eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
21
25
10.21608/bfsa.1999.65968
65968
Original Article
Biologically active abietane diterpenes from Taxodium distichum seeds
Amany Ahmed,
1
Nasr Ei-Emary
2
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Four diterpenes, taxodone, taxodione, 11-hydroxymontbretol, and ferruginol, were isolated from Taxodium distichum (L.) Rich seeds. Taxodone and taxodione were isolated before from the same source and have been reported to possess antitumor activity. 11-Hydroxymontbretol and ferruginol were isolated for the first time here from the genus Taxodium. The structures of the isolated compds. was detd. through intensive spectral anal. HIV-1 PR inhibitory activity for the four compds. showed that only taxodione had a potent effect in 0.1 mM concn.
https://bpsa.journals.ekb.eg/article_65968_3d338f26d62be46b20055ded99921c88.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
27
34
10.21608/bfsa.1999.65969
65969
Original Article
A study on the powder, tableting and stability characteristics of Cellactose and other selected direct compression excipients
Sayed Khidr
1
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Egypt
The powder characteristics of the direct compression excipients Cellactose, Tablettose, spray dried lactose (SDL) and Avicel PH101 were compared. These excipients and a mixt. of Avicel:SDL (1:3) were used for the prepn. of glibenclamide tablets. The tablet characteristics, including the phys. properties, av. drug content, as well as the dissoln. rate were evaluated before and after the tablets were subjected to storage under two accelerated conditions: 40°C/30% relative humidity (RH) for 16 wk and 40°C/80% RH for 12 wk. The results showed that SDL has the best flow properties followed by Tablettose, Cellactose and Avicel. With regard to tablet characteristics, Tablettose produced tablets with the least wt. variations before and after storage at both low and high relative humidity, while a mixt. of Avicel:SDL (1:3) produced tablets that gave the highest values. Cellactose was the best vehicle in preserving the tablet size and glibenclamide content during storage. On the other hand, the least changes obsd. in the dissoln. profiles of glibenclamide tablets due to storage was found for tablets made of Avicel followed by these of Cellactose and a mixt. of Avicel:SDL (1:3).
https://bpsa.journals.ekb.eg/article_65969_23cf0d8ef5f25fcaece5fced480be504.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
35
45
10.21608/bfsa.1999.65970
65970
Original Article
Synthesis of certain nitropyridine derivatives bearing 2-thiazolyl hydrazines with expected monoamine oxidase inhibitory activity
Hoda Hassan
1
Department of Pharmaceutical, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
Two series of nitropyridine derivs. bearing 2-thiazolyl hydrazines were synthesized and evaluated for their monoamine oxidase (MAO) inhibitory activity by in vitro tests to assay their effect on rat liver mitochondria by a kynuramine fluorimetric assay. The two key intermediates, 6-methyl-5-nitropyridine-2-carboxaldehyde thiosemicarbazone (I) and 1-(6-methyl-5-nitropicolinoyl)thiosemicarbazide (II), were prepd. by conventional methods. The target compds., N-(6-methyl-5-nitropyridin-2-ylmethylidene)-N'-(4-substituted thiazol-2-yl)hydrazines III (R = Me, Ph, 4-BrC6H4, 4-ClC6H4, 4-MeOC6H4, 4-O2NC6H4, X = CH:NNH) and 6-methyl-5-nitropyridine-2-carboxylic acid N'-(4-substituted thiazol-2-yl)hydrazides III (R = Me, Ph, 4-BrC6H4, 4-ClC6H4, 4-MeOC6H4, X = CONHNH), were prepd. by condensation of I or II with the appropriate α-halogeno-ketone, chloroacetone or phenacyl bromides. All the assayed compd. posses in vitro monoamine oxidase inhibitory activity at a concn. of 0.33 - 1.66 x 105 M.
https://bpsa.journals.ekb.eg/article_65970_9412c423bd5b52e655323e375cf0d0f9.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
47
53
10.21608/bfsa.1999.66076
66076
Original Article
Quinovic acid glycosides from Zygophyllum aegyptium
Mahmoud Mohamed
1
Department of Pharmacognosy, Faculty of Pharmacy, Al-azhar University; Assiui 71524, Egypt
Seven known quinovic acid glycosides were isolated for the first time from the n-BuOH fraction of the 70% ethanol ext. of Zygophyllum aegyptium A. Hosny sp. nov. These compds. were identified as: quinovic acid 3β-O-β-D-quinovopyranoside, quinovic acid 3β-O-β-D-glucopyranoside, 3-O-[α-L-arabinosyl-(1→2)-β-D-quinovopyranosyl]quinovic acid , 3-β-O-β-D-quinovopyranosylquinovic acid-28-O-β-D-glucopyranosyl ester, 3-β-O-[β-D-2-O-sulfonyl quinovopyranosyl]-quinovic acid-28-O-β-D-glucopyranosyl ester (zygophyloside F), 3-β-O-β-D-glucopyranosylquinovic acid 28-O-β-D-glucopyranosyl ester , 3β-O-[β-D-2-O-sulfonyl glucopyranosyl]-quinovic acid-28-O-[β-D-glucopyranosyl] ester (zygophyloside G), in addn. to, β-sitosterol glucoside. The structure elucidation of these compds. was detd. by phys., chem. and spectroscopic methods.
