Vol. 29, March, 2009.

meilleur site pour achat cialis 1/29 DESIGN OF NIMESULIDE FAST DISINTEGRATING BUCCAL LIQUISOLID TABLETS AND THEIR IN VITRO AND IN VIVO EVALUATION

Mona H. Aboul-Einien

Pharmaceutics Department, Faculty of Pharmacy, Cairo University

The aim of the present work was to formulate nimesuide as fast disintegrating buccal liquisolid tablets and to evaluate the feasibility of improving the rate of drug dissolution and in vivo absorption via such formulation. The drug was dissolved in non- volatile solvent blend and its solution was converted into dry- looking powder using liquisolid technology. The drug solution was absorbed onto microcrystalline cellulose (carrier material) and any excess solution was adsorbed by colloidal silicon dioxide (coating material). The appropriate quantities of the liquisolid system components were calculated by assessing the flow and compression properties of systems containing different proportions of carrier and coating materials. The flow properties were assessed using the angle of slide, the angle of repose and the compressibility index while the compression properties were assessed using the liquisolid compact pacticity. Differential scanning calorimetry and X- ray diffraction studies revealed that nimesulide retained in solution form in the prepared liquisolid system even after compression. Liquisolid powder formula with appropriate flowability and compressibilty was compressed into tablets, which in vitro performance was evaluated. The main physical characteristics of the prepared tablets were found to comply with the pharmacopoeial specifications and no significant differences from freshly prepared tablets were shown on storage. The in vitro dissolution rate of nimesulide was found to be enhanced from the prepared liquisolid tablets compared to that from commercially available oral ones and plain drug powder. In vivo study was performed in rabbits, which showed rapid and enhanced absorption of nimesulide from the prepared liquisolid tablets where the AUC0-24 was 1.46- folds that of the commercially available oral tablets. It could be concluded that formulation of nimesulide in fast disintegrating buccal liquisolid tablets succeeded in improving its dissolution rate as well as in vivo absorption leading to improved bioavailability.

viagra agit pendant combien temps  

qu'est ce que fait le viagra  

age pour prendre du viagra 2/29 SYNTHESIS OF PYRIDAZINE DERIVATIVES FROM 2-AMINO-3-CARBAMIDO-4,5,6,7-TETRAHYDROBENZO[b]THIOPHENE DERIVATIVES AND THEIR ANTIMICROBIAL ACTIVITY

Wagnat W. Wardakhan* and Mastoura M. Edress

National Organization for Drug Control & Research, NODCAR, P.O. 29 Cairo, Egypt

The reaction of cyanoacetanilide derivatives tadalafil 20mg avis 1a,b with cyclohexanone and elemental sulfur gave the 2-amino-3-anilido-4,5,6,7-tetrahydrobenzo[b]thiophene derivatives combien de temps dure les effets du cialis 4a,b. The reactivity of the latter products towards chemical reagents were studied to give pyrazole, pyridazine and pyrimidine derivatives. The antimicrobial activity of the newly synthesized compounds were studied.

tarif cialis 5mg boite 28  

prix du cialis 5 mg en pharmacie

acheter viagra par paypal 3/29 CYTOTOXIC EFFECT OF ESSENTIAL OILS OF TUMERIC (CURCUMA LONGA L.) AND THYME (THYMUS VULGARIS, L.) ON SOME HUMAN TUMOR CELL LINES

Naglaa H.M. Hassanen and Hany A. Fahmy

Special Food and Nutrition Department, Food Technology Research Institute, Agricultural Researches Center, Giza , Egypt.

Turmeric ( viagra a domicile Curcuma longa L.) and thyme ( Thymus vulgaris L.) have been used throughout the world as spice, food and traditional herb because each of them contain naturally occurring antioxidative components which could be used instead of synthetic antioxidant in food processing. Turmeric and thyme essential oils fractions were analyzed by GC-MS. Turmeric and thyme were identified and classified into chemical categories namely, Monocyclic terpenes (3.15, 7.74 %), Bi cyclic tecrpenes (6.19, %5.87), Aliphatic hydrocarbons (0.0, 0.23%), Aromatic hydrocarbons (0.65, 1.59 %), Oxides (1.40, 0.49 %), Alcohol (3.65, 20.38 %),Phenol and phenol ethers (1.08, 62.20 %) as major compound in thyme, Ketones (72.56, 0.0%) as major compound in turmeric and Sesequiterpene (8.07, 0.0 %), respectively. Also, turmeric and thyme essential oils at (50,100 and 150 ppm) were tested for antioxidant activity using the (Rancimat assay) compared with BHT (200ppm). The corresponding values were (70.19, 73.67%), (79.87, 84.38%), (85.41, 91.48%) vs. (72.90 %), respectively. In this study, we tested in vitro the effect of turmeric and thyme essential oils in a variety of human cancer cell lines HEPG2 (Liver carcinoma cell line), U251(Brain tumor cell line ), MCF7(Breast carcinoma cell line), HCT116 (Colon carcinoma cell line). The results showed that, the turmeric and thyme essential oils concentration required to inhibit 50% of cell growth were 0.87, 2.82 µg/ml (HEPG2), 1.07, 0.67µg/ml (U251), 1.01, 1.21 µg/ml (MCF7) and 0.74, 0.67 µg/ml (HCT116), respectively. The present results indicated that, the tested volatile essential oils could be used to inhibit tumor growth.

