Vol. 11, April, 2003.

qui à testé priligy 1/11 SPECTROPHOTOMETRIC DETERMINATION OF THREE BENZAMIDE ANTIPSYCHOTICS IN PURE AND PHARMACEUTICAL PREPARATION USING CHARGE TRANSFER COMPLEX.

M.F. Radwan

Pharmaceutical Medicinal Chemistry Department, Faculty of Pharmacy, Minia University, El-Minia , Egypt.

Simple and sensitive spectrophotometric methods were described for the determination of three substituted benzamides, namely: sulpiride, tiapride and veralipride. These methods were based on the formation of charge transfer coloured complexes between the studied benzamides as n-electron donors and iodine as s-acceptor or different p-acceptors; 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), 7,7,8,8-tetracyano-quinodimethan (TCNQ) and tetracyanoethylene (TCNE). The colour of the formed complex chromogen is depending on the electron affinity of the acceptors. Different experimental parameters affecting the reaction were carefully studied and incorporated into the procedure. Beer’s plots were obeyed in a general concentration range of 3-190 mg/ml for the investigated compounds. Lower detection limits were ranged from 0.2-21.43 mg/ml for the studied drugs. No interference was observed from additives commonly present in pharmaceutical preparations. The methods were successfully applied in the determination of these drugs in the pure forms as well as in their pharmaceutical preparations.

tadalafil francais  

2/11 SYNTHESIS AND ANTICONVULSANT ACTIVITY OF SOME NEW N-SUBSTITUTED-1,8-NAPHTHALIMIDES.

A.A. El-Helby, M.A.A. El-Zahaby and M.F. Radwan*

Dep. of Pharm. Chemistry, Faculty of Pharmacy,Al-Azhar University Nasr City, Cairo, Egypt.

* Dept. of Med. Chemistry, Faculty of Pharmacy, Minia University Cairo, Egypt

Some new N-substituted-1,8-naphthalimide derivatives were synthesized. Thus, the potassium salt of 1,8- naphthalimide prepared and condensed with different chloroacetate or chloro-3-propionate esters to afford the target compounds III1-9. Different amides IV1-10 were obtained by reacting the ester III2 with the appropiate amino compounds. Some of the new imide derivatives (V1-11) were also prepared by heating the 1,8-naphthalic anhydride with different aliphatic and aromatic amines. Some of the synthesized compounds were evaluated for their anticonvulsant activity. Some of the tested compounds showed significant protection against PTZ-induced convulsions in frogs.

quel est l'effet du viagra sur une femme  

3/11 VALIDATED HPLC METHOD FOR THE DETERMINATION OF DIMINAZENE ACETURATE AND PHENAZONE IN VETERINARY MIXTURE

O.I. Abd El-Sattar, A.A. Ahmad* and T. Elkady*

Pharm. Chem. Dept., Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

* Quality Control Dept, Egyptian Co. for Chemicals and Pharmaceuticals (Adwia),10th of Ramadan City, Egypt.

Asimple, accurate, sensitive and reproducible method hase been developed for the determination of diminazene aceturate (DMN) and phenazone (PHN) in veterinary mixture. The method is based on isocratic high-performance liquid chromatography (HPLC) separation on a reversed phase column (Hypersil BDS, 15 cm x 4.6 mm. I.D., 5 mm particle size) using a mobile phase of acetonitrile - 0.05 M KH2PO4 solution, its pH adjusted at 3.5 with H3PO4 (10:90, v/v). The flow rate was 1.5 ml min-1 and samples were detected at 254 nm. The linear range for DMN and PHN were between 10-200 mg ml-1 and 8-180 mg ml-1, respectively. The limits of detection (LOD) were 3.20 mg ml-1 and   2.40 mg ml-1 and limits of   quantification   (LOQ) were 10 mg ml-1 and 8 mg ml-1 for DMN and PHN, respectively .The precision of the method was excellent and with RSD%<2. The method accuracy ranged between 98.15% and 99.96% for DMN and between 99.02% and 101.85% for PHN. The recovery study by adopting standard addition technique gave results close to 100%. The developed method was used for the determination of the cited drugs in pharmaceutical preparation with mean percentage recoveries 99.96% and 101.61% for DMN and PHN, respectively. The optimized method proved to be selective, robust and rugged for the analysis of the studied compounds.

