Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
01
MACRO- AND MICROMORPHOLOGY STUDIES OF THE LEAF, STEM AND STEM BARK OF FICUS PANDURATA HANCE. CULTIVATED IN EGYPT
1
28
EN
M.
A. Ramadan
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
A.
S. Ahmad
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
A.
M. Nafady
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
A.
I. Mansour
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
10.21608/bfsa.2008.156593
<em>Ficus pandurata (Hance) Fiddle leaf fig (Family, Moraceae) is a tree indigenous to South Africa and cultivated in Egypt for its shade in public and private gardens. Previous investigations of Ficus species showed many medicinal uses; externally they have been used for treatment of leprosy, ulcers, itching, leucoderma and warts. Internally used as anti-inflammatory, to reduce fever, cure tuberculosis and against intestinal parasites. In the present work, the detailed macro-and micromorphological characters of the leaf, stem and stem bark of Ficus pandurata Hance were studied with the aim to find out the diagnostic elements of these organs, which facilitate their identification in both entire and powdered forms.</em>
https://bpsa.journals.ekb.eg/article_156593.html
https://bpsa.journals.ekb.eg/article_156593_fa446b6004a7ca9898a3ea79d85b4759.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
SYNTHESIS AND PHARMACOLOGICAL SCREENING OF CERTAIN IMIDAZOQUINAZOLONE DERIVATIVES
29
48
EN
Fatma
A. Ragab
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt
Hassanein
H. Hassanein
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt
Enayat
I. Ali
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt
Hanan
H. Georgey
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt
10.21608/bfsa.2008.156596
<em>Certain imidazoquinazolin-5(4H)-one derivatives have been synthesized by replacement of the 4-amino group compound I with different moieties of expected biological activity.</em>
<em>Representative example of the synthesized compounds were tested for their anti-inflammatory, analgesic, antipyretic and anticonvulsant activities. Certain derivatives showed activities higher than that of the reference drugs.</em>
https://bpsa.journals.ekb.eg/article_156596.html
https://bpsa.journals.ekb.eg/article_156596_8fe67fbb035ae64a7263b83c65ddab4f.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
CONTROLLED-RELEASE PREDNISOLONE POLY (DL-LACTIDE) MICROSPHERES: IMPACT OF FORMULATION PARAMETERS, CHARACTERIZATION AND RELEASE MECHANISM
49
67
EN
Khaled
A. Khaled
Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt
Hatem
A. Sarhan
Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt
Mohamed
A. Ibrahim
Department of Pharmaceutics, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
Youssef
W. Naguib
Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt
10.21608/bfsa.2008.156598
<em>The steroidal drug prednisolone was encapsulated into microspheres using the biodegradable polymer poly (DL-lactide) using emulsion-solvent evaporation method. The produced microspheres were characterized using scanning electron microscopy, X-ray diffractometery, FT-IR spectroscopy, DSC, and laser light diffraction. The morphology, particle size distribution, encapsulation efficiency (EE%), and drug release showed marked dependence upon formulation parameters viz. initial polymer concentration, surfactant concentration, drug-to-polymer ratio, and volume of the external aqueous phase. The effect of the addition of hydrophilic additives such as PVP or PEG 8000 was also investigated. The encapsulation efficiency percent and the mean particle size were increased by increasing the initial polymer concentration and drug polymer ratio. On the other hand, increasing the surfactant concentration resulted in decreasing the mean particle size and increasing the drug release from the microspheres. The probable mechanism of drug release was estimated and found to be via diffusion through channels and/or pores present within the polymeric matrix. Release data of almost all formulae fitted Higuchi's planar model better than spherical model. This finding could be due to the small extent of drug release (~ 40%), or the presence of a large fraction of the encapsulated drug nearby the surface of the microspheres.</em>
https://bpsa.journals.ekb.eg/article_156598.html
https://bpsa.journals.ekb.eg/article_156598_8a3e0c1724ea298f1c4e980001a21fe8.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
SYNTHESIS AND IN-VITRO CYTOTOXIC ACTIVITY OF NOVEL BENZO[b]PHENAZINE-6,11-DIONE AND 1,4- NAPHTHOQUINONE DERIVATIVES
69
80
EN
Maha
M.
