Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
NEW IONOL GLYCOSIDES FROM MAERUA CRASSIFOLIA FORSSK GROWN IN ETYPT
89
95
67956
10.21608/bfsa.1998.67956
EN
Mahmoud A.
Ramadan
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Z. Z.
Ibraheim
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
A. M.
Abdel-Baky
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
D. W.
Bishay
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
H.
Itokawa
Tokyo College of Pharmacy, Tokyo, Japan
Journal Article
1998
05
12
<em>Further investigation of the methanolic extract of the air-dried aerial parts of Maerua crassifolic Forssk (F. Capparaceae) resulted in the isolation of three new ionol glycosides. The structure of the isolated compounds had been established by extensive chemical and spectroscopic techniques.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
INVESTIGATION OF PETROLEUM ETHER EXTRACT OF THE BULBS OF CRINUM AUGUSTUM ROX.
97
102
67957
10.21608/bfsa.1998.67957
EN
Mahmoud A.
Ramadan
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1998
05
12
<em>The bulbs of Crinum augustum Rox. Fam. Amaryllidaceae were extracted with ethanol (95%) by maceration and percolation. From the petroleum ether fraction four saturated straight chain hydrocarbons, 24-methylene cycloartanol and cycloeucalenol were isolated and identified. The identification of these compounds was based on GLC-Mass spectrometry. In addition, an alkaloid (ungeremine) was also isolated and characterized from the n-butanol extract.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
FLAVONOIDS FROM PULICARIA ARABICA (L.) CASS.
103
108
67958
10.21608/bfsa.1998.67958
EN
Mahmoud A.
Ramadan
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1998
05
12
<em>From the chloroformic extract of the aerial parts of Pulicaria arabica (L.) Cass. eight flavonoids were isolated. Their structures were established by spectroscopic methods (UV, MS and NMR spectroscopy) and proved to be 3,7-dimethoxy kaempferol, 3-methoxy kaempferol, kaempferol, dihydro kaempferol, 3,7-dimethoxy quercetin, 3-methoxy quercetin, quercetin and dihydro quercetin. In addition, and acetophenone was also isolated.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
TWO NEW TRITERPENES AND OTHER CONSTITUENTS FROM LUPINUS VARIUS AND LUPINUS HARTWEGII
109
115
67960
10.21608/bfsa.1998.67960
EN
H. A.
Hassanean
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1998
04
14
<em>Two new genuine triterpenes previously semisynthesized and given the names dimethyl serratagenate and acetyl dimethyl serratagenate, besides three known coumaronochromones named lupinalbins A, C and E, in addition to three common Lupin isoflavones known as genistein, luteone and 2'-hydroxy genistein as well as, the more frequent β-sitosterol glucoside and the less frequent syringin were isolated from the chloroform fraction of the aerial parts of L. varius.</em>
<em>Moreover, the same compounds were almostly detected by co-chromatography with the corresponding fraction obtained from L. hartwegii. The identification of these compounds was based on different methods of chemical and spectral evidences.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
DEVELOPMENT, CHARACTERIZATION AND IN VIVO EVALUATION OF POLYELECTROLYTE COMPLEX MEMBRANE GEL MICROCAPSULES CONTAINING MELATONIN-RESIN COMPLEX FOR ORAL USE
117
139
67961
10.21608/bfsa.1998.67961
EN
Ibrahim
El-Gibaly
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Mamdouh M.
