Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
PREPARATION AND EVALUATION OF PIROXICAM - PLURONIC SOLID DISPERSIONS
97
108
65474
10.21608/bfsa.2003.65474
EN
M.
Fathy
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M.
El-Badry
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
2003
03
02
With an objective of enhancing the dissolution rate of piroxicam (PXM), solid dispersions<br />(SDs) of piroxicam were prepared using different grades of pluronic F-68 (Pl. F-68), pluronic<br />F-98 (Pl. F-98), and pluronic F-127 (Pl. F-127) adopting the solvent evaporation technique.<br />The solid dispersions were prepared at different (drug: polymer) ratio (1:1, 1:3 and 1:5).<br />Piroxicam- pluronic solid dispersions were investigated by inferared spectroscopy (IR), x-ray<br />diffraction (XRD) and differential scanning calorimetry (DSC). The IR spectra prevailed no<br />chemical interaction between the drug and copolymer. The powder x-ray diffraction (XRD)<br />patterns and differential scanning calorimetry (DSC) thermograms demonstrated that<br />piroxicam was existed in a solid solution state in the SD. Phase diagram for solid dispersion of<br />piroxicam in pluronic F-98 indicated that the solid solution of piroxicam was obtained at a<br />concentration of PXM less than 35% in the SD. The stability study was carried out for the solid<br />dispersion prepared at 1:1 (piroxicam/ Pl. F-98) at 40 ° for 40 weeks prevailed that; the drug is<br />stable during the storage period in the dispersion. The solubility study of piroxicam was carried<br />out at different concentrations of pluronics, also the dissolution rate of the drug was improved<br />either by physical mixture or the solid dispersions.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
FORMULATION AND EVALUATION OF TETRACAINE HYDROCHLORIDE POLYMERIC FILMS FOR TOPICAL APPLICATION
109
117
65476
10.21608/bfsa.2003.65476
EN
A. E.
Aboutaleb
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut
E. M.
Samy
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut
Ahmed
Ismail
Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Assiut Branch,
Assiut
M.
Amin
Department of Pharmaceutics and Industrial Pharmacy, Al-Azhar University, Assiut Branch,
Assiut
Journal Article
2003
04
02
Eudragit polymeric films were investigated as a potential drug delivery system for<br />controlling the release of tetracaine HCl. The effect of modification in polymeric ratio of both<br />Eudragit RS100 and RL100, drug loading and nature of plasticizer on the in vitro release of the<br />drug from each film into a receiving medium of citrate buffer (pH=5) was measured. The<br />obtained results indicated that the film containing Eudragit polymer and plasticizer affected the<br />drug release rate and that the release followed Higuchi-diffusion model. The release rate was<br />found to be enhanced with increasing Eudragit RL100 ratio. The release rate was also found to<br />be directly proportional to drug concentration. Tetracaine HCl was slowly released from<br />Eudragit RS100 / dimethylphthalate films and Eudragit RS100 / diethyl-phthalate films.<br />Eduragit films plasticized with GTA, PEG400 and PG produced a fast drug release. This study<br />demonstrated that tetracaine HCl was compatible with Eudragit RS100 as indicated by the<br />clear and transparent formed films. Also, the characterizations of Eudragit films were<br />conducted by IR-spectroscopy, X-ray diffraction pattern and differential thermal analysis to<br />explore the possibility of the drug polymer interaction occurring between tetracaine HCl and<br />either Eudragit RS100 or Eudragit RL100. The therapeutic potential of tetracaine HCl Eudragit<br />polymeric films was evaluated using "Tail-Flick" method on a Techano analyiseometer model.<br />Results indicated that tetracaine HCL polymeric film composed of Eudragit RS100: Eudragit<br />RL100 ratio (8:2) and plasticized with 20% w/w diethylphthalate gave a long duration of<br />analgesic response.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
UTILIZATION OF PLANTAGO, PECTIN AND COMPRITOL FOR THE PRODUCTION OF SUSTAINED RELEASE TRAMADOL MATRIX TABLETS BY DIRECT COMPRESSION
119
136
65477
10.21608/bfsa.2003.65477
EN
Adel M.
Aly
College of Pharmacy, Alisra University, Amman, Jordan
Sara A.M.
