Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
SYNTHESIS AND ANTINEOPLASTIC ACTIVITY OF CERTAIN TRIAZENE AND TRIAZENO-ACRIDINE COMBILEXIN DERIVATIVES
89
110
64146
10.21608/bfsa.2007.64146
EN
Samir M. El-Moghazy
Aly
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
Hanan H.
Georgey
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
Mohammed A.
Mohammed
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
Nagwa M.
Abdel Gawad
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
Noha H.
Amin
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University and Bani-Sueif University, Egypt
Journal Article
2007
06
14
Four series of bifunctional ligands have been synthesized as DNA-binding combilexins. These novel agents contain a triazenobenzene sulfonamide linker moiety that is attached to an intercalating acridine or acridone chromophore by a functionalized amide or ester residue. In order to obtain these combilexins three series of the anticipated antitumor triazeno-benzene sulfonamide were synthesized. The synthesis and bioscreening of the new antineoplastic compounds are depending on the structural correlation with several reported antineoplastic acridines. 2-Chlorobenzoic acid was reacted with anthranilic acid to give N-(2-carboxyphenyl) anthranilic acid which upon cyclodehydration with sulfuric acid afforded 9-oxo-9,10-dihydroacridine-4carboxylic acid, (acridone-4-carboxylic acid) 8. This latter intermediate has been converted to 9-chloroacridine carbonyl chloride 9 using thionyl chloride. Selective substitution of 9 with derivatives of 4-(piperazine-1-yldiazenyl) benzenesulfonamides 4ae or derivatives of 4-(2-hydroxyethyl)piperazine-1-yl)diazenyl) benzenesulfonamides 5a-e to yield their 9-chloroacridine-4carboxamides 10a-e and 9-chloroacridine-4-carboxylic acid esters 13a-e respectively. Those intermediates have been reacted either with different sulfonamides to give derivatives of 4-{4-[4-(4 sulfamoylphenyldiazenyl)piperazine-1-carbonyl]-9-ylamino}benzenesulfonamides 11a-h and derivatives of 2-[(4-(4-sulfamoylphenyl)diazenyl)piperazine-1-yl]ethyl 9-(4-sulfamoylphenylamino)-9,10-dihydroacridine-4-carboxylates 14a-i respectively or subjected to mild acid hydrolysis to yield derivatives of 4-{4-[(9oxo-9,10-dihydroacridine-4-carbonyl)piperazine-1-yl]diazenyl}benzenesulfonamide 12a-e and derivatives of 2-{4-[(4-sulfamoylphenyl)diazenyl]piperazine-1-yl}ethyl-9-oxo-9,10-dihydroacridine4-carboxylate 15a-e respectively. Besides, the synthesis of derivatives of 4-(piperazine-1yldiazenyl) benzenesulfonamides 4a-e and derivatives of 4-(2hydroxyethyl)piperazine-1-yl)diazenyl) benzenesulfonamides 5a-e has been achieved via diazotization of various substituted benzene sulfonamides with sodium nitrite and hydrochloric acid followed by various amines coupling to yield the target triazeno-benzene sulfonamides. Fourteen new compounds were selected for screening their antitumor activity against breast cell line in National Cancer Institute. Six of them were found to be active as antitumor agents, while two were found to be mild active.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
FORMULATION AND CHARACTERIZATION OF BIODEGRADABLE CHITOSAN FILMS FOR TOPICAL APPLICATION OF TERBINAFINE HCl
111
129
64178
10.21608/bfsa.2007.64178
EN
S. M.
Ahmed
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M. A.
Ibrahim
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, El-Azhar University, Assiut branch, Egypt
H. A.
Sarhan
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, El-Minia University, El-Minia, Egypt
