eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
1
6
10.21608/bfsa.2002.65503
65503
Original Article
Flavones and quaternary alkaloid from Tarchonanthus camphoratus L.
D. Bishay
1
A. Attia
2
M. Fayed
3
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Pharmacies Department, Assiut University Hospital. Assiut, Egypt
From Tarchonanthus camphoratus L., the authors isolated a new quaternary alkaloid tarchonanthine (I) and five flavones, viz. 5,7,4'-trihydroxy-6-methoxyflavone (hispedulin), apegenin, 5,3',4'-trihydroxy-6,7-dimethoxyfavone, 5,7,3',4'-tetrahydroxy-6-methoxyflavone (nepetin), and luteolin. The structure of these components was established through spectral studies. All of the flavones were reported for the first time from the genus Tarchonanthus.
https://bpsa.journals.ekb.eg/article_65503_d49afa6f308a7dab0f35697b681644a2.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
7
14
10.21608/bfsa.2002.65504
65504
Original Article
Enhancement of dissolution rate of meclozine HCl by co-grinding and loading onto certain adsorbents
A. Aboutaleb
1
A. Abdel-Rahman
2
M. Ahmed
3
U. Abu Uwaida
4
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Egypt
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Egypt
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Egypt
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Egypt
The aim of this work was to improve the soly. and dissoln. rate of, the sparingly water-sol. drug, meclozine hydrochloride (Mz). Two approaches were utilized namely, solvent deposition onto certain adsorbents and co grinding with these adsorbents. Phys. mixts. of Mz with the investigated adsorbents were also prepd. The used adsorbents were porous silica (Florite), veegum and bentonite. The mol. behavior of Mz in the investigated systems were studied using x-ray diffraction anal. and differential scanning calorimetry (DSC). The DSC results showed that the drug melting peak was reduced in intensity or disappeared totally in the obtained thermograms. This was noticed to be dependent on the adsorbent type as well as the wt. ratio of the drug to the adsorbent in the mixt. The obtained results indicated that Mz was transformed from the cryst. to the amorphous state in both the ground and the loaded mixts. with Florite. This transformation resulted in a significant enhancement in the dissoln. rate of the drug. In addn., it was noticed that the drug: adsorbent wt. ratio of the prepd. mixts. influenced the drug dissoln. rate enhancement. Accordingly, it can be concluded that by increasing the wt. ratio of the used adsorbent in the mixt., the larger the enhancement in the dissoln. rate of Mz was obtained
https://bpsa.journals.ekb.eg/article_65504_5a37bbfc47872874368d664af2540e4d.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
16
21
10.21608/bfsa.2002.65505
65505
Original Article
Flavonoid glycosides and hypotensive effect of Juglans nigra L. cultivated in Egypt
D. Bishay
1
A. Attia
2
S. Youssef
3
I. Khallaf
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, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
From a methanolic ext. of the leaves of Juglans nigra L. (black walnut; Juglandaceae), kaempferol-3-O-β-glucoside, quercetin-3-O-β-glucoside and quercetin-3-Oβ-glucuronide-6"-Et ester were isolated for the first time, along with stigmasterol-3-O-β-glucoside. Most of the structures were established on the basis of UV, MS and NMR (1H, 13C-NMR and DEPT) spectroscopic data. Moreover, hypotensive and toxicol. studies were done.
https://bpsa.journals.ekb.eg/article_65505_45003960ef9185133d1845a81af08446.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
23
30
10.21608/bfsa.2002.65506
65506
Original Article
Study of effect of various disintegrants on the physical properties and dissolution behavior of the directly compressed theophylline tablets
N. Aldouri
1
M. Ahmed
2
S. El-Jamal
3
Faculty of Pharmacy, Applied Science University, Amman, Jordan.
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Egypt
Faculty of Pharmacy, Applied Science University, Amman, Jordan.
The objective of this work was to study the efficiency of certain disintegrants in low levels on the phys. characteristics and dissoln. behavior of directly compressed tablets contg. theophylline as a model drug. A directly compressible formula based on Avicel PH 102/Emcompress 1:1 wt. ratio was used in the prepn. of theophylline tablets after being efficiently mixed together in a turbula mixer with or without the addn. of disintegrants. The used disintegrants namely were cross-linked CM-cellulose sodium (Ac-Di-Sol), sodium starch glycolate (Explotab), cross povidone (Polyplasdone XL10) and Starch 1500, in low concns. from 1 to 4 %wt./wt. The phys. properties and the dissoln. behavior of the directly compressed theophylline tablets were evaluated according to USP XXIII (1995) limits. All the formulations of theophylline tablets showed good mech. properties and complied with the std. requirements for uniformity of dosage units and friability. Directly compressed theophylline tablets without disintegrants (control) gave longer disintegration time which exceeds 30 min (outside the limits of USP), and slow dissoln. rate. While the batches of tablets contg. disintegrants exhibited rapid disintegration and faster dissoln. rate except those tablets contg. starch 1500. Mechanisms of the drug release were investigated from dissoln. data of theophylline tablets according to zero-order, first-order and the matrix-diffusion controlled kinetics. The behavior of drug release from theophylline tablets (control) and those contg. either Explotab or Starch 1500 occurred predominantly by diffusion mechanism, while the drug release from tablets contg. either Ac-Di-Sol or Polyplasidone followed first-order kinetics.