 

 

4/29 EFFECT OF ACRYLIC COLLOIDAL NANOPARTICLE SUSPENSIONS ON ENHANCEMENT OF ACYCLOVIR ORAL BIOAVAILABILITY.

Ahmed H. Elshafeey, *Amany O. Kamel and *Gehanne A.S. Awad

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

*Department of Pharmaceutics, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

Acyclovir (ACV), an antiviral drug used to treat herpes simplex viruses in immunocompetent and immunocompromised patients was encapsulated in acrylic colloidal nanoparticle (NP) suspensions using positively charged Eudragit RS and RL 100 in an attempt to control its release and enhance its oral bioavailability. Different drug to polymer ratios were employed viz 1:2, 1:3 and 1:5. The physicochemical properties of ACV NPs were analyzed by laser diffraction for particle size, zeta potential for surface charge and transmission electron microscopy for morphology. The encapsulation efficiency and in vitro drug release were determined using HPLC. The bioavailability of ACV NP colloids were evaluated in human volunteers, compared with commercial product using a validated LC-MS/MS method with a lower limit of quantification (LLOQ) of 0.02 µg/ml. ACV colloidal NPs with a particle size of 356-472nm, zeta potential range of +34.4 to +42.4 mv and encapsulation efficiency range of 73.5% to 96.13 % were reproducibly prepared. The time for 75% of drug to be released (t75) of F2 and F5 prepared with RS and RL respectively (drug to polymer ratio 1:3) was 9.1 and 8.5 hrs respectively with drug release mechanism of zero order. Both F2 and F5 colloidal nanosuspension sustained the oral absorption of ACV, expressed by the significant lower Cmax, significant delayed Tmax and the significant higher HVDt50% Cmax. The mean Cmax of F2, F5, and Zovirax® were 0.61± 0.06, 0.73±0.07 and 0.92 ± 0.21 µg/ml respectively. Furthermore, the AUC0-12 of F2 and F5 was significantly higher than that of Zovirax® with values of 4.37± 0.88, 5.14± 0.87 and 3.21± 0.53 µg/ml.hr respectively. The higher AUC0-12 for both F2 and F5 reflected high relative bioavailability of 136.2 and 159.9 % respectively.

 

5/29 STUDY OF MELOXICAM/ CYCLODEXTRINS INTERACTION IN BINARY AND TERNARY SYSTEMS

Galal M. El-Mahrouk, Mona H. Aboul-Einien and Nermin A. Elkasabgy

Department Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy,

Cairo University

The aim of the present work was to study the interaction between meloxicam and different cyclodextrins CyDs as beta- CyD (β- CyD) and its methyl-( M- β- CyD), hydroxypropyl- (HP- β- CyD) and sulfobutyl ether- (SBE- β- CyD) derivatives that may be used to enhance its aqueous solubility. Estimation of the interaction was carried out using differential scanning ultraviolet spectroscopy and phase solubility methods. The continuous variation method was used to determine the stoichiometric ratios of the formed complexes. Phase solubility diagrams of meloxicam were constructed in the presence of the investigated CyDs at different temperatures (37, 45 and 600 C) and pH values of 3,7 and 9 and they were used to calculate the values of the stability constant of complexation (K1:1). Van’t Hoff plots were also constructed and the main thermodynamic parameters for the complexation process were calculated. The influence of different water- soluble additives viz. tryptophan, sodium cholate, polyethylene glycol 4000 and tartaric acid on the complexation interaction was investigated by comparing the values of K1:1 in the ternary systems to those of the corresponding binary ones. A molecular inclusion binding interaction was detected between meloxicam and the investigated CyDs at different stoichiometric ratios. Phase solubility diagrams showed AL-type plots with b- and M-b-CyDs and Ap-type ones with HP- and SBE-b-CyDs. The value of K1:1 decreased by increasing the temperature or the pH of the medium. Thermodynamic analysis of the complexation interaction at the studied conditions revealed that it was accompanied by a large negative total standard free energy change (Gº), large negative standard enthalpy change (Hº) and a small negative standard entropy change (Sº). This indicated that such interaction was an enthalpy- driven inclusion reaction associated with intermolecular hydrogen bonding and van der Waals forces. Among the investigated additives, only tartaric acid with SBE- β- CyD was found to increase the value of K1:1 when compared to that of the corresponding binary system.

 

6/29 ACYLATED TRITERPENOIDAL SAPONIN AND STEROL GLUCOSIDE FROM THE FRUITS OF GLEDITSIA CASPICA DESF CULTIVATED IN EGYPT

Ehab A. Ragab and Usama Y. Shaheen

Pharmacognosy Department, Faculty of Pharmacy, Al-Azhar University,

Naser City, Cairo, Egypt.

A bisdesmosidic triterpenoidal saponin acylated with monoterpenoid unit, named gleditsioside A (1) and β-sitosteryl-3-O-β-glucopyranoside (2) were isolated for the first time from the fruits of Gleditsia caspica. Their structures were established by means of extensive 1D (1H, 13C and DEPT) and 2D (COSY, HMQC and HMBC experiments) NMR studies and MS analysis. The anti-inflammatory activity of the EtOAc and n-BuOH soluble fractions as will as the isolated compounds were evaluated.

 

 

7/29 TWO DIFFERENT APPROACHES FOR TRANSDERMAL DELIVERY OF TOLTERODINE TARTRATE USING SOLVENT AND MICROEMULSION SYSTEMS: IN VITRO PERMEATION AND IN VIVO PHARMACOKINETIC STUDY

Ahmed H. Elshafeey, *Amany O. Kamel, **Mohsen M. Fathallah

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

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

Cairo, Egypt.

