ORIGINAL_ARTICLE
ENHANCEMENT OF DISSOLUTION RATE OF CARBAMAZEPINE: I- IN VITRO STUDIES
Carbamazepine (CBZ) is an antiepileptic drug which shows variable absorption and variable bioavailability due to poor solubility. Three approaches were utilized to enhance the dissolution rate namely, solvent deposition onto porous silica, co-grinding with porous silica, egg albumin or polyvinylpyrrolidone and surface hydrophilization with non-ionic surfactant or propylene glycol. The molecular behavior of CBZ in the investigated systems were studied using X-ray diffraction analysis and differential scanning calorimetry. The dissolution rate of the drug was also investigated. The obtained results indicated that CBZ was transformed to the amorphous state in both the ground and loaded mixtures with porous silica. This transformation resulted in significant enhancement of the dissolution rates of the drug. Surface hydrophilized rug using 1% w/w polyoxyethylene sorbitan monolaurate (polysorbate 20) showed higher dissolution rate and good compliance with respect to tablet characteristics according to BP 1993 limits.
https://bpsa.journals.ekb.eg/article_68732_846f172a4b7552e3eba1b75b2c69d4d9.pdf
1997-06-30
1
8
10.21608/bfsa.1997.68732
Ahmed
Ali
1
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
FORMULATION AND EVALUATION OF COLON-TARGETED TEGAFUR MICROSPHERES
Tegafur (TGF) is an antineoplastic drug which used for treatment of neoplasm of gastro-intestinal tract including colon cancer. Cellulose acetate butyrate microspheres containing the drug were prepared by using the emulsion-solvent evaporation technique. The microspheres were spherical and free flowing. The yield was greater than 97% and more than 95% of the drug was encapsulated. The effect of microsphere size and pH of the dissolution medium on the drug release was investigated. Sustained release profiles of TGF from TGF-CAB microspheres were observed. In all cases the drug release followed Higuchi diffusion model. Microspheres of smaller size gave a relatively higher dissolution rate of the drug. The drug release was slower in acidic medium (pH 1.2) suggesting that using CAB microspheres would be of value for controlling the drug release and potential colonic-targeting of the drug.
https://bpsa.journals.ekb.eg/article_68733_304cdaec8677a67cd1e0c39104b7a73f.pdf
1997-06-30
9
15
10.21608/bfsa.1997.68733
F.
Mohamed
1
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
G.
El-Gendy
2
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
A.
Ali
3
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
UTILITY OF 5-DIAZO-1,2,4-TRIAZOL-3-CARBOXYLIC ACID FOR COLORIMETRIC DETERMINATION OF SOME DIBENZAZEPINES
A simple, rapid, and accurate spectrophotometric method for determination of four dibenzazepines has been developed. The method is based on the interaction of 5-diazo-1,2,4-triazole-3-carbaxylic acid (DTCA) with dibenzazepine drugs in 10% nitric acid media. The resulting colored products possess 2 absorption maxima, one in the range of 475-495 nm with higher molar absorptivity and the other in the range of 570-575 nm with lower molar absorptivity. Measurements were performed in the range of 475-495 nm. Beer's law is obeyed in the concentration range of 2-10 µg/ml for both imipramine HCl and desipramine HCl and 2-14 µg/ml for both clomipramine HCl and trimipramine maleate. The molar absorptivities of the studied drugs are 2.877x 104 for imipramine HCl at 487 nm., 3.164 x 104 for desipramine HCl at 495 nm., 2.002 x l04 for clomipramine HCl at 475 nm. and 2.350 x 104 for trimipramine maleate at 475 nm. The proposed method is applied successfully for the determination of studied drugs in pure form and in commercial and laboratory prepared tablets. The obtained results are in good agreement with those obtained from official methods.