M. A.
Amin
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, El-Azhar University, Assiut branch, Egypt
Journal Article
2007
07
14
Chitosan biodegradable films containing terbinafine HCl (Tr.HCl) were evaluated for their potential drug delivery at a controlled rate. Terbinafine HCl could be loaded at 1.8% w/w of polymer in films, which were translucent and flexible. The effect of drug loading and nature of plasticizers on the in-vitro release of Tr.HCl have been examined. Physicochemical characterization of Tr.HCl via thermal, spectroscopic, X-ray diffraction, and scanning electron microscopy techniques revealed information on the solidstate properties of Tr.HCl as well as chitosan in films. While chitosan was in an amorphous form, Tr.HCl seemed to be present in crystalline form in the films. It was found that the release rate of the drug was directly proportional to drug concentraton. Also medicated chitosan films plasticized with water- soluble plasticizers as glycerol triacetate (GTA), propylene glycol (PG), and polyethylene glycol 400 (PEG 400), produced fast release in comparison with water insoluble plasticizers as glycerol tributyrate (GTB), dimethyl phthalate (DMPH), and diethyl phthalate (DEPH). The characterizations of chitosan films conducted by IR, X-ray, and DSC, showed that no interaction occurred between Tr.HCl and chitosan polymer. The minimum inhibitory concentration (MIC) of the drug against candida albicans was investigated. Results showed that MIC of Tr.HCl was 1.4 µg/ml. The inhibition zone diameter of Tr.HCl chitosan films was higher than that of Tr.HCl normal dressing. Also antifungal activity of Tr.HCl was enhanced in plasticized chitosan films. The results were promising for topical formulation of Tr.HCl in biodegradable chitosan films and have the potential to be used as a novel drug delivery
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
ANTIBIOTIC SUSCEPTIBILITY OF E. COLI O157:H7 ISOLATED FROM BEEFBURGER
131
134
64179
10.21608/bfsa.2007.64179
EN
Naser A.
Al-Wabel
Department of Veterinary Medicine, Faculty of Agriculture and Veterinary Medicine, Qassim University, Saudi Arabia
Journal Article
2007
07
22
E. coli transmitted from under-cooked hamburger may cause life threatening conditiosn including hemorrhagic colitis, hemolytic uremic syndrome and thrombotic-thrombocytopaenic purpurea. Unfortunately, the emergence of resistance has become increased. Therefore, the antimicrobial susceptibility of the causative strain E. coli "O157:H7" was determined in this study. Results showed that E. coli O157:H7 was resistant to all tested antibiotics except danofloxacin. Therefore, this study recommend the use of danofloxacin in controlling infections caused by E. coli transmitted from hamburger.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
DEVELOPMENT AND EVALUATION OF NEFOPAM HYDROCHLORIDE MICROCAPSULES
135
147
64180
10.21608/bfsa.2007.64180
EN
M.
El-Mahdy
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
2007
08
22
An attempt was performed to encapsulate Nefopam hydrochloride, a highly water soluble drug, by a modified emulsion solvent evaporation / extraction technique, using cellulose acetate butyrate (CAB) as a coating polymer. The influence of core/coat ratio (1:2, 1:1 and 2:1 ratio) on the yield, drug loading, size distribution as well as the release characteristics and surface topography of the prepared microcapsules was investigated. The obtained microcapsules exhibited higher encapsulation efficiency and a decreased release rate in simulated gastric fluid (S.G.F. pH 1.2) and simulated intestinal fluid (S.I.F. pH 7.4). On the other hand, the entrapment efficiencies increased (from 104.66 to 141.26, core coat ratio 1:1) and the release rate decreased with increasing microcapsule size (from 250 to 512.5 µm) and/or theoretical drug loading of microcapsules. Kinetic assessment of the release rate of microcapsules using different mathematical models has shown that the release rate followed Ritger-Peppas diffusion release kinetics
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
LIPOSOMAL GEL OF DICLOFENAC SODIUM AS TOPICAL DELIVERY SYSTEM
159
167
64181
10.21608/bfsa.2007.64181
EN
Mahmoud
El-Badry
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. BOX 2457, Riyadh 11451, Saudi Arabia
Journal Article
2007
09
05
This study the preparation of diclofenac sodium in lecithin vesicles and loading in pluronic F-127 gel, the effect of sodium cholate on the diffusion of the drug through rat skin and the antiinflammatory activity of the liposomal gel formulations. Lecithin vesicles were prepared in the presence or absence of sodium cholate by the dry film method and sonication. The size of liposomal vesicles ranged from 100-700 nm and the encapsulation efficiency of the diclofenac sodium was between 60-80%. The lecithin vesicles were loaded in pluronic F-127 gel. The highest cumulative of drug diffusion through rat skin was 19.31± 1.50 (µg/cm2) for lecithin vesicles in the presence of sodium cholate (F4). Also the highest cumulative of drug diffusion through rat skin was 12.20± 0.50 (µg/cm2) for liposomal gel (F8). The antiinflammatory activity of the liposomal gel formulations was studied on carrageenan induced paw edema in rats. The results show that, F8 and F6 show superior anti-inflammatory activity in comparison with the other gel formulations. From the results, lecithin vesicles and liposomal gel of diclofenac sodium appear to be advantagesous for topical delivery of the drug.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
PREPARATION AND IN–VITRO EVALUATION OF EUDISPERT HYDROGEL RECTAL SUPPOSITORIES CONTAINING SALICYLAMIDE
169
179
64182
10.21608/bfsa.2007.64182
EN
Afaf A.