**Genuine Research Center, Cairo, Egypt.

The aim of this work was to investigate the feasibility of transdermal delivery of tolterodine tartrate, a potent competitive muscarinic receptor antagonist used for the treatment of over active bladder. The effect of different vehicles and microemulsion systems on the permeation of tolterodine tartrate through miniature pig skin was studied in vitro using Franz diffusion cell. Furthermore tolterodine tartrate pharmacokinetics was studied after transdermal application to human volunteers compared to the commercial oral dosage form using a newly developed LC-MS/MS assay. The results obtained indicated that PEG 400:Phosphate buffer pH 7.4 in the ratio 1:1 significantly enhanced tolterodine tartrate permeation across pig’s skin with a steady state flux of 0.019 mg.cm-2.hr-1. Also the microemulsion system formed of 40% w/w Labrasol: Plurol (3:1) as a surfactant: co-surfactant mixture, 10% w/w isopropyl myristate and 50% water significantly enhanced permeation with Q24 of 0.746 mg.cm-2 and steady state flux of 0.02 mg.cm-2.hr-1. In contrast to oral delivery, a sustained activity was observed over a period of 72 hrs after transdermal application of this microemulsion to human volunteers with a significant lower Cmax (1.06 ng/ml), significant delayed Tmax (3.17 hrs) and significant higher MRT value (147.82 hrs) (p<0.05). This sustained activity was due to the controlled release of drug into the systemic circulation with expected increase in the patient compliance and prevention of nocturnal enuresis.

 


8/29 NEW DIGLYCERIDE ESTER FROM THE RED SEA GORGONIAN RUMPHELLA TORTA

Sherief I. Khalifa

Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, Egypt

A new metabolite, diglyceride ester (1) was isolated from the Red Sea gorgonian, Rumphella torta. Other previously reported compounds including the rare C27 fatty acid heptacosanoic acid (2) and ergost-5,11-dien-3b-ol (3) were isolated for the first time from this genus. GLC analysis of the unsaponifiable matter revealed that it contained a high percentage of hydrocarbons with 1-hexadecanol as a major component (34.94%). GLC analysis of the fatty acid methyl esters revealed that hexadecanoic acid, is the major fatty acid (58.90%). Structure elucidation was achieved using one- and two-dimensional nuclear magnetic resonance spectroscopy and high resolution mass spectrometry.

 

 

9/29 EFFECT OF INHALATIONAL ANAESTHESIA (ISOFLORANE) IN COMPARISON TO TOTAL INTRAVENOUS ANESTHESIA (TIVA) (PROPOFOL) ON STRESS RESPONSE AND CYTOKINES

Mohamed Marie El-Sayed, Tarek Mohamed El-Saied and Fatma H. Ashour

Anaesthesia Department, Faculty of Medicine for Girls, Al-Azhar University

Stress response is the term given to the hormonal and metabolic changes which follow injury or trauma. This part of systemic reaction to injury, which encompass a wide range of endocrinal, immunological and hematological effects. The magnitude and duration of the response are proportional to the surgical injury. In our study we compared total intravenous anesthesia TIVA using propofol versus inhalational technique using isoflurane. The study included 40 patients ASA1 and II classified into two groups according to the type of anesthesia used, inhalational or isoflorane group and TIVA or propofol group. Both groups received fentanyl in the same regeimen. Venous blood samples were obtained for estimation of plasma levels of both IL-6 and cortisol at different test times. Although propofol anesthesia decreased the serum level of cortisol but did not affect IL-6 level but anaesthesia with isoflurane does not completely prevent the perioperative rise in the plasma levels of different stress hormones. The relation between the severity of tissue trauma and the level of both IL-6and cortisol was proportionate in both grops.

 

 

10/29 FREE RADICAL SCAVENGING CAPACITY AND INHIBITION OF LIPID PEROXIDATION ACTIVITY OF SOME PLANTS AND NATURAL HERBS

Moustafa M. Said and Zeinab Y. Ali

Department of Biochemistry, National Organization For Drug Control And Reach, NODCAR, Egypt.

Current research is directed to finding potent naturally occurring antioxidants of plant origin. In-vitro screening methods for antioxidant activity could provide the need preliminary observations necessary to select crude plant extracts with potentially useful properties for further chemical and pharmacological investigations. So, this in-vitro study was carried out to evaluate the total phenolic contents and the antioxidant potential of 70% ethanolic leaves extracts of Jakfruit (Artocarpus heterophyllus), Mulberry (Morus indica), Moringa (Moringa oleifera) and Purslane (Portulaca oleraceae). Total phenolic content was determined by Folin-Ciocalteu reagent. The antioxidant potential of individual extract at different concentrations was measured by the most common and reliable methods. Both % free radical scavenging activity of individual extract at different concentrations and IC50 values was determined using ascorbic acid or α-tocopherol as standard. The results revealed that M. oleifera has the highest level of total phenolic compounds followed by P. oleraceae, M. indica and A. heterophyllus. All tested extracts showed antioxidant activity by different mechanisms in six different models of assay (reducing power, 1,1-Diphenyl-2-picrylhydrazyl (DPPH), superoxide, hydroxyl and hydrogen peroxide radicals scavenging activity and inhibition of lipid liposome peroxidation). Therefore, it can be concluded that the antioxidant activity of all tested extracts was correlated to their phenolic content in dose-dependent manner. The ethanolic extract of the four selected dried leaves could be considered for preparation of nutraceuticals with potent antioxidant activity suitable for maintenance of good health, inhibition of membrane lipid peroxidation and prevention of free radical-linked human disease.