A. Khalifa
Department of Pharmaceutical Chemistry, Faculty of Pharmacy
(Girls), Al-Azhar University, Nasr City, Cairo, Egypt
Magda
M.
F. Ismail
Department of Pharmaceutical Chemistry, Faculty of Pharmacy
(Girls), Al-Azhar University, Nasr City, Cairo, Egypt
Eman
Noaman
Department of Radiation Biology, Natural Center for Radiation
Research and Technology, Atomic Energy Authority, Cairo, Egypt
10.21608/bfsa.2008.64215
5,12-Dihydrobenzophenazine-6,11-diones,2-Arylamino-3-<br />chloro-1,4-naphthoquinones and 6,11-dihydrobenzo[b]phenazine-<br />6,11-diones, were synthesized from 2,3-dichloro-1,4-naphthoquinone<br />and arylamines/phenylenediamines. Studying the<br />cytotoxicity using EAC and human cell lines revealed that 5,12-<br />dihydrobenzo[b]phenazine-6,11-dione (3) and 3-chloro-2-(2-<br />pyridylamino)-1,4-naphthoquinone (10) showed selective<br />cytotoxicity against the human lung carcinoma cell line (H460)<br />superior to doxorubicin. Compound 3 (16.25 uM) was 1.3 times<br />higher than that of doxorubicin. However, IC50 value of compound<br />10 was 9.90 uM which was 2 times higher than that (20.10 uM) of<br />doxorubicin. These compounds were inactive against liver<br />carcinoma (HEPG2), brain tumor (U251), cervix carcinoma<br />(HELA) and breast carcinoma (MCF7) cell lines.
https://bpsa.journals.ekb.eg/article_64215.html
https://bpsa.journals.ekb.eg/article_64215_c0866a43803af81ab4386049a2668844.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
FORMULATION AND EVALUATION OF KETOPROFEN CELLULOSE ACETATE MICROCAPSULES
81
91
EN
Wael
A.
Abdelhafez
Department of Pharmaceutics, Faculty of Pharmacy, Al-Azhar
University, Assiut, Egypt
Khaled I. Saleh
I.
Saleh
Department of Pharmaceutics, Faculty of Pharmacy, Al-Azhar
University, Assiut, Egypt
10.21608/bfsa.2008.64216
Ketoprofen is a potent non-steroidal anti-inflammatory,<br />analgesic, and antipyretic drug used for treatment of various<br />rheumatic diseases and painful conditions. It is rapidly absorbed<br />regardless the route of administration. Its half life is only 1-2 hrs<br />after oral administration. The aim of this work was to formulate<br />some controlled release oral dosage forms containing ketoprofen.<br />Cellulose acetate was chosen for this purpose. Ketoprofen-cellulose<br />acetate microcapsules were prepared by solvent evaporation<br />technique. Polyvinyl alcohol was used as an emulsifier. The<br />prepared microcapsules were evaluated in terms of their release<br />and surface characteristics. Also, the anti-inflammatory activity of<br />ketoprofen was evaluated using the carrageenan-induced rat's pawedema method. The release of ketoprofen from the microcapsules<br />was pH dependant and decreased by increasing the polymer<br />content and by increasing the organic phase volume. The particle<br />size of the produced microcapsules was decreased by increasing<br />the volume of organic phase, whereas it was increased by<br />increasing the polymer content. In conclusion, these results<br />suggested that microencapsulation of ketoprofen using cellulose<br />acetate could be a useful approach for controlled release of the<br />drug.
https://bpsa.journals.ekb.eg/article_64216.html
https://bpsa.journals.ekb.eg/article_64216_30b2c3f0e1e0acc22f0acb1240b31c51.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
THERMAL STABILITY OF Ni(II) AND Cu(II) MIXED LIGAND COMPLEXES DERIVED FROM BIOLOGICALLY IMPORTANT SCHIFF BASES, AZOLES AND MORPHOLINE
93
108
EN
Aref
A.
M. Aly
Department of Chemistry, Faculty of Science, Assiut University,
Assiut, Egypt
Ahmed
H.
