensitivity.

 


10/24 ESTABLISHMENT OF A NEW CLONE OF HePG2 (ZHR) CELL LINE HARBOURINGHEPATITIS C VIRUS GENOTYPE 4

A-R. N.Zekri, M. Hafez* and S.M.R. Radwan**

Immunology and virology Unit, *Cancer Biology Department, National Cancer Institute, Cairo University.

** Microbiology Department, Faculty of Pharmacy, Al- Azhar University.

Hepatitis C virus is a major cause of chronic viral hepatitis. Development of anti-viral strategies has been hampered by the lack of efficient cell systems to propagate HCV in vitro. To establish a tissue culture system for Egyptian HCV strain , a human hepatoma (HepG 2) cell line was tested for its susceptibility to HCV by incubating with a serum from a patient with chronic hepatitis C. Cells and supernatants were harvested at various phases during the culturing period. The presence of HCV- RNA in cells and/or supernatant was examined by nested RT-PCR and Real Time. Infectivity of the released HCV in the culture supernatant was applied on naïve HepG2 cells. It was found that HCV-RNA could be detected intermittently in both cells and supernatant, also HCV-RNA titre showed an increase during the culture period. The fresh cells could be infected by supernatant from cultured infected cells and the viral genome could be detected in cells and supernatant after freezing in liquid nitrogen for about a year. The hepatoma line HepG2 is not only susceptible to HCV but also supports its long –term replication in vitro.

 

 

11/24 MICROBIOLOGICAL MONITORING OF HATCHERY SANITATION

S.T. Moubarak

Dept. of Hygiene and Management, Fac. Veterinary Medicine, Cairo University.

A comparative microbiological evaluation of sanitary practices used in four commercial broiler hatcheries was carried out using open-plate method. The sampling areas included setters, hatchers, egg holding rooms and chick handling rooms. Ten minutes open-plates were made for heterotrophic plate counts, mould and yeast counts and total coliform counts. Higher heterotrophic plate counts were recorded in chick handling rooms (hatcheries B and C). Mould and yeast counts were generally low. Hatchery B showed relatively higher mould and yeast counts in setters, hatchers, egg holding and chick handling rooms. Samples from hatchery D were negative for coliform in all sampling areas in contrast to the other 3 hatcheries. Hatchery D was given an “excellent” sanitary rating. The open plate method was found to be an easy to perform and reliable inexpensive monitoring procedure for hatchery sanitation.

 

 

12/24 ATTENUATION OF GENTAMICIN- INDUCED NEPHROTOXICITY IN RATS BY GRAPE SEED EXTRACT

M.A. Abd El Kader

Biochemistry Department, National Research Center, Dokki, Cairo, Egypt

Gentamicin is widely used and effective antibiotic against sever gram-negative infections. However, its clinical use is limited by its nephrotoxicity in human and animals. Since the pathogenesis of gentamicin-induced nephrotoxicity involves oxygen free radicals, this study was performed to investigate the possible protective effect of grape seed extract (GSE) as antioxidant on gentamicin-induced nephrotoxicity in rats. Twenty-four male Swiss albino rats were divided into four groups of six rats in each one: control group; gentamicin group: rats were treated intraperitoneally (i.p.) with gentamicin sulphate alone (100 mg/ kg/ day) for 6 successive days; GSE group: rats were administered intragastric (i.g.) with GSE (100 mg/ kg/day) for 6 successive days and gentamicint+GSE group: rats were treated 6 days of simultaneous GES and gentamicin sulphate. Biochemical examinations were utilized for evaluation of nephrotoxicity and oxidative stress. Creatinine, urea, potassium and sodium levels were estimated in serum as markers of glomerular filteration rate. Activities of N-acetyl- β- D- glucosaminidase (NAG) and g-glutamyltransferase (g-GT) and level of glucose were measured in urine as markers for tubular damage. Malondialdehyde (MDA), reduced glutathione (GSH) levels & superoxide dismutase (SOD) and catalase (CAT) activities were determined in kidney tissue as index for oxidative stress and antioxidant activities. Administration of gentamicin, induced nephrotoxicity as evidenced by marked elevation in serum creatinine and urea levels associated with decreased level of potassium; increase in urinary activity of NAG and g-GT as well as in urinary excretion of glucose. In addition, gentamicin caused significant increase in kidney content of MDA and significant decrease in GSH concentration & SOD and CAT activities. GSE supplementation for gentamicin- treated rats significantly lowered the elevated serum creatinine and urea levels, inhibited urinary activities of NAG and g-GT and prevented glucosuria. In addition, GSE treatment ameliorated the rise in renal content of MAD and enhanced GSH content as well as SOD and CAT activities. The present work indicates that, GSE with its content of antioxidant proanthocyanidins has potential protective effects against gentamicin nephrotoxicity.