 

 

11/29 NEW CERAMIDES FROM THE RED SEA SPONGE NEGOMBATA CORTICATA

Sherief I. Khalifa

Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal Ismailia, Egypt

Five new ceramides were isolated from the Red Sea sponge Negombata corticata. Complete structure elucidation was achieved through extensive spectroscopic analysis including one- and two-dimensional nuclear magnetic resonance spectroscopy and time-of-flight mass spectrometry.

 

12/29 COMPARATIVE EFFECTS OF PROPOFOL INFUSION VERSUS SEVOFLURANE FOR MAINTENANCE OF DEIIBERATE ARTERIAL HYPOTENSION DURING ANESTHESIA FOR SPINE SURGERY

Soliman M.M. Ali*, Kamel I. Hady**, Ahmed M. Abd Elmabod*** and

Saad El-Dean El-Kateeb*****

*Department of Anesthesia, Faculty of Medicine, El-Azahar Univeristy (Assiut), **Faculty of Medicine, Assiut Univeristy, *** Faculty of Medicine, Sohag Univeristy, **** Faculty of Medicine, El-Azahar Univeristy.

Sixty patients of ASA1and 11posted for elective spine surgery in prone postion under general anaesthesia were selected for the study . The patients were randomly assigned into two groups . Sevoflurane (Group S, n=30) and Propofol (Group P, n=30).Astandard premedication and induction regimen was followed in all cases. Group S patients received N2O / O2 / Sevoflurane / atracurium and Group P received N2O / O2 / Propofol infusion atracurium / for maintenance of anesthesia to a desired level. Recovery was assessed with a simulated wake up test and a simple behavioral score was employed to assesses the over all recovery. The observation revealed that propofol and sevoflurane combined with fentanyl provided adequate deliberate hypotension and similar clear surgical fields. Both agents can be used safely for deliberate hypotension. Also, maintenance of anesthesia with sevoflurane is associated with a faster recovery than propofol anesthesia. But propofol anesthesia seems to be a better anesthetic than sevoflurane-fentanyl in reducing the incidence of nausea and vomiting postoperative.

 

13/29 SARCOSAPROPHAGOUS FLIES IN SUEZ PROVINCE.

III- HUMAN PATHOGENIC BACTERIA ISOLATED FROM FIELD COLLECTED FLIES

Refaat M. Gabre

Department of Entomology, Faculty of Science, Cairo University, Giza, Egypt

Flies pose a serious threat to human health due to their filthy breeding habits. They breed in fresh excrement and fermenting vegetation. They act as primary vector for the spread of bacterial diseases. Many poor countries suffer the wrath of fly-borne disease despite eradication efforts. Twenty-four species of human pathogenic bacteria were isolated from nine species of sarcosaprophagous flies that collected during the summer and winter seasons for two successive years (2004 & 2005) from El-Arbaeen fish market, El-Arbaeen District, Suez Province, Egypt. The results revealed that twenty out of the 24 isolated bacteria belong to the Gram negative bacilli group of genera Escherichia, Klebsiella, Salmonella, Shigella, Proteus, Morganella, Enterobacter, Yersenia and Pasteurella. Meanwhile, the last four species belong to the Gram positive cocci group of genera Enterococcus, Streptococcus and Staphylococcus. Chrysomya megacephala, Lucilia cuprina and Musca domestica success to carry bacteria either externally or internally significant (P < 0.001) than that the other studied sarcosaprophagous species.

 

 

14/29 PSEUDOMONAS AERUGINOSA CLINICAL ISOLATES PRODUCING METALLO Β-LACTAMASES VIM IN SAUDI ARABIA

Mohamed H.M. Al-Agamy

Department of Pharmaceutics and Microbiology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia

A total of 480 clinical isolates (135 P. aeruginosa and 345 Enterobacteriaceae) were screened for production of MBL by imipenem/EDTA disk method. The prevalence of MBL was relatively high (16.3%) and MBL-producing P. aeruginosa isolates were resistant to imipenem (MIC ³ 32 mg/ml). However, Enterobacteriaceae were found to be not harboring MBL and Enterobacteriaceae were susceptible to imipenem (MIC ≤ 0.25 mg/ml). MBL-producing P. aeruginosa isolates were 100% resistant to b-lactams except aztreonam and ceftazidime, which showed resistance rate of 77.3 % and 86.3% respectively. Only 31% and 22% of the MBL-producing isolates were resistant to ciprofloxacin and polymyxin B respectively while non-MBL producers were sensitive to polymyxin B. PCR assay revealed that all MBL-producing isolates were harbor blaVIM like gene and encoded on class 1 integron. This is the first study in Saudi Arabia was undertaken to determine the prevalence and characterization of MBL genes.