Aly
College of Pharmacy, Alisra University, Amman, Jordan
Raslan H. M.
Kittaneh
College of Pharmacy, Alisra University, Amman, Jordan
Journal Article
2003
04
03
Tramadol is an opioid analgesic. It is indicated for the relief of moderate to<br />moderately sever pain across the full range of acute and chronic pain syndromes. Due<br />to its short half-life (5 to 7 hours) and its short duration of action (3 to 7 hours), it was<br />highly desirable to slow the rate of absorption of tramadol and spread the absorption<br />process over a longer interval, with increasing patient compliance and decreasing the<br />risk and severity of adverse effects. Consequently, sustained release tramadol tablets<br />were prepared utilizing the following materials: Compritol (CT), Plantago (PT),<br />Pectin (PC), and HPMC. The inclusion of HPMC with CT, prolongs the release of<br />tramadol more than CT alone. Also, by increasing HPMC concentration more<br />sustaining effect could be obtained, but at 15% less sustaining effect was observed.<br />The inclusion of NaAlg retards the release more than NaCMC, either with or without<br />Avicel. PC showed pronounced sustaining effect with NaAlg alone (either with or<br />without Avicel) compared to those containing NaCMC alone or with NaAlg. However,<br />in case of tablets containing PT; the inclusion of NaCMC, either alone or in<br />combination with NaAlg, retards the release of drug more than NaAlg alone. Aiming<br />for more sustaining properties smaller tablets (250 mg) containing the same<br />proportions of CT and HPMC but lower % of Avicel, NaCMC or NaAlg were<br />prepared. Formula containing NaCMC alone showed the most sustaining effect (more<br />than Tramal®) followed by those including NaCMC and Avicel.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
IN-VITRO STUDIES ON CORTICOSTERONE PERMEATION THROUGH HAIRLESS MOUSE SKIN: ( PART I)
137
144
65479
10.21608/bfsa.2003.65479
EN
Fahima M.
Hashem
Department. of Pharmaceutics, Faculty of Pharmacy, Helwan University
Abdel
Ghanem
Faculty of Pharmacy, University of Utah, USA
Eman. S.
El-leithy
Department. of Pharmaceutics, Faculty of Pharmacy, Helwan University
Dalia. S.
Shaker
Department. of Pharmaceutics, Faculty of Pharmacy, Helwan University
Journal Article
2003
04
13
The use of penetration enhancer adjuvants was emerged as a growing trend in<br />transdermal drug delivery. These adjuvants may reduce the capacity for drug binding to skin<br />and promote the permeation of bimolecules through the skin. The main objective of this study<br />was to evaluate the effect of polyvinylpyrrolidone (PVP) and hydroxypropyl–beta-cyclodextrin<br />(HP- -CD) as well as certain chemical enhancers on solubility of unlabeled corticosterone<br />(CS) and its transdermal permeation through skin. The results revealed that autoclaving CS<br />with PVP maintained supersaturated state through inhibition of crystal growth and in turn<br />increased its flux across hairless mouse skin. The data showed also that HP- -CD had no effect<br />on CS permeation but could be used as solubilizing agent for highly lipophilic skin permeation<br />enhancers octyl pyrrolidone (OP) and dodecyl pyrrolidone (DDP). It also prevented depletion<br />of such lipophilic enhancers into skin, increased by this way the permeation enhancement of<br />these adjuvants
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
EVALUATION OF THE EFFECT OF POLYVINYLPYRROLIDONE AND CERTAIN ENHANCERS ON THE PERMEATION OF CORTICOSTERONE FROM TRANSDERMAL DELIVERY SYSTEMS: (PART II)
145
151
65480
10.21608/bfsa.2003.65480
EN
Fahima M.
Hashem
Department of Pharmaceutics, Faculty of Pharmacy, Helwan University
Abdel Halim
Ghanem
Faculty of Pharmacy,University of Utah, USA
Eman S.
El-leithy
Department of Pharmaceutics, Faculty of Pharmacy, Helwan University
Dalia S.