Ramadan
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt
Amal S.
Abou El- Eineen
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt
Dalia A.
Attia
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt
Journal Article
2007
09
24
This article aimed to formulate and evaluate salicylamide suppositories. The prepared formulae with and without different concentrations of gels were tested for hardness, melting time, content uniformity and drug release. The stability of some of the selected formulae was assessed. Salicylamide was formulated as a rectal suppository with emulsifying fatty bases (witepsol H15, W25 and w35) and water – soluble bases (PEG) adopting the molding from a melt technique. Physical characteristics and dissolution profiles of the prepared formulations were determined. The effects of adding gel (eudispert hv) in concentrations of (2, 4 and 6%) were also investigated. Formulations showing high rank order were scaled up for shelflife stability study for one year. The results showed that all the investigated formulae have acceptable physical characteristics with respect to hardness, melting time and uniformity of drug content. The amount of drug released during 120 min. was inversely affected by the melting point of the fatty base. The release from PEG bases was found to be molecular weight dependent. Addition of 2% eudispert gel increased the release from all the investigated formulae. Increasing gel concentration to 4% then to 6% showed different effects on the release. Rectal suppository of salicylamide could be prepared as an alternative to the oral dosage form to circumvent the first - pass metabolism1
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
SYNTHESIS OF NEW 4(3H)-QUINAZOLINONE DERIVATIVES OF POTENTIAL ANTIMICROBIAL ACTIVITY
181
192
64183
10.21608/bfsa.2007.64183
EN
Awwad A.
Radwan
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71527, Egypt
Salah G.
Ali
Department of Botany and Microbiology, Faculty of Science, Al-Azhar University, 71524 Assiut, Egypt
Journal Article
2007
10
06
A new series of quinazoline-4(3H)-one derivatives containing hydrazone, thiosemicarbazide, pyrazole moiety and 1,2,4triazolo[4,3-a]quinazolin-5-(4H)-one derivatives, were prepared in order to study the effect of such combinations on the expected antimicrobial activity. Synthesis of target compounds (3-8) has been achieved through an interaction of the starting 2a or 2b with different alkyl or aryl isothiocyanate. Condensation of 2a or 2b with various aromatic aldehydes or ketones afforded the corresponding hydrazones 9-12. 1-(4-Pyridinyl)-1,2-dihydro-4phenyl(allyl)-1,2,4-triazolo[4,3-a]quinazolin-5-(4H)-one deriva tives 13, 14 have been synthesized through reflux of compound 9 or 10 in glacial acetic acid. On the other hand, 1-(3-substituted-3,4dihydro-4-quinazolinon-2-yl)-3-(4-chlorophenyl) pyrazole-4-carbaldehyde 15 or 16 has also been synthesized through interaction of compounds 11 or 12 with Vilsmeier-Haack reagent1. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their in vitro antibacterial and antifungal activities. The tested compounds showed moderate antibacterial activity and weak or no antifungal activity.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
THE EFFECT OF BINDER TYPE AND MAJOR DILUENT ON THE MIGRATION AND BIOAVAILABILITY OF RIBOFLAVIN SODIUM PHOSPHATE DURING TABLET MAKING
193
212
64185
10.21608/bfsa.2007.64185
EN
Hassan M.
ELSabbagh
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Ahmed T.
Nouh
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Osama A.
Soliman
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Mariza F.