Osman
Department of Chemistry, Faculty of Science, Assiut University,
Assiut, Egypt
Mohamed
Abd
El-Mottaleb
Department of Chemistry, Faculty of Science, Al-Azhar University,
Assiut, Egypt
Gamal
A.
H. Gouda
Department of Chemistry, Faculty of Science, Al-Azhar University,
Assiut, Egypt
10.21608/bfsa.2008.64218
Thermogravimetry (TG) and differential thermogravimetry<br />(DTG) have been applied to the investigation of the thermal<br />behavior of six mixed ligand complexes of Ni(II) and Cu(II)<br />comprising the Schiff bases: o-hydroxyacetophenoneethanolimine<br />(OHAE), N-salicylidene-o-iminophenol (SOP) and N-salicylideneo-<br />toluidine (SOT) as well as morpholine (Morph) and certain<br />azoles. The azoles used are: 2-amino-thiazole (2-Atz),<br />benzothiazole (Btz), 2-methylbenzothiazole (2-Mbtz), 3-methyl-2-<br />selenoxobenzothiazole (3-Msbtz) and thiabendazole (Tbdz).<br />Heating the compounds first results in a release of the morpholine<br />or the azoles. Kinetics of the decomposition reactions were studied<br />using non-mechanistic equations.
https://bpsa.journals.ekb.eg/article_64218.html
https://bpsa.journals.ekb.eg/article_64218_58a6380a49a70e45553e2ef986dc456f.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
SYNTHESIS OF 2-TRIFLUOROMETHYL-4,7-DIHYDRO-7- OXO-(1,2,4)TRIAZOLO[1,5-a]PYRIMIDINE-6-CARBOXYLIC ACID DERIVATIVES AS POTENTIAL ANTIMYCOBACTERIAL AND ANTIMICROBIAL AGENTS
109
121
EN
Nawal
A.
El-Koussi
Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut
University, Assiut 71526, Egypt
10.21608/bfsa.2008.64214
Syntheses of the target compounds were achieved by reaction of<br />3-amino-5-trifluoromethyl-1,2,4-triazole 1 and diethylethoxymethylenemalonate<br />(DEEM) in glacial acetic acid to afford<br />ethyl 2-(trifluoromethyl)-4,7-dihydro-7-oxo[1,2,4]-triazolo[1,5-<br />a]pyrimidine-6-carboxylate 2. Reaction of compound 2 with<br />hydroxylamine hydrochloride gave hydroxamic acid 3, while<br />reaction with hydrazine hydrate in methanol gave the<br />corresponding carbohydrazide 4. Schiff bases of compound 4 with<br />appropriate aldehyde yielded series 5a-g. Refluxing of hydrazide 4<br />with appropriate isothiocyanate gave thiosemicarbazides 6a-f.<br />The antimycobacterial evaluation was determined against<br />Mycobacterium tuberculosis H37Rv(ATCC 27294). Compound 5e<br />and 5b showed activity with IC90(6.672, 7.362 μg/ml respectively) and IC50 (4.627, 6.382 μg/ml respectively). In vitro antibacterial<br />screening for the prepared compounds were determined against<br />certain strains of gram positive and gram negative bacteria. The<br />results showed that compounds 3, 5a, 6b possessed higher activity<br />than ampicillin against all strains, also the activity range from half<br />to sixth activity of nalidixic acid against E. coli. Compounds 3, 5a,<br />5b, 5c, 5f, 6b exhibited activity against P. aeruginosa, while<br />nalidixic acid possessed no activity. Compounds 3, 5a, 5b and 6b<br />possessed antifungal activity.