 

13/24 A STABILITY INDICATING ASSAY OF CLOMIPHENE CITRATE USING HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

A.A. Abd El-Rahman*, S.F. El-Menshawe**, and M.A. El-Majri***

*Department of pharmaceutics and industrial pharmacy, Cairo University, Cairo, Egypt.

**Department of pharmaceutics and industrial pharmacy, Beni Suef University, Beni Suef, Egypt.

***Department of pharmaceutics and industrial pharmacy, Great Al-Fateh University for Medical Sciences, Tripoli, Libya.

Clomiphene is used to stimulate ovulation, increase progesterone secretion during the second half of the cycle, and make menstrual cycle lengths more predictable. A novel stability indicating high performance liquid chromatographic (HPLC) method was developed and validated for assay of clomiphene citrate. The HPLC method utilized a C18 reversed phase column and a mobile phase containing a mixture of methanol: acetonitrile: water (30:60:10), pH 5, adjusted with glacial acetic acid and filtered through a millipore filter of 0.45 mm pore size. The mobile phase flow rate and UV detection wave length were 0.9 ml/min and 245nm respectively. The method was linear over the concentration range of 0.5 – 40 mg/ml (r = 0.999827). The method has the requisite suitability, precision and accuracy to assay clomiphene citrate in bulk form and pharmaceutical dosage forms. Degradation products resulting from the stress studies did not interfere with the detection of clomiphene and the assay is stability indicating.

 

14/24 INHIBITION OF PLASMA CHOLINESTERASE BY CHLOROQUINE (RESOCHIN)

M.M. Al-Enazi

Department of Medical Laboratory Sciences, College of Applied Medical Science, Al-Jouf University, P.O. Box 2014, Sakaka, Al-Jouf, Saudi Arabia

Inhibition kinetics of human plasma butyrylcholinesterase (BchE) (acylcholineacylhydrolase, EC 3.1.1.8) by Resochin was studied using butyrylthiocholine (BTch) as a substrate. The enzyme was inhibited by Resochin with an IC50 of 2.2×10-3µM. The type of inhibition and the inhibition constant Ki, were estimated graphically by using Lineweaver-Bruk plots. The initial velocity revealed a mixed-type inhibition by the above-mentioned drug. The secondary plots of inhibition with respect to BTch, indicates a dissociation constant (KI) of 1.25 µM for the enzyme substrate complex (ES). The value of dissociation constant (KI) being greater than inhibition constant (Ki) value, indicates that the non-competitive inhibition is predominant over the competitive inhibition at the substrate-binding site.

 

15/24 MICROBIOLOGICAL QUALITY CONTROL OF NON-STERILE PRODUCTS AND COSMETICS PRODUCED BY SOME EGYPTIAN PHARMACEUTICAL COMPANIES

M.S.E. Ashour, S.M.R. Radwan and R.S.A. El-Dahshan

Faculty of Pharmacy, October University for Modern Sciences and Arts ( MSA), Department of Microbiology & Immunology, Faculty of Pharmacy (Girls),

Al-Azhar University,

This study was carried out to demonstrate the microbiological quality of non- sterile pharmaceutical & cosmetic products produced by some Egyptian companies. For this purpose the following steps were performed: A total of 2660 samples of three different manufacturers and 39 different brand names were analyzed according to the united states pharmacopoeia (USP).the detected growth was identified using gram stain followed by subsequent identification using either conventional biochemical methods or commercial identification kits. PCR was used as an alternative rapid and accurate technique for testing the absence of USP indicator bacteria. None of the four indicator bacteria were detected by both methods. Challenge testing was done, to detect the preservative activity, using microorganisms specified in USP 28. logarithmic reductions were calculated at time intervals and all preserved samples were found to be efficiently preserved according to USP limits. In conclusion, the tested non-sterile pharmaceutical products and cosmetics were of acceptable quality regarding microbial limits and absence of objectionable bacteria as specified in pharmacopoeias (USP, EP).

16/24 EFFECT OF BETA-CAROTENE ON MURINE SCHISTOSOMA MANSONI AS ADJUVENT TO ANTIBILHARZIAL THERAPY.