https://bpsa.journals.ekb.eg/article_68734_55b2fdd8c3418e07891952db40012884.pdf
1997-06-30
17
22
10.21608/bfsa.1997.68734
Nawal
El-Koussi
1
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
Horria
Mohamed
2
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
Abd El-Maaboud
Mohamed
3
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
TWO PHENYLPROPANOID GLUCOSIDES FROM GLINUS LOTOIDES L. VAR. DICTAMNOIDES
A new phenylpropanoid glucoside (dictamnoside A) and another known one (Citrusin C) were isolated from the chloroform-soluble fraction of Glinus lotoides L. var. dictamnoides extract. Their structures were determined by means of spectroscopic methods.
https://bpsa.journals.ekb.eg/article_68735_d20acf0586c4e0140864ad50eed667dd.pdf
1997-06-30
23
26
10.21608/bfsa.1997.68735
Arafa
Hamed
1
Faculty of Science, South Valley University, Aswan 81528, Egypt
AUTHOR
Irina
Springuel
2
Faculty of Science, South Valley University, Aswan 81528, Egypt
AUTHOR
Nasr
EI-Emary
3
Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
AUTHOR
Hidemichi
Mitome
4
Tokyo College of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-03, Japan
AUTHOR
Hiroaki
Miyaoka
5
Tokyo College of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-03, Japan
AUTHOR
Yasuji
Yamada
6
Tokyo College of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-03, Japan
AUTHOR
ORIGINAL_ARTICLE
SPECTROPHOTOMETRIC DETERMINATION OF SOME FLUOROQUINOLONE DERIVATIVES THROUGH OXIDATION WITH CERIUM (IV)
A simple, rapid and sensitive spectrophotometric method is described for the determination of the fluoroquinolones; amifloxacin, difloxacin, norfloxacin, ofloxacin, ciprofloxacin, pefloxacin and lomefloxacin. The method is based on their oxidation with cerium (IV) ammonium sulphate in 4 M perchloric acid and subsequent measurement of the residual cerium (IV) via its reaction with p-Dimethylaminobenzaldehyde (p-DMAB) to give a reddish colored product to be then measured at 463 nm. The method obeys Beer's Law over a general concentration range of 0.5-12 µg/ml. Accuracy and precision of the method were checked. Molar ratio determination to the reaction with norfloxacin, as an example, indicates 1:12 (drug to Ce (IV)) and 1:4 (p-DMAB to Ce (IV)) ratios, respectively. A good negative correlation is found between the molar absorptivities of the reacted compounds with their pK2 (piperazine moiety). Mechanism of reaction between each of fluoroquinolones and p-DMAB with Cerium (IV) was studied. The proposed procedure was applied for the assay of dosage forms containing fluoroquinolones without interference from common additives. Interference from sodium ascorbate present in peflacine ampoules is eliminated by its oxidation with 1 ml 0.1% potassium bromate solution before applying the proposed procedure.
https://bpsa.journals.ekb.eg/article_68736_d41d8cd98f00b204e9800998ecf8427e.pdf
1997-06-30
27
36
10.21608/bfsa.1997.68736
Gamal
Saleh
1
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
PHYTOCHEMICAL INVESTIGATION OF WEDELIA PROSTRATA HOOK et ARN. (HEMSL.); II- TILE ETHYL ACETATE SOLUBLE FRACTION OF THE METHANOL EXTRACT
Phytochemical investigation of the ethyl acetate soluble fraction of the MeOH extract of the powdered aerial parts of Wedelia prostrata resulted in the isolation and identification of sulfurein; coreopsin; stillopsin; 3,5-dicaffeoyl quinic acid and 3,4-dicaffeoyl quinic acid. The identification of the isolated compounds was established through the different methods of spectral analysis.
https://bpsa.journals.ekb.eg/article_68737_197b29de0dd4b13ac528c77a39ac0620.pdf
1997-06-30
37
46
10.21608/bfsa.1997.68737
S.
Farag
1
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
N.
El-Emary
2
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
M.
Makboul
3
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
H.
Hasanean
4
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
M.
