2024-03-28T19:01:01Z
https://bpsa.journals.ekb.eg/?_action=export&rf=summon&issue=9857
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
SOLUBILIZATION OF SOME NON-STEROIDAL ANTIINFLAMMATORY DRUGS (NSAIDs) BY PLURONIC F-127 BLOCK COPOLYMER
M.
EL-Badry
M.
Fathy
M.
Abdel Mohsen
This work is an attempt to solubilize certain non-steroidal anti-inflammatory drugs suchas Piroxicam (PXM), Ibuprofen (IBU) and Indomethacin (IND), through the use of hydrophilicsurfactant pluronic F-127 (Pl. F-127), which was used in different concentrations above itscritical micelle concentration (CMC). The solubility of the investigated drugs was enhanced,and was linearly correlated with the surfactant concentration. The effect of temperature on thesolubilization capacity of the surfactant and the distribution coefficient of the drugs between themicellar and aqueous phases was determined. It was found that, there is a direct relationshipbetween the solubilization capacity of surfactant toward the used drugs and temperature andthere is an inverse relationship between the distribution coefficient and temperature. Theseobservations were more obvious for IBU than IND and PXM.The change in heat of solution (H), free energy (G) and entropy (S) as a result ofsolubilization of the investigated drugs were calculated. The data prevailed that, the presence ofPl. F-127 energetically favors the solubility of the used drugs and more favorable by increasingthe surfactant concentration. The dissolution study was performed for these drugs. Pl. F-127proved its ability to enhance the dissolution rate of the investigated water insoluble drugs.
2004
06
30
1
9
https://bpsa.journals.ekb.eg/article_65384_513c059799d9ef856484e91b60a0a32f.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
SPECTROPHOTOMETRIC DETERMINATION OF INDAPAMIDE AND CO-DERGOCRINE MESYLATE
Niveen
Mohamed
Two simple and sensitive spectrophotometric methods for the determination of indapamideand co-dergocrine in pure form and in pharmaceutical preparations were developed. Themethods were based on the interaction of the cited drugs with either ammonium vanadate orsodium nitrite in strongly acidic media. The resulting coloured products were measured at 530and 550 nm for indapamide and co-dergocrine respectively. The effect of different variables onthe involved reactions and the colour development were studied and optimised. Beer,s law wasobeyed in the range of 1.8-12 g ml-1 for indapamide using ammonium vanadate and sodiumnitrite and 12-40 g ml-1 for co-dergocrine with both ammonium vanadate and sodium nitrite.The reproducibility and recovery of the methods are excellent. The methods were appliedsuccessfully to the determination of some commercially available dosage forms purchased fromthe local market. The results were comparable to those obtained by official or reportedmethods.
2004
06
30
11
18
https://bpsa.journals.ekb.eg/article_65385_1333496f42fed77b830bb6b97436c850.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
MODIFICATION OF THE RELEASE OF DIPYRIDAMOLE FROM CERTAIN POLYMERIC SYSTEMS
Ahmed
Aboutaleb
Ali
Abdel-Rhaman
Mahrous
Ahmed
Amany
Abdel-Rheem
The objective of the present study is to modify the release of dipyridamole (DIP); whichhas a pH dependant solubility in order to overcome its irregular and incomplete absorptionfrom the gastrointestinal tract. This was achieved by incorporation of a dissolution retardersuch as cellulose acetate phthalate CAP and a dissolution enhancer such as cyclodextrins;(dimethyl beta cyclodextrin DM-βCD and hydroxypropyl betacyclodextrin HP-βCD). This wasan effective mean of moderating the drastic dissolution behaviour of that basic drug at acidicpH. Coevaporates of DIP with DM-βCD and DIP with HP-βCD in 1:2 molar ratio wereprepared, followed by coating of these coevaporates by an enteric polymer (cellulose acetatephthalate, CAP) in 1: 3 drug : polymer weight ratio. In vitro release study was performed forcapsules containing the modified granules at pH values of 1.3, 5 and 6.8. It was found that thedrug release from the modified granules was decreased in a simulated gastric fluid and wasenhanced in a simulated intestinal fluid and reached up to 100%. This could be attributed to theprotecting effect of CAP for the drug granules in the acidic medium, followed by dissolving ofCAP coat in the intestinal fluids which lead the drug to be released easily from the granules.