 


16/29 PREVALENCE AND CHARACTERIZATION OF EXTENDED SPECTRUM-b-LACTAMASE-PRODUCING KLEBSIELLA PNEUMONIAE IN SAUDI ARABIA

Mohamed Hamed Al-Agamy, Atef Mohamed Shibl and Abdelkader Farid Tawfik

Division of Microbiology, College of Pharmacy, King Saud University,

Riyadh, Saudi Arabia

A total of 400 K. pneumoniae were isolated during 2007 from two hospitals in Riyadh and these isolates were screened for phenotypic detection of ESβL using ESβL-E-strips and combined disk methods. Phenotypic characterization identified a high ESβL rate of 55%. MIC was determined for ESβL-producing isolates using E-test. High percentage of isolates showed elevated MIC breakpoint (256µg/ml) for ceftazidime (79.5%), aztreonam (72.7%) and cefotaxime (55.9%). PCR assay was used to detect blaTEM, blaSHV, and blaCTX-M genes in ESβL-producing K. pneumoniae. Those isolates were PCR positive for SHV, TEM, and CTX-M β-lactamase genes with prevalence of 97.3% 84.1%, and 36.4% respectively. Within CTX-M family, two groups of enzymes, CTX-M-1 and CTX-M-9 group likes, were found with prevalence of 60% and 40% respectively. This study confirms the high rate of ESβL in K. pneumoniae and consequently, treatment options were further limited as most isolates produced ESβLs also, demonstrates the high incidence of blaCTX-M genes in Saudi Arabia.

 

17/29 A SIMPLE COLORIMETRIC METHOD FOR THE EVALUATION OF CHITOSAN

Mohamed I.A. Abou-Shoer

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

A simple sensitive and rapid colorimetric method has been developed, and herein described, for the qualitative and quantitative chemical assessment of the commercially available chitosan products. The described method relies on the reactivity of the basic amino function of chitosan with the acid dye bromocresol purple. The applied technique allows assessment of variability and selectivity changes in the quality of the marketed chitosan products.

 

 

18/29 EFFECT OF SPIRULINA PLATENSIS EXTRACT ON GROWTH, PHENOLIC COMPOUNDS AND ANTIOXIDANT ACTIVITIES OF SISYMBRIUM IRIO CALLUS AND CELL SUSPENSION CULTURES

Gehan H. Amin**, Amal A. Al-Gendy *, Yassin, M. El-Ayouty**

and Amira Abdel-Motteleb**.

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

** Botany Department, Faculty of Science, Zagazig University, Egypt.

Several trials for induction of Sisymbrium irio L. callus were carried out on Murashige and Skoog (MS) medium supplemented with different concentrations of auxins and kinetin. Maintenance of calli on MS medium treated with Spirulina aqueous extract (SAE) as a source of vitamins and phytohormones was achieved. Growth and growth parameters of calli revealed that an obvious extension in the exponential phase with variable enhancement of the growth rate by 1 to 4 times more than irrespective control. Doubling time (td) and the relative growth rate (RGR) of callus were also estimated at different treatments. Antioxidant capacities of calli grown on MS medium supplemented with different SAE were enhanced up to 12 times more than control calli. The previous results were coincidentally with an obvious accumulation of both flavonoids and total phenolic compounds in cultures treated with SAE. The complementary between the previous results manifested the longevity and viability of calli on modified MS medium. Antioxidant activity also confirmed the different results. Successful suspension cultures were established using MS medium without vitamins and phytohormones and supplied with 18% SAE. Growth parameters, total flavonoids, phenolic compounds and antioxidant activity were highly increased compared with the untreated cultures.

 

19/29 Cytotoxic Sterol and Triterpenes from

Ficus binnendijkii (Miq.) Miq. Cultivated in Egypt

Miriam F. Yousif, Hanaa H. Eid and Shahira M.Ezzat

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr-El-Ainy, Cairo, Egypt.

The cytotoxic activity of the ethanol extract of the leaves of Ficusbinnendijkii (Miq.) Miq. (Moraceae), as well as, its fractions were investigated. Bioassay-guided fractionation led to the isolation of six compounds from the n-hexane fraction viz., lupeol acetate 1, β-amyrin acetate 2, α-amyrin 3, 3β-acetoxy-1-β-(2-hydroxy-2-propoxy)-11-α-hydroxyolean-12-ene 4, and a sterol, stigmasterol 5 and its glucoside 6. The compounds were identified by spectroscopic and chemical methods. This is the first report for the isolation of compounds 1-6 from the title plant and of compound 4 from the genus Ficus. Compounds 1 and 3 exhibited specific in-vitro cytotoxic activity against breast cancer cell line (MCF 7) and colon cancer cell line (HCT116) while compounds 2 and 6 were only active against MCF 7.

 

 

20/29 DETERMINATION OF ALIZARIN IN CRUCIANELLA MARITIMA L. USING HIGH PERFORMANCE THIN LAYER CHROMATOGRAPHY

Jihan M. Badr

Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, Ismailia

A high performance thin layer chromatographic separation method with UV spectrophotometric detection has been developed for the determination of alizarin in the roots and aerial parts of Crucianella maritima L. The anthraquinone was analyzed after treatment of the powdered plant with 5% Na2CO3 followed by regeneration of the phenolic compounds by acidification then extraction with chloroform. Different validation parameters were found to be satisfactory regarding requirements of the International Committee on Harmonization (ICH) guidelines. Separation of the spots was performed using chloroform: glacial acetic acid (50:1.5) after development for 13 min and the linear compact zones were quantified by scanning at l 424 nm. The method has been successfully applied for the quantitative analysis of alizarin without any interference of other chloroform soluble phenolic components.

 

21/29 PHARMACOGNOSTICAL AND BIOLOGICAL studY OF SpinachFruitS

Miriam F. Yousif and Amany A. Sleem*

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr-El-Ainy St. 11562 Cairo, Egypt.                                

*Pharmacology Department, National Research Center, El-behoose St., El-Dokki, Giza, Egypt.