K.A. Mohamed

Parasitology Department, Faculty of Medicine, Al-Azhar University

(Damiette branch)

b-carotene is a lipid soluble chain breaking antioxidant and is the most common carotenoid in food Eighty mice were included in this study and they were divided into   4 groups: Group (I): (treated infected group) included 20 mice received b-carotene 2mg/kg body wight daily for five consecutive days and then infected with 80±1 S. mansoni cercariae for each mouse. Group (II): (treated non-infected control group) included 20 mice received b- carotene 2mg/kg daily for five consecutive days. Group (III): (infected control group) included 20 mice infected with 80±10 S.mansoni cercariae per-mouse. Group (IV): normal control included 20 mice representing (non-infected non- treated). Scarification of mice was done 9 weeks post infection. we concluded that b-carotene has a protective efficacy against schistosomal infection which can be attributed to its enhancement of gap junction intracellular communication of dermal cells, thus enhance skin integrity that retard or hinder cercarial skin penetration. This resulted in less worm burden and less tissue egg load. b-carotene has an immunoprotective or immunomodulatory effect for hepatic schistosomal pathogenesis which may be through its anti-inflammatory activity, its enhancement of T-lymphocyte proliferation, its-cytotoxic activity, its enhancement of phagocytosis, or both of the above mentioned actions . The immunomodulatory effect of b-carotene on hepatic schistosomal pathogenesis reflected as smaller granulomas with less inflammation and fibrosis contributed in normalization of the elevated serum enzymes AST. b-carotene has no toxic effect as serum proteins and enzymes and did not altered after its administration to normal non infected animals.

 

17/24 EFFICACY OF HORMONAL AND NON HORMONAL TREATMENT METHODS IN OVARIAN DYSFUNCTION IN EGYPTIAN BUFFALOES

*A.A. Nasra and **M.M. Al-Enazi

*Animal Reproduction Research Institute (ARRI), Al-Haram, Giza, Egypt.

**Department of Medical Laboratory Sciences, College of Applied Medical Science, Al-Jouf University, P.O. Box 2014, Sakaka, Al-Jouf, Saudi Arabia

The study was carried out on 67 Egyptian Buffaloes. Rectal examinations accompanied by blood plasma progesterone determinations was performed twice in a 10-days interval to diagnose the mentioned above number of buffalo-cows that were suffering from an ovarian dysfunction cases, they were consequently divided into 4 groups according to treatment regimen: controls; massage; Lugol’s solution; and GnRH. Oestrus, first insemination and total pregnancy rates, artificial insemination (AI) index, and service period length were determined following treatment. The service period in all, treated groups, was statistically shorter (P ≤ 0.05) than in control. The overall results showed that GnRH treatment of ovarian dysfunction affected buffaloes was the most effective method. Other regimens such as Lugol’s solution and uterine as well as ovarian massage could be considered.

 


18/24 MOLECULAR DIFFERENTIATIONS OF SEVERAL KLEBSIELLA PNEUMONIA CLINICAL ISOLATES

K.N. Khatan

Biology-Chemistry Department, Faculty of Radfan Education,

Aden University, Yemen

TheGram-negative Klebsiella pneumoniae is the clinically most important member of the Klebsiella genus. Because it is an opportunistic pathogen for the immunocompromised individuals and more commonly implicated in hospital-acquired such as urinary tract, wound infections, chronic pulmonary disease, enteric pathogenicity, nasal mucosa atrophy, and rhinoscleroma. The alarming emergence of multi-antibiotic resistant strains of K. pneumoniae to a wide-spectrum of β-lactam-β-lactamase inhibitor dictates implementation of accurate strain identification and antibiotic resistance programs in clinical setups. These classical methods for identification of the clinical isolates of K. pneumoniae were based on morphological and metabolic characteristics that empirically did not provide absolute discriminating information. Additional molecular biology techniques such as plasmid profile, cellular protein banding patterns and RAPD-PCR were used to establish the accurate identity of each clinical isolate. However, plasmid profile and the antibiotic susceptibility tests did not provide good differentiating tool between the five clinical K. pneumoniae isolates compared to the RAPD-PCR analysis. Result of this study, clearly demonstrated the capability of RAPD-fingerprint to distinguished the closely related isolates of Klebsiella and hence its qualification to be used routinely for strain speciaition.

