Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
POSSIBLE CNS DEPRESSANT EFFECTS OF SOME NEWLY SYNTHESIZED QUINAZOLINONE DERIVATIVES
137
144
70558
10.21608/bfsa.1990.70558
EN
M. M.
Abdel-Rahman
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Eqypt
S. A.
Mangoura
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Eqypt
H. I.
El-Bitar
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Eqypt
Journal Article
1989
11
13
<em>In the present investigation, five recently synthesized derivatives (designated as compounds <strong>I, II, III, IV</strong> and <strong>V</strong>) of 2,3-disubstituted 4 (3H)-quinazolinone (<strong>I</strong>) were evaluated for their CNS depressant activities in mice. In the course of this study, all compounds were suspended in a 5% suspension of gum acacia in water and were injected i.p. with the test compound in a dose level of 60 mg/kg.</em>
<em>All tested compounds were found to decrease spontaneous locomotor activity of mice. Only compound IV was found to potentiate pentobarbitone induced hypnosis. Regarding the effect on the skeletal muscle activity, quinazolinone derivatives <strong>II</strong> and <strong>III</strong> led to motor incoordination in 40% of mice. Out of the five tested compounds, compounds <strong>I, II</strong> and <strong>IV </strong>resulted in an increase in the mean survival time of strychnine-injected mice and a greater protection against death in these animals. However, the anticonvulsant effects exerted by quinazolinone was less efficient than those produced by phenobarbitone.</em>
<em>In conclusion, quinazolinone compounds <strong>II</strong> and <strong>IV</strong> are more likely to be the most potent as CNS depressant compounds, whereas compound <strong>V</strong> appears to be the least efficient one.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
SYNTHESIS AND BIOLOGICAL ACTIVITY OF CERTAIN 1,3-AND 1,5-DIMETHYL-N-SUBSTITUTED PYRAZOLE CARBOXAMIDES
145
158
70559
10.21608/bfsa.1990.70559
EN
Tarek A.
Fadl
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Adel F.
Youssef
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Abdel-Hamed N.
Ahmed
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Hussein I.
El-Bitar
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Egypt
Journal Article
1990
06
27
<em>Positional isomers of dimethyl pyrazole carboxylic acid derivatives were prepared. Some of these compounds showed variable binding capacities towards Cu (II), Zn (II) and Mg (II). The most active chelators <strong>Ig</strong> and its isomer <strong>IIg</strong> showed antidotal and antiinflammatory activities higher than D-penicillamine. Both are more active in dose levels much lesser than their median lethal doses (LD50). 5(3)-Methylpyrazole-3(5)-carboxamide showed significant growth inhibition of R. solani. The other derivatives tested displayed growth stimulating activity rather than growth inhibition of the fun</em><em>gus.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
EVALUATION OF COMMERCIAL BENZOYL METRONIDAZOLE SUSPENSION
159
168
70562
10.21608/bfsa.1990.70562
EN
S. A.
Ibrahim
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. Shawky
Tous
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
T. H.
El-Faham
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M. A.
Hassan
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1990
12
08
<em>Benzoyl metronidazole is available in the Egyptian market as suspension. It was reported that its suspension is physically unstable. Hence, it is aimed in this study to evaluate marketed benzoyl metronidazole suspension. Four batches of benzoyl metronidazole suspension were evaluated for sedimentation volume, drug content, particle length distribution, dissolution rate and bioavailability of the drug. The results revealed significant differences in these parameters between and among the batches of the same brand. The commercial suspensions showed physical and chemical stability along 10 months of aging concerning the preceding parameters, except that the number of the large particles increase by aging. The in-vivo evaluation of two benzoyl metronidazole batches was performed in healthy human volunteers. A direct correlation could exist between the in-vitro dissolution characteristics and the in-vivo parameters.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
FORMULATION AND EVALUATION OF BENZOYL METRONIDAZOLE SUSPENSION
169
180
70565
10.21608/bfsa.1990.70565
EN
S. A.
Ibrahim
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. Shawky
Tous
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
T. H.
El-Faham
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M. H.