2004
06
30
19
24
https://bpsa.journals.ekb.eg/article_65386_61993d0e2d5ab25c53298e344310db70.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
MACRO- AND MICROMORPHOLOGY OF FLACOURTIA CATAPHRACTA ROXB CULTIVATED IN EGYPT: STEM, LEAF, AND STEM-BARK
H.
Sayed
M.
Mohammed
F.
Darwish
A.
Mohammed
The detailed macro-and micromorphological characters of the stems, leaves and stembarkof Flacourtia cataphracta Roxb. (Syn. F. jangomas Raeusch) were studied with the aim tofind out the diagnostic elements of these organs, which facilitate their identification in bothentire and powdered forms.
2004
06
30
25
40
https://bpsa.journals.ekb.eg/article_65387_258d1dc05f48c9e3fb99dbbb2f70257e.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
THE UTILIZATION OF A HYDROPHILIC WAXY BINDER IN THE PREPARATION OF ORALLY DISINTEGRATING TABLETS BY MEANS OF TWO DIFFERENT GRANULATION METHODS
G.
Abdelbary
P.
Prinderre
C.
Eouani
J.
Joachim
Ph.
Piccerelle
The demand for rapidly disintegrating tablets (RDT) has been growing during the last decade especially for elderly and children who have swallowing difficulties. The problem of certain RDT is their low physical resistance and high friability. This work describes a new approach to prepare RDT with sufficient mechanical integrity, involving the use of a hydrophilic waxy binder (Superpolystate , PEG-6-stearate). Superpolystate is a waxy material with a melting point of 33°-37° and an HLB value of 9. So it will not only act as a binder and increase the physical resistance of tablets but it will also help the disintegration of the tablets as it melts in the mouth and solublises rapidly leaving no residues. The incorporation of Superpolystate in the formulation of RDT was realized by means of two different granulation methods: wet granulation by using an emulsion of this waxy binder as granulating liquid and melt granulation where the molten form of the binder was used. Granule size distributions of both wet and melt granulates of crystallised Paracetamol and D-mannitol were compared using laser light diffractometer. Scanning electron microscopy (SEM) was used to examine their morphological characteristics. The potential of the intragranular addition of croscarmellose as a disintegrating agent was also evaluated. The subsequent step encompassed the preparation and the evaluation of the tablets, including the effect of the extragranular introduction of croscarmellose. An improvement in tablet hardness and friability was observed with both granulation methods where we were able to obtain RDT with a disintegration time of 40 2 s and a hardness of 47.9 2.5 N.
2004
06
30
41
51
https://bpsa.journals.ekb.eg/article_65407_962406d2a285418df3575657ca552ae4.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
PREPARATION AND EVALUATION OF NAPROXEN ADSORBATE AS AN ATTEMPT TO IMPROVE DRUG DISSOLUTION CHARACTERISTICS
Ahmed
Ismail
K.
Saleh
S.
Khalaf
Naproxen is a nonsteroidal anti-inflammatory drug which shows variable absorption and bioavailability due to its poor solubility. In this study we aimed to improve the dissolution rate of the drug by solvent deposition onto certain adsorbents including porous silica, Avicel and Bentonite. Physical mixtures of naproxen with the investigated adsorbents were also prepared. The molecular behavior of naproxen in the investigated systems were studied using infrared absorption spectra, differential scanning calorimetry and X-ray diffraction analysis. The dissolution rate of the drug was also investigated. The obtained results indicated that naproxen was transformed to the amorphous state in case of mixtures loaded with porous silica. This transformation resulted in a significant enhancement of the dissolution rates of the drug. In addition, it was noticed that, the drug: adsorbents weight ratio of the prepared mixtures influenced the drug dissolution rate enhancement. Accordingly, it can be concluded that, by increasing the weight ratio of the used adsorbent in the mixture, the larger the enhancement in the dissolution rate of naproxen will be obtained.
