2024-03-29T06:53:50Z
https://bpsa.journals.ekb.eg/?_action=export&rf=summon&issue=10639
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
ACCELERATED STABILITY TESTING OF IBUPROFEN-EUDRAGIT RSPM SUSTAINED RELEASE TABLETS USING 1H-NMR, HPLC AND TLC
Aly
Abdel Rahman
A.
Aboutaleb
A.
Stamm
S.
Abdel Rahman
E.
Samy
Ibuprofen-Eudragit RSPM sustained release tablets, already have been formulated, were subjected to accelerated stability testing for 6 months at 25, 37 and 45°C.The tablets were stored in firmly closed glass bottles in order to eliminate the effect of humidity, a condition simulating the actual shelf storage.
The drug content of the stored tablets was evaluated using 1H-NMR, HPLC and TLC techniques in order to investigate the effect of temperature on ibuprofen stability.
A small reduction (2-4 % w/w) in the drug content was detected in the tablets stored at 37 and 45°C for 6 months using 1H-NMR and HPLC techniques. The decomposition of ibuprofen in the preformulated tablets was found to be first order reaction kinetics.
It was concluded that the expiry date of ibuprofen in the formulated sustained release tablets is up to 3 years. Thus this formulation could be considered as a convenient pharmaceutical formulation of ibuprofen.
1993
06
30
1
11
https://bpsa.journals.ekb.eg/article_70021_6f5e911d31471ce99076cbbba6c1e61a.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
SOLID STABILITY TESTING OF IBUPROFEN - EUDRAGIT RESPM SUSTAINED RELEASE TABLETS
Aly
Abdel Rahman
A.
Aboutaleb
A.
Stamm
S.
Abdel Rahman
E.
Samy
Preformulated ibuprofen-Eudragit RSPM sustained release tablets were subjected to accelerated stability testing at 25, ·37 and 45°C for 6 months. The stored tablets were evaluated for the intact drug in the formula, drug-polymer interaction and compatibility of the drug with the formulated excipients using infra red spectroscopy (I.R.) and differential scanning calorimetry (DSC).
The IR spectrum of ibuprofen in the tablets prepared by 15% w/v Eudragit RSPM as a granulating agent and containing 23% w/w Avicel pH 102 as an excipient was similar to the IR of standard ibuprofen. There was no change in the IR spectra of the tablet components before and after storage of those tablets at the different investigated temperatures for 1, 3 and 6 months.
The DSC thermograms of ibuprofen stored tablets showed that the drug was still in the highly pure (>98%) crystalline form and there was no significant degradation after storage indicating the stability of the drug on storage.
In detecting ibuprofen purity in the stored tablets, plotting of the sample temperature versus the reciprocal of the fraction of ibuprofen melted showed deviation from Van't Hoff linear plot.
1993
06
30
12
24
https://bpsa.journals.ekb.eg/article_70025_5a06535bbc8ef35ddbc0f062db0cb6d9.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
EVALUATION OF IBUPROFEN-CELLULOSIC POLYMERS SUSTAINED RELEASE TABLETS
Aly
Abdel Rahman
A.
Aboutaleb
A.
Stamm
S.
Abdel Rahman
E.
Samy
Ibuprofen sustained release tabletse were formulated using wet granulation technique and cellulosic polymers as granulating agents including ethyl cellulose 20, hydroxypropyl methyl cellulose (pharmacoat 606) and hydroxypropyl methyl cellulose phthalate (HP 55 F).
The effect of tablet excipients including Avicel PH 102, Lactose, Emcompress and Emedex on the release rate of ibuprofen from the prepared tablets was also investigated using shift dissolution method.
It was found that among the formulated ibuprofen sustained release tablets, those tablets granulated with 3% w/v ethyl cellulose 20 and containing 23% Emcompress as an excipient were proved to be superior for ibuprofen sustained release. Higher Avicel PH 102 concentration (39 and 40% w/w) was found to enhance the release.
Comparing the effect of 1% w/v of the investigated cellulosic polymers on ibuprofen retardation, it was found to be in the following order: ethyl cellulose 20 > HP 55 F > pharmacoat 606.
Various kinetic models including zero order, first order and Higuchi equation were applied to explain the release mechanism from the prepared tablets. It was found that the best fit with the highest correlation coefficient was achieved with the zero-order equation.