achat viagra 50mg  

prix du generique du viagra en france 4/11 VALIDATED AND STABILITY INDICATING HPLC-METHOD FOR DETERMINATION OF ALENDRONATE SODIUM USING PHTHALDIALDEHYDE AS A PRE-COLUMN DERIVATIZING AGENT

O.I. Abd El-Sattar*, A.A. Ahmad** and T. ElKady**

* Pharm. Chem. Dept., Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

**Quality Control Dept., Egyptian Co. for Chemicals and Pharmaceuticals (Adwia), 10 th of Ramadan City, Egypt.

A specific and stability indicating high-performance liquid chromatographic (HPLC) assay, involving precolumn derivatization was developed and validated for quantitation of alendronate sodium (ALND) in commercial tablets and bulk powder. The method based on precolumn derivatization of ALND with phthaldialdehyde and elution from Hypersil BDS C18 column with mobile phase consisting of acetonitrile-0.005 M sodium hexane sulfonate solution containing 0.1% triethanolamine, its pH adjusted to 2.8 with H3PO4 (30:70, v/v) and UV-detection at 325 nm. The calibration curve was linear between 10 and 120 mg ml-1. The limits of detection (LOD) and quantification (LOQ) were 2.5 and 10 mg ml-1, respectively. The developed method was found to be accurate (mean percentage recovery ± RSD%, n=6 was 99.97% ± 0.13) and precise (the intra and inter-day precision were less than 2.17 and 2.65, respectively). Forced degraded samples in acidic medium, produced no interfering peaks in the chromatogram of derivatized alendronate sodium (ALND-D), revealing that, the method is stability indicating. The developed method was used for the determination of ALND in tablets with mean percentage recovery ± SD ,102.36 ± 1.38. The optimized method proves to be selective, robust and rugged for the analysis of ALND.

 

le cialis est il en vente libre en espagne

ou trouver du viagra sur paris 5/11 SYNTHESIS OF SOME NEW 1,2,4-TRIAZINE DERIVATIVES AND EVALUATION OF THEIR ANTIMICROBIAL AND CYTOTOXIC ACTIVITIES

M.M. Said

Organic Chemistry Department, Faculty of Pharmacy,

Cairo University, Cairo Egypt

Some new triazine containing compounds have been prepared in order to investigate their antimicrobial and cytotoxic activities. Some of the tested compounds showed promising action. The detailed synthesis, spectroscopic and biological data are described.

cialis less side effects  

sildenafil et cialis  

cialis 5 mg moins cher 6/11 DESIGN AND SYNTHESIS OF SOME NEW DERIVATIVES OF 2(3H)-SULFANLBENZOXAZOLE FOR TESTING AS ANTICONVULSANT

(PART I)

A.A. El-Helby; M.A. Amin; M.K. Ibrahim and K. El-Adl.

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

Some new derivatives of 2-(substituted sulfanyl)-5-methyl/chloro/nitro and unsubstituted-(3H)benzoxazole were synthesized through the reaction of the later or their potassium salts with different chloroacetates and chloro-3-propionates esters to afford alkyl 2-(5-substituted-benzoxazol–2-ylsulfanyl) acetates and propionate esters IIIa-c. Other condensation reaction with chloroacetamides or chloro-3-propionamides gave 2[alkyl/cycloalkyl/substituted aryl(5-substituted-benzoxazol-2-ylsulfanyl)] acetamides and or propion-amidesIVa-d. Some of the synthesized compounds were evaluated for anticonvulsant activity, some of them showed promising anticonvulsant activity against PTZ in mice using phenobarbitone as reference compound.

 

 

7/11 BIOCHEMICAL STUDIES ON CONTRACEPTIVE EFFECTS OF HOT WATER EXTRACT OF SILYBUM MARIANUM LEAVES IN FEMALE ALBINO RATS.