Anwar
Department of Physiology, Faculty of Medicine, Assiut University, Assiut, Egypt
Journal Article
1998
06
10
<em>A novel oral multiple-unit delivery system for melatonin, (Ca) alginate/polyethyleneimine (PEI) gel microcapsules containing melatonin-resin (Dowex 1-X<sub>8</sub> Cl<sup>-</sup>) complex, which overcome many of the problems encountered with the conventional dosage forms, Ca-alginate gel beads was designed through an ionic crosslinking/interpolyelectrolyte complexation technique. The effect of different processing variables viz., gelation time, PEI concentration, melatonin/resin ratio, core/coat ratio, pH and ionic strength of the dissolution medium on the release characteristics of microcapsules in comparison with alginate beads was investigated. The results obtained indicated that a PEI concentration of 2% and gelation time of 24 h. were the optimal conditions for a marked release retardation. Of ultimate importance is the ionic character of the synthetic polyelectrolyte complex (PEC) membrane (alginate/ PEI) that produced microcapsules which did not disintegrate in simulated intestinal fluid (S.I.F., pH 7.4) over a period of 3 days of testing and allowed a pH-independent release rate of melatonin up to 2 h. in phosphate buffer (0.154 M Na<sup>+</sup> ions) (K<sub>1</sub> = 5.42x10<sup>-1</sup>, 5.995x10<sup>-1</sup> and 5.78x10<sup>-1</sup> hr<sup>-1</sup> for pHs of 5.5, 7.4 and 9.0, respectively). The metatonin release rate of microcapsules (K<sub>1</sub>= 1.144z`0<sup>-1</sup> hr<sup>-1</sup>) in S.I.F. (pH 7.4) was significantly reduced when compared to that of the original alginate beads (K<sub>1</sub>= 19.59x10<sup>-1</sup> hr<sup>-1</sup>) which showed a dramatic disintegration and dissolution in S.I.F. (pH 7.4) within 1 h. Most importantly, successful attempts to prepared crosslinked protein or polyamide/PEI-graft co-polymer membranes-coated alginate microcapsules were achieved by making use of a modified interfacial polymerization process. The coated microcapsules offered a remarkable reduction of the release rate in simulated gastric fluid (S.G.F., pH 1.2) as compared to alginate beads. The modulatory influence of melatonin (biological half-life = 24 min) on liver detoxifying and antioxidant enzyme systems (glutathione-S-transferases (GSTs) and glutathione peroxidase (GSH-Px), as well as lipid peroxides (LPER) levels was studied in rats. The obtained results revealed that melatonin resonates-loaded (Ca) alginate/PEI gel microcapsules (T<sub>50%</sub> = 6.06 h) produced a significant marked elevation in hepatic cytosolic activities levels of GSTs and GSH-Px as well as glutathione (GSH) content with a reduction in (LPER) levels, when compared with the corresponding controls, suggesting that alginate/PEI gel microcapsules could be a useful reservoir system for controlled-release melatonin delivery.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
MACRO- AND MICROMORPHOLOGY OF AILANTHUS ALTISSIMA SWINGLE CULTIVATED IN EGYPT: LEAF, STEM AND STEM-BARK
141
159
67980
10.21608/bfsa.1998.67980
EN
A. M.
Abdel-Baky
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
F. M. M.
Darwish
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Z. Z.
Ibraheim
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Y. G.
Gouda
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1997
10
07
<em>The detailed macro- and micromorphological characters of the leaf, stem and stem park of Ailanthus altissima Swingle syn. Ailanthus glandulosa Desf. (Tree of heaven) are studied with the aim to find out the diagnostic elements of these organs which facilitate their identification in both entire and powered forms. </em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
EFFECT OF MICROSPHERONIZATION ON THE RELEASE AND ULCEROGENIC ACTIVITY OF SULINDAC
161
170
67981
10.21608/bfsa.1998.67981
EN
A.
Abd-Elmageed
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1998
09
15
<em>Sulindac (SUL) NSAIDS has irritation and ulcerogenic activity on the human stomach. Sulindac microspheres were prepared adopting the solvent evaporation method, using cellulose acetate butyrate as coating polymer with 1-2 drug : polymer ratio. The influence of microsphere particle size and pH of the dissolution medium on the release profile of the drug was investigated. In all cases the drug release mechanism followed Higuchi diffusion model with sustained release profile of sulindac from SUL-CAB microspheres. The smaller particle size gave significantly higher release rate of the drug. The release rate was slower in acidic medium (pH 1.2) than that at pH 7.4. The effect of microspheronization on the ulcerogenic activity of the drug in the stomach of rabbits was studied. It was observed that the ulcerogenic activity of the drug was disappeared and the mucosal surfaces showed free of hemorrhage and inflammations when the drug is used as microspheres.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
EFFECT OF STORAGE ON THE IN-VITRO AND IN-VIVO CHARACTERISTICS OF SOME MARKETED SUSTAINED-RELEASE CARDIOVASCULAR TABLETS
171
183
67982
10.21608/bfsa.1998.67982
EN
Sayed H.
Khidr
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Esmail M.
Niazy
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box: 2457, Riyadh 11451, Saudi Arabia
Yousry M.
El-Sayed
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box: 2457, Riyadh 11451, Saudi Arabia
Journal Article
1998
04
30
<em>The in-vitro and in-vivo characteristics of the sustained-release cardiovascular drugs: nifedipine (N) nad procainamide (PA), commercially available as Adalat-Retard and Procainamide durules tablets were evaluated both before and after their storage at ambient condition and under different accelerated conditions of temperature and relative humidity (RH) for twelve months. The effect of storage on the physical properties, the release rate profiles, the chemical stability and the bioavailability of these tablets in beagle dogs was studied. The results showed no or small change in the physical properties or in the drug contents of both drugs under the storage conditions of the study, indicating good physical and chemical stability of these products. In spite of statistically significant difference found in the dissolution results between the prestorage and stored tablets, this difference was not considered to be of practical significant in case of these sustained release products. The in-vivo studies indicated a statistically significant difference in the area under the curve and in the average peak concentration between the prestored tablets and the tablets stored for twelve months under ambient and at 40°C/80% RH in case of PA durules. This is a sign for a possible change in the bioavailability of this product with storage regardless the conditions under which the product is stored. </em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
DEVELOPMENT AND EVALUATION OF A PROLONGED-RELEASE MATRIX TABLETS OF DICLOFENAC SODIUM RESINATE
185
202
67983
10.21608/bfsa.1998.67983
EN
Ibrahim
El-Gibaly
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Eman M.