Hassan
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1990
12
08
<em>Two formulae of benzoyl metronidazole suspension were prepared. One consisted of Tween 40 (0.2%), sodium carboxymethyl cellulose (1%), and potassium dihydrogen phosphate (0.002%) [formula No. 1] and sodium chloride (.005%) instead of potassium, dihydrogen phosphate (formula No. 2]. The formulated suspensions, were found to be superior than the commercial one. The sediment was one layer compared to two layers sediment of the commercial product. The supernatants were clear and the suspensions were easily re-dispersed. The percent drug dissoluted was higher than that of the commercial product. The prepared suspensions showed physical and chemical stabi1ity even after 12 months of aging.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
FORMULATION AND EVALUATION OF TOPICAL METRONIDAZOLE
181
194
70570
10.21608/bfsa.1990.70570
EN
S. A.
Lbrahim
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. Shawky
Tous
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
T. H.
El-Faham
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M. A.
Moubasher
Department of Dermatology, Faculty of Medicine, Assiut University, Assiut, Egypt
M A.
Hassan
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1990
09
09
<em>Formulation of metronidazole in the form of topical preparations did not take much attention. Thus, the aim of this work is to formulate metronidazole in the form of gel and ointment. Ten ointment bases were used viz., oleagenous, absorption, emulsion and water soluble bases. The rate of release of the drug from the water soluble polyethylene glycol base was the highest. The effect of some penetration enhancers e.g. dimethylsulfoxide, urea and ethanol on the release rate of the drug from the water soluble and the o/w emulsion bases was studied.</em>
<em>For metronidazole gels, several cellulose derivatives were used viz., methylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, methocel. Eudragit RL 100 and Eudragit RS 100. The in-vitro release of the drug was maximum from methylcellulose gel followed by Eudragit RL 100. In general the in-vitro release of metronidazole from gel was higher than that from ointment bases.</em>
<em>Preliminary clinical investigations of metronidazole in an ointment and in a gel formulae were performed. These preliminary studies were impressive but further clinical studies are required before recommending metronidazole as an effective topical therapy.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
BIOAVAILABILITY STUDIES OF THEOPHYLLINE MICROCAPSULES
195
203
70576
10.21608/bfsa.1990.70576
EN
S.
El-Shanawany
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. M.
Safwat
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1990
09
17
<em>The release of theophylline from microcapsules prepared by using different concentrations of ethylene-vinyl acetate (EVA) copolymer as a coacervation-inducing agent was investigated in simulated gastric and intestinal fluids. Also the bioavailability of theophylline from its microcapsules following oral administration in volunteers using the saliva drug concentration was investigated.</em>
<em>The results pointed out that the higher the concentration of EVA compolymer used the more sustainment of theophylline from microcapsules. The investigation painted for a good correlation between the in-vitro release rate characteristics and the in-vivo salivary bioavailability parameters of theophylline microcapsules. The prepared theophylline microcapsules were proven to achieve excellent sustainment pattern and could be used to avoid sub-/or/super therapeutic levels of conventional theophylline products.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
MACRO- AND MICROMORPHOLOGY OF RHYNCHOSIA MINIMA L. DC. (ROOT, STEM AND LEAF)
205
220
70578
10.21608/bfsa.1990.70578
EN
A. A.
Khalifa
Department of Pharmacognosy, Faculty of Pharmacy, University of Assiut, Assiut, Egypt
O. M.
Abdallah
Department of Pharmacognosy, Faculty of Pharmacy, University of Assiut, Assiut, Egypt
Journal Article
1990
10
24
<em>The macro- and micromorphological characters of the root, stem and leaf of Rhynchosia minima L.DC., growing in Egypt are presented with the aim of finding out the characteristic features by which these organs could be identified in both the entire and powdered forms.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
IN-VITRO RELEASE CHARACTERISTICS OF PAPAVERINE HYDROCHLORIDE FROM MULTIPLE EMULSION SYSTEMS
221
233
70580
10.21608/bfsa.1990.70580
EN
H. Abdel-Monem
Sayed
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
E.
Hafez
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. M.