E.A.M. Khalil

Dept. of Medical Biochemistry National Orgnization For Drug Control and Research,

Cairo, Egypt

Hot water extract of Silybum marianum leaves prevented pregnancy in female albino rats treated orally at 500mg /kg B.W.daily dose on day 1-5 post-coitum.The dose (500mg/kg)of hot water extract of Silybum marianum leaves which proved to have antifertility activity was administered to adult female albino rats for 12 weeks. Significant increase in body weight, total protein and albumin was observed. No significant variation in haemoglobin values,erythrocyte counts, concentration in serum aspartate aminotransferase and serum alanine aminotransferase activities was recorded .Significant reduction in concentration of serum total cholesterol,serum globulins,creatinine,blood urea nitrogen and blood sugar. No significant histopathological lesions were observed in liver,kidney, spleen and ovarian tissue following treatment. Meanwhile the most affected organ was the uterus in which the uterine wall had hyperplasia and metaplasia according to that fertlized ova did not implant in the wall. The results of this research indicated that the hot water extract of Silybum marianum leaves may be more safe, cheap, effective antifertility agent and the leaves could be used in a form of tea bags to prevent pregnancy in women.

 

 

8/11 DESIGN AND SYNTHESIS OF SOME NEW DERIVATIVES OF DIBENZ[C,E]AZEPINE-5,7-DIONES FOR TESTING AS ANTICONVULSANT AGENTS

A.A. El-Helby, M.A. El-Zahabi, M.A. Amin, M.K. Ibrahim,

S.G. Abdel-Hameed and A.M. Ebaid.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy,

Al-Azhar University, Cairo, Egypt.

Some of the new 2'-(Substituted carbamoyl)-biphenyl-2-carboxylic Acids (Va-I), 6-(aralkyl/aryl)-dibenz[c,e]azepine–5,7-diones(VIa-I),6-(alkyl/arylcarbonylmethyl)–dibenz [c,e] azepine-5,7-diones(Xa-d),6-(alkyl/aryloxycarbonylmethyl)-dibenz [c,e]azepine- 5,7-diones (XIa-g), 6-(alkyl/arylaminocarbonylmethyl)dibenz[c,e] azepine-5,7- dione derivatives (XIIa-i) and 6-[2-(alkyl/arylcarbonyloxy)ethyl]-dibenz[c,e]azepine-6,7-diones (XIIIa-e) were synthesized. Some of the synthesized compound were evaluated for anticonvulsant action in mice. Some derivatives showed promosing activity in protection of the experimental animals against pentylenetetrazol-induced convulsion comparing with phenobarbitone.

 

9/11 ANTITUMOR ACTIVITY OF INOSITOL HEXAPHOSPHATE (PHYTIC ACID) IN MICE LOADED WITH SOLID TUMOR

M.A.M. El-Gawish

Radiation Biology Department, National Center for Radiation Research and Technology, Cairo, Egypt.

The present study was designed, aiming at the highlighting the effect of inositol hexaphosphate (phytic acid) on the growth of transplanted Ehrlich ascites carcinoma (EAC) in female mice as well as its protective effect against the damage caused by EAC through some biochemical analysis including the determination of ATP-ase activity as well as Na+, K+, Ph, Zn, Mg+2, Ca+2 and Fe in serum, liver and tumor in mice bearing EAC after 30 days of inoculation. Cell cycle kinetics in tumor tissue in response to IP6 was also investigated by DNA flow cytometry. This study revealed that injection of mice with phytic acid at a dose of (250mg/100g b.w.) at the same day of tumor transplantation could significantly delay the growth of solid tumor as compared with EAC group. The data of the current study indicated that phytic acid could ameliorate the recorded disturbances in the levels of the investigated elements as well as the activity of ATP-ase in serum, liver and tumor of animals bearing EAC. Such amelioration may be attributed to the defense strategies (defense mechanism) of phytic acid against tumor growth as well as its behavior as chelating agent. Flowcytometric DNA analysis of rat tumor (EAC) showed aneuploidy of 54.5 % while administration of IP6 induced a reduction of aneuploidy to 22.5 % comparable to control group. In addition, the protective role of phytic acid when given prior and during tumor inoculation, in counteracting the damaging effects of EAC is due to its highly antioxidative activity as a free radical scavenger as well as a chemopreventive agent.

