eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-01
32
1
1
21
10.21608/bfsa.2009.63328
63328
Original Article
PREPARATION AND EVALUATION OF CIPROFLOXACIN/CHITOSAN IMPLANTS AS A CONTROLLED BIODEGRADABLE DRUG DELIVERY SYSTEM
Eman El-Leithy
1
Department of Pharmaceutics, Faculty of Pharmacy, Helwan University
This work aimed to prepare and evaluate physically crosslinkedimplantable matrices based on chitosan as a site-specificdelivery of ciprofloxacin hydrochloride (CFX.HCl) for theprevention of post-surgical wound infection. Biodegradablematrices were prepared from chitosan and different polyanionpolymers by direct compression. The potential of formulationvariables on the in-vitro drug release from polymeric matrices hasbeen studied. A matrix system of CFX.HCl based on the polyanioncomplex of chitosan and pectin showed a sustainable drug releaseover three days. The swelling and in-vitro drug release experimentssuggested that complex formation between chitosan and pectin hasoccurred at ratio 1:2. The results also suggested that CFX.HClrelease from chitosan matrices was markedly influenced by thenature of polyanion polymers, mixing ratio and total weight ofmatrices, whereas the compression force did not significantly affectthe drug release. With increasing CFX.HCl loading, a decrease ofthe percent cumulative release was observed. Approximately 13%of loaded drug was released from matrix containing 25% w/w drugduring 72 hrs in phosphate buffer pH 7.4. Fitting the in-vitro drugrelease data to Korsmeyer equation indicated that combined effectof diffusion and polymer chain relaxation could be the mechanismsof drug release. Microbiological simulated test revealed theefficient microbial inhibitory effect of chitosan: pectin (1:2) matrixwith 25% drug load over extended period of time.In conclusion: Cross-linked chitosan implantable device forseptic wounds or post surgical treatment with antimicrobialcapability and wound healing properties was developed to serve asa site-specific delivery system for antibiotics.
https://bpsa.journals.ekb.eg/article_63328_1fa4bb358d038dace23e759fd153e818.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
23
43
10.21608/bfsa.2009.63340
63340
Original Article
MACRO- AND MICROMORPHOLOGY OF GRINDELIA CAMPORUM VAR. CAMPORUM GREENE. FAMILY ASTERACEAE, CULTIVATED IN EGYPT: LEAF, STEM AND ROOT
A. El-Moghazy
1
F. Darwish
2
E. El-Khayat
3
M. Mohamed
4
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
The detailed macro-and micromorphological characters of thestems, leaves and roots of Grindelia camporum varity camporumGreene (syn. Grindelia Robusta) were studied with the aim to findout the diagnostic elements of these organs, which facilitate theiridentification in both entire and powdered forms.
https://bpsa.journals.ekb.eg/article_63340_76f939d51d7d0a7be6e344f961d44f07.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
45
64
10.21608/bfsa.2009.63344
63344
Original Article
FORMULATION AND EVALUATION OF A BUCCOADHESIVE CAPTOPRIL TABLETS
Mohammed El-Shabouri
1
Hamdy Abd El-Aleem
2
Osama Soliman
3
Marwa El-Dahhan
4
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Buccoadhesive tablets of captopril were prepared by directcompression of the drug with different polymers; Carbopol 934 (CP934), Eudragit RS 100 (EU RS 100), Chitosan (Ch), Hydroxpropylmethylcellulose (HPMC) and Polyvinylpyrrolidone K30 (PVP K30)either singly or in blends of different ratios. The tablets wereevaluated for their weight variation, drug content uniformity,friability, hardness, swelling index, surface pH, in-vitrobioadhesive strength and release characteristics. Thebioavailability and the pharmacokinetics parameters of captoprilfrom two selected formulations (CP 934:HPMC 6:4 and Ch:HPMC6:4) were evaluated.The in-vitro bioadhesive strength and release characteristicswere found to be a function of the type of polymer and ratio ofpolymer blends. Swelling and bioadhesive characteristics weredetermined for both plain and medicated tablets. The highconcentration of carbopol and chitosan containing formulationsshowed the greatest adhesive strength. The mean pharmacokineticparameters of captopril after buccoadhesive tablet administrationwere: Cmax 506.9 ng/ml, Tmax 4 hr, AUC0-8 2359.5 ng.hr/ml for CP934: HPMC (6:4), while Cmax 429.02 ng/ml, Tmax 2.67 hr, AUC0-81637.43 ng.hr/ml for Chitosan: HPMC (6:4). In comparison, incase of oral administration of control tablet the Cmax 591.28 ng/ml,Tmax 1.5 hr, AUC0-8 1869.29 ng.hr/ml.