Samy
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1998
09
29
<em>The preparation of a potential prolonged-release matrix tablets (IER-tablets) containing diclofenac sodium – anion exchange resin (Dowex I-X<sub>8</sub>.Cl<sup>-</sup>) complexes has been performed by direct compression of the drug-resin complex (drug resinate) with various release-regulating excipients (Avicel PH 101, lactose, sodium carboxymethylcellulose, and compritol). All the formulations produced tablets with good mechanical properties. The in-vitro release rate of diclofenac sodium from the drug-resin complex samples with different loaded concentrations and from the prepared IER-tablets (K<sub>h</sub> = 0.92-5.52 mg/min<sup>-0.5</sup>) was determined using a rotating paddle dissolution apparatus. The results obtained showed that drug release from these formulations was slower than from the tabletted diclofenac sodium alone (K<sub>h</sub> = 6.55-15.10 mg.min<sup>-0.5</sup>) or a commercial sustained-release tablet formulation of diclofenac sodium (K<sub>h</sub> = 8.23 mg.min<sup>-0.5</sup>) and that IER-tablets containing sodium carboxymethylcellulose or compritol exhibited the lowest release rates (K<sub>h</sub> = 0.92 and 1.27 mg/min<sup>-0.5</sup>, respectively). The kinetics of the drug release from resinate was evaluated on the basis of the mass low. In most cases, the profiles for both the effect of drug/resin ratio and sodium ion concentration upon drug release from the resonates exhibited two release rate processes: rapid release during the initial period, followed by a decreasing release rate, suggesting a particle diffusion release process. The release rate data of the tablets were investigated by using zero-order and the matrix-diffusion-controlled kinetics. The calculated exponential release exponents (n-values) revealed that release behaviour of all IER-tablets was a Fickian-diffusion kinetics (i.e., The Higuchi-linear square root of time relationship), confirming that a matrix diffusion-controlled mechanism was operative. To evaluate the feasibility of the drug resinate tablet system, the optimum IER-tablet formulations, drug resonates, sustained-release commercial tablet product and plain drug were examined for their ulcerogenic activity in rabbits. The results proved the superiority of the drug resinate and IER-tablets containing Avicel PH 101 over the plain drug, commercial product or IER-tablets containing compritol or sodium carboxymethylcellulose. Overall, this study demonstrated the significance of using ionic complex systems in offering a simple gastro-protected tablets and showed the characteristics of the matrix materials and their influence on the drug activity as well as tablet performance in-vivo.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
MICROENCAPSULATION OF ALLOPURINOL USING A FULLY IMPROVED NON-SOLVENT ADDITION TECHNIQUE AND A NOVEL BINARY BLEND BASED ON POLYVINYL CHLORIDE: FACTORIAL DESIGN APPLICATION
203
228
67984
10.21608/bfsa.1998.67984
EN
Ibrahim
El-Gibaly
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
1998
09
22
<em>A fully improved non-solvent addition coacervation-phase separation process which utilizes tetrahydrofurfuryl alcohol – cyclohexane : hexane (1:1 v/v ratio) as a solvent-non solvent pair, a novel binary blend comprising of polyvinyl chloride in combination with poloxamer 188 [a triblock copolymer of poly (ethylene oxid) – poly (propylene oxide) – poly (ethylene oxide)] as the wall material and ethylene-vinylacetate copolymer or polyisobutylene as coacervation-inducing agents has been developed for encapsulating allopurinol. The role of the coaddition of dioctylphthalate as a plasticizer and poloxamer 188 as a complementary coating polymer to the polymer solution phase on the properties of the microcapsules was investigated. The results indicated that plasticized / blended microcapsules resulted in a great shift to a narrow particle size distribution and a significant reduction in the drug loss percentage and the drug release rate in comparison with unplasticized / unblended microcapsules or plasticized polyvinyl chloride microcapsules.</em>
