ENHANCEMENT OF DISSOLUTION AND THE ANTIINFLAMMATORY EFFECT OF NIMESULIDE, USING LIQUISOLID COMPACT FOR ORAL APPLICATION
M.
Hassan
Department of Pharmaceutics, Faculty of Pharmacy, King Saud University
author
H.
El-Saghir
Department of Pharmaceutics, Faculty of Pharmacy, King Saud University
author
text
article
2011
eng
Nimesulide is a poorly soluble drug, the rate of its oral absorption is often controlled bythe dissolution rate in the gastrointestinal tract. There are several techniques to enhance thedissolution of poorly soluble drugs. Among them the technique of liquisolid compacts which is apromising one. The liquisolid compacts were prepared using 20 mg nimesulide, Avicel PH102as a carrier, and Aerosil 200 as a coating material in a ratio of 20:1, as well as AC-DI-SOL asa disintegrant in a concentration of 5% from the total weight of the compact. The liquids usedinclude PEG400, PG, and a mixture of these solvents with Tween 80. From the results obtainedit is concluded that the suitable loading factor (Lf) is 0.2 which gave good flowability andcompressibility. Friability, hardness, disintegration time and the dissolution rate were carriedout. All the liquisolid compacts showed higher dissolution rate than the conventional tablets.The liquisolid compacts containing the PEG400 showed the highest dissolution rate than theother preparations. The effect of different concentrations of drug on the dissolution rate wasstudied, and it was observed that 20% of drug gave the maximum dissolution rate, and nosignificant increase of the dissolution rate with increasing the drug concentration. Conventionaltablets and liquisolid compacts containing PG and PEG400 were tested for their antiinflammatoryeffects using paw oedema test. liquisolid compacts exhibited a pronouncedinhibition of swelling than that of conventional tablets. In conclusion liquisolid compact ofnimesulide can be used as a technique to improve the dissolution rate and the antiinflammatoryeffect of nimesulide.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
1
8
https://bpsa.journals.ekb.eg/article_63212_ce4313150a12b0f6380bd428df1671b7.pdf
dx.doi.org/10.21608/bfsa.2011.63212
PHYTOCHEMICAL AND BIOLOGICAL STUDY OF PETREA VOLUBILIS L. (VERBENACEAE)
M.
Abdelwahab
Department of Pharmacognosy, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt
author
A.
Abdel-Lateff
Department of Health Information Technology, Jeddah Community College, King Abdul-Aziz
University, 21589 Jeddah Saudi Arabia
author
M.
Fouad
Department of Pharmacognosy, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt
author
S.
Desoukey
Department of Pharmacognosy, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt
author
M.
Kamel
Department of Pharmacognosy, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt
author
text
article
2011
eng
Petrea volubilis L. was studied for its secondary metabolites and biological activities. Thephytochemical screening of dried aerial parts revealed the presence of different constituentssuch as unsaturated sterols, triterpens, and flavonoids. The biological activities of the totalextract and different fractions were evaluated in a series of bioassays (antioxidant, antiinflammatory,analgesic, antipyretic and antibacterial), the majority of them showed significantactivities in the applied test systems. Extensive purification of the ethyl acetate extract led toisolation of apigenin (1), quercetin (2), 4`, 6-dimethylscutellarien (3), hypogallic acid (3,4-dihydroxybenzoic acid) (4), trans-caffeic acid (5) vanillic acid (6) and acteoside (7). Thestructure elucidation of 1-7, was carried out by 1H-NMR, UV and MS analyses.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
9
20
https://bpsa.journals.ekb.eg/article_63213_870f9af2308d9dd692494958b0a017b9.pdf
dx.doi.org/10.21608/bfsa.2011.63213
MUCOADHESIVE BUCCAL PATCHES OF LORNOXICAM: II– IN-VIVO EVALUATION AND CLINICAL EFFICACY
Fawzia
Habib
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
Salah
Shaltout
Department of Surgery, Faculty of Medicine, Assiut University, Assiut, Egypt
author
Maha
Azeem
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
Gihan
Fetih
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
Mohamed
Safwat
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
text
article
2011
eng