https://bpsa.journals.ekb.eg/article_66076_53a917858ecd30ad4caa2bdfb1ef0c41.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
55
66
10.21608/bfsa.1999.66077
66077
Original Article
QUINIDINE-CYCLODEXTRINS INCLUSION COMPLEXES
I. El-Gibaly
1
M. Fathy
2
M. Mohamed
3
S. Ahmed
4
Department of Pharmaceutics
Department of Pharmaceutics
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiu, University, Assiut, Egypt
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiu,University, Assiut, Egypt
The complexation behavior of quinidine with four cyclodextrins (CDs), namely β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), methyl-β-cyclodextrin (M-β-CD) and α-cyclodextrin (α-CD) was investigated for the purpose of improving the low aq. soly., stability and side effects of the drug. The aq. soly. of quinidine was increased as a function of CD concn. generating linear AL phase soly. profiles. The interaction was quantified for quinidine-CDs by detn. of the stability const. using the soly. method at various temps. and the thermodn. parameters were calcd. The results revealed a very strong evidence for mol. interaction between the drug and HP-β-CD or M-β-CD, suggesting the formation of an equimolar complex. The estd. enthalpies and entropies for the interaction of quinidine with CDs indicate that the interaction is exothermic. The prepd. coevaporates were studied by x-ray diffractometry, differential scanning calorimetry and IR spectroscopy, in order to investigate the possibility of complexation of the drug with CDs. The relative potency of the CDs to enhance the dissoln. rate of quinidine was in the following order: M-β-CD ≥ HP-β-CD > α-CD > β-CD, which, generally fits the magnitude of the stability const. data of the complexes. The dissoln. profiles of the drug, phys. mixts. of the drug with CDs, as well as, the prepd. complex show higher dissoln. rate of the complex compared with the drug alone or its phys. mixts.
https://bpsa.journals.ekb.eg/article_66077_9946cd8c238efc307c6a17080823115a.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
67
72
10.21608/bfsa.1999.66080
66080
Original Article
Triterpenes and flavonoids from Fagonia mollis Del var. Grandiflora
Ahmed Attia
1
Samia Youssef
2
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
The aerial parts of the Fagonia mollis var. grandiflora afforded lupeol, lupeol acetate, lupeol palmitate, and unidentified triterpene together with four flavonoids kampferol, herbacetin-8-Me ether, isorhamnetin and quercetin. Triterpenes were identified by 1H-NMR, 13C-NMR and mass spectral anal. and flavonoids by U.V., 1H-NMR and mass spectral anal.
https://bpsa.journals.ekb.eg/article_66080_9ce775a9bce1705c9a539e8837a51227.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
73
80
10.21608/bfsa.1999.66082
66082
Original Article
Preparation and evaluation of sulindac alginate beads
A. Abd-Elrnageed
1
Department of Pharmaceutics Faculty of Pharmacy, Assiu, University, Assiut, Egypt
Sulindac (SUL) is one of the potent nonsteroidal anti-inflammatory drugs (NSAIDS) which has deleterious side effects on the gastrointestinal tract (GIT) such as irritation, ulceration and hemorrhage. Calcium alginate beads loaded with sulindac were prepd. at 2:1 and 4:1 polymer to drug ratio. The effect of polymer to drug ratio and the pH of the dissoln. medium (5.5 and 7.4) on the release profile of sulindac was investigated. In all cases, the release rate mechanism followed Higuchi model with sustained release of sulindac from alginate beads. The Higuchi model mechanism was confirmed by the linearization of the data when spherical matrix model was adopted. As the polymer to drug ratio increased the amt. of drug released progressively decreased. Also the release rate was significantly slower in the acidic side (pH 5.5) than that of pH 7.4. The effect of the intact drug as well as sulindac alginate beads on the ulcerogenic activity of the drug in the stomach of rabbit was carried out. The ulcerogenic activity of the intact drug disappeared and the mucosal surface was free of hemorrhage and inflammation when the drug is loaded with alginate beads.