https://bpsa.journals.ekb.eg/article_63344_e3816339d90277a2b580d011aea7a868.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
65
84
10.21608/bfsa.2009.63346
63346
Original Article
PREPARATION AND EVALUATION OF THEOPHYLLINE LOADED BOVINE SERUM ALBUMIN MICROSPHERES
K. Saleh
1
M. Ibrahim
2
T. Faris
3
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al- Azhar University at Assiut, Assiut, Egypt
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al- Azhar University at Assiut, Assiut, Egypt
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al- Azhar University at Assiut, Assiut, Egypt
Theophylline-loaded bovine serum albumin (BSA) microsphereswere prepared by an emulsion polymerization method usingglutaraldehyde as the crosslinking agent. The study was designedto evaluate the effects of different formulation parameters as BSAconcentration, surfactant concentration, hydrophilic lipophilicbalance (HLB), dispersion medium viscosity and glutaraldehydeconcentration on the extent of drug loading, size of microsphereand the in-vitro as well as the in-vivo release rates of theophyllinefrom such microspheres. Drug polymer ratios of 1:1, 1:2, 1:3, 1:4, 1:5 and 1:6 were investigated. Span 80 was used as a surfactant atdifferent concentrations. Moreover, Different span 80 / tween 80blend concentrations; 0.5, 1.0 and 2.0% w/v were used to study theeffect of HLB. Also different dispersion media; isooctane, lightparaffin oil, olive oil and Linseed oil were used for microspherespreparation. In addition, different glutaraldehyde concentrations;5, 10 and 25% v/v were used. It was found that all micro-sphereswere spherical with the mean particle size of 90-180 μm. Theresults revealed also that: as the concentration of BSA increases,the drug loading is increased. Increasing surfactant concentrationand viscosity of the dispersion medium has led to decrease theparticle size, while increasing glutaraldehyde concentration nearlyhad no effect. Furthermore, encapsulation efficiency was found tobe directly proprortional to albumin content, surfactantconcentration, viscosity of the dispersion medium andglutaraldehyde concentration. Drug release from the preparedmicrospheres displayed a biphasic pattern characterized by aninitial burst, followed by a slower release period, which may beattributed to the presence of theophylline material near to or ontothe microspheres surfaces. The bioavailability of theophylline fromthe prepared microspheres was evaluated in rabbits. The preparedmicrospheres were found to control theophylline release even up to10 hrs. The peak serum concentrations of such microspheres werewithin the therapeutic level. The results indicate also that theprevioiusly mentioned formulation parameters have a prnouncedimpact to control the release of the entrapped drug.
https://bpsa.journals.ekb.eg/article_63346_5b4115f03d0b339484661ee8de148c71.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
85
109
10.21608/bfsa.2009.63348
63348
Original Article
MACRO- AND MICROMORPHOLOGICAL STUDY OF THE LEAF, STEM AND INFLORESCENCE OF ERANTHEMUM NERVOSUM T. ANDERS (FAM. ACANTHACEAE), CULTIVATED IN EGYPT
Mahmoud Assaf
1
Yaser Gouda
2
Ehab El-Khayat
3
Reda Abd El-Hamid
4
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
Many ornamental plants belonging to the family Acanthaceae,showed interesting medicinal activities in treating: cough, chronicbronchitis, rheumatism, jaundice, ear troubles and fever. Inaddition to treatment of some skin diseases. In the present work, thedetailed macro- and micromorphological characters of the leaf,stem and inflorescence of Eranthemum nervosum T. Anders familyAcanthaceae, were studied with the aim to find out the diagnosticelements of these organs, which facilitate their identification inboth entire and powdered forms.