2004
06
30
53
62
https://bpsa.journals.ekb.eg/article_65408_386ba1990e7253f23ab80baa7351e54c.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
ANTI-FREE RADICALS: SOURCE, ROLE AND APPLICATION IN DERMO-COSMETOLOGY
Joëlle
Joachim
G.
Abdelbary
P.
Prinderre
J.
Reynier
J.
Kister
P.
Piccerelle
Many environmental factors attack our skin continuously: Sun, wind, pollutants and tobacco which constitute the principle skin aggressors. Free radicals which are highly reactive chemical compounds, induce cellular and tissue injuries, and subsequently lead to aging. These free radicals are normally produced by cellular metabolism. They are represented by: OH°, RCOO°, NO° radicals and singlet oxygen. Free radicals are involved in cutaneous aging. Normally these radicals are neutralised by natural or human antiradical agents like superoxide dismutase, glutathione reductase, glutathione peroxidase and others. Some pathologic situations (cancer, Alzheimer disease, Crohn’s disease, atherosclerosis, diabetes mellitus …) are characterized by an over production of these radicals where the natural defences become overwhelmed. Oral administration of exogenous substances like vitamin A, C, E, oligoelements Cu, Zn, Se, Mn decrease free radical harmful and deleterious effects. Nature has several means to fight against oxidative stress: polyphenols, flavonoïdes and lipids are antiradical substances of plant origin. The future belongs to understand natural antiradical mechanisms as well as the synthesis of new molecules which would be effective in prevention of harmful effects produced by these radicals.
2004
06
30
63
68
https://bpsa.journals.ekb.eg/article_65409_6a0378463133fbc4b368bd2946a6c49b.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
PREPARATION OF SUBTILISIN COMPLEXES WITH ALPHA-2MACROGLOBULIN AND THEIR CHARACTERIZATION
S.
Hassan
The subtilisin complexes with dexamethasone and Alpha-2 macroglobulin were synthesized and were found to be immunoreactive to the specific antidexamethasone antibodies. These complexes also retain proteolytic activity when low molecular weight substrate was used by Homogeneous colorimetric method. The doubly labelled substrate was also used to study the enzyme activity in complex form. The Dex-subtilisin showed the proteolytic activity whereas Dex-subtilisin A2M did not show the proteolytic activity due to no access of small molecular weight substrate towards the large molecular weight protein in a co-complex form.
2004
06
30
69
74
https://bpsa.journals.ekb.eg/article_65410_0ffcf5b6356f8f1d070abf9f476b75f9.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
THE EFFECTS OF TEUCRIUM POLIUM LEAVES ON HEMATOLOGICAL INDICES AND SOME BIOCHEMICAL PARAMETERS IN RATS
Luay
Al-Essa
Khaled
Al-Kubaisy
The effects of T. Polium leaves extract were evaluated on rats during three weeks of administration. Blood picture and some biochemical parameters were investigated. Significant decrease was demonstrated in red blood corpuscles (RBCs), hemoglobin (Hb), and packed cell volume (PCV). However, other blood indices, mean corpuscular hemoglobin (MCH), mean corpuscular hemoglobin concentration (MCHC) and mean corpuscular volume (MCV) were not changed. There was significant decrease in the platelets (PLT), while white blood cells showed a significant increase. Serum glucose level change was insignificant while the level of serum cholesterol was significantly reduced. Significant increases were found in the serum activities of glutamate oxaloacetate transaminase (GOT), alkaline phosphatase (ALP) and lactate dehydrogenase (LDH) while glutamate pyruvate transaminase (GPT) was decreased.
2004
06
30
75
78
https://bpsa.journals.ekb.eg/article_65412_bbeeb5a3166c02ff565df5001a4a6569.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
NATURAL HAIR RECIPE
T.
Abou-Khalifa
O.
El-Gindi
H.
El-Nazer
A.
Ahmed
Biological evaluation of natural preparations used for treatment of hair loss revealed that the saponifiable fraction was the active fraction. The main constituents of this fraction were palmitic, stearic saturated fatty acids and oleic and linoleic unsaturated fatty acids. Certain modifications were done to increase the activity by addition of Cantharidin or Pilocarpine to the most active subfraction of saponifiable matter. The superior effect on treating hair loss was shown with the formulation containing cantharidin than that which contain pilocarpine
2004
06
30
79
85
https://bpsa.journals.ekb.eg/article_65413_d0730cfd42e8a43c9a651d279e8cf810.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
DIETARY PHYTOCHEMICALS AS CHEMOPREVENTIVE FOR LIVER CANCER
S.