 

10/11 SPECTROPHOTOMETRIC DETERMINATION OF FOUR DRUGS ACTING AS REDUCING AGENTS FOR 1, 10 PHENANTHROLINE – FERRIC REAGENT

M.Y. El-Maamli

Analytical Chemistry Department, Faculty of Pharmacy- Zagazig University,

Zagazig, Eygpt.

A simple, rapid, sensitive and accurate method for the determination of carbocisteine, cefoperazone Na, flunarizine HCl and isoxsuprine HCl in pure samples and in pharmaceutical formulations is developed. The method is based on the formation of tris (o-phenanthroline)iron(II) complex (Ferroin) upon reaction of the cited drugs with iron(III) -o- phenanthroline mixture. The ferroin complex is colorimetrically measured at lmax 510 nm against a reagent blank. Optimization of the experimental conditions is described. Beer’s law is obeyed in the concentration range from 0.6-77µg ml-1 with molar absorpitivities (e) ranging from 3.01 x 103 –11.98 x 104 L.mol-1.cm-1 and Sandell sensitivities (S) of 1.22 – 69.6 ng cm-2 . The developed method is applied successfully for the determination of the cited drugs in pure samples and in the corresponding pharmaceutical formulations without any interferences from common excipients.

 

11/11 HERBAL DRUGS IN EGYPT. QUALITY CONTROL OF TWO DIETARY FIBER PRODUCTS

M.M. Shabana; M.H. Goneid; M.F. Yousif and *A.A. Sleem

Pharmacognosy Department, Faculty of Pharmacy, Cairo University and              

* Pharmacology Department, National Research Center, Egypt

Two dietary fiber products, namely: Mepaco Bran and Goanet were subjected to quality control analysis to establish their identity, purity, safety, stability and efficacy. The methods applied included organoleptic characters, physicochemical tests and microscopical examination of the diagnostic elements of their components, bran and guar gum respectively as well as pharmacopoeial constants. Percentages of protein content of both products were also determined. Quantitative determination of total dietary fiber content of Mepaco Bran and total galactomannan content of Goanet was carried out by different methods. The forementioned analyses were applied on the product, raw material of bran and guar gum as well as on the product at the expiry date in each case. Potential contaminants: pesticide residue, heavy metals, radioactive contaminants, micro-organisms and microbial toxins in both products were also investigated. Pharmacological evaluation of both preparations was carried out, namely: hypolipidaemic, hypoglycaemic, anti-ulcerogenic activities and effect on stool weight and consistency in male albino rats.

12/11 PREVALENCE OF HEPATITIS B, C AND BILHARSIASIS among PATIENTS WITH HEPATOCELLULAR CARCINOMA

H.A. Osman, A. Abou-El Fotuh* and A. Osman**

Tropical Medicine, General Medicine* and Community Medicine Departments,**Faculty of Medicine, Al Azhar University, Cairo, Egypt.

            The incidence of hepatocellular carcinoma (HCC) has been increasing world wide over the last years. A great number of HCC develop from chronic liver disease. In Egypt S. mansoni and hepatitis viruses constitute the most common causes of chronic liver diseases. This study designed to detect the prevalence of hepatitis B, C infection and bilharsiasis among HCC patients in comparison with normal subjects. For this purpose twenty patients with HCC (Group 1) compared to twenty apparently normal subject (Group 2). All patients and control group under clinical, laboratory examination for detection of HBsAg, HCV Ab., bilharsiasis antibodies by ELISA technique and detection of hepatitis C-RNA by PCR technique. Results: revealed high prevalence of the HCC in males than female 4 :1, and the age of patient with HCC ranging from 28– 72 years. The seromarkers of hepatitis B, C infection and bilharsiasis infection in sera of HCC patients (group I), show that, the only significant ratio is that the HCV infection (P < 0.001) as 90% of studied cases were infected by HCV, 55% of cases were infected by bilharsiasis and only 5% of cases have +ve HBsAg, all of bilharsial cases and HBV infection cases found to have HCV infection. The presence of significant number (90%) of patients infected with HCV indicate that HCV infection considered one of the most important causes of HCC in Egypt. Also the concomitant infection with bilhasiasis and hepatitis B may be the cause of increased incidence of hepatocarcinogenesis in those patients. We concluded that preventing the transmission of hepatitis viruses is most important for reducing the risk of HCC.