https://bpsa.journals.ekb.eg/article_66082_fb7b1f2f585b913a9fd99be567eba1ed.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
81
89
10.21608/bfsa.1999.66084
66084
Original Article
Utility of certain π-acceptors for spectrophotometric determination of fluoxetine hydrochloride
Hesham Salem
1
Mohamed Radwan
2
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar •University, Assitu, 71524, Egypt
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar •University, Assitu, 71524, Egypt
Fluoxetine hydrochloride was detd. through charge transfer complexes (CTC) formation with three electron acceptor reagents. The methods involve the reaction of Fluoxetine as n-donor with either Chloranil (tetrachloro 1,4-benzoquinone), tetracyanoethylene (TCNE) or 7,7,8,8-tetracyanoquinodimethane (TCNQ) as n-acceptors, to give a stable and highly colored radical anion. The colored products were quantified spectrophotometrically. The condition ranges adhering to Beer's law are 0.05-3.00 mg/mL. The molar ratios of the reactants were ascertained. The different parameters were carefully studied and optimized. Statistical anal. of the results revealed equal precision and accuracy to the results of the Amax method. The methods were applied for detn. of Fluoxetine hydrochloride in pure form and in Prozac capsules.
https://bpsa.journals.ekb.eg/article_66084_4c39d3733106b4759719c7aa12618d08.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
91
95
10.21608/bfsa.1999.66085
66085
Original Article
The occurrence of polyisoprenoids in the leaves of Sterculia rupestris Benth
E. Desoky
1
D. Bishay
2
Department of Pharmacognosy, Faculty of Pharmacy, Assiut, University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut, University, Assiut, Egypt
Polyisoprenyl acetates with an av. no. of isoprene residues of 9-12 were isolated from the leaves of Sterculia rupestris Benth. (Sterculiaceae). Spectroscopic anal. revealed that all the polyisoprenyl acetates I (n = 4 - 7), were long-chain homologues with the following sequence of isoprene residues: ω-trans, two-trans, five to eight cis and cis-α-terminal.
https://bpsa.journals.ekb.eg/article_66085_128d43627f48fc37d9764f6e5661ff2b.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
97
108
10.21608/bfsa.1999.66086
66086
Original Article
Synthesis and chelating properties of substituted formyl pyridine thiosemicarbazones of potential biological activity
Hoda Hassan
1
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
The synthesis of a series of 4-(un)substituted thiosemicarbazones of 6-methyl-5-nitropyridine-2-carboxaldehyde, I (R = H, n-Bu, 4-ClC6H4, etc.), is reported by two different routes. The prepd. compds. were tested for their binding ability against Cu(II), Hg(II) and Zn(II). Four derivs. were tested for their complexing potentials in vivo. These compds. showed promising antidotal activities against Cu(II) relative to D-penicillamine. I (R = Ph) exhibited marked and significant increase in the mean threshold LD of CuSO4 in dose level (5 mg/kg) equal to the effect of D-penicillamine at dose level (30 mg/kg). The copper chelate and zinc chelate showed good activity against both Gram-pos. and Gram-neg. bacteria while the ligands showed activity against Gram-pos. bacteria only.
https://bpsa.journals.ekb.eg/article_66086_091ff3ccb59443874b35394457b444f7.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
109
115
10.21608/bfsa.1999.66087
66087
Original Article
Minor constituents from Maerua crassifolia Forssk growing in Egypt
Mahmoud Ramadan
1
Z. lbraheim
2
A. Abdel-Baky
3
D. Bishay
4
H. Itokawa
5
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiui, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiui, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiui, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiui, Egypt
Tokyo College of Pharmacy, Tokyo, Japan
Three minor components, viz, 6-N-methyl-9-β-D-glucoside adenine, 3,4,5,-trimethoxyphenol-1-O-β-D-glucopyranoside and Guaiacylglycerol were isolated and characterized by chem. and spectral anal. from Maerua crassifolia.
https://bpsa.journals.ekb.eg/article_66087_4b0e3a2e3b817ee44ab83354cbbe99cd.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
1999-06-30
22
1
1
20
10.21608/bfsa.1999.66089
66089
Original Article
COMPARATIVE MACRO-. AND MICROMORPHOWGY OF HIBISCUS CANNABINUS L. AND H. ROSA-SINENSIS L. PART II: THE FLOWER'
M. Afifi
1
M. Karawya
2
O. Salama
3
M. Ahmed
4
Department of Pharmacognosy, Faulty of Pharmacy, Mansoura University, Mansoura, Egypt
Department of Pharmacognosy, Faulty of Pharmacy, Mansoura University, Mansoura, Egypt
Department of Pharmacognosy, Faulty of Pharmacy, Mansoura University, Mansoura, Egypt
Department of Pharmacognosy, Faulty of Pharmacy, Mansoura University, Mansoura, Egypt
The macro- and micromorphological characters of the flowers of Hibiscus cannabinus L. and H. rosa-slnensls L. growing in Egypt are studied/or the sake of their identification in both entire and powdered forms.
https://bpsa.journals.ekb.eg/article_66089_4cafdcbb39cbf83de04cd4bed3fb530f.pdf