Boughdady
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Journal Article
2007
10
18
The migration of riboflavin sodium phosphate (RSP) upon drying of its wet granules was studied through the formulation of granules using different diluents (lactose monohydrate and anhydrous dibasic calcium phosphate), different binders of different concentrations; polyvinyl pyrrolidone (PVP k25), methylcellulose (MC), hydroxypropylmethyl cellulose (HPMC) and gelatin at different drying temperatures (50°C and 70°C). The prepared granules were compressed into tablets and evaluated. In vitro drug release from the formulated tablets was performed. In addition, in vivo study was conducted on some selected tablet batches. The results showed that, the granules prepared with dibasic calcium phosphate showed lower migration for the drug than those prepared with lactose. Also, drug migration decreased with increasing the binder concentration and viscosity. The degree of tablet mottling was inversely proportional to the binder concentration. Tablets prepared with 10% w/w gelatin were found to be the least mottled ones. In addition, they showed the least friability percentage, the highest hardness value and the highest disintegration time. Tablets prepared with 0.5% MC showed the highest dissolution rate, however, those prepared with 10% gelatin had the lowest dissolution rate. Generally, increasing the binder concentration resulted in slowing the in vitro drug release from tablets. The in vivo study showed that, tablets prepared with 10% w/w gelatin showed the lowest excretion rate and the highest Tmax (1.5 hours). Meanwhile, tablets prepared using 0.5% w/w MC exhibited higher excretion rate and Tmax of 0.5 hour.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
01
IMIDAZOLE ALKALOIDS FROM THE INDOPACIFIC SPONGE PERICHARAX HETERORAPHIS
149
157
64196
10.21608/bfsa.2007.64196
EN
A. A.
Ali
Department of Pharamcocnosy, Faculty of Pharmacy, Assiut University, 71526 Assiut, Egypt
H. A.
Hassanean
Department of Pharamcocnosy, Faculty of Pharmacy, Assiut University, 71526 Assiut, Egypt
Ehab S.
Elkhayat
Department of Pharamcocnosy, Faculty of Pharmacy, Al-Azhar University (Assiut branch , 71524 Assiut, Egypt)
Ru AnGelie
Edrada
Institut für Pharmazeutische Biologie, Heinrich-Heine-Universität, Universitätsstr 1, 40225 Düsseldorf, Germany
Rainer
Ebel
Institut für Pharmazeutische Biologie, Heinrich-Heine-Universität, Universitätsstr 1, 40225 Düsseldorf, Germany
Peter
Proksch
Institut für Pharmazeutische Biologie, Heinrich-Heine-Universität, Universitätsstr 1, 40225 Düsseldorf, Germany
Journal Article
2007
09
04
Chemical investigation of the sponge Pericharax heteroraphis (Polejeff) collected in Indonesia, has led to the isolation of three imidazole alkaloids, preclathridine-A (1), leucettamine-B (2) and leucettamine-A (3). The structures of the isolated compounds were unambiguously established by 1D and 2D NMR and mass data. This is the first report of this class of compounds from the P. heteroraphis sponge. Investigation of the antimicrobial activities of the isolated compounds showed that leucettamin-A (3) was active against the gram-positive bacteria Staphylococcus aureus and the fungus Cladosporium herbarum, while other compounds were inactive.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
DESIGN AND SYNTHESIS OF SOME SUBSTITUTED ACRIDINE DERIVATIVES OF ANTICIPATED ANTITUMOR ACTIVITY
213
234
64201
10.21608/bfsa.2007.64201
EN
S. M.
El-Moghazy Aly
Department of Pharmaceutical Chemistry, Faculty of Pharmacy,
Cairo University, Cairo-11562, Egypt
D. E.
Abdel Rahman
Department of Pharmaceutical Chemistry, Faculty of Pharmacy,
Cairo University, Cairo-11562, Egypt
S. E.
-S. Abbas
Department of Pharmaceutical Chemistry, Faculty of Pharmacy,
Cairo University, Cairo-11562, Egypt
M. A.
- A. Mohammed
Department of Pharmaceutical Chemistry, Faculty of Pharmacy,
Cairo University, Cairo-11562, Egypt
A. H.
Amin
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Beni
Sueif University, Egypt
Journal Article
2007
10
22
Four series of new acridine derivatives of anticipated antitumor<br />activity have been designed and synthesized. The first series<br />belongs to 4-substituted phenylhydrazinocarbonylmethyl 9-oxo-<br />9,10-dihydroacridine-4-carboxylate 10a-h. The second series consists of phenylhydrazinocarbonylmethyl 9-(4-substituted<br />phenyl)aminoacridine-4-carboxylate 12a-k, while the third series<br />comprises 4-substituted phenylcarbamoylmethyl 9-(4-substituted<br />phenyl)aminoacridine-4-carboxylate 15a-k. The fourth one belongs<br />to phenylcarbamoylmethyl 9-(4-substituted phenyl)aminoacridine-<br />4- carboxylate 17a-j. The chemical structure of synthesized<br />compounds was elucidated by spectral data and elemental analysis.<br />Seventeen selected compounds (10a, 10g, 10h, 12a, 12d, 12g, 12h,<br />12k, 15a, 15c, 15g, 15h, 15k, 17a, 17f, 17g and 17j) were tested<br />against breast cancer cell line (MCF7) and eight compounds (12g,<br />12h, 12k, 15g, 15h, 17f, 17g, 17j) were found to exhibit significant<br />antitumor activity