 

13/11 development of economic corneal formula containing azole derivative for the treatment of human fungal keratitis

M. A. El-Nabarawi, H. M. El-Mofty*,M. H. Ahmed** and I. K. Behiry***

1-Department of Pharmaceutics, Faculty of Pharmacy, Cairo University; 2,3-Department of Ophthalmology, Faculty of Medicine, Cairo University; 4-Department of Clinical Pathology, Faculty of Medicine, Cairo University.

This study aimed to formulate an economic dosage form (with low cost for patient) containing azole drug for treatment of fungal keratitis.Two azole compounds (ketoconazole and fluconazole) were chosen for this study. The traditional eye ointments (oleaginous and absorption) and gels (methylcellulose MC, Pluronic F127and polyethylene glycol) were used as vehicles for either drugs. The concentration of drug was 2%w/w. Each formula was characterized in terms of drug release, pH measurements, viscosity, mucoadhesion (in-vitro and in-vivo) and stability studies. The release rate of drugs from different formulations decreased in the following order: PEG base > PF127 gel > methylcellulose gel > absorption ointment > oleaginous ointment. The release of both drugs from different formulations was found to follow first-order kinetics. The addition of polyvinyl pyrrolidone, PVP, as an enhancer to selected formulae improved the release of both drugs. The release of ketoconazole (K) was increased by about ~7.8 , 13 and 1.2 folds for oleaginous, absorption, and MC bases respectively. While in case of fluconazole (F), the release increased by about 7.6, 20 and 1.4 folds for oleaginous, absorption, and MC bases respectively. From the economical point of view, the selected bases (MC/PVP and absorption/PVP formulations) for both drugs (K and F) were preferred to Pluronic F127 in formulations due to their lower costs and high drug release. These bases were used for microbiological studies (in-vitro and in-vivo) using different fungal species isolated from cases of keratomycosis.These are Aspergillus species (flavus and fumigatus), Candida albicans, and non-Candida. In-vitro tests revealed that MC/PVP base gave a larger inhibition zone than absorption/PVP base for both drugs. This result was in a good agreement with the release data. In-vivo microbiological test was done on rabbit`s eye. The rabbits infected with fungus responded better and showed improvement in size and depth of ulcer. Hypopyon was improved when using both formulae of ketoconazole. The medicated MC/PVP base was more effective compared to absorption/PVP base. Ketoconazole bases showed better results than fluconazole bases. The formulation containing 5% MC, 5% PVP and 2% ketoconazole (high drug release, large inhibition zone and high activity against infected rabbit`s eye) was chosen for the clinical study. Twenty patients having fungal keratitis with indolent ulcers were chosen among patients presented to Department of Ophthalmology, Kasr El-Aini University Hospital, Cairo, Egypt. Treating these twenty patients with the prepared ketoconazole gel was done by instructing them to apply the gel five times daily. There was an improvement in size and depth of the ulcer in 15 of the patients, 75%, while 5 patients did not improve. The improved clinical ulcers showed also an improvement of posterior segment reaction which decreased especially in aphakic patient. The improvement in visual acuity was minimal due to late presentation of cases.

14/11 APPLICATION OF HIGH PERFORMANCE LIQUID CHROMATOGRAPHY (HPLC) AND SPECIAL COMPUTER PROGRAM FOR CALCULATING THE PHARMACOKINETICS AND BIOAVAILABILITY OF INDOMETHACIN TABLETS FOLLOWING THEIR ORAL ADMINISTRATION TO HUMAN VOLUNTEERS

A.M.S. Ahmed*, N.M. Al-Abasawy**, A.H.R. Mohamed* and M.I.A. Fetouh*

Pharmaceutics Dept.* and Pharmaceutical Chemistry Dept.**,

Faculty of Pharmacy, Al-Azhar Univerity, Nasr City, Cairo, Egypt.