Ibrahim
M.
Mostafa
Y.
Elhassaneen
M.
El-Soadany
Phenolic acids content of potato tubers, subjected to different types of cooking as well as in the peels and peeled fresh tubers, were determined by HPLC. The higher value of phenolic acids was noticed in the tubers cooked by grilling and in the peels of the fresh tubers. The cytoxicity of the aqueous solution of the prepared dried ethanolic extracts was tested by the use of isolated liver cells of Bolti fish in RPMI 1640 medium at 330 mOsm/kg in the presence of 5% CO2 and incubated at 27°. Benzo(a) pyrene, B(a) P, was used as toxicating agent. After the incubation period the media were removed, stained with neutral red and incubated for 3 hours. The dye of the stained cells was extracted with 1% acetic acid: 50% ethanol mixture and the absorbance of the extracts was measured at 490 nm. The result of the assay indicated that phenolic acids decrease the cytotoxicity of B (a) P in all treatments. The more effect was noticed for phenolic acid extracts in commitment with B(a) P followed by post then pre-treated ones.
2004
06
30
87
94
https://bpsa.journals.ekb.eg/article_65415_7e4ed7541f9d512afb0775b0236c67de.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
PHYTOCHEMICAL AND BIOLOGICAL INVESTIGATION OF THE VOLATILE CONSTITUENTS OF NEPETA SEPTEMCRENATA EHRENB., GROWING IN EGYPT
Mohamed
El-Hamouly
Atef
El-Hela
The volatile constituents of Nepeta septemcrenata Ehrenb. herb growing in Egypt were prepared by hydrodistillation of the fresh herb and analysed by GC/MS. Sixteen major compounds (represent 94.96% of total) were detected and identified. They contain ten oxygenated compounds (70.67%) and six hydrocarbons (24.29%). The major oxygenated compounds were 1,2 benzene-dicarboxylic acid dibutyl ester (33.16%) and 4-methyl-2,6ditertbutyl phenol (23.30% w/w), while the major hydrocarbon is 4-nonyne C9H16, (9.00%). The volatile constituents had promising antimicrobial activities against some tested microorganisms.
2004
06
01
95
98
https://bpsa.journals.ekb.eg/article_65416_f89870e7172ac9cc3a7644e595e20859.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
PHYTOCHEMICAL INVESTIGATION AND MOLLUSCICIDAL ACTIVITY OF OREOPANAX RETICULATUM DONN
Abdel-Gawad
M.
El-Nahas
A.
El-Sayed
M.
Abdel-Hameed,
S.
The unsaponifiable part of the petroleum ether fraction of the leaves and stems of Oreopanax reticulatum Donn (Family Araliaceae) was analysed by GLC to reveal the presence of a series of hydrocarbons, cholesterol, stigmasterol and -sitosterol. Also, eight fatty acids were identified on the saponifiable part. The butanolic fraction was chromatographed over silica gel and sephadex-LH20 columns and preparative thin layer chromatography to afford two flavonoid glycosides (I and IV) as well as four bidesmosidic triterpenoidal saponins (II, V, VII and VIII). Alkaline hydrolysis of two bidesmosidic saponins (II and V) gave two monodesmosidic (III and VI). Their structures were elucidated using spectroscopic and chemical techniques. Molluscicidal screening of the isolated compounds (I-VIII) against Biomphalaria alexandrina snails, the intermediate host of Schistosoma mansoni in Egypt revealed that the two monodesmosidic triterpenoidal saponins (III and VI) have strong activities (LC90= 7 and 6 ppm) after 24 hours exposure whereas the two flavonoid glycosides and four bidesmosidic saponins were inactive up to 50 ppm.
2004
06
30
99
111
https://bpsa.journals.ekb.eg/article_65417_10bcb923b8c4b0ece0ccfab22885e02a.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
BIOTRANSFORMATION OF INDOLE ALKALOID BY TERRESTRIAL STREPTOMYCES GW 14/587 STRAIN INTO A SELECTIVE PHYCOTOXIC AGENT
E.