Miwa
5
Faculty of Pharmacy, Meijo University, Nagoya, Japan
AUTHOR
ORIGINAL_ARTICLE
SYNTHESIS AND INVESTIGATION OF CERTAIN 3(5)- SUBSTITUFED-1,2,4- TRIAZOLE-5(3)-CARBOXYLIC ACID DERIVATIVES
A series of 3(5)-substituted 1,2,4-triazole-5(3)-carboxylic acid amides, hydroxamic, hydrazide, iminosemicarbazide, semicarbazide and thiosemicarbazide have been synthesized. Most of the prepared compounds were tested for their growth inhibitory activity against Staph. aureus and E. coli and none of them revealed antibacterial activity at concentration up to 2.5 mg/mL. The 5(3)-iminosemicarbazides (8h, 9h, 10h, 11h), 5(3)-semicarbazides (8i, 9i, 10i, 11i) and 5(3)-thiosemicarbazides (8j, 9j, 10j) were chosen for evaluation of their potentialities to lower blood glucose level in rats. The oral glucose tolerance test was used as preliminary test for evaluation of hypoglycemic activity of these compounds. The tested compounds showed different onset and duration of action.
https://bpsa.journals.ekb.eg/article_68738_75e3ca242f7ff835110ca3b1cbddefc0.pdf
1997-06-30
47
61
10.21608/bfsa.1997.68738
A.
Abd-Elhafez
1
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiui, Egypt
AUTHOR
H.
Mohamed
2
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiui, Egypt
AUTHOR
H.
Hassan
3
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiui, Egypt
AUTHOR
G.
El-Karamany
4
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiui, Egypt
AUTHOR
N.
El-Koussi
5
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiui, Egypt
AUTHOR
A.
Youssef
6
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiui, Egypt
AUTHOR
ORIGINAL_ARTICLE
TRITERPENOIDS AND FLAVONOIDAL GLYCOSIDE FROM FRUITS OF SORBUS AUCUPARIA (DC) CULTIVATED IN EGYPT
From the chloroform soluble fraction of ethanolic extract of the dried fruits of Sorbus aucuparia (DC)four triterpenes were isolated and identified as a-amyrin, ursolic acid, methyl 2a-hydroxy ursolate, 2a-hydroxy ursolic acid in addition to b-sitosterol. The major component of ethyl acetate fraction was isolated and identified as rutin. Their structures were established by physical, chemical and spectral methods. This is the first report of isolation of ursolic acid and its derivatives from the plant.
https://bpsa.journals.ekb.eg/article_68739_ee23f779b5df9925d993f6a76bef60fb.pdf
1997-06-30
63
65
10.21608/bfsa.1997.68739
S.
Youssef
1
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
SPECTROPHOTOMETRIC DETERMINATION OF SOME AROMATIC DIAMINES USING SODIUM SULPHIDE AND AN OXIDANT
A simple and selective colorimetric method was developed for quantitative determination of aromatic diamines; p-phenylenediamine, N,N-dimethyl p-phenylenediamine and N,N-diethyl-p-phenylenediamine. The method is based on the reaction of sodium sulphide with an aqueous solution of the diamine in presence of an oxidant at ambient temperature to form a methylene blue or ethylene blue like dyes. Absorption maxima of 597, 665 and 670 nm were obtained for the three compounds; respectively. Different oxidizing agents were tried e.g. Ce(IV), Fe(III) and N-bromo-succinimide (NBS). The color was developed within 5 minutes and remained stable for at least 24 hours. Linear calibration graphs with very small intercepts were obtained. The proposed method was applied successfully for determination of aromatic diamines in spiked water samples and in presence of other aromatic amines and excellent recoveries were obtained. Reaction products have been isolated and identified using microanalysis, UV and IR spectrometric methods.