1993
06
30
25
35
https://bpsa.journals.ekb.eg/article_70026_9e25037f54f42387e7f20cef11e5a5ec.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
IN VITRO RELEASE OF DIAZEPAM FROM DIFFERENT SUPPOSITORY FORMULATIONS
Sayed
Ismail
Sohair
El-Shanawany
The effect of suppository vehicles, drug concentrations, liquid additives and some nonionic surfactants on the in vitro release of diazepam from different suppository formulation were investigated. The obtained data revealed that the drug release is significantly higher from suppository prepared using PEG than the other formulations. The drug release from oleaginous base was related inversely to its partition coefficient and the melting range of the tested oleaginous bases. The incorporation of 'some liquid additives (10%) was found to improve the release pattern of the drug from a PEG base. The degree) of improvement is correlated well to the solubility of the drug .in the utilized additives. The data, also, reveal that the release rate is directly proportional to the drug concentration. The incorporation of nonionic surfactants into Witepsol H15 in a 5% concentration was found to increase the release rate of diazepam. The enhancing effect was found to be dependent on the chemical structure of the surfactants. The release rate of medicament from different solid nonionic surfactants, as suppository bases, was also studied. The magnitude of drug release was markedly reduced as compared with PEG bases.
1993
06
30
36
46
https://bpsa.journals.ekb.eg/article_70027_ba0e097dbc3bf65e9b146f1b56a6d18d.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
THE MODE OF INCLUSION COMPLEXATION OF BROMAZEPAM WITH DIMETHYL -CYCLODEXTRIN
S.
Saleh
Aly
Abdel-Rahman
A.
Aboutaleb
Y.
Nakai
M.
Ahmed
Inclusion complex formation of bromazepam with heptakis- (2 ,6-di-O-methyl)-b-cyclodextrin (DM-b-CD) in aqueous solution was confirmed by the solubility method. AL-type phase solubility diagram was obtained with 50 folds increase in the solubility of bromazepam. Crystalline inclusion complexes of bromazepam with DM-b-CD in 1 : 1 and 1 : 2 molar ratios were obtained by the co-precipitation method as indicated by the X-ray diffraction analysis. Infrared (IR) spectra of the inclusion complex ,of bromazepam and DM-b-CD was different depending on the molar ratio, whether it is 1: 1 or 1 : 2. In the same time, the differential scanning calorimetry (DSC) analysis showed different thermal behaviour depending on the molar ratio of the inclusion complex. These results revealed that the mode of molecular interaction of 1 : 1 inclusion complex of bromazepam with DM-b-CD was different from that of 1 : 2.
1993
06
30
47
55
https://bpsa.journals.ekb.eg/article_70028_031ee247b14facbe99a69a7f074a980b.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
PHARMACOKINETIC STUDY OF NORETHINDRONE COPRECIPITATE
S.
Abou-El-Ela
S.
Safwat
Pharmacokinetic parameters of norethindrone (NE) were studied in 12 adult female guinea pigs following either oral or rectal administration of a single dose of 2.5 mg. The animals were divided into three groups (4 animals each) and each group was given the single dose either in capsule, tablet or suppository form. NE in blood plasma was determined by HPLC at various time intervals (0.5, 1, 2, 4, 6, 8, 12 hour). The results indicate that NE was readily absorbed by, both routes but the maximum plasma concentration (Cmax) and the area under the plasma concentration time curve AUC of NE were significantly high by the rectal route. No significant differences in the plasma half-life (t1/2), absorption (Ka) and elimination (Ke) rate constants and the time to maximum plasma concentration (tmax) were observed between the oral and rectal administrations. These findings suggest that the rectal route offers the possibility of reducing the effective dose of NE, which is widely used for contraception and hormone replacement therapy.
1993
06
30
56
62
https://bpsa.journals.ekb.eg/article_70029_0f6964b0a6e81d2c477660292db75d5e.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
SUSTAINED RELEASE FORMULATIONS OF PHENAZOPYRIDINE HYDROCHLORIDE WITH CELLULOSE ACETATE PHTHALATE
A.
Aly
S.
Ahmed
S.
Abdel-Rahman
S.
Saleh
A.
Aboutaleb
Cellulose acetate phthalate (CAP) was utilized for the preparation of sustained release formulations of phenazopyridine hydrochloride (PHCl) by three different techniques: (a) solid dispersion (coprecipitation), (b) microencapsulation. by phase separation coacervation using non-solvent addition technique and (c) pan coating. The three techniques studied resulted in different extents of sustaining the release of PHCl, in vitro, compared to the untreated drug. Pan coating proved to be the easiest and most convenient: technique for the preparation of sustained release PHCl microcapsules. With regard to the release kinetics of PHCl from each of the formulations prepared, the first order model was found to be the most suitable mechanism describing the release of the drug.