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
THE PREVALENCE OF INTESTINAL PARASITES IN AMMAN, JORDAN
235
239
64203
10.21608/bfsa.2007.64203
EN
A. M.
Chazal
Faculty of Pharmacy, Al-Isra Private University, Amman, Jordan
H. K.
Adi
Faculty of Pharmacy, Al-Isra Private University, Amman, Jordan
Journal Article
2007
10
25
Intestinal parasitic infections were investigated in Amman,<br />Jordan, during the period extending from 2003 until 2005. A total<br />number of 1280 specimens were included in the study. Entamoeba<br />histolytica was found to be the most prevalent parasite with an<br />infection rate of 27.81%.<br />The highest incidence of this infection was during spring and<br />summer seasons and at an early age (1-10 years). Helminthic<br />infections were uncommon during this survey.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
SIMULTANEOUS DETERMINATION OF INTACT LOMEFLOXACIN AND CIPROFLOXACIN IN THE PRESENCE OF THEIR ACID DEGRADATION PRODUCTS
241
258
64205
10.21608/bfsa.2007.64205
EN
Sonia T.
Hassib
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo
University, Egypt
Ramzia
El-Bagary
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo
University, Egypt
Hanaa M.
Hashem
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo
University, Egypt
Maha M.
El-Hakim
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo
University, Egypt
Journal Article
2007
11
10
A reversed phase HPLC method was developed for the<br />determination of lomefloxacin and its degradation product. In<br />addition, two other methods have been developed for the<br />determination of lomefloxacin hydrochloride (LF.HCl) and<br />ciprofloxacin hydrochloride (CF.HCl) in presence of their acid<br />induced degradation products.<br />For the reversed phase HPLC method (determination of<br />LF.HCl), the mobile phase used was a mixture of water:<br />acetonitrile: triethylamine (80:20:0.6, v/v/v) adjusted to pH 3.0<br />with o-phosphoric acid. The flow rate was 1.5 ml/min. and the<br />detection was carried out at 328 nm. The linearity range was found<br />to be 0.5-6 μg / 20 μl for LF.HCl. The limits of detection and<br />quantification (LOD & LOQ) were 0.22 μg / 20 μl & 0.74 μg / 20<br />μl respectively.<br />The second method was densitometric method for the<br />determination of both LF.HCl and CF.HCl, the developing system<br />used was a mixture of methanol and ammonia buffer (80:20, v/v).<br />Detection was carried out at 288 nm & 279 nm. for intact LF.HCl<br />and CF.HCl respectively. The linearity ranges were found to be 1-6<br />μg / 10 μl & 0.25-2.5 μg / 10 μl for intact LF.HCl and CF.HCl<br />respectively. LOD & LOQ were 0.1, 0.34 μg / 10 μl & 0.05, 0.18 μg<br />/ 10 μl for both drugs, respectively.<br />The third method was derivative spectrophotometric method for<br />the determination of (LF.HCl) & (CF.HCL). The linearity ranges<br />were found to be 2-8 μg/ml & 5-12 μg/ml for LF.HCl and CF.HCl<br />respectively. LOD & LOQ were 0.39 μg, 1.29 μg/ml & 1.03, 3.45<br />μg/ml for LF.HCl and CF.HCl, respectively.<br />Separation and identification of the acid degradation products<br />of lomefloxacin hydrochloride and ciprofloxacin hydrochloride<br />were carried out.<br />The three described methods proved to be sensitive, precise and<br />applicable to both dosage forms and laboratory prepared mixtures<br />of the intact drugs and their acid degradation products.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
A NEW SCAFFOLD FOR D3 DOPAMINERGIC AFFINITY CONTAINING ARYLPIPERAZINE FRAGMENT: MOLECULAR MODELING, SYNTHESIS, IN VITRO AND IN VIVO PHARMACOLOGICAL EVALUATION
259
273
64208
10.21608/bfsa.2007.64208
EN
Dalal A.
Abou El Ella
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams
University, El-Khalifa El-Maamoon St., 11566, Abbassia, Cairo, Egypt
Franziska K.