19/24 CHEMICAL COMPOSITION AND BIOACTIVITY OF VOLATILE OILS FROM OCIMUM BASILICUM L.var. MINIMUM CULTIVATED IN EGYPT.

W.T. Islam and M. M. Salama.

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

The chemical composition of the hydrodistilled volatile oils from the stem, leaf and inflorescence of Ocimum basilicum L. var. minimum growing in Egypt were investigated by GC/MS analysis, where significant qualitative and quantitative variations were observed. This resulted in the identification of 39, 34, and 39 compounds representing 99.39 %, 100% and 99.70 % of the total components of the essential oils of the stem, leaf and inflorescence, respectively. The plant oils were rich in oxygenated compounds amounting to 74.11%, 70.08% and 69.15% of the total composition of the oils of inflorescence, stem and leaf volatile oils respectively, while the rest were hydrocarbons. The major oil components were localized as follows: linalool (19.34%), estragole (17.91%), cadinol (11.93%), bornyl acetate (7.90%), ocimene <β-> (6.39%) and cadinene < γ->( 5.19%) in stem while estragole (23.82%), linalool (18.60%), 1,8-cineole (11.04%), ocimene <β-> (7.77%), bornyl acetate (7.56%), cadinol (5.35 %)and cadinene < γ->( 3.42%) in leaf and linalool(22.9%), estragole (19.93%), cadinol (10.54 %), bornyl acetate (8.71%), 1,8-cineole (5.57%), ocimene <β-> (5.34%)and cadinene < γ->( 4.21%) in inflorescence. Moreover, the antibacterial activity of the oils of leaf and inflorescence revealed more promising results against all the tested organisms, especially Pseudomonas aeruginosa and Mycobacterium phlei. The cytotoxic activity of the leaf oil against Ehrlich ascites carcinoma (EAC) was the highest effect reported relative to the inflorescence and stem oils. Moreover, the antiwormal activity of the three tested oils exhibited significant potency.

20/24 SYNTHESIS AND STABILITY STUDY OF DIFLUNISAL DERIVATIVE COMPOUND

S.A.Al-Mikhlafi and *A.M. Sabati

FROM

Department of Medicinal Chemistry, Faculty of Pharmacy, Sana'a University

* Department of Pharmaceutics, Faculty of Pharmacy, Sana'a University

The synthesis of 2 -[5-(2, 4–Difluorophenyl) aetamido]-5 –methyl –1, 3, 4 –thiadiazol –salicylamide which designed as potential cox-2 inhibitor and the Preliminarykinetic study for hydrolysis of this compound is discussed in this paper . The compound was prepared from the corresponding 5– (2,4–difluorophenyl)–acetylsalicylic acid and   2–amino–5–methyl–1,3,4–thiadiazole in the presence of N,N-dicyclohexylcarbodiimide (DCC) as coupling agent. The preliminary kinetic study for hydrolysis of this compound and the effect of pH on the rate of hydrolysis in citrate–phosphate–borate/Hcl buffer solution was studied. The structure was confirmed by IR spectra, 1H NMR spectra, and elemental analyses. The compound underwent partial hydrolysis at low and high pH with considerable stability so, provide a chance to be absorbed intact with higher bioavailability, longer half life, and may exerts cox-2 selectivity.

 

21/24 PHYTOCHEMICAL AND BIOLOGICAL STUDY OF ESSENTIAL OILS OF FOUR EUCALYPTUS SPECIES GROWN IN EGYPT

H.H.Eid, *T.A.Ibrahimand **A.A. Sleem

FROM

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University,

Cairo, Egypt.

*Department of Pharmacognosy, Faculty of Pharmacy, King Saud University, Riyadh Saudi Arabia.