The fruit of Spinach (Spinacea oleracea L.) was analyzed for its lipoidal, carbohydrate, protein, vitamin and mineral contents, and its biological activities evaluated. The physico-chemical characters of the extracted fixed oil (6.5%) were determined. GLC analysis of the saponifiable fraction of the oil revealed that omega-6 (linoleic acid 20.739%) and omega-9 (oleic acid 33.417%) were the major unsaturated fatty acids; while palmitic (36.258%) and stearic (3.101%) acids were the major saturated ones. In addition, spinasterol, stigmasterol, campesterol, β-sitosterol and α-amyrin, as well as, a series of hydrocarbons were identified in the unsaponifiable fraction. 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, sucrose, galactose, fructose and galacturonic acid. The polysaccharide hydrolysate afforded four sugars: galactose, glucose, fructose and galacturonic acid. The amount of crude protein was 17.64 g/100 g; total amino acids amounted to 10.8424 g/100g, among which were 3.3244 g/100 g essential amino acids. Vitamins C, B1, B2, B6, A, D, and E reached 3650 ppm, 236.9 ppm, 38.916 ppm, 5051.3 ppm, 38.272 ppm, 64.543 ppm, and 33.484 ppm respectively. The major minerals were K 686.2 mg/100 g, Mg 206.6 mg/100 g, Fe 69.9 mg/100 g, Mn 6.2 mg/100 g, Zn 2.8 mg/100 g, and, B 1.8 mg/100 g, Cu 1.1 mg/100 g, Cr 0.5 mg/100 g and Co 0.1 mg/ 100 g. The effect of the different fruit extracts, fixed oil and polysaccharide on blood glutathione level was used as a measure to assess its antioxidant activity. The effects of the same fruit extracts on carbon tetrachloride toxicated liver rats were investigated.

 

 

22/29 ANTI-DIABETIC ACTIVITY OF SYZYGIUM CUMINI (L.) FRUITS EXTRACT ON STREPTOZOTOCIN INDUCED DIABETIC RATS

Sherien K. Hassan, Nermin M. El-Sammad, Mamdouh M. Ali,, *Azza S.A. Hegaziand **Naglaa M. Nazif

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

*National Hepatology and Tropical Medicine Research Institute, Cairo, Egypt.

**Phytochemistry Dept, National Research Center, El Bohooth St. Dokki, Cairo, Egypt.

The aim of the present study is to investigate the antidiabetic activity of Syzygium cumini (L.) fruits (Bambozia) cultivated in Egypt on streptozotocin (STZ) induced diabetic rats. Diabetes was induced in male Sprague Dawley rats by a single intraperitoneal injection of STZ at a dose of 65 mg/kg b. w. Oral administration of an ethanolic fruits extract at a concentration of 100 mg/kg b.w. for 30 days showed a highly significant decrease in fasting blood glucose, and a significant increase in α-amylase activity and insulin level. The hepatic glucose-6-phosphatase (G-6-Pase) activity and lipid peroxidation (LPx) level were significantly decreased by the treatment. The treatment also resulted in a significant improvement in both liver function and lipid profile. The extract exerted protective effect against lipid peroxidation by scavenging of free radicals thereby reducing the risk of diabetic complications. Histological studies of liver of diabetic rats showed dilated congested central vein, parenchymal lytic necrosis and inflammation around the central vein. Treatment with syzygium cumini reduces the histopathological abnormalities associated with STZ-diabetes. However, treatment with Syzygium cumini did not alter the normal function or morphology of control rats. The results clearly suggest that Syzygium cumini (L.) fruits possess an antidiabetic effect by improvement in the above biochemical and pathological alternations and can be useful for control and management of diabetes mellitus progression.

 

 

23/29 RELEASE STUDIES OF ACECLOFENAC FROM DIFFERENT TOPICAL FORMULATIONS

Wedad S. Sakran

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

Aceclofenac is a well established anti-inflammatory drug. Because of gastrointestinal disorders, topical dosage forms are recommended. This study comprised formulation of aceclofenac in four topical bases (FI---FIV). FI and FII were prepared as emulsion gels using either liquid paraffin or isopropyl myristate respectively. FIII was prepared as Carbopol 940 gel, and FIV was prepared as o/w cream. The prepared formulations as well as the commercial product Bristaflam diffuCream were characterized for their physical appearance, pH, rheological properties, and in vitro drug release in both pH 5.5 and pH 7.4. All the formulations recorded pH values within the accepted range for topical use, and all exhibited non-Newtonian with shear thinning behavior. The release results revealed that, the release profile of aceclofenac in both pH values was found to proceed according to the following order: FIII > FII > FI > commercial > o/w cream. However, comparative ex vivo permeation profile of aceclofenac from FIII and the commercial product Bristaflam diffuCream through pig skin showed flux (Jss) values of 14.34& 14.41(µg/cm2/h) and permeation coefficients (Kp) of 0.0234 & 0.0235 (cm/h) for FIII and the commercial product Bristaflam diffuCream respectively. These results suggest the convenience of topical aceclofenac as gel formulation to improve patients’ acceptance, and the potential use of topical aceclofenac for its localized anti-inflammatory effect. This localized anti-inflammatory effect might be relied upon in addition to the conventional oral therapy in order to decrease the frequent oral administration and gastrointestinal disorders.

 

 

24/29 COMPARATIVE STUDY OF TEM & SHV Β-LACTAMASEGENES IN KLEBSIELLA PNEUMONIAE ISOLATES

Dalia S. Marzouk, *Ahmed S. Attia, Hayam M. Hamouda, *AbdElGawad Hashem and *Hussein Shoeab

Microbiology Department, NODCAR.