https://bpsa.journals.ekb.eg/article_63348_5a5381e663da15ad60d7013f97097c86.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
125
140
10.21608/bfsa.2009.63350
63350
Original Article
SYNTHESIS OF NEW 1,2,4-TRIAZOLE DERIVATIVES OF NALIDIXIC ACID AS POTENTIAL ANTIBACTERIAL AND ANTIFUNGAL AGENTS
Samia Abdelmoty
1
Helal Heta
2
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt,
Department of Microbiology and Immunology, Faculty of Medicine, Assiut University, Assiut 71526, Egypt
Triazole and triazole fused heterocyclic ring systems possessdiverse applications in the fields of medicine, agriculture andindustry. A new series of nalidixic acid derivatives having 1,2,4-triazole moiety at position 3 were synthesised to achieve enhancedbiological activity and wide spectrum of activity. Nalidixic acid wasfirst converted into its methyl ester which upon hydrazinolysisafforded nalidixic acid hydrazide. Condensation of the hydrazidewith CS2/KOH furnished the potassium dithiocarbazate salt, whichcyclized to the 3-[4-amino-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl]-1-ethyl-7-methyl-1H-[1,8]naphthyridin-4-one, (4), on refluxing with hydrazine hydrate. Condensation of the keyintermediate 4 with aryl aldehydes afforded Schiff's bases 5a-f,while its reaction with alkyl or aralkyl halides gave compounds6a-e. Furthermore, compounds 5a,e were reacted with benzylchloride to afford 7a,b. The chemical structure of the targetcompounds was confirmed by IR, 1H-NMR, FAB-MS, EI-MSspectra and elemental analyses. The title compounds and thestarting Nalidixic acid; were tested for their in-vitro antibacterialand antifungal activities. Most of the tested compounds showedcomparable antibacterial activity with those of Nalidixic acid andhigher activity than ampicillin. The tested compounds and Nalidixicacid showed non or moderate antifungal activity in comparison toclotrimazole as a reference drug.
https://bpsa.journals.ekb.eg/article_63350_0f057c0cde565ee594374ec7fd5c8090.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
141
152
10.21608/bfsa.2009.63352
63352
Original Article
ENHANCEMENT OF DISSOLUTION AND ANALGESIC ACTIVITY OF CELECOXIB USING TERNARY SYSTEM
Mohamed Amin
1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al- Azhar University, Assiut, Egypt
The purpose of the present study is to investigate the drugloaded solid dispersion system consisting of a drug, a carrier and asurfactant. Solid dispersions of a water insoluble drug celecoxib(CX) with PVP 40000, namely binary solid dispersion systems, wasprepared at different ratios of drug to carrier [(1:1), (1:3), and(1:5)]. Polysorbate 80, a nonionic surfactant, was incorporatedinto the binary solid dispersion systems as a third component toobtain the ternary solid dispersion system. The solubilizing andabsorption enhancement properties of ternary solid dispersionsystem have been investigated. The prepared solid dispersionsystems (binary or ternary), at various drug- polymer ratios bymixing or co-precipitation, were characterized by differentialscanning calorimetery and X- ray diffractometry. The results show a remarkably improved dissolution of the drug from the ternarysolid dispersion systems when compared to the binary soliddispersion systems. The therapeutic activity of the ternary systemwas evaluated using acetic acid- induced writhing method. In-vivoexperiments in mice demonstrated that the investigated ternarysystem (drug, polymer and surfactant) shows a greater reduction ofacetic acid- induced writhing in comparison with pure drug.Moreover, the ternary system of (CX) demonstrated antiwrithingpotency 1.45 times higher than the respective binary system. Thus,the solubilizing power, the dissolution effect, and the analgesiceffect were enhanced upon the addition of the investigatedsurfactant to the binary system of celecoxib and the polymer.