**Department of Pharmacology, National Research Center, Dokki, Cairo, Egypt.

The essential oils of the leaves of Eucalyptus ficifolia F. Muell. (1.56%), Eucalyptus camaldulensis F. Muell. ex Miq. var. brevirostris (0.59%), Eucalyptus lehmannii Preiss. (0.1%) and Eucalyptus melliodora A. Cunn. ex Schauer (0.54%) were prepared by hydro- distillation. GC/MS analysis revealed the presence of 25, 28, 31 and 23 compounds in the essential oils of E. ficifolia, E. camaldulensis var. brevirostris, E. lehmannii and E. melliodora, respectively. 22, 24, 26 and 21 compounds were identified representing 99.22%, 98.14%, 97.93% and 99.75% of the total composition of the essential oils of E. ficifolia, E. camaldulensis var. brevirostris, E. lehmannii and E. melliodora, respectively. 1,8-cineole (79.22%) was the major constituent in the essential oil of E. ficifolia, while spathulenol (52.46% and 25.09%) and p-cymene (17.53% and 30.04%) were the major components in the essential oils of E. camaldulensis var. brevirostris and E. melliodora, respectively, in addition to a high percentage of cryptone (21.47%) in the essential oil of E. melliodora. On the other hand, p-cymene (28.23%), α-terpineol (11.88%) and isoborneol (11.54%) were the major constituents in the essential oil of E. lehmannii. The four essential oils under investigation exhibited a significant broad spectrum antibacterial activity against Gram-positive and Gram–negative microorganisms with different potencies compared to standard ofloxacin. The tested essential oils presented a significant antifungal effect except the essential oil of E. melliodora using Amphotericin B as a positive control. The minimum inhibitory concentrations (MIC) of the tested oils were also determined. Moreover, the anti-inflammatory and analgesic effects of the essential oils under investigation were studied where promising results were obtained, especially for Eucalyptus ficifolia and Eucalyptus melliodora.

 

22/24 EFFECT OF SEASONAL VARIATION ON COMPOSITION AND BIOACTIVITIES OF THE ESSENTIAL OIL OF EUCALYPTUS CITRIODORA HOOKGROWN IN EGYPT

S.M. El-Zalabani*, M.M. Koheil**, K.M. Meselhy*,H.A. El-Gizawy**

and A.A. Sleem***.

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

**Pharmacognosy Department, Faculty of Pharmacy, 6th October University, Egypt.

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

The hydrodistilled oils of the leaves of Eucalyptus citriodora Hook (Myrtaceae) were prepared from samples collected along the four seasons viz., winter (January), spring (April), summer (July) and autumn (October). GC/MS was used for qualitative and quantitative analyses. The influence of seasonal variation on the yield and composition of the essential oil was recorded. The oil yield ranged from 3.0 -5.0 % (calculated on dry weight basis) with maximal value in autumn. The oils were lemon-scented and of close physical properties. The essential oils were characterized by a high citronellal content ranging from 31.1-77.9 % of the total oil composition (with maximal percentage in autumn) together with citronellol (12.5-17.0, highest amount in winter) and citronellyl acetate (2.1-14.2 %, highest percentage in spring). Other constituents detected in lower amounts in all the samples were caryophyllene oxide (up to 5.5 %) and trans-caryophyllene (up to 3.5 %). The winter sample was distinguished by the presence of appreciable amounts of cineol (3.45 %), linalool oxide (2.44 %) and sesquiterpenoids. The ethanol (95 %) extract of the leaves, as well as the tested oils exerted significant, although variable, biological effects including: analgesic, anticonvulsant, anti-inflammatory, antipyretic, anti-hyperglycemic and antioxidant. In addition to assessments of the antiwormal and antimicrobial activities of the ethanol extract and oil samples were performed using Allobophora caliginosa and a series of selected microorganisms, respectively.


23/24 Lipoids, Carbohydrates AND IN VIVO bioactivities of Senecio rowleyanus Jacobs

S.S. El-Hawary, A.M. Galal, M.F. Yousif, *A.A. Sleem, and F.N. Kirollos

Pharmacognosy Department, Faculty of Pharmacy, Kasr El-Einy Street, 11562, Cairo University, Cairo and* Pharmacology Department, National Research Center,

Giza, Egypt.

Three compounds were isolated from Senecio rowleyanus Jacobs herb. These were identified as β-amyrin, β-sitosterol and oleanolic acid.Identification of the aforementioned compounds was carried out on the basis of physicochemical characters and spectroscopic analyses, viz.: m.p., and EI-MS. GLC analysis of the unsaponifiable matter revealed the presence of 18 components; the major constituent being triacontane. Sixteen fatty acids were identified as their methyl esters: the major one was methyl palmitate. Investigation of the free sugar content and the polysaccharide hydrolysate was carried out by HPLC analysis. Five free sugars were detected and identified as: glucose, arabinose, sucrose, galactose, and mannose. The polysaccharide hydrolysate afforded 5 sugars: xylose, galactose, arabinose, glucose, and mannose. The aqueous and alcoholic extracts were subjected to in- vivo studies. The LD 50 of both extracts was 3.1 and 2.9 g/kg b.wt., respectively, in the acute toxicity test. However long term administration (8 wks) of the tested extracts caused a significant rise in the liver enzymes (AST and ALT) and a significant reduction of blood sugar. The tested extracts were screened for anti-inflammatory, analgesic, antipyretic and hypoglycemic activities.