*Department of Microbiology and Immunology, Fac. of Pharmacy, Cairo Univ.

Resistance to antimicrobial agents has increased greatly among gram negative microbes. Production of extended-spectrum β -lactamases (ESBLs) is one of the main mechanisms of resistance to broad-spectrum β -lactam antibiotics among the Enterobacteriaceae. This resistance is mainly associated with the production of enzymes called Temoniera (TEM) and sulphydryl variable (SHV) that are generally plasmid-mediated in Klebsiella pneumoniae. Our study, therefore, focused on prevalence of TEM & SHV β-lactamase genes. Among ten isolates, one K. pneumoniae exhibited reduced susceptibility to the cephalosporins tested. Using PCR technique, TEM was detected in 2 strains (20%), SHV was detected in 2 strains (20%) and both of them were detected together in 4 strains (40%).Comparison of these genotype and susceptibility phenotypes of these strains showed 100% agreement between the presence of TEM & SHV and resistance to ceftazidime, cefotaxime and cefepime. Of two strains carrying TEM gene, one strain had an MIC > 256 µg/ml to cefotaxime (CTX), ceftazidime (CAZ) and cefepime (CPM) and the other resistant ranged from (64-256) µg/ml. Strains carrying SHV gene showed decreased in MIC ranged from (0.125-256) µg/ml. Plasmid DNA was detected in 50% of total isolates and the size of the plasmids ranged from 20 to 45 kb. The results of this study indicate that ESBLs TEM and SHV are widely spread among K. pneumoniae isolates included and their presence was confirmed genetically and phenotypically. However, further studies are required to determine the prevalence of these ESBLs and their effect in treatment outcomes on the Egyptian hospitals.

 

25/29 EFFECTS OF MATERNAL ADMINISTRATION OF FLUPYRAZOFOS ON PREGNANT RATS AND THEIR FOETUSES

Samia M. Abd El Wahab

Zoology Department, Faculty of Science, Al-Azhar University For Girls,

Cairo, Egypt.

Flupyrazofos (FPF) is one of the most potent broad spectrum organophosphates used against diamond back-moth (Plutella xylostella) and other pests. Repeated exposure to FPF may endanger general population with resultant toxic effects on many organs. This work was carried out to ascertain the toxic effect on the pregnant rats and their foetuses. The study was conducted on 100 pregnant rats divided into four equal groups. The first group served as a control, and the other three groups received doses of FPF; 7 (1/10), 14 (1/5) and 35 (1/2 LD50) mg/kg body weight respectively. Flupyrazofos was administered orally once daily to pregnant rats during organogenesis from day 6 to 19 and the specimens were taken on day 20 of gestation. Sections of liver, kidney, heart and intestine of foetuses were prepared and stained with H & E for histological study. Maternal toxicitywas observed at 35 mg/kg, including mortality (3 of 25 pregnant),reduced body weight, weightgain, reduced liver and increased lung weights, and reducedgravid uterine weight. Developmental toxicity wasalso observed at 35 mg/kg including reduced foetalbody weights (and related reduced placental weights) and an increased incidence of foetal skeletal retardations. The insecticide did not induce abortion however induced mortality of the pregnant females. The mean implantation and resorption sites were not significantly affected. Examination of foetuses showed no apparent teratological effects. However, skeletal preparations indicated growth retardation. Histological examination of the foetal liver, kidney, heart and intestine obtained from pregnant mothers treated with 14 and 35 mg/kg of FPF showed degenerative changes. It is apparent from the present study that FPF has possible toxic effect on foetuses whose mothers were treated with different doses of the insecticide during organogenesis.

 

 

26/29 EFFECT OF HELICOBACTER PYLORI ERADICATION THERAPY AND SOME EXOGENOUS ANTIOXIDANTS ON ULCER HEALING RATES AND OXIDATIVE STRESS BIOMARKERS IN PATIENTS WITH HELICOBACTER PYLORI-INDUCED DUODENAL ULCER

Ahmed M. Ali and *Thanaa G. Awaad

FROM

Department of Pharmacology & Toxicology. Faculty of Pharmacy, October 6 *University, October 6 Governate, Egypt.General Organization of Health Insurance, Cairo, Egypt.

The aim of this study is to evaluate the status of endogenous antioxidant defense system in H. pylori-infected endoscopically diagnosed chronic duodenal ulcer patients through the assessment of certain oxidative stress biomarkers. These biomarkers namely plasma malodialdehyde (MDA) and blood activities of superoxide dismutase (SOD) and glutathione peroxidase (GPx) are to be evaluated before and after the administration of the histamine H2 antagonist nizatidine alone or with either vitamin E (α-tocopherol) or thioctic acid (α-lipoic acid) or a combination of both. The same biomarkers were also assessed before and after administration of H. pylori eradication therapy. The effect of antioxidant and H.pylori eradication therapies on ulcer healing rates was also investigated. Moreover, the efficacy of H.pylori eradication by combined use of nizatidine with the macrolide antibiotic "clarithromycin" and amoxicillin was also evaluated in close association to ulcer healing. H.pylori-infected duodenal ulcer patients are subjected to massive oxidative stress as reflected by a significant decrease of erythrocytic GPx and SOD activities and elevation of plasma MDA levels. Treatment of H.pylori-infected duodenal ulcer patients with nizatidine alone failed to produce any significant change in any of the measured oxidative stress biomarkers. Treatment with nizatidine in combination with either vitamin E, thioctic acid or a combination of both resulted in a significant increase in erythrocytic GPx and SOD activities and a significant decrease in plasma MDA level. Some post-treatment values of certain oxidative stress biomarkers (e.g. MDA, GPx and SOD) were not significantly different from normal control values following oral treatment with H.pylori eradication therapy or nizatidine combinations with either vitamin E, thioctic acid or a combination of both. The use of triple H.pylori eradication therapy consisting of nizatidine (300mg once daily for 6-weeks), clarithromycin (500mg twice daily for 10 days) and amoxicillin (1000mg twice daily for 10 days) resulted in 100% eradication rate of the organism in H.pylori-infected duodenal ulcer patients. Attenuation of oxidative stress in H.pylori-infected peptic ulcer patients either by combined nizatidine/antioxidant treatment or by H.pylori eradication therapy was associated with higher ulcer healing rates (on a percentage basis) as compared with patients treated with nizatidine alone. In patients receiving H.pylori eradication therapy, the ulcer healing rate was 100% compared to 60% in those treated with nizatidine alone and 86.67%, 73.34% and 93.34% in patients treated with nizatidine in combination with either vitamin E, thioctic acid or a combination of both respectively.