https://bpsa.journals.ekb.eg/article_68740_2dc0a2bc1a110f9ecc5e3a9a0071a9b9.pdf
1997-06-30
67
74
10.21608/bfsa.1997.68740
Fardos
Mohamed
1
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
Mohamed
Abdalla
2
Department of Chemistry, Faculty of Science, King Saud University, Riyadh Saudia Arabia
AUTHOR
Soad
Shammat
3
Department of Chemistry, Faculty of Science, King Saud University, Riyadh Saudia Arabia
AUTHOR
ORIGINAL_ARTICLE
REDOX SPECTROPHOTOMETRIC DETERMINATION OF FLUOROQUINOLONE ANTIBIOTICS DOSAGE FORMS
A general difference spectrophotometric procedure for the determination of seven antibacterial 7-piperazine fluoroquinolone derivatives in the range of 2-20 µg/ml is proposed. The procedure is based on the oxidation of these antibiotics using 1 ml of 0.5 mg/ml potassium permanganate in presence of 20% sulphuric acid at room temperature (25±5°C) for 10 min. The decrease in permanganate color (DA) due to the interaction with such organic compounds is measured at 520 nm. Molar ratio determination indicated 1:3 (drug: permanganate). Assay precision (RSD) values were ±1.5% or better for the bulk drugs and ranged from ±1.38 to ± 1.2% for tablets and ampoules. Drug recoveries were quantitative from the dosage forms tested. The proposed procedure is simple, rapid, accurate and readily applied to the determination of this new class of antibiotics in pharmaceutical products without interference from other ingredients or common additives.
https://bpsa.journals.ekb.eg/article_68743_e8931169da59d547f829c1d295abd4e5.pdf
1997-06-30
75
85
10.21608/bfsa.1997.68743
Hassan
Askal
1
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
SPECTROPHOTOMETRIC DETERMINATION OF SOME CEPHALOSPORINS USING 2,2'-DIPHENYL-1-PICRYLHYDRAZYL
A spectrophotometric method was developed for the determination of some cephalosporins using 2,2'-diphenyl-1-picrylhydrazyl (DPPH). The latter employed to abstract a hydrogen atom from the drug thereby promoting a process of radical coupling. This results in a reduction of the violet color (520 nm) of DPPH with the formation of the yellow colored 2,2'-diphenyl-1-picrylhydrazine (DPPH). This fading in color of DPPH reagent depends on the concentration of the drug being determined. Beer's law was obeyed in the ranges of; 5-30, 5-25 and 10-30 µg/ml for cephalexin, cefadroxil and cephradine respectively. The validity of the method was tested by carrying out standard addition procedure analyzing the studied drugs in pure form as well as in their pharmaceutical preparations without interference from common additives. The percentage recovery ranged from (97.98-101.21) ±1.15-0.98.
https://bpsa.journals.ekb.eg/article_68744_d1984f5b56c6b6deb7eca7de65d78c46.pdf
1997-06-30
87
93
10.21608/bfsa.1997.68744
Hosny
Elsherief
1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
AUTHOR
ORIGINAL_ARTICLE
IN VITRO RELEASE OF FREEZE-DRIED MEFENAMIC ACID-POLOXAMER FROM SUPPOSITORY BASES AND EVALUATION OF ITS ANTI-INFLAMMATORY EFFECT
The in vitro release of mefenamic acid (MFA) as well as its freeze-dried forms with poloxamer 409 (PF-127) in different ratios [(9:1), (1:1)] from suppository bases was investigated and confirmed with DSC and X-ray.
The release rate of MFA from lipophilic base (WH15) and hydrophilic base (3PEG 1000:7 PEG 4000) in NaOH, KH2PO4 buffer at 37°C was performed. The release pattern of MFA:PF-127 freeze-dried samples from both selected bases was remarkably higher than that of pure untreated drug. However, the release of the drug as indicated by permeability rate constant was much more faster from WH15 compared to PEG using the same ratio of drug:PF-127 (8.037 vs 1.827, respectively).
MFA:PF-127 (1:1) freeze-dried formulated in WH15 and PEG suppository bases were evaluated by the carrageenin induced rabbit hindpaw edema. Both formulas resulted in inhibition of edema formation l hr post medication (58.6%, and 41.4%, respectively) which was significantly greater than the rectal MFA as received in WH15 (14.7%).
https://bpsa.journals.ekb.eg/article_68745_b452714c4bd6ebf351c57a35ebe24de6.pdf
1997-06-30
95
104
10.21608/bfsa.1997.68745
S.
El-Harras
1
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
AUTHOR