Shaker
Department of Pharmaceutics, Faculty of Pharmacy, Helwan University
Journal Article
2003
04
13
The purpose of the present study was to evaluate the permeation profiles of unlabeled<br />corticosterone (CS) drug from gels and adhesive patches as transdermal delivery systems. The<br />effect of polyvinylpyrrolidone and certain chemical enhancers octylpyrrolidone (OP) and<br />dodecylpyrrolidone (DDP) on the flux of drug through hairless mouse skin was also studied.<br />The results show that presence of solubilizing agents such as hydroxypropyl–beta-cyclodextrin<br />(HP- -CD) decreased the drug flux from hydroxypropyl methylcellulose (HPMC) gel dermal<br />base and controlled the diffusion kinetics. Increasing the drug thermodynamic activity by its<br />autoclaving with 0.25% polyvinylpyrrolidone (PVP) (supersaturation) improved the drug flux<br />through the skin by 3 fold from HPMC gel base dermal preparations. The results also reveal<br />that chemical enhancer/HP- -CD mixtures represent a suitable combination for controlling the<br />release as well as increasing the flux of drug through skin. The addition of 5% HP- -CD to OP<br />solution not only increased the drug flux but also showed a controlled release that approached<br />the zero order. Use of the chemical enhancer DDP in presence of HP- -CD shows a 10-fold<br />increase in CS flux from HPMC gel base. The results of transdermal patches show that<br />increasing the concentration of OP increased the cumulative amounts of Labeled corticosterone<br />(3H-CS) permeated through the skin from two adhesives patches Duro-tak 2516 and 2287.<br />There is a difference between the two adhesives patches in terms of skin permeation. The rate of<br />drug permeated from the Duro-tak 2516 patch is 2 times greater than Duro-tak 2287, where<br />there permeability coefficient is 9.05 and 4.67 x 10–9 respectively.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
BIOACTIVE PRINCIPLES OF THE FLOWERS OF PANCRATIUM MARITIMUM
171
177
65481
10.21608/bfsa.2003.65481
EN
Diaa T.A.
Youssef
Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522,
Egypt
Journal Article
2003
07
06
Bioactive-guided fractionation and purification of the ethyl acetate fraction of an<br />ethanolic extract of fresh flowers of Pancratium maritimum (Amaryllidaceae)<br />cultivated in Egypt yielded an alkaloid, pancratistatin (1), together with 3-<br />caffeoylquinic acid methyl ester (2). Their structures were determined on the basis of<br />extensive 1D (1H and 13C) and 2D (COSY, HMQC, HMBC, and NOESY) NMR studies<br />and high-resolution mass spectral measurements. Both compounds showed potent<br />cytotoxic activity against HeLa cells and moderate anti-tuberculosis activity against<br />Mycobacterium tuberculosis H37Rv. This is the first report of pancratistatin in<br />Pancratium maritimum and the first report of 3-caffeoylquinic acid methyl ester in the<br />family Amaryllidaceae.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
PREPARATION AND EVALUATION OF CONTROLLED-RELEASE SODIUM VALPROATE / VALPROIC ACID (VALDISOVAL) TABLETS
179
186
65482
10.21608/bfsa.2003.65482
EN
Sayed H.
Khidr
Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Journal Article
2003
09
28
Valdisoval (VL) is a mixture of sodium valproate (SV) and valproic acid (VA) in a 2:1<br />ratio. Different polymers were used to develop a controlled-release tablet formulation for VL<br />using either direct compression or wet granulation techniques. Eudragits RSPO and RLPO in<br />different concentrations were used as direct compression and rate controlling polymers, while<br />ethyl cellulose (EC), hydroxy propyl methyl cellulose (HPMC) and hydroxy ethyl cellulose<br />(HEC) were used as release retardants in the wet granulation matrix formulations. Tablets<br />prepared showed good physical properties; e.g. hardness, friability, weight variations, using<br />different polymers by direct compression and wet granulation techniques. The release profile of<br />SV from the compressed tablets was studied using the USP dissolution apparatus II at 100 rpm<br />in either distilled water for 8 hours or in 0.1 N HCl for one hour followed by phosphate buffer,<br />pH 6.8 for another 7 hours. Sodium valproate release was found to decrease by increasing the<br />concentration of Eudragit RSPO in the formula and was less affected by the concentration of<br />Eudragit RLPO.The release of SV from the tablets containing ethyl cellulose as tablet matrix<br />was affected by the type of the binder in the wet granulation process. This was indicated by the<br />difference in T50% (time for 50% of the drug to be released). HEC was used as a release<br />retardant in a concentration range 10 to 25% w/w. The release of SV from these tablets was<br />inversely proportional to HEC concentration in the formula.Tablets containing 12.5% w/w of<br />this polymer were film coated using Eudragit L100-55.When the release profile of SV from these<br />tablets was compared to a marketed product (Depakine ChronoR) under the same conditions, an<br />almost identical dissolution pattern was found. Zero order release kinetics was elucidated from<br />the dissolution data.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
PHARMACOKINETICS AND PHARMACODYNAMICS EVALUATION OF PREPARED ZINC ASPIRIN SUPPOSITORIES
187
199
65483
10.21608/bfsa.2003.65483
EN
Fergany A.