Lornoxicam is a NSAID of the oxicam class and it has the same side effects of this groupwhen taken orally. In attempts to avoid the systemic side effects of lornoxicam (e.g. gastricirritation) and to achieve sustained release of the drug, several buccal patch formulationscontaining lornoxicam were prepared using different polymers and were evaluated for in-vitrocharacteristics in part I of this study. In the current study, the selected formulations (based onthe previous in-vitro data) are evaluated for in-vivo performance using experimental animalsand clinical efficacy on human volunteers. Pharmacokinetic parameters were assessedfollowing application of the selected patches in rabbits. A comparative clinical study wasconducted on patients with post-operative pain and edema following maxillofacial operations.The results of the in-vivo animal experiment showed that lornoxicam formulated in differentbuccal patches was successfully delivered to the systemic circulation and showed high absolutebioavailability of lornoxicam. The clinical study results revealed that sodium carboxy methylcellulose (NaCMC, 3%) formulation applied to the buccal mucosa was slightly better or equallyeffective to the orally administered commercial oxicam product (Feldene Flash® tablets) inreducing pain level, swelling and tenderness within a period of 4 days with no observed sideeffects. These findings suggest that lornoxicam administered in this buccal patch may present apotential therapeutic use as a strong anti-inflammatory and analgesic agent.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
21
30
https://bpsa.journals.ekb.eg/article_63214_a5d0d074937a26318ae161db0e274b73.pdf
dx.doi.org/10.21608/bfsa.2011.63214
PHARMACY TOXICOLOGICAL ANALYSES FOR POISONED PATIENTS AT A TEACHING HOSPITAL IN SAUDI ARABIA
Abdlatif
Ali Aldhawailie
Department of Clinical Pharmacy, College of Pharmacy, King Saud University, Riyadh 11451,
Saudi Arabia
author
text
article
2011
eng
The pharmacist and pharmacy services roles in hospital setting were well recognized forthe management of poisoned patients. Pharmacist consultation through pharmacy drug andpoison information centre was very beneficial to the treating physician at accident andemergency department (AE). The inclusion of the drug toxicological analyses unit withinpharmacy department services gave the chance to utilized the pharmacological background forpracticing pharmacists for better handling of poisoning cases. The advantage(s) of pharmacysupervision of drug toxicological analyses unit and the role of pharmacist within such unit inteaching hospital will be determined.In this study, a survey of 1160 poisoned cases arrived to (AE) department during sixmonths period. Body fluids samples were taken for 228 poisoned cases for analysis by utilizingthe pharmacy toxicological analyses unit.The findings of the study represented the positive impact of pharmacy supervision of drugtoxicological analyses unit beside the drug and poison information centre in the management ofpoisoned cases. The time and efforts of AE physicians were saved and appreciated by theintegrated pharmacy services especially for poisoned patients attending AE in teachinghospital.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
31
35
https://bpsa.journals.ekb.eg/article_63215_f8a3c169dd1a003ad2e5556ae7ef1d5c.pdf
dx.doi.org/10.21608/bfsa.2011.63215
SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NEW SUBSTITUTED DIHYDROPYRIMIDINE DERIVATIVES
Mostafa
Hussein
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University,
Egypt
author
Samia
Abdel Moty
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University,
Egypt
author
Salah
Abdel Aziz
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Al Azhar
University, Assiut, Egypt
author
Mahrous
Abou- Salim
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al Azhar
University, Assiut, Egypt
author
text
article
2011
eng
A new series of ethyl 6-methyl-4-(substituted)phenyl-2-(substituted)-phenacyl-thio-1,4-dihydropyrimidine-5-carboxylate (2a-x) was prepared by reaction of ethyl 1,2,3,4-tetrahydro-6-methyl-4-(substituted)phenyl-2-thioxopyrimidine-5-carboxy-late 1(a–d) with phenacylbromides. Compounds 1(a–d) were synthesized using the principle of Bignelli condensation byone pot reaction of the appropriate araldehyde, ethyl acetoacetate and thiourea in acidicmedium. Confirmation of the chemical structure of the synthesized compounds (2a-x) wassubstintiated by different spectral data IR, 1H-NMR, MS in addition to their microanalyses. Thenewly synthesized compounds were evaluated for their antimicrobial activities. Theantibacterial and antifungal testing identified compounds 2b, 2e, 2k, 2l, 2m, 2n, 2o, 2p, 2q, 2rand 2x as the most effective agents in comparison to Chloramphenicol and Clotrimazole asreference antibacterial and antifungal drugs respectively.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
37
52
https://bpsa.journals.ekb.eg/article_63216_a32fe9180e1402195d2ff331ec0dd1be.pdf
dx.doi.org/10.21608/bfsa.2012.63216
MACRO- AND MICROMORPHOLOGY OF THE LEAF, STEM, STEM BARK AND FLOWER OF VANGUERIA EDULIS CULTIVATED IN EGYPT
D.