The aim of the following paper is to study the bioavailability of the chosen formulated Indomethacin tablets prepared by solid dispersion with different Eudragit polymers as compared to plain tablets and commercial enteric coated capsules, after their oral administration to human volunteers. HPLC procedure was used for the above purpose. Sample preparation involves extraction of Indomethacin and its 4 – chlorobenzoic acid metabolite from plasma by acetonitrite. The analysis is carried out on reversed phase chromatographic system using Alpha Bond C18 column with a mobile phase consisting of 65 % methanol and 35 % orthophosphoric acid at pH = 4.0. The pharmacokinetic parameters of different Indomethacin treatments have been calculated by applying special computer program. Also the relative bioavailability of the chosen Indomethacin tablets was estimated. ANOVA test was applied to the investigated treatments relative to the standard commercial capsule taking into consideration the pharmacokinetic parameters (Cmax, kab, kel, AUC0-24 and AUMC0-24). The following treatments were administered to the human volunteers: I- a tablet containing 50 mg Indomethacin with Eudragit L100 (1:6) as solid dispersion; II- a tablet containing 50 mg Indomethacin with Eudragit S100 (1:4) as solid dispersion; III- a tablet containing 50 mg Indomethacin with an equal mixture of Eudragit L100 and S100 (1:6) as solid dispersion; IV- a plain tablet containing 50 mg Indomethacin and V- an enteric coated soft gelatin capsule containing 50 mg Indomethacin. Formula containing Eudragit L100/S100 with the ratio 1:6 drug–polymer was found to be the best studied treatment as it showed: short tmax, medium Cmax, medium MRT, good kab, and kel, and the best relative bioavailability.

 

15/11 Protective effect of Thymoquinone against diet-induced hypelipidemia in rats

A.D. Mariee and M.A. El-Mahdy*

Departements of Biochemistry and *Pharmacology & Toxicology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

The purpose of this study was to investigate the effect of thymoquinone (TQ), the main constituent of the volatile oil of Nigella sativa seeds, on serum lipids and liver enzymes of rats fed with a high-cholesterol diet (HCD). Therefore, different groups of animals were used. One group was orally administered TQ in a dose of 5 mg/kg for twenty consecutive days. A second group was received by gavage, a hypercholesterolemic diet for consecutive fifteen days, while the third one was treated with HCD-enriched with TQ. In the third group, rats were received TQ for five days before the HCD and continued for another 15 days concomitantly with HCD. Corresponding control animals were also used. The diet-induced high serum levels of total cholesterol (TC) and low-density lipoprotein LDL-cholesterol were significantly reduced by thymoquinone administration compared to HCD-treated animals. Thymoquinone administration prevented, as well, the decrease in high-density lipoprotein HDL-cholesterol induced by the same hypercholesterolemic diet. The atherogenic indices: TC/HDL-C and LDL-C/HDL-C have been remarkably reduced, following TQ treatment. No significant difference in the level of triglycerides (TG) was found among all studied groups. This study also revealed that thymoquinone administration protects against the increase of serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) activities induced by feeding the animals HCD. Finally, lipid peroxidation and certain antioxidant parameters were studied in liver tissues. Results showed that thymoquinone-treated hypercholesterolemic animals exhibited a reasonable improvement of the studied hepatic parameters of oxidative stress, when compared to HCD-treated animals. The solitary administration of thymoquinone did not significantly affect the serum level of lipid profile or liver enzyme activity, and it has no sensible effect on oxidative stress parameters, compared to the control group. The data revealed that thymoquinone had obviously a hypocholesterolemic effect, and it suggests that thymoquinone protects against hyperlipidemia, possibly through participation in the prevention of oxidative damage to liver, and/or through the regulation of cholesterol metabolism. These observations propose that thymoquinone might be applicable as a potective agent for hyperlipidemia associated with bad nutritional habits.