https://bpsa.journals.ekb.eg/article_63352_f3e5528795b8cd46572cd94a67a04e78.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
153
187
10.21608/bfsa.2009.63355
63355
Original Article
SYNTHESIS, ANTI-BRONCHOCONSTRICTIVE, AND ANTIBACTERIAL ACTIVITIES OF SOME NEW 8- SUBSTITUTED-1,3-DIMETHYLXANTHINE DERIVATIVES
Walid Elgaher
1
Alaa Hayallah
2
Ola Salem
3
Abdel Alim Abdel Alim
4
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
Methylxanthines especially theophylline have been recognizedas potent bronchodilators for the relief of acute asthma for over 50years. Recently, it was found that bacterial infection has a role inasthma pathogenesis. Accordingly, the present work involves thesynthesis of different series of 8-substituted (aryl, aralkyl,cycloalkyl, and heteroaryl)-1,3-dimethylxanthines. The chemicalstructures of these compounds were elucidated by IR, 1H NMR, 13CNMR, elemental analyses, and high resolution EI-MS or FAB-MSfor some compounds. The bronchodilator activity was evaluatedusing acetylcholine induced bronchospasm in guinea pigs, and most of the compounds showed significant anti-bronchoconstrictiveactivity in comparison with aminophylline as a standard. Also, theantibacterial activity of all the target compounds was investigatedin-vitro against Gram-positive and Gram-negative bacteria usingampicillin as a reference drug. Results showed that some of thetested compounds have potent antibacterial activity. Apharmacophore model was computed to get useful insight on theessential structural features of bronchodilator activity.
https://bpsa.journals.ekb.eg/article_63355_3b53775ff5265bf5e7ffa4acee9a40df.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
189
197
10.21608/bfsa.2009.63356
63356
Original Article
CHEMICAL AND BIOLOGICAL INVESTIGATIONS OF THE ROOTS OF SONCHUS OLERACEUS L. GROWING IN EGYPT
Ehab Elkhayat
1
Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut branch, Assiut 71524, Egypt
Phytochemical study of the roots of Sonchus oleraceus L.(Astraceae) growing in Egypt, afforded loliolide 1 for the first timefrom the genus Sonchus in addition to 15-O-β-glucopyranosyl-11β,13-dihydrourospermal A 2, ursolic acid 3, lupeol 4, and β-sitosterol-3-O-β-glucopyranoside 5 for the first time from thespecies. The biological evaluation of the isolated compoundsshowed cytotoxic activity of 1 and 2 against L5187Y cell line, whilecompound 2 showed activity against PC33 cell line. In addition toantibacterial activity of compounds 1 and 2 against S. aureus, B.subtilis, E. Coli, and N. gonorrhoea. The structures of the isolatedcompounds were elucidated using 1D (1H and 13C), 2D (H-HCOSY, HMQC and HMBC) NMR and MS spectroscopic data.
https://bpsa.journals.ekb.eg/article_63356_cfe620d14f14ddec30eb9c243006e597.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
199
212
10.21608/bfsa.2009.63358
63358
Original Article
PREPARATION AND IN-VITRO EVALUATION OF SUSTAINED RELEASE THEOPHYLLINE MICROSPHERES
W. Sakran
1
Department of Pharmaceutics, Faculty of Pharmacy, October 6 University, Giza, Egypt
A modified emulsion-solvent evaporation technique was utilizedto prepare sustained release microspheres containing theophylline(TH). Two polymers were used for microspheres preparation,namely cellulose propionate (CP) and ethyl cellulose (EC). The twopolymers were used at 1:1, 2:1, and 3:2 (drug - polymer ratios). The prepared microspheres were evaluated for their total recovery,drug loading, particle size distribution, surface morphology, drugcontent and drug release rate characteristics. The results haveshown that, the total percentages drug recovery reached 96,97.7and 90.3 for cellulose propionate at 1:1, 2:1 and 3:2 (drug -polymer ratios), and that of drug loading reached 89, 90, and 92respectively. However, with ethyl cellulose, the total % drugrecovery reached 99, 100, and 94 using the same drug – polymerratios, and the total % drug loading reached, 85, 90, and 90respectively. The results obtained have shown a significantcomplete recovery with an excellent drug loading and thus theefficiency of the procedure utilized to encapsulate the drug. Thedrug release characteristics from the prepared microspheres insimulated gastric fluid (pH 1.2) and phosphate buffer (pH 6.8) werecompared with commercial sustained release capsules oftheophylline (Theo SR 100). Results have revealed that, the releaserate of theophylline was influenced by the type of polymer,microsphere size, pH as well as drug to polymer ratio. Thedecrease in particle size of the prepared microspheres led toincrease in the release rate. However, the prepared microspheresshowed more retarded release of theophylline than from the testedcommercial product. Moreover, ethyl cellulose as a polymer wasmore effective for sustained effect. The release data were fitted toPeppas diffusion equation. Results have indicated that the releasepattern of theophylline followed zero-order kinetics.