Mohamed
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Saida A.
Aly
Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Egypt
Hamdy M.
Abdel-Rahman
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University,
Assiut Egypt
Journal Article
2003
10
08
In an attempt to reduce the gastrointestinal side effects of aspirin, zinc aspirin complex<br />was prepared and formulated into suppositories. The prepared suppositories were evaluated invitro<br />for their hardness, melting range, uniformity of weight and drug content and in-vivo drug<br />release.<br />The pharmacokinetic and pharmacodynamic properties of zinc aspirin were evaluated in<br />comparison with that of aspirin and aspirin lysinate (aspegic) following rectal and oral<br />administration in experimental animals. Blood samples were collected at different time intervals<br />after adminstration of drugs under evaluation. Salicylic acid (main metabolite of aspirin) was<br />determined in plasma by using high performance liquid chromatography (HPLC). The antiinflammatory<br />activity was studied in albino rats using carrageenan oedema model; and the<br />analgesic activity was studied using hot plate and writhing methods.<br />The results revealed that following rectal administration, the bioavailability of zinc aspirin<br />was significantly (P<0.05) greater than that of aspirin and aspirin Lysinate. The absolute bioavailabilities were 94, 88.89 and 83.63 for zinc aspirin; aspirin lysinate and aspirin<br />respectively. The peak plasma concentration (Cmax) were 54.5188, 50.271.68 and 48.091.15<br />ugl-1 for zinc aspirin, aspirin lysinate and aspirin, respectively. There was significant difference<br />in the tmax. The area under the plasma concentration-time curve (AUC) values were<br />148.932.79, 140.832.3 and 132.493.56 ug.h/ml for zinc aspirin, aspirin lysinate and<br />aspirin, respectively. There were significant differences in the Cmax, tmax and AUC following oral<br />administration. The anti-inflammatory and analgesic studies revealed that zinc aspirin<br />administered rectally or orally was more effective as anti-inflammatory and analgesic. The invivo<br />studies were correlated with the in-vitro release studies of aspirin from the prepared<br />suppositories.<br />Based on the obtained results, the authors recommend the possible use of zinc aspirin as a<br />substitute of aspirin containing products.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
31
PHYTOCHEMICAL INVESTIGATION OF OCIMUM BASILICUM L. AND ITS HYPOTENSIVE AND CARDIOVASCULAR ACTIVITY
201
205
65484
10.21608/bfsa.2003.65484
EN
M. H.
Assaf
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
2003
11
12
Investigation of the lipid contents of Ocimum basilicum L. herb revealed the presence of <br />& amyrins, -sitosterol, stigmasterol and ursolic acid besides nine fatty acids, the majors<br />were oleic, linoleic, palmitic and Linolinic acids. Forskolin diterpenoid was isolated and<br />identified from the semipurified extract. The hypotensive and cardiovascular effects of both<br />ethanolic and the semipurified extract of the herb was similar to that of Forskolin.
Assiut University, Faculty of Pharmacy
Bulletin of Pharmaceutical Sciences Assiut University
1110-0052
26
2
2003
12
01
MACRO- AND MICROMORPHOLOGY OF THE STEM AND LEAF OF CALLIANDRA HAEMATOCEPHALA (HASSK.) CULTIVATED IN EGYPT
153
170
208202
10.21608/bfsa.2003.208202
EN
N.
A. El-Emary
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M.
A. Makboul
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M.
A. Abdel-Hafiz
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
M.
M. Magdy
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut, Egypt
Journal Article
2003
05
21