https://bpsa.journals.ekb.eg/article_64214.html
https://bpsa.journals.ekb.eg/article_64214_f7e681d30d2967764c4a0f701de98310.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
30
PREPARATION AND CHARACTERIZATION OF ALBENDAZOLE MICROPARTICLES PREPARED BY FREEZE-DRYING TECHNIQUE
123
135
EN
Mahmoud
El-Badry
Department of Pharmaceutics, College of Pharmacy, King Saud
University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
elbadry@aun.edu.eg
10.21608/bfsa.2008.64219
The aim of this work is preparation of albendazole (ABZ)<br />microparticles with certain hydrophilic polymers such as<br />hydroxypropyl methylcellulose (HPMC), and polyvinyl pyrrolidone<br />(PVP) using freeze-drying technique. Microparticles of ABZ with<br />these polymers were prepared in different ratios of 1:1, 1:2, and<br />1:4. Morphology of the prepared ABZ microparticles was studied<br />using a scanning electron microscope. Spherical microparticles<br />with smooth surface of ABZ were detected by this method.<br />Physicochemical properties of drug alone and its freeze-dried<br />microparticles were investigated using differential scanning<br />calorimetry (DSC) and powder X-ray diffractometry (PXRD). DSC<br />and PXRD analysis showed that ABZ was transformed from the<br />crystalline state to amorphous state by freeze-drying with the<br />chosen polymers as confirmed by disappearance of its melting peak<br />and characteristic crystalline peaks. Dissolution rate of ABZ from the prepared microparticles was determined and compared to its<br />corresponding physical mixtures. Results showed that, the<br />dissolution of freeze-dried microparticles was faster than the<br />corresponding physical mixtures and drug alone. This indicates<br />that, the freeze-drying technique improved ABZ dissolution.<br />Moreover, it was found that the dissolution rate of the drug was<br />affected by the polymer type and the ratio of ABZ to polymer.
https://bpsa.journals.ekb.eg/article_64219.html
https://bpsa.journals.ekb.eg/article_64219_abff3ce87fb02aab0f2b91f4fb9a7b68.pdf
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
31
1
2008
06
01
EVALUATION OF NEW ANTI-NEOPLASTIC ACTIVE INGREDIENT IN VITRO
137
151
EN
B.
A.
El-Fiky
Genetic Engineering& Biotech., Institute, Menouf. Univ., Sadat City,
Egypt
K.
A.
Halfawy
Genetic Engineering& Biotech., Institute, Menouf. Univ., Sadat City,
Egypt
M.
I.
El-Naggar
Department of Forensic Medicine & Toxic, Faculty of Medicine, Alex.
Univ., Egypt
N.
A.
Gobba
Department of Pharm. & Toxic, Faculty of Pharmacy, Misr Univ. for
Science and Tech., Egypt
10.21608/bfsa.2008.64220
Drug development programs for identification of new antineoplastic<br />agents involve extensive preclinical evaluation of vast<br />numbers of chemicals for detection of anti-neoplastic activity. Cell<br />culture systems have figured largely in the field of cancer<br />chemotherapy, where the potential value of such systems for<br />cytotoxicity and viability testing is now widely accepted.<br />The aim of this study is to evaluate cytotoxicity and viability<br />testing of new anti-neoplastic active ingredient compared to<br />Methotrexate and Adriamycin anti-neoplastic active ingredients<br />which are commonly used for cancer chemotherapy on HEPG2,<br />HEP2 and VERO cell lines.<br />Cytotoxicity, LD50, therapeutic dose, drug exposure, recovery<br />period and stability bioassay are determined.<br />Cytotoxicity bioassay of tested active ingredient on HEPG2 cells<br />showed punching of all monolayer cells with few regenerative cells<br />after 48 hr and no regenerative cells after 72 hr while Methotrexate<br />and Adriamycin showed 75% cytopathic effect on monolayer cells<br />after 24 hr then cells begins to regenerate with few rate after 48-72<br />hr.<br />Cytotoxicity bioassay of tested active ingredient on HEP2 cells<br />showed 25% cytopathic effect on monolayer cells then regenerated<br />to reach complete monolayer after 72 hr compared to<br />Methotrexate50% and Adriamycin 75% cytopathic effect on<br />monolayer cells then reached to 75% of monolayer after 72 hr.<br />Cytotoxicity of tested active ingredient onVero cells showed<br />retraction of monolayer cells then retains its original pattern after<br />24 hr of exposure while Methotrexate and Adriamycin showed<br />destruction of more 50% of monolayer cell population then reached<br />to 75% of monolayer after 72 hr.<br />In conclusion; cytopathological studies showed that the tested<br />active ingredient has low cytotoxicity, more stable and more<br />telorated compared to controls.
https://bpsa.journals.ekb.eg/article_64220.html
https://bpsa.journals.ekb.eg/article_64220_19dd05d4259de3d4fdcb6e1c3529550d.pdf