eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-01
34
2
93
103
10.21608/bfsa.2011.63247
63247
Original Article
DETECTION OF EXTENDED-SPECTRUM -LACTAMASE ENZYMES (ESBLs) PRODUCED BY ESCHERICHIA COLI URINARY PATHOGENS AT ASSIUT UNIVERSITY HOSPITAL
Amany Thabit
1
Tharwat El-Khamissy
2
Maggie Ibrahim
3
Adel Attia
4
Department of Microbiology and Immunology, Faculty of Medicine, Assiut University
Department of Microbiology, Faculty of Pharmacy, Al-Azhar University, Assiut
Department of Microbiology and Immunology, Faculty of Medicine, Assiut University
Department of Microbiology, Faculty of Pharmacy, Al-Azhar University, Assiut
This study was conducted to evaluate the rate of urinary tract infection at Assiut University Hospitals, and to determine the prevalence of extended-spectrum β-lactamase enzymes producing community- and hospital-acquired E. coli uropathogens at Urology Department in Assiut University Hospitals. Also, to perform the antimicrobial sensitivity testing for E. coli isolates to extended-spectrum cephalosporins according to CLSI. Phenotypic confirmatory tests (combined disc method, double disc diffusion method and ESBL-E-Test) were performed to test E. coli isolates for ESBL production and it was concluded that 30 (39.47%) of community isolates and 42 (70%) of nosocomial isolates were ESBLs producers.
https://bpsa.journals.ekb.eg/article_63247_3e4cd1ca99149b3abf823d574b90d525.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-01
34
2
105
120
10.21608/bfsa.2011.63250
63250
Original Article
ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF DOMPERIDONE BY UTILIZING DIFFERENT TECHNIQUES
E. Ibrahim
1
T. El-Faham
2
F. Mohammed
3
N. El-Eraky
4
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, P.O 71526, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, P.O 71526, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, P.O 71526, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, P.O 71526, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, P.O 71526, Egypt
https://bpsa.journals.ekb.eg/article_63250_73b2403c141a1a8b54c1234b05b87c2f.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-31
34
2
159
179
10.21608/bfsa.2011.63272
63272
Original Article
SYNTHESIS OF SUBSTITUTED DIHYDROPYRIMIDINES AS HYPOTENSIVE AGENTS
Salah Abdel-Aziz
1
Nawal El-Koussi
2
Hoda Hassan
3
Adel Youssef
4
Magda Yousri
5
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Al-Azhar University
Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University
Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University
Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University
Department of Pharmacology, Faculty of Medicine, Assiut University
A series of Dihydropyrimidines (DHPMs) with variable substituents at four positions in pyrimidine nucleus (I-IV), were prepared and tested for their calcium channel blocker and hypotensive effect using amlodipine as a reference compound. Molecular alignment revealed a direct correlation between fitting and in-vitro rat ileum relaxation. A pharmacophore was developed for compounds with hypotensive and/or calcium channel blocking activity. Series IV showed hypotensive and calcium antagonist effect, while series I and II showed calcium antagonist activity without hypotensive action. Series III were devoid of either effect.
https://bpsa.journals.ekb.eg/article_63272_030e992fb910efe5304215ff77376071.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-30
34
2
181
187
10.21608/bfsa.2011.63273
63273
Original Article
THE EXPRESSION PATTERN OF GALECTIN-3 IN THE RAT HEPATOCELLULAR CARCINOMA
Omar Mohafez
1
Mohamed Abd EL-Aziz
2
Ahmed Abd El-Ghany
3
Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, Assiut branch, Egypt
Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, Assiut branch, Egypt
Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, Assiut branch, Egypt
Hepatocellular carcinoma (HCC) is the third most frequent cause of cancer death world wide, with an estimated mortality rate of about one million deaths annually. Galectin-3 is widely spread among different types of cells and tissues. Galectin-3 found intracellularly in nucleus and cytoplasm. Galectin-3 affects numerous biological processes and seems to be involved in different physiological and pathophysiological conditions, such as development, immune reactions, and neoplastic transformation and metastasis. In this study, we found over expression of galectin-3 protein and mRNA, in HCC tissue compared with normal liver tissue. In addition, we found expression of galectin-3 in the nuclear protein fraction. The overexpression of galectin-3 was accompanied with elevated levels of serum nitrite and aminotransferases (AST and ALT).
https://bpsa.journals.ekb.eg/article_63273_db8e31ca28a2b738fa8dca9be737030b.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-01
34
2
121
129
10.21608/bfsa.2011.63257
63257
Original Article
CYTOTOXICITY OF ACULEATISIDE-A TO HEPATOCELLULAR CARCINOMA CELLS DETERMINED BY MTT BIOASSAY
Alaa Nafady
1
Omar Mohafez
2
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt
Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt
From the methanolic extract of fresh fruits of Solanum reflexum Schrank, a major compound was isolated and identified as; aculeatiside-A 1. The structure of the isolated compound was elucidated on the basis of 1H and 13C and DEPT-13C-NMR; in addition to comparison with reported data. The cytotoxic effect of aculeatiside-A on hepatocellular carcinoma cells and its mechanism was investigated. It was accomplished that aculeatiside-A inhibit the growth of HepG-2 cells significantly by induction of apoptosis. Marked morphological changes of apoptosis were observed clearly. The results for the first time demonstrate that aculeatiside-A has significant anti-proliferation effect by induction of apoptosis on hepatocellular carcinoma cells in-vitro, down regulation of Survivin and Bcl-2 expressions as well as up regulation of Bax and P53 expression may be one of the important apoptotic inducing mechanisms.