U. Müller
Biological Screening Units, Institute of Pharmacy, Philosophenweg 14,
D-07743 Jena, Germany
Journal Article
2007
11
17
A new series of N-(6-substitutedbenzo[d]thiazol-2-yl)-2-(4-<br />arylpiperazin-1-yl) acetamides (3a-f) and 2-(3-(4-arylpiprazin-1-<br />yl)propylthio)benzo[d]thiazoles/-oxazoles/-imidazole (6a-f) was<br />synthesized by connecting arylpiperazine through a semi-rigid or<br />flexible spacer to a heterocyclic moiety, respectively. The<br />radioligand binding experiments for the D1, D2, D3 and D5 subtypes<br />expressed in CHO cells were examined for the target compounds<br />3a-f, 6a, 6b, 6d and 6f. Compound 6a showed the best binding<br />affinity for dopamine D3 receptor and is considered as a new<br />scaffold for D3 dopaminergic affinity. Furthermore, molecular<br />modeling of the best-fitted conformer of target compounds 3a, 6b,<br />6c, 6d and 6f to <br />1-adrenoceptor ( <br />1-AR) antagonist hypothesis<br />was performed using CATALYST software, HipHop modules. Based<br />on the results of simulation studies, these target compounds were<br />evaluated for their in vivo hypotensive activity on blood pressure of<br />normotensive cats.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
30
2
2007
12
31
BIOAVAILABILITY AND OCULAR DISPOSITION OF KETOROLAC TROMETHAMINE FROM VARIOUS OPHTHALMIC PREPARATIONS
275
297
64211
10.21608/bfsa.2007.64211
EN
Hamdy M.
Abd El-Aleem
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura
University, Mansoura, Egypt
Farouk M.
Sakr
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura
University, Mansoura, Egypt
Osama A.
Soliman
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura
University, Mansoura, Egypt
Hatem,
El-Awady
Ophthalmic Center, Faculty of Medicine, Mansoura University,
Mansoura 35516, Egypt
Germeen N.
Salama
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura
University, Mansoura, Egypt
Journal Article
2007
12
10
Ketorolac tromethamine was formulated in different ophthalmic<br />preparations namely; eye drops, gels, ocuserts and ointments using<br />the following carriers; sodium carboxymethyl cellulose (sod.<br />CMC), polyvinyl alcohol (PVA), hydroxypropylmethyl cellulose<br />(HPMC), absorption base and gelatin. The ophthalmic<br />formulations were prepared containing 0.5% of the drug. All<br />prepared formulae containing the drug were subjected to stability<br />study and release characteristics. Also, the effect of these drug<br />carriers on the uptake and ocular disposition of ketorolac<br />tromethamine by the eye tissues of rabbits (conjunctiva, cornea,<br />iris-ciliary body and aqueous humor) was studied.<br />The obtained results revealed that, the released amounts from<br />the ophthalmic preparations after six hours can be arranged in the<br />following order; Eye drops > ocuserts > gel > ointments. Sod CMC<br />eye drops exhibited the higher rate of release than sod CMC gel,<br />PVA and absorption base ointments. Gelatin ocuserts exhibited the<br />higher rate of release than HPMC ocuserts and carbopol 934 &<br />sod CMC ocuserts. The release rate of the drug from eye drops and PVA ointment obeys first order kinetics, while, other preparations<br />obey Higuchi diffusion model with non-Fickian kinetics.<br />Most formulations (including eye drops) could be stored for 6<br />months at 25°C, 35°C, 45°C without physical or chemical<br />degradations of the drug. However, PVA and absorption bases<br />showed some changes in the drug content (t90 was 2.84 months for<br />both at 45°C). The decomposition rate of ketorolac tromethamine<br />followed the first-order degradation kinetic. The highest stable<br />formulae are, sod CMC eye drops and gel (t90 values were, 151.9<br />and 91.18 months, respectively at 45°C). The highest concentration<br />of the drug (Cmax) from all tested formulations is provided in<br />conjunctiva followed by cornea, iris-ciliary body, then aqueous<br />humor. The peak time for maximum drug concentration (Tmax)<br />from sod CMC eye drops was two hours. While, that for sod CMC<br />gel, PVA ointment and gelatin ocuserts was three hours in all<br />tissues after the application of the tested formulations. In addition,<br />the total availability of the drug from the tested formulations was in<br />the following order: gelatin ocuserts > sod CMC gel > PVA<br />ointment > sod. CMC eye drops.