Haggag
H.
Laatsch
Methyl indole was isolated as a metabolite from the culture broth of terrestrial Streptomyces GW 14/587 strain which was fed with indole after two days growth and then inoculated for another two, three and four days to optimize the experiment condition for highest metabolite concentration. The structure of the isolated methyl indole was established using spectral techniques of HPLC-MS, EI-MS, 1H and 13CNMR. Also the bacterial extract showed a high selective phycotoxic activity against Scendensmus subspicatus among the different tested microalgae, yeast, fungi and bacteria.
2004
06
30
113
122
https://bpsa.journals.ekb.eg/article_65420_73b8e9bbad737b45de1a30b4bcc24607.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
TRITERPENOID SAPONIN FROM ZYGOPHYLLUM DUMOSUM
Kamel
Shaker
The new triterpenoid saponin, 3-O--L-rhamnopyranosyl-(12)--L-arabinopyranosyl-(12)- -D-xylopyranosyl-taraxast-20(21)-en-28-oic acid-28-O-2-O-R- -D-glucopyranosylester has been isolated from the roots of Zygophyllum dumosum. The structure was establishedprimarily by NMR spectroscopy. All NMR signals were assigned by 1H-1H COSY, HMQC,HMBC, ROESY and TOCSY experiments.
2004
06
01
123
126
https://bpsa.journals.ekb.eg/article_65461_87d018f6549da25fe41e81ccf2067d90.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
POTENT ESTROGENIC FLAVONE GLYCOSIDES FROM ATRIPLEX SEMIBACCATA
Kamel
Shaker
M.
Mostafa
Three known flavone glycosides 1, 2, and 3 were isolated for the first time from the whole plant of Atriplex semibaccata. The assignment of the NMR signals was performed by means of 1H-1H COSY, HMQC, and HMBC experiments. The isolated compounds showed potent estrogenic, and promising anti-microbial activities.
2004
06
30
127
132
https://bpsa.journals.ekb.eg/article_65429_7f8049fab6e70021da84cdc26ae9afc0.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
ENTEROCOCCAL ISOLATES FROM RAW MILK AND DAIRY PRODUCTS IN RIYADH REGION AND THEIR SUSCEPTIBILITY TO COMMON ANTIBIOTICS
L.
Nasser
T.
Elkersh
S.
Mejally
A total of 100 samples of raw milk, various cheeses, labnah, yogurt, and egett were collected from appropriate suppliers and markets in Riyadh region. Bacteriological analysis for typing of enterococci and other lactic Acid Bacteria (LAB) was carried out by plating appropriate dilutions of each sample on sheep blood agar and Edwards blood agar plates. After overnight aerobic incubation at 37°, the presumptive identification was done by colony morphology, cultural characteristics, Gram-stain and catalase production. Final identification to the genera and species level of the total 125 bacterial isolates was completed by API-20 strips as well as Lancefield-serogrouping. Results revealed that Enterococcus faecium (88 isolates) accounts of 70% of total bacterial isolates, while Enterococcus faecalis (26 isolates) accounts of up to 21% and other LAB constituted about 9% of total recovered isolates. The later isolates comprises 3, 3, and 5 isolates of Enterococcus gallinarum, Enterococcus durans, and Aerococcus viridans respectively. The results revealed that nature of sample, its pH, and salinity clearly affect the incidence and number of recovered bacterial isolates. Thus as pH rises towards neutrality, with no salt or low salinity, E. faecalis and other LAB were recovered more frequently, and vice versa. In contrast, E. faecium was routinely isolated from most of the examined samples regardless of their pH range and salinity- content, reflecting its ubiquitous nature and its tolerance to drastic environmental conditions, thereby facilitating person to person transmission. The dominance or persistence of enterococci in examined samples is most probably attributed to their wide range of growth temperatures, their tolerance to heat, salt and acid. In addition, the MIC of each of the tested 120 isolates was determined by serial dilution in Muller Hinton sheep blood agar against 9 antibiotics. All isolates were sensitive to ampicilin with the exception of one E. faecalis strain that showed an MIC of 4 ug/ml. While Erythromycin (EM) exhibited also a good activity with an MIC50/MIC90 of 1/1, 1/4, 2/8 and 4/4 ug/ml. for E. gallinarum, E. faecalis, E. faecium, and E. durans or Aerococcus viridans isolates respectively. Whereas all isolates were resistant to cefoxitin and about 50% were also resistant to Chloramphenicol (CM), Tetracycline (TC), or Trimethoprim / Sulfamethoxazole (SXT). Thus at the breakpoint of MIC (>16 ug/ml.) (TC) resistance rate for E. faecalis was 16% and for E. faecium and E. gallinarum was 35% and 100% respectively. Whereas that for vancomycin (VM) the figures were 44%, 19% and 100% respectively. It is concluded that the examined samples may constitute a potential source for the dissemination of antibiotic resistant determinants to human.