https://bpsa.journals.ekb.eg/article_63257_30dfdd116f9cd23f8dfee7d086486b09.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-01
34
2
131
140
10.21608/bfsa.2011.63259
63259
Original Article
THREE REVERSED PHASE LIQUID CHROMATOGRAPHIC METHODS FOR THE DETERMINATION OF SOME ANTICHOLENERGIC DRUGS IN THE PRESENCE OF THEIR DEGRADATION PRODUCTS AND / OR IN MIXTURE WITH OTHER DRUGS
Sonia Hassib
1
Naglaa El-Kousy
2
Al-Shimaa Alian
3
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr ElAini street, Cairo 11562, Egypt
National Organization of Drug Control and Research (NODCAR), Cairo, Egypt
National Organization of Drug Control and Research (NODCAR), Cairo, Egypt
Three RP-LC methods have been developed for the quantitative determination of some anticholinergic drugs in the presence of their degradation products and/or in mixture with other drugs. In method (I) pipoxolan HCl is estimated in the presence of its alkaline-induced degradation products, 0.02 M phosphate buffer pH 7.5: acetonitrile (30:70 v/v) was used as a mobile phase with UV detection at 215 nm. Drofenine HCl was used as an internal standard. Method (II) describes the simultaneous determination of drofenine HCl and propyphenazone in the presence of drofenine HCl alkaline-induced degradation product. This method used 0.05 M phosphate buffer pH 3.5: acetonitrile (60:40 v/v) as a mobile phase with UV detection at 215 nm. In method (III) the simultaneous determination of isopropamide iodide and triflouperazine HCl is presented. In this method 0.05 M phosphate buffer (containing 0.1% triethylamine) pH 3.5: acetonitrile (50:50 v/v) was used as a mobile phase with UV detection at 210 nm. Pipoxolan HCl was used as an internal standard in the determination of the two binary mixtures.
https://bpsa.journals.ekb.eg/article_63259_68999151ec53acad4c95edb2c08cc953.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-01
34
2
141
148
10.21608/bfsa.2011.63260
63260
Original Article
FORMULATION AND EVALUATION OF MECLIZINE HCl ORALLY DISINTEGRATING TABLETS
Gamal Mahrous
1
Gamal Shazly
2
Mohamed Ibrahim
abbma71@gmail.com
3
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia
Recent advances in novel drug delivery system aims at achieving better patient compliance. One of these advances is the formulation of orally dissolving tablets (ODTs) which dissolve instantaneously, releasing the drug, within a few seconds without the need of water. The main objective of this paper was to prepare and develop ODTs of Meclizine (MZ HCl) with sufficient mechanical integrity, content uniformity, and acceptable palatability to assist patients of any age for easy administration. Meclizine HCl is an anti-emetic drug used for management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting. The interaction of meclizine and used excipients was studied using differential scanning calorimetry (DSC). The ODTs were prepared by direct compression method. The effect of varying concentrations of different superdisintegrants such as crospovidone, croscarmellose sodium, and sodium starch glycolate on disintegration time and dissolution rate was studied. The prepared tablets were evaluated for hardness, friability, disintegration time and in-vitro drug release. DSC studies revealed that no interaction between the drug and the used excipients. All tablets had hardness in the range 4.25.6 kp and friability less than 1%. Weight variation and drug content of all formulations were within official limit according to BP. In-vitro drug release study of ODTs tablets showed that more than 90% of the drug was released within 10 min. Palatability test by 12 volunteers showed acceptable taste and mouth feel. Thus, results obtained conclusively demonstrated successful rapid disintegration of the formulated tablets and acceptable palatability.
https://bpsa.journals.ekb.eg/article_63260_9cd1dbbe5ef63b132c69e735a7064a6c.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2011-12-01
34
2
149
158
10.21608/bfsa.2011.63262
63262
Original Article
DESIGN, SYNTHESIS AND ANTIDIABETIC ACTIVITY OF SOME NEW 4-AMINO (OR 6-OXO)-2-METHYL/BENZYLTHIO (OR SUBSTITUTED AMINO) PYRIMIDINE DERIVATIVES
Salah Abdel-Aziz
1
Mostafa Hussein
2
Ihab Abdel-Raheem
3
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut-71524, Egypt
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71526, Egypt
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Al-Azhar University, Assiut-71524, Egypt
A new series of 4-amino-5-cyano-2-methyl/benzylthio (or substituted amino) 6-substituted phenyl pyrimidines 5a-l, and 2-methyl/benzylthio (or substituted amino)-5-cyano-1,6-dihydro-6oxo-4-(substitutedphenyl) pyrimidines 6a-l was prepared. The reaction of S-methyl (or benzyl) isothiourea salts 1a,b with benzylidenemalononitriles 2a-c afforded compounds 5a-f. Reaction of compounds 5a-c (R= methylthio) with the appropriate amines 4a,b (cyclohexylamine or 2phenylethylamine) afforded 4-amino-2-substituted amino-5-cyano-6- (substituted phenyl) pyrimidines 5g-l. On the other hand, reaction of S-methyl (or benzyl) isothiourea salts 1a,b with ethyl α-cyanocinnamates 3a-c afforded compounds 6a-f. Reaction of compounds 6a-c (R= methylthio) with the appropriate amines 4a,b afforded 2-substituted amino-5-cyano-4-oxo-6(substituted phenyl) pyrimidines 6g-l. The purity of the new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1H-NMR, and mass spectrometry along with elemental microanalyses. All the target compounds were evaluated for their in-vivo antidiabetic effects in rates in comparison with metformin as a reference drug.
https://bpsa.journals.ekb.eg/article_63262_94b77d1f432b7bef95bb5f3146341a6f.pdf