24/24 PATTERN OF BACTERIAL ANTIBIOTIC RESISTANCE IN NORTHERN AREA ARMED FORCES HOSPITAL (KSA)

S. Al-Yousef and M.A. Al-Azzouny *

Department of Microbiologist at Northern Area Armed Forces Hospital (KSA)

* Department of Clinical & Chemical Pathology, Faculty of Medicine,

Benha University

There is a general consensus that antimicrobial resistance has emerged as an important variable related to patient outcomes in hospitals. This retrospective study aimed to determine the percentage of different pathogenic microorganisms and identify local endemic antimicrobial resistance patterns among common bacterial isolates from patients in Northern Area Armed Forces Hospital (NAAFH) during the years 2005 and 2006. In this work, all clinical specimens were cultured and antimicrobial susceptibility testing was performed using standard microbiological methods. A total of 2796 and 2854 isolates were registered during 2005 and 2006 respectively. During the 2-year period, the most frequently encountered Gram negative isolates were E. coli (41.1%) and Pseudomonas spp. (20.1%) in 2005 and E. coli (38.4%) and Klebsiella spp. (19.1%) in 2006. Gram positive isolates were S. aureus 32.5% in 2005 and 36.5% in 2006 and S. agalactia 27% in 2005 and 28.9% in 2006. All E. coli, Proteus and Enterobacter isolates were sensitive to imipenem and meropenem, whereas the sensitivity of klebsiella to imipenem was 99 % during the 2-year period. For Gram-positive isolates, all S. aureus isolates were sensitive to imipenem, while the sensitivity to meropenem, ciprofloxacin and cefotaxime were 98 %, 99 % and 100 % in 2005 and 97 %, 96 % and 97 % in 2006 respectively. No vancomycin resistance was detected among all staphylococcal isolates and enterococci. Statistically significant differences were present regarding the distribution of extended spectrum b-lactamases (ESBLs)-producing E. coli (p value = 0.03), Klebsiella (p value = 0.04) and Pseudomonas spp. (p value = 0.003) in ICU and non-ICU areas during the studied period. In conclusion, monitoring antimicrobial resistance can identify national trends in resistance prevalence affecting certain hospital locations, including patients outside the ICU. The antimicrobial resistance surveillance methods can generate information on resistance patterns that is useful guide for empiric therapy of infections. It can help alert clinicians of trends of antimicrobial resistance. Further studies with a well-standardized approach to antimicrobial resistance surveillance are recommended to help in controlling and preventing infections caused by resistant organisms.  

25/24 MELT AGGLOMERATION OF ALLOPURINOL IN ZANCHETTA HIGH SHEAR MIXER

A.A. Badawi, *M.F. El-Miligi, **W.S. Sakran and K.A. Ibraheem

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

*Department of Pharmaceutics, Faculty of Pharmacy, Misr University for Science and Technology (MUST), Egypt

**Department of Pharmaceutics, Faculty of Pharmacy, October 6 University, Egypt. Department of Pharmaceutics, Faculty of Pharmacy, MSA University, Egypt.

In an attempt to enhance the dissolution of the poorly water soluble drug, allopurinol (AP), melt agglomeration in Zanchetta high shear mixer using poly ethylene glycol (PEG) 6000 as a meltable binder, and lactose as a filler was studied. There was no interaction between the drug and the PEG as manifested by IR spectroscopy. The prepared agglomerates were subjected to visual inspection, microscopic examination, particle size analysis, flow properties evaluation, friability measurements, drug distribution between different size fractions, and in vitro dissolution studies. The dissolution rate of AP was markedly enhanced; the mean dissolution time (MDT) of the plain drug was 25.9 minutes, while it was between 3.47 and 4 minutes for the different sizes of the prepared agglomerates. Additionally, the agglomerates under 800 μm were tabletted under 6 levels of compression forces. The prepared tablets were evaluated for their uniformity of content, hardness, friability, disintegration time, and in-vitro dissolution according to the USP 27. It was found that the prepared agglomerates could give smooth tablets with constant properties under a wide range of compression forces without the use of external additives. After compression, the dissolution of allopurinol showed a slight initial decrease, followed by faster dissolution and almost all the drug was dissolved in 25 minutes from all tablets.

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