2004
06
30
133
140
https://bpsa.journals.ekb.eg/article_65430_ed25360840e397e69549c458769ed2a7.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
SYNTHESIS AND ANTIBACTERIAL SCREENING OF SOME 2,5,7TRIARYL-1,2,4-TRIAZOLO[1,5-a]PYRIMIDINES
Nawal
El-Koussi
Farghaly
Omar
Salah
Abdel-Aziz
Mohamed
Radwan
Three novel series of 5,7-diaryl-2-(pyridyl)-1,2,4-triazolo[1,5-a]pyrimidines were prepared as antibacterial and antifungal agents. The triazolopyrimidines (21-23)a-m were synthesized by reaction of the respective 3-amino-5-(2-,3- or 4-pyridyl)-1,2,4-triazoles (14-16) with substituted chalcones analogues (17a-m) in ethylene glycol. As the cyclocondensation reaction of such heterocyclic amines with α,β-unsaturated ketones might produce isomeric triazolopyrimidines, the isolated products were identified by studying their IR, 1H-NMR and MS. Their purity have been ascertained through TLC and elemental analyses. The antibacterial activity of the prepared compounds was screened against several bacterial species in comparison to Amoxycillin. As general features the 2-pyridyl series (21a-m) exhibited higher activity than the corresponding 3- or 4-pyridyl analogues (22-23)a-m. The 3-pyridyl derivatives (22a-m), particularly those having electron-donating substituent on the phenyl nucleus, showed selective antibacterial activity against S. marcescens. The synthesized derivatives were tested for antifungal activity, in comparison to Clotrimazole but no activity has been observed.
2004
06
30
144
154
https://bpsa.journals.ekb.eg/article_65432_ac0a31e7f753e6ea6182b586e96800ee.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
SOLID LIPID NANOPARTICLES - EFFECT OF LIPID MATRIX AND SURFACTANT ON THEIR PHYSICAL CHARACTERISTICS
Mamdouh
Ghorab
Heba
Abdel-Salam
Mohamed
Abdel-Moaty
Solid lipid nanoparticles (SLN) have gained increasing attention as a colloidal drug carrier system, particularly for lipophilic drugs, because SLN combine the advantages of polymeric nanoparticles, fat emulsions, and liposomes but avoiding their disadvantages. Solid lipid nanoparticles are composed of high melting point lipid as a solid core coated by surfactants. The solid core allows the prolonged and controlled release of drugs and may protect incorporated drugs against chemical degradation. Lipid and surfactant nature are important in drug loading capacity, also affect size distribution and physical stability. In this study SLN were prepared by using different ratios of lipid/surfactant. The lipid nanopellets were produced by using the high speed homogenizer and by high pressure homogenizer. The particle size measurements were carried out using the photoncorrelation spectroscopy and laser diffraction. The results showed that the diameter of SLN were influenced by lipid matrix and surfactant nature as well as their concentrations. Particle size diameter was decreased as a function of surfactant concentration till it reach a certain limit after which it has no effect. Methods of preparation showed a potential effect on the presence of large particles and on the polydispersity index. In conclusion, physical characteristics of SLN are not only influenced by variation in process parameters but also by chemical nature of the used surfactant and lipid matrix that have a potential influence on the particle size distribution of SLN.