1993
06
30
63
72
https://bpsa.journals.ekb.eg/article_70030_d859d1e1a9d99b4ea05d429253973b0c.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
MICROENCAPSULATION OF NITROFURANTOIN BY COACERVATION USING CERTAIN POLYMERIC MATERIALS
A.
Aly
S.
Saleh
S.
Ahmed
S.
Abdel-Rahaman
A.
Aboutaleb
Microencapsulation of nitrofurantoin was carried out in order to prepare sustained release formulations with less side effects. Three coacervation techniques, using three different coating materials, were adopted for this purpose as follows: non - solvent addition using Eudragit RS 100 (ERS), temperature change using ethylcellulose (EC) and salt addition using sodium alginate (SA). The physical properties as well as the dissolution characteristics were investigated. Microencapsulation of nitrofurantoin (NF) gave rise to sustaining its release at pH 1.12. NF-SA and NF-EC microcapsules showed more retarded release than NF-ERS microcapsules. Increasing the proportion of ERS in its microcapsules resulted in a marked sustaining of NF release whereas, no significant effect was obtained upon increasing the proportion of EC in NF-EC microcapsules. NF microcapsules showed fast release at pH 7.8 specially in case of SA. Regarding the release kinetics, first order model proved to be the most operative mechanism explaining the release of NF from NF-ERS microcapsules. On the other hand, Baker and Lonsdale equation was found to be the most suitable model for explaining the release of NF from EC or SA microcapsules.
1993
06
30
73
87
https://bpsa.journals.ekb.eg/article_70031_4d742f897b87d5c19aa6ba443c177e9c.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
SYNTHESIS OF NOVEL SUCCINIMIDES: SPIRO-, AND N-MANNICH BASE DERIVATIVES WITH POTENTIAL ANTICONVULSANT ACTIVITY
Ragab
Shafik
El-Sebai
Ibrahim
Magdi
Abdel-Khalek
Mona
El-Semary
Several substituted N-aminomethylsuccinimides (I) and 1'-alkyl, or aralkyl Spiro [indolin-2-one-3,3'-pyrrolidine-2',5 -diones1 (III, XVI) were prepared. The pKa values and the anti-MMS activity of some selected members are reported. Compound XVI showed matching protection mode when compared with ethosuximide.
1993
06
30
88
96
https://bpsa.journals.ekb.eg/article_70032_2d61bbf36e492032d1c26312bd449b00.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
PREPARATION AND EVALUATION OF ISONIAZID MICROCAPSULES
S.
Safwat
F.
Omar
Spherical microcapsules of isoniazid (INH) using ethylcellulose and ethylene vinyl acetate copolymer (EVA) were prepared by a coacervation-phase separation method. The dissolution characteristics of isoniazid from microcapsules with different concentrations of EVA were almost independent of the content of EVA in phosphate buffer PH 7.4 but dissolution properties of microcapsules in 0.lN HcL and water were found to be affected by the content of EVA and there was a negative correlation between the release rate and the content of EVA in the microcapsules. Kinetic data revealed that the release mechanism from microcapsules followed diffusion controlled and zero order Kinetic.
The bioavailability of INH microcapsules was studied in rabbits. The mean maximum serum levels (Cmax) and time to maximum serum levels (tmax) were significantly different for INH microcapsules prepared using ethylcellulose only and those prepared with ethylcellulose and EVA copolymer, compared with INH powder. With regard to the area under the curve (AUC) value, there was no significant difference between INH powder and INH microcapsules.
1993
06
30
97
105
https://bpsa.journals.ekb.eg/article_70033_f096863237b28646e006b89bb9460bd0.pdf
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
1110-0052
1993
16
1
FLUOROMETRIC•DETERMINATION OF ACYCLOVIR IN SPIKED HUMAN PLASMA
A.
Habeeb
M.
Mabrouk
A highly sensitive fluorometric method for determination of acyclovir is described. The method depends on the interaction between acyclovir .and 7-hydroxy-4-methylcoumarin where a fluorophore of high fluorogenic activity is formed which has wavelengths of maximum excitation and emission of 342 and 452,respectively. The method is used for determination of acyclovir in human plasma in the range of 5-10 ngm-1 in a rectilinear relationship. The mean percentage recovery was 99.954 S.D. ± 1.450 in case of bulk drug while it was 99.893 S.D.+ 0.711 in case of 6 concentrations of human plasma. The method is recommended for drug monitoring of acyclovir.
1993
06
30
106
111
https://bpsa.journals.ekb.eg/article_70034_e65a51ba588e1b482c503e1e1004ba32.pdf