Safwat
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1990
11
08
<em>A two-step emulsification procedure was adopted to prepare stable multiple emulsion of the W/O/W type. An aqueous solution of the drug and paraffin oil at ratio of 1:2 were used to prepare a W/O type primary emulsion (1<sup>st</sup> step) using blend of surfactants (HLB 3.8) at 10% concentration. While a blend of surfactants (HLB 12.3) was used as the second emulsifying agent for incorporating the prepared primary emulsion into the outer aqueous phase (1:2) to produce the final emulsion. Drug release from the prepared system was evaluated 24 hours after preparation and periodically at weekly intervals thereafter for four weeks. Multiple emulsion system, each containing either sodium chloride, sorbitol or methylcellulose were similarly prepared and evaluated for drug release thereof. Drug release from the prepared system was found to be greatly retarded in comparison with that from the corresponding aqueous solutions. The drug release rate from the prepared system, with the exception of those containing methylcellulose was slightly changed to lower values. The effect was greater at the second week testing while, a constant release pattern was found thereafter. The presence of methyl cellulose lead to a greater lowering in the release rate.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
PREPARATION AND EVALUATION OF SUSTAINED RELEASE ETHYLCELLULOSE ENCAPSULATED ASPIRIN
235
246
70581
10.21608/bfsa.1990.70581
EN
S. A.
Ibrahim
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
H. A.
Sayed
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
E.
Hafez
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
A. M.
El-Sayed
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. S.
Ali
Department of Histology, Faculty of Medicine, Assiut University, Assiut, Egypt
Journal Article
1990
12
12
<em>Aspirin microcapsules were prepared by the solvent evaporation method. Ethylcellulose was used as the coating material at 18:2, 17:3 and 16:4 core : coat ratios. The prepared microcapsules were separated into sieve fractions. Each fraction was evaluated for drug content and dissolution characteristics. Scaling-up was developed to evaluate the adopted microencapsulation method for large scale production.</em>
<em>The adopted method was simple, efficient and reproducible. A prolonged release pattern of the drug was obtained by increasing the coat/core ratio. Larger microcapsules released aspirin at a slower rate than did smaller microcapsules. Scaling-up did not significantly affect the release characteristics of drug from the prepared microcapsules. Histological studies on the Guinea pig gastric mucosa after the oral administration of encapsulated aspirin revealed a lower incidence of this product compared to unencapsulated drug.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
RELEASE CHARACTERISTICS OF CAFFEINE AND MEBEVERINE HYDROCHLORIDE FROM ISOPROPYL MYRISTATE MULTIPLE EMULSIONS
247
254
70582
10.21608/bfsa.1990.70582
EN
M. S.
Mohamed
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
F. S.
Ghazy
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
M. A.
Mahdy
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
M. A.
Gad
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
Journal Article
1990
12
18
<em>Double emulsions (w/o/w) were prepared by two steps emulsification procedure using isopropyl myristate as the oily phase. The influence of the inner aqueous phase volume and emulsifier concentration on the release characteristics of either caffeine or mebeverine hydrochloride from the prepared emulsions was studied. For the purpose of comparison, the release of each drug from either o/w or w/o emulsion was investigated. The results showed that the release of both drugs from w/o/w emulsions was independent on the inner aqueous phase volume. The release of mebeverine hydrochloride was sustained from either w/o/w or w/o emulsions while that of caffeine was not significantly retarded as indicated by the amount released after 24 hours. Increasing the concentration of the hydrophilic emulsifier (Tween 20) had a little effect on the release of both drugs from w/o/w emulsions. On the other hand, the release of mebeverine hydrochloride was more prolonged on increasing the concentration of the lipophilic emulsifier (Span 80), while the release of caffeine was not significantly retarded.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
FORMULATION AND EVALUATION OF MIDAZOLAM SUPPOSITORIES: 1- FORMULATION OF MIDAZOLAM SUPPOSITORIES ADOPTING HPLC TECHNIQUE FOR ANALYSIS
255
264
70584
10.21608/bfsa.1990.70584
EN
H.
Hafez
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S. M.
El-Gizawy
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1991
01
06
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
13
2
1990
12
31
PREPARATION AND EVALUATION OF HYDROXYZINE SUPPOSITORIES
265
280
70586
10.21608/bfsa.1990.70586
EN
F. S.
Habib
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
H. A.
Sayed
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
S.
Ismail
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
A. A.
Gomea
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Egypt
A.
Shaker
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1991
04
02
<em>Hydroxyzine is a piperazine derivative recommended for treatment of anxiety. The drug was formulated in suppository forms using different types of fatty, emulsion and water soluble bases. Non ionic surfactants as well as aerosils were used as formulating additives. The drug release from the formulating bases as well as the tranquilizing potency in mice were evaluated. It was found that formulations which afford the higher release rates in the in-vitro study, give also the more pronounced tranquilizing effect in the animal testing.</em>