Bishay
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
E.
Backheet
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
Y.
Gouda
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
S.
Moustafa
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
text
article
2011
eng
Vangueria edulis belongs to Rubiaceae which includes about 620 genera with almost13000 species which is widely distributed but mainly tropical. Biological studies showed thatsome species of the genus Vangueria showed antimicrobial activity, reported to haveanthelmintic action and antiplasmodial activity and fed to cattle suffering from East CoastFever. No detailed information could be traced concerning the macro- and micromorphology ofthe plant. This provoked the authors to carry out this study to identify the drug in both entireand powdered forms.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
53
76
https://bpsa.journals.ekb.eg/article_63217_1b52a5beab1c3ac77a40657562f8e330.pdf
dx.doi.org/10.21608/bfsa.2011.63217
SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME BENZIMIDAZO-1,2,4-TRIAZOLE DERIVATIVES AS ANTIMICROBIAL AND ANTI-INFLAMMATORY AGENTS
Anber
Mohammed
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University,
Assiut-71526, Egypt
author
Mostafa
Hussein
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University,
Assiut-71526, Egypt
author
Samia
Abdel-Moty
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University,
Assiut-71526, Egypt
author
Abdel- Alim
Abdel-Alim
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University,
Assiut-71526, Egypt
author
text
article
2011
eng
Three new series of N`-(aryl or heteroarylmethylidene)-2-(1H-1,2,4-triazolo[2,3-a]benzimidazol-2-ylsulfanyl) acetohydrazides (4a-k), N`-(α-arylethylidene)-2-(1H-1,2,4-triazolo[2,3-a]benzimidazol-2-ylsulfanyl) acetohydrazides (5a-d), and 2-({[5-(alkyl oraralkylsulfanyl)-1,3,4-oxadiazol-2-yl]methyl}sulfanyl)-1H-1,2,4-triazolo[2,3-a]benzimidazoles(7a-e) were synthesized. Reaction of compound (1) with methyl bromoacetate afforded (2),which when refluxed with hydrazine hydrate yielded (3). The latter was condensed witharomatic aldehydes and substituted acetophenones to afford compounds (4a-k) and (5a-d)respectively. Treatment of compound (3) with carbon disulfide in the presence of potassiumhydroxide resulted in the formation of (6). The latter was alkylated with the appropriate alkyl oraralkyl halides to afford compounds (7a-e). The purity of all new compounds was checked byTLC and elucidation of their structures was confirmed by IR, 1HNMR, and mass spectrometryalong with elemental microanalyses. All the target compounds were evaluated for their in-vitroantimicrobial and in-vivo anti-inflammatory activities in comparison with ampicillin,fluconazole, and indomethacin as reference drugs respectively. In addition to moleculardocking of compound 5c was performed.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
34
v.
1
no.
2011
77
92
https://bpsa.journals.ekb.eg/article_63218_164b51ebc72e7c82594aca83a70f3112.pdf
dx.doi.org/10.21608/bfsa.2011.63218