 

 

16/11 STABILITY INDICATING HPLC- METHOD FOR DETERMINATION OF ENROFLOXACIN AND FLUMEQUINE IN VETERINARY PREPARATIONS AND BULK FORMS

O. Abd El-Sattar

Pharm. Chem. Dept., Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

A sensitive high-performance liquid chromatographic (HPLC) method was developed and validated for the quantitation of enrofloxacin (ENF) and flumequine (FLQ) in bulk powder and in pharmaceuticals. Separation of ENF was undertaken on SynChropak C18 column (25 cm x2.1 mm I.D., 10 mm particle size) using a mobile phase consisting of water-acetonitrile (85:15, v/v) ,its pH adjusted at 3.5 with H3PO4. FLQ separation was made on AlphaBond C18 column (30 cm x 3.9 mm I.D., 10 mm particle size) with a mobile phase containing water-acetonitrile-H3PO4 (65:35:1,v/v/v). Separations were done at flow rate of 1 ml min-1 with UV- detection at 270 nm ( ENF) or at 240 nm   (FLQ). The linearity of ENF and FLQ was within concentration ranges 1-20 mg ml-1 and 4-25 mg ml-1, respectively. The limits of detection (LOD) and quantitation (LOQ) were 0.30 and1 mg ml-1 for ENF and were 1.60 and 4 mg ml-1 for FLQ and with RSD% <2. The mean percentage recovery ranges were 99.65 %- 99.98 %for ENF and 99.14% - 100.12% for FLQ. Acid degraded ENF and FLQ were separated from the pure drug with significant Rt values differences showing a stability indicating characteristics of the method.

 

 

17/11 BIOACTIVE EXTRACTS OF DIFFERENT ORGANS OF CRYPTOSTEGIA GRANDIFLORA R. BR. GROWN IN EGYPT

S.M. El Zalabani, E. Abdel-Sattar, F.I. Fathy and N.G. Shehab

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

The alcohol extracts of the flowers, seeds and non-flowering branches of Cryptostegia grandiflora R.B. were successively fractionated with light-petroleum, chloroform and n-butanol. The parent extracts and their respective fractions were comparatively investigated for their antimicrobial and cytotoxic potentials. Selected gram positive and gram negative bacteria, and fungi were used for antimicrobial screening. Cytotoxic activity was determined using Erhlich ascites carcinoma (EAC) cell-line, in vitro.The tested samples showed variable antimicrobial efficacy, the highest was detected in the light-petroleum fraction of the alcohol extract of the flowers. The antifungal activity is for thefirst time reported, and exceeds in most cases the antibacterial effect. The alcohol extract of the seed exhibited a significant cytotoxic activity, its light-petroleum fraction being the most active. Alcohol extracts of the other organs showed no cytotoxic activity.Carbohydrates and/or glycosides, cardenolides, flavonoids, and sterols and/or triterpenes were detected in appreciable amounts in the different organs.

 

18/11 CEFADROXIL QUANTIFICATION IN HUMAN PLASMA BY MICROBIOLOGICAL TECHNIQUE. APPLICATION FOR BIOEQUIVALENCE STUDY.

S. Shalaby, E. Ezz El-Din and R. El-Maadawy

National Organization for Drug Control and Research., Cairo, Egypt.

This study was conducted to asses the bioequivalence of 500 mg Cefadroxil capsules (generic A) and relative bioavailability of 1000 mg tablets of the same company (generic B) relative to the reference capsules 500 mg. The in-vitro dissolution study of the both formulations was found conforming to the USPXXIII requirements of dissolution test (NLT 80% after 30 minutes) of the labeled amount of cefadroxil. Twenty-four healthy adult male subjects were enrolled in a randomized, three-period crossover design. All subjects were within 15 % ideal body weight, and between 20 – 45 years of age. Sixteen samples were collected for 24 hours following oral dosing and assayed applying the microbiological agar cylinder diffusion method using Bacillus subtilus ATCC No. 6633 , as well as a selected HPLC method for the determination of cefadroxil plasma concentration in volunteers. Pharmacokinetic parameter values of Cmax and tmax were obtained directly from plasma data, kel was estimated by log-linear regression, and AUC0-t, AUC0-inf were calculated by mixed linear-logarithmic trapezoidal rule. Different statistical tests were performed on the basis of untransformed and log-transformed data and the overall residual variance from ANOVA. Results of cefadroxil plasma concentration analysis applying microbilogical method showed no significant difference in-comparison to the results obtained from the HPLC method. All the generally accepted tests showed that the generic formulation (500 mg capsules) can be considered as bioequivalent, also the generic formulation (1000mg tablets) are relative in bioavailability to the reference one, with respect to the extent of absorption, given by the AUC0-inf and with respect to rate of absorption as assessed by Cmax and tmax. The present microbiological method was found , from the accuracy and economical point of view is suitable enough for the bioequivalence study in comparison to the HPLC method.