https://bpsa.journals.ekb.eg/article_63358_2290311403c771a28caed7f8d118f5ff.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
213
224
10.21608/bfsa.2009.63359
63359
Original Article
PREPARATION, IN-VITRO RELEASE AND ANTIINFLAMMATORY ACTIVITY OF MELOXICAM IN DIFFERENT GEL FORMULATIONS
Mahmoud El-Badry
elbadry@aun.edu.eg
1
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University 71526, Assiut, Egypt
This study was designed to evaluate different polymers to theirsuitability for formulation as vehicles for topical delivery system.Meloxicam (MX) was incorporated into the gel vehicles in aconcentration of 1.0% w/w. It is a non-steroidal anti-inflammatorydrug (NSAID) of the enolic acid class of compounds.Polymers used in this study are methylcellulose (MC), tylose(Ty), polyvinyl alcohol (PVA), poloxamer 407 (polo), polyethylene glycol (PEG), carbopol 974P (Carb. and eudispert mv. (Eud). Theyare used in a suitable concentration for gel formation.In-vitro release characteristics of the drug from different gelswere carried out using dialysis membrane in phosphate buffer pH6.8. The release data were treated with various kinetic principles toassess the relevant parameters.The general rank order of MX release was MC > Ty > polo >PVA > other gel forms. The results also showed that, the release ofdrug from the prepared gels obeyed the diffusion model (Higuchi’sequation).The influence of some formulation and processing variables(initial drug concentration of 0.5, 1.0 and 2.0% w/w, poloxamer407 concentration of 20, 25, 30% w/v in the aqueous gelformulation) on the release patterns have been studied. The resultsrevealed an inverse correlation between the drug release rate andthe poloxamer 407 concentration and direct correlation betweenthe drug release rate and the initial drug concentration.The anti-inflammatory activity of the drug in different gelformulations was studied using carrageenan induced rat pawedema method. The results obtained show an excellent antiinflammatoryactivity on rat paw edema.
https://bpsa.journals.ekb.eg/article_63359_644f2a4752668459d12cb8b02b02daa6.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2009-06-30
32
1
225
240
10.21608/bfsa.2009.63361
63361
Original Article
DESIGN, SYNTHESIS AND MOLECULAR MODELING STUDY OF 1,2,4-TRIAZOLE CARBOHYDRAZIDE DERIVATIVES WITH POTENTIAL ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITIES
Nawal El-Koussi
1
Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, 71526, Egypt
The present investigation is concerned with the synthesis of1,2,4-triazole carbohydrazide derivatives (6a-l) with the objectiveof discovering novel and potent antimicrobial and antiinflammatoryagents.The chemical structures of the target compounds wereelucidated by elemental analyses, IR, 1H-NMR, 13C-NMR and massspectral data. The antimicrobial activity of the target compoundswere evaluated and compared with ampicillin trihydrate andclotrimazole as references compounds. The results showed that compound 6i revealed a similiar level of activity as ampicillinagainst Staphylococcus aureus, while compounds 6j and 6lexhibited comparable activity against Escherichia coli. Allcompounds were less active against Candida albicans whencompared with clotrimazole. The results of anti-inflammatoryshowed that compounds 6d, 6l possessed higher anti-inflammatoryactivity than celecoxib in carageenan-induced rat paw edema testwith low gastric ulcerogenicity compared with indomethacin.Molecular modeling studies were performed in order to rationalizethe obtained biological results.
https://bpsa.journals.ekb.eg/article_63361_399dcdfb737625ce9c2d4b1f77c66474.pdf