<em>In the preparation of the plasticized / blended microcapsule formulations, a 2<sup>3</sup> full factorial design based on three independent variables viz.; polymers blend concentration, amount of allopurinol and the type of the coacervation-inducing agent was applied. The mean influences of these variables on the micromeritic parameters (geometric mean particle diameter, span value and drug content) and dissolution properties of the microcapsules were characterized quantitatively and represented by predictor polynomial equations. The kinetic model according to the Rosin-Rimmler-Sperling-Bennett-Weillbull (RRSBW) distribution was applied for the linearization and parametric representation of the dissolution curves. The surface morphology of the microcapsules was examined by using scanning electron microscopy. The results revealed that using a lower polymers blend concentration level, a higher drug loading and ethylene-vinylacetate copolymer as a coacervation-inducing agent resulted in the formation of fairly spherical microcapsules of high monodispersity and better surface characteristics and extended the drug release period (t: time at which 63.2 percent of the medicament dissolved = 6.052 h in simulated gastric fluid (S.G.F, pH 1.2) – 5.151 h in simulated intestinal fluid (S.I.F, pH 7.4). in contrast, polyisobutylene microcapsules prepared under the same experimental conditions were irregular, macroporous, and having the fastest release rate (t= 4.48 h (S.G.F, pH 1.2) – 2.051 h (S.I.F, pH 7.4)). Studies of the drug release thermodynamics by the Arrhenius equation demonstrated clearly that the release of allopurinol is an energy-linked process by a single release mechanism. The formulation of microcapsules prepared using ethylene-vinylacetate copolymer into tablets, prolonged greatly the drug release.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
INVESTIGATION OF CONTROLLED RELEASE SOLID DISPERSION OF NAPROXEN USING EUDRAGIT RS AND RL POLYMERS
229
236
67985
10.21608/bfsa.1998.67985
EN
Mohammed G.
Abd El-Mohsen
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Ahmed
Ismail
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Assiut 71524, Egypt
Journal Article
1998
07
29
<em>Naproxen was used as a model drug and Eudragit RS and RL were used as inert carriers in an attempt to study the controlled release solid dispersion. Naproxen solid dispersion was prepared using solvent evaporation technique. IR study illustrated Naproxen/Eudragits interaction. Dissolution-rate studies showed that the amounts of Naproxen released were found to be fitted to the Higuchi-Square root of time model. The study proved that the solid dispersions composed of Eudragit RS exhibited slow release rates when compared with those composed of Eudragit RL. By a simple modification in the polymeric ratio of both Eudragit RS and Eudragit RL, the kinetics of release can be modulated. A marked reduction in the magnitude of release rates was observed upon increasing the particle size. It was found that there was a linear relationship between the logarithmic value of release rate constant and the fraction of Eudragit RL in the coevaporate composed of Naproxen/RS/RL. The finding was a confirmatory indication that the release was following Higuchi-diffusion model. The study also proved that the compression forces had no effect on the release rate constant. The incorporation of polyvinylpyrrolidone in the coevaporates containing Eudragit RS improved and increased the release profile of Naproxen.</em>
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
21
2
1998
12
31
STUDY OF THE SAPONIN CONTENT OF ATRIPLEX STYLOSA VIV. AND ITS MOLLUSCICIDAL EFFECT
237
243
67986
10.21608/bfsa.1998.67986
EN
Mortada M.
El-Sayed
Laboratory of Medicinal Chemistry, Theodor Bilharz Research Institute, Imbaba, Giza, Egypt
Journal Article
1998
08
05
<em>From the aerial parts of Atriplex stylosa Viv, four triterpenoidal saponins have been isolated. Their structures were established as 3-O-</em><em>a</em><em>-L-rhamnopyranosyl-(1</em><em>®</em><em>3)-</em><em>b</em><em>-D-glucuronopyranosyl hederagenin; 3-O-</em><em>b</em><em>-D-glucopyranosyl-(1</em><em>®</em><em>3)-</em><em>b</em><em>-D-glucuronopyranosyl hederagenin; 3-O-</em><em>a</em><em>-L-rhamnopyranosyl-(1</em><em>®</em><em>3)-</em><em>b</em><em>-D-glucuronopyranosyl hederagenin; 28-O-</em><em>b</em><em>-D-glucopyranoside and 3-O-</em><em>a</em><em>-L-rhamnopyranosyl-(1</em><em>®</em><em>)-[</em><em>b</em><em>-D-glucopyranosyl-(1</em><em>®</em><em>2)]-</em><em>b</em><em>-D-glucuronopyranosly oleanolec acid by spectroscopic methods (IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR and FAB-MS) as well as on basis of acidic and alkaline hydrolysis. The three monodesmosidic saponins exhibited various molluscicidal activities against the two aquatic snails; Biomphalaria alexandrina and Lymnaea cailliaudi, the intermediate hosts of Schistosoma mansoni and Fasciola gigantica respectively in Egypt whereas the bidesmosidic saponin was inactive against the two snail species. </em>