2004
06
30
155
159
https://bpsa.journals.ekb.eg/article_65434_358854452aedeaca06ae4ff5414723e2.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
CHEMICAL CONSTITUENTS AND MOLLUSCICIDAL ACTIVITY OF IRIS PSEUDACORUS L. CULTIVATED IN EGYPT
H.
Sary
N
Ayoub
A.
Singab
A.
Ahmed
M.
Al-Azizi
The molluscicidal activity of leaves and rhizomes extracts of Iris pseudacorus L. family Iridiaceae against Biomphalaria alexandrina snails were evaluated and proved activity. The successive extracts of leaves viz; n-hexane, chloroform, diethyl ether and ethyl acetate (LC50 values ranged from 0.8~14.65 mg/L) were found to be more potent than those of rhizomes. Bioactivity guided fractionation of leaves extracts resulted in the isolation of (13) compounds. The structural determination of the isolated compounds was established upon the study of their physicochemical and spectral data including UV, IR, 1H, 13C-NMR and MS as well as comparison with the data reported in literature. These compounds were identified as: apigenin (1), luteolin (2), -sitosterol-3-O-glucoside (3), catechol (4), protocatechuic acid (5), gallic acid (6), (-)-epicatechin (7), iso-vitexin (8), vitexin (9), iso-orientin (10), orientin (11), vicenin II (12) and mangiferin (13). Reviewing the available literature, this is the first report regarding the determination of molluscicidal activity as well as isolation and identification of these compounds from Iris pseudacorus L.
2004
06
30
161
169
https://bpsa.journals.ekb.eg/article_65438_a3ef37efba78b1b4367824644f6bc465.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
2004
27
1
DESIGN AND SYNTHESIS OF SOME P-SUBSTITUTED STYRYLISOXAZOLE CARBOXYLIC ACID DERIVATIVES AS ANTI-INFLAMMATORY AGENTS
Farghaly
Omar
Atef
Abdel-Hafez
Montaser
Ahmed
A series of 5-(p-substitutedstyryl)-isoxazole-3-carboxylic acids (4a-g), carboxylic acid ethyl esters (3a-g) and their corresponding amides (6-29) as well as their hydroxamic acid analogues (5a-g) were synthesized and evaluated for their anti-inflammatory activity. The 1,3dicarbonyl systems 2,4-dioxo-6-arylhex-5-enoic acid ethyl esters (2a-g) were the key intermediate for synthesis of the target isoxazole derivatives. The synthesis of these intermediate was achieved through the reaction of chalcones (1a-g), prepared via aldol condensation of the respective substituted benzaldehyde with acetone in alkaline medium, with diethyloxalate. The purity of the synthesized derivatives was determined by thin layer chromatography (TLC) in addition to the microanalyses and their structures were confirmed by different spectroscopic means. The anti-inflammatory activity of twenty-one compounds [(3a,e,f and g); (4a-g); (5a-g); 22; 24 and 25] were assessed, at a dose of 100 mg/kg, by carrageenan-induced paw edema in rats in comparison to indomethacin as a reference drug. The ulcerogenicity of the compounds 3g, 4g and 5g as representatives of the anti-inflammatory active compounds (ester, carboxylic acid and hydroxamic acid) and indomethacin as reference drug was examined under scan electron microscope, after 24 hours of administration of single dose (100 mg/kg) in rats. Significant anti-inflammatory activity was displayed by most of the target derivatives. p-Nitro and p-methoxystyryl isoxazole carboxylic acid derivatives (4e and 4f) revealed 75% inhibition of inflammation after 1 hr reflected the rapid onset of action of these derivatives, which may sustained up to 5 hr as in case of 4e. The anti-inflammatory activity of 5-(p-nitro and pdimethylaminostyryl)-isoxazole-3-carboxylic acid ethyl esters (3e and 3g) being favorably comparable with indomethacin in terms of potency and ulcerogenic liability. The rational behind the synthesis of these compounds and the structure activity relationship are discussed.
2004
06
30
171
186
https://bpsa.journals.ekb.eg/article_65439_3e5756058eb3a03bb46460f365c5c22d.pdf