https://bpsa.journals.ekb.eg/article_65506_b7c26ca17712060ab0a9d506f762ecbc.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
31
41
10.21608/bfsa.2002.65507
65507
Original Article
Quantitation of tolnaftate by spectrophotometric methods in pharmaceutical formulations
P. Khashaba
1
Department of Pharmaceutical Analytical Chemistry, Assiut University, Egypt E-mail: pakinaz@yahoo.com
Two selective spectrophotometric methods are described for the assay of tolnaftate in single and/or combined pharmaceutical formulations. The first one depends on the formation of a methylene blue dye (λmax 665 nm) by the reaction of N,N-di-Me p-phenylene diamine dihydrochloride in the presence of ceric ammonium sulfate with sodium sulfide resulting from the alk. hydrolysis of the thiono ester-tolnaftate. All variables affecting hydrolysis of tolnaftate were studied. Also other parameters affecting the color development as sulfuric acid and reagent concns., reaction time, temp. and diln. solvents were optimized. The second method depends on the simultaneous estn. of tolnaftate and clioquinol in the presence of gentamycin sulfate and betamethasone by the measurement of the first deriv. spectrum in
https://bpsa.journals.ekb.eg/article_65507_9231108e796654d523c4cf4b2503e9d7.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-01
25
1
43
52
10.21608/bfsa.2002.65508
65508
Original Article
Inhibitory effect of flavonoids isolated from some Juncus species (flowers & callus) on blood platelets aggregation
S. Moustafa
1
T. El-Alfy
2
N. Hasan
3
K. Abou El-Se'oud
4
Department of Pharmacognosy, Faculty of Pharmacy, Tanta University, Tanta, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Tanta University, Tanta, Egypt
Department of Botany, Faculty of Agriculture, Tanta University, Tanta, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Tanta University, Tanta, Egypt
The anti-platelets aggregation effect of the different dose levels of plant exts. prepd. from the flowers and the tissue culture as well as the pure isolated flavonoids were tested using human blood of healthy fasting volunteers. The hydroxylation pattern of the tested compds. affected their activities. The more no. of (OH) group the lesser activity of the compd. The isolated flavonoids were quant. detd. by chromatog. & spectrophotometric methods of anal.
https://bpsa.journals.ekb.eg/article_65508_591bb1b9e8c62801fadb4bac4c8d982c.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
53
68
10.21608/bfsa.2002.65509
65509
Original Article
Solubilization of tenoxicam via different techniques
M. Fetuoh
1
S. Ismail
2
S. El-Harras
3
M. Abbas
4
Department of Pharmaceutics, Faculty of Pharmacy, Al-zhar University
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt
Department of Pharmaceutics, Faculty of Pharmacy, Al-zhar University
In this study, several techniques were employed to improve the aq. soly. of tenoxicam. These techniques include co-solvency, micellar solubilization and solid dispersions using different water-sol. polymers. The aq. soly. of tenoxicam in presence of 10% of formamide, DMF and DMSO was enhanced about 4.5, 3.1 and 2.8 times, resp. In addn., the results show that the hydroxylated cosolvents (glycerol, PG, PPG, PEG 200, PEG 300, PEG 400 and PEG 600) just potentiated the aq. soly. of the drug. Several classes of non-ionic surfactants were studied for their solubilizing action on tenoxicam. These classes were polysorbates (Tweens), polyoxyethylene alkylethers (Brijs) and polyoxyethylene stearates (Myrjs). Tween 80 exhibited a better solubilizing capacity on tenoxicam than other investigated tweens and they could be arranged according to their solubilizing capacity on the drug and the distribution coeff. of the drug between their micelles as: Tween 80 > Tween 60 > Tween 40. It is clearly evident that the solubilizing effect of these micellar forming agents increases as the hydrophobic chain length of the surfactant increases. In addn., Brij 35 exhibited a higher solubilizing capacity on the drug than Brij 58. Furthermore, Myrj 59 exhibited higher solubilizing power on tenoxicam compared to Myrj 53 and Myrj 52. These results indicate the relationship between the aq. soly. of the drug in presence of the above tested surfactants and its distribution coeff. between micellar and aq. phases. The dissoln. rate of tenoxicam in presence of PEG 4000 and PVP 40000 in its solid dispersions was improved esp. with PVP 40000 (in a drug: polymer ratio 1:9). IR, DSC and x-ray diffraction studies were conducted to investigate the mechanism responsible for this improvement
https://bpsa.journals.ekb.eg/article_65509_0b0fb0bde8a7db885f5e28822d9f6387.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
69
78
10.21608/bfsa.2002.65510
65510
Original Article
Formulation, bioavailability and pharmacokinetic properties of combined paracetamol/orphenadrine in tablets
M. Youssef
1
E. Zein El-Din
2
M. Fouda
3
M. Osman
4
Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt
Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt
Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt
Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt
In this investigation, the in-vitro characters, the bioavailability, as well as the pharmacokinetic parameters of two different paracetamol/orphenadrine citrate tablet formulations were compared. The first formulation (product A) was Norgesic tablets (Manufd. by E.I.P.I.Co., A.R.E) while the other (product B) was formulated tablets of the same compn. The in-vitro dissoln. revealed faster dissoln. rate in case of product A. Bioavailability study was conducted on healthy male subjects after receiving a single oral dose of either product A or B according to a 2-way crossover study. Blood samples were collected over an eight hour period and analyzed for their drug contents using HPLC. Pharmacokinetic parameters were detd. for both formulations including, mean max. plasma concn. (Cmax), time of max. concn. (Tmax), half-life (t1/2), terminal rate of elimination (Ke) and area under serum concn.-time curve (AUC). It was found that Cmax obtained with product A was higher than that with product B. Regarding Tmax, t1/2, and Ke, both products were found to be not statistically different. Furthermore, the two products were not found significantly different in the extent of absorption as indicated by area under serum concn.-time curve. These findings may indicate that the two products are bioequivalent in terms of bioavailability and pharmacokinetic properties detd. in normal healthy male volunteers
https://bpsa.journals.ekb.eg/article_65510_6d676e369d5d9bbd90049cf8fce31d37.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
79
83
10.21608/bfsa.2002.65511
65511
Original Article
Production of flavonoids in cell cultures of Astragalus sieberi DC
A. Abd El-Mawla
1
A. Attia
2
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
The flavonoid glycosides kaempferol-3-O-β-D-glucopyranoside (astragalin), kaempferol-3-O-rutinoside and kaempferol-3-O-(2-gal-rhamnosyl-robinobioside) (mauritianin) as well as the aglycons apigenin, kaempferol and quercetin were isolated from the cell suspension cultures of Astragalus sieberi DC. (Leguminosae). The isolated compds. were detected by TLC and HPLC in varying amts. and identified by spectral anal. and comparison with authentic samples
https://bpsa.journals.ekb.eg/article_65511_c2a7f891c71e2ecf2fb0956c760aa167.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
85
94
10.21608/bfsa.2002.65512
65512
Original Article
Saponins, naphthohydroquinone and anthraquinone glycosides from Rubia cordifolia L.
Zedan Ibraheim
1
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
From the butanol fraction of the chloroform-methanol ext. (1:1) of the dried roots of Rubia cordifolia L, several compds. were isolated and identified viz, the saponins hederagenin-3-O-α-L-arabinopyranoside and 3-O-α-L-arabinopyranosyl-hederagenin-28-Oβ-D-glucopyranosyl-(1→6)-β-D-glucopyranoside ester, the naphthohydroquinone glycosides: 2-carbomethoxy-3-prenyl-1,4-naphthohydroquinone 4-O-β-glucoside and 2-carbomethoxy-3-prenyl-1,4-naphtho-hydroquinone 1,4-di-O-β-glucoside, the anthraquinone glycosides: 1-hydroxy-2-hydroxymethyl-9,10-anthraquinone-11-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside, 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-α-rhamnopyranosyl (1→2)-(4'-O-acetyl)-β-glucopyranoside and 2-carbomethoxy, 1,3-dihydroxy-9,10-anthraquinone-3-O-α-rhamno-pyranosyl-(1→2)-β-glucopyranoside and adenosine. The identification of the isolated compds. was done using different phys., chem. and spectral methods
https://bpsa.journals.ekb.eg/article_65512_1bc0f78cf5985a20eb4a343ca0dc1513.pdf
eng
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
3009-7703
2002-06-30
25
1
105
110
10.21608/bfsa.2002.65513
65513
Original Article
Bioavailability of propranolol HCL following oral and transdermal administration in rabbits
K. Khaled
1
Y. El-Sayed
2
I. Al-Bawardi
3
A. El-Gorachi
4
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
Propranolol hydrochloride gel formulation was developed and the in-vivo percutaneous absorption of the drug was studied and compared with oral absorption using rabbits as animal model. Drug plasma concns. were detd. using a validated HPLC method of assay. The gel formulation appeared to produce acceptable sustained blood levels of the drug and the mean residence time (MRT) and the mean absorption time (MAT) were dramatically increased following gel application as compared to the oral soln. administration. The mean abs. bioavailability (F%) was found to be 8.8% for oral administration and 53% for the transdermal formulation. These results could be, at least in part, due to the continuous absorption of drag from gel formulation as well as the substantial hepatic first-pass metab. assocd. with the oral administration of the drug.
https://bpsa.journals.ekb.eg/article_65513_79ee9e53a18ec040d67f9dd5b5af114e.pdf