 

27/29 HISTOLOGICAL AND HISTOCHEMICAL STUDIES ON THE EFFECT OF THE ALTERNATING MAGNETIC FIELD ON THE MICE LUNG

Boshra A.A. El-Salkh

Zoology Department, Faculty of Science (Girls), Al-Azhar University

            Electromagnetic fields cause the major environmental danger to our population. We are exposed daily to a variety of radiations which are harmful to all the living organisms. The present study aimed to investigate the effect of continuous daily exposure to alternating magnetic field. Adult male mice were classified into four groups, the first group was kept as control, the second, third and fourth groups received 50Hz/Ac & 2mT daily for 10, 15 and 20 days. Histological and histochemical studies were carried out on lung tissue. Many histological and histochemical changes were observed in lungs of exposed animals. These changes included: congested blood vessels with sing of haemolysis, presence of granuloma, dilated bronchioles, thickened alveolar septae with increased collagenous bundles, proteins and polysaccharides in lung tissue.

 

 

28/29 ARGELONE: AN ADDITIONAL NEW COMPOUND FROM SOLENOSTEMMA ARGEL

Gamal A. Dora and Mohamed M. Afifi Amer

*Department of Pharmacognosy, Faculty of Pharmacy and **Agricultural Biochemistry Department, Faculty of Agriculture, University of Zagazig, Egypt

Reinvestigation of the chloroform extract of Solenostemma argel (Fam. Asclepiadaceae) through repeated column chromatography afforded a new compound 1 identified as: 3,4-dihydro-4-hydroxyindeno[2,1-b] pyran-9(2H)-one and was given the name “Argelone”, and β-amyrin 2 . The structure of the isolated compounds was elucidated by means of the spectral methods UV, IR, MS, 1HNMR, 13CNMR, DEPT, HMBC, HSQC experiments. The anti-oxidant activity of the different plant extracts using DPPH free radical scavenging method revealed that only the ethyl acetate extract demonsterates remarkable activity with EC50 =3.23 μg/ml against vitamin C (EC50 = 8.55 μg/ml).

 

 

29/29 A NEW BIANTHRAQUINOID C-GLYCOSIDE FROM ASPHODELUS MICROCARPUS SALZM. ETVIVI GROWING IN EGYPT

Abd El-Salam I. Mohammad

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

A new bianthraquinoid C-glycoside; asphodeoloside B (asphodelin-10`-oxanthrone-10`-β-D-arabinopyranoside) [1] and a known compound ramosin [2], were isolated from the tubers of Asphodelus microcarpus. Structure elucidation of compound [1] was based on 1D (1H and 13C) and 2D (COSY, HMQC and HMBC) NMR analysis. The ethyl acetate fraction showed a promising activity in the treatment of dandruff and Alopecia areata.

 

30/29 SYNTHESIS AND IN VITRO EVALUATION OF SULFAMETHOXAZOLE AND SULFADIMIDINE DERIVATIVES AS ANTIMICROBIAL AGENTS.

Karam A. El-Sharkawy, E. E. El-Arab* and R. A. Ibrahim**

Organic Chemistry Department, Faculty of Pharmacy, October University of Modern Sciences and Arts (MSA), El-Wahat road, 6 October City, Egypt.

* Organic Chemistry Department, National Organization of Drug Control & Research (NODCAR), Cairo, Egypt

** Chemistry Department, Faculty of Engineering, New Cairo Academy,

El- Tagammoe El-Khames, Egypt.

The reaction of 5-Chlorosulfonyl-2-hydroxy-benzoic acid 1a with each sulfamethoxazole and sulfadimidine to produce compounds 1b and 1c respectively, these compounds can be undergo some type of reactions with amino-acid methyl esters followed by reaction with hydrazine hydrate to produce the corresponding hydrazide derivatives 2-9, which is easily directed toward the reaction with either ethyl isothiocyanate or phenylisothiocyanate, the thiosemicarbazides were produced 10-17, the latter synthesized compounds were cyclized in acidic medium to produce triazole derivatives compounds 18-25, some of the newly synthesized compounds were found to possess antimicrobial activities against two different series of microorganisms including gram-positive, gram-negative microorganisms Bacillius subtilis, salmonella typhi, Staphylococcus aureus, Escherichia coli and the fungi Candida utilis.

Scroll to top