 

 

19/11 PRODUCTION OF AMINOOLIGMERS BY THE ENZYMATIC HYDROLYSIS OF CHITIN AND CHITOSAN

S.M. Abdel-Aziz and A.S. Gad*

Microbial Chemistry Dept. and Chemistry of Natural and Microbial Products Dept.,* National Research Center, Cairo, Dokki, Egypt.

Five bacterial strains (B. megaterium, B. subtilis, B. cereus, E. coli and
pseudomonas sp.
) were examined for chitinase and chitosanase activity with chitin or partially acetylated chitosan. Results indicated that the degree of deacetylation of chitosan greatly affected the enzyme activity. It was also found that B. megaterium and B. Subtilis, individually, or by co-culturing system possess the ability to degrade chitin, partially acetylated chitosan, or fully deacetylated chitosan as a sole carbon source. These results may reflect presence of co-enzymes with broad-specificity towards chitineous polymers. The chitinase-chitosanase enzyme obtained from the hydrolyzate of B. megaterium and B. subtilis mixed culturewas found to be highly active on a variety of substrates. The biochemical characterization of this enzyme was studied. In General, mixed culturing system, apparently may overcome limitation of substrate specificity and yield large-scale production of aminooligomers.

 

 

20/11 ISOLATION OF NOFORMYCIN FROM A NITRIC OXIDE SYNTHASE CONTAINING SPECIES OF NOCARDIA

M. Hosny

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

Cairo, Egypt.

(+)-Noformycin, (5S)-2-imino-pyrrolidine-5-carboxylic acid-(2-carbamimidoyl-ethylamide) was isolated from cultures of Nocardia sp. NRRL 5646, purified chromatographically, and its structure was completely established by mass and NMR spectroscopic analyses, and by comparison with an authentic synthetic standard of noformycin. The occurrence of noformycin in a species of Nocardia that contains a nitric oxide synthase (NOS) enzyme system presents important evidence of a possible role for the bisamidino compound in Nocardia resistance to nitric oxide, the product of NOS oxidation of arginine.

21/11 CYTOTOXIC NEOCLERODANE DITERPENOIDS FROM CLERODENDERUM splendens

M. Hosny

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

Cairo, Egypt.

1D-NMR (1H and 13C) and 2D-NMR spectroscopy as well as high resolution electrospray ionization mass spectrometry (HRESI-MS) have been used to determine the structures of two new neo-clerodane diterpenoids, splendensins A (1) and B (2), isolated from the aerial parts of Clerodendrum splendens Gaertn. Both 1 and 2 showed dose-dependant inhibitory activities against murine (L1210, leukemia. B16-F10, melanoma) and human cancer cell lines, A549 (lung adenocarcinoma), SK-OV3 (ovarian) and K562 (leukemia) with EC50 values of 4.32-21.68 mg/mL.

 

 

22/11 SYNTHESIS OF SOME NEW DERIVATIVES OF 3H-QUINAZOLIN-4-ONE WITH ANTICEPATED ANTICONVULSANT ACTIVITY

A.A. El-Helby and M.H. Abdel Wahab*

Department of Pharmaceutical Chemistry and *Department of Pharmacology,

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

A new series of 3-substituted -2-substituted methylsulfanyl-3H-quinazolin-4-one derivatives (4a-l) were synthesized through condensation reaction of their potassium salts (3a-l) with methyl, ethyl and phenylisocyanate. The newly synthesized derivatives (4a-l) were evaluated for anticonvulsant activity. It was found that these compounds showed high anticonvulsant activity at low doses (50 -100 mg/kg), whereas at dose over 100 mg/kg showed stimulant effect on central nervous system which potentiated the effect of convulsive agent, pentylenetetrazole in mice. A series of halogenated derivatives, 3-methyl, 3-ethyl and 3-phenyl-6-mono and 6,8-disubstituted 3H-quinazolin-4-one derivatives (4m-z) were also synthesized and evaluated for anticonvulsant activity. Reduced anticonvulsant activity was recorded.. phenobarbitone sodium was used as reference drug.

Scroll to top