Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
COMPARATIVE STUDY OF THE PROTECTIVE EFFECT OF SILYMARIN AND COLCHICINE IN INDUCED LIVER FIBROSIS
1
13
EN
Asmaa
El-Kersh
Export Regulatory Affairs Section Head at Future Pharmaceutical Industries
10.21608/ajps.2016.6685
https://ajps.journals.ekb.eg/article_6685.html
https://ajps.journals.ekb.eg/article_6685_a3d5cac1779a87c6a488dcb66fc32ef5.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
STUDY OF THE ANTICANCER POTENTIAL OF CELERY SEED OIL AGAINST CHEMICALLY INDUCED HEPATOCELLULAR CARCINOMA IN RATS: A MECHANISTIC APPROACH.
14
28
EN
Omaima
Ahmedy
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Cairo, Egypt
10.21608/ajps.2016.6686
https://ajps.journals.ekb.eg/article_6686.html
https://ajps.journals.ekb.eg/article_6686_0353be55fabfbc08862b5c9ce22536b1.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
MONOCYTE CHEMOATTRACTANT PROTEIN-1 (MCP-1) IS ASSOCIATED WITH PANCREATIC BETA-CELL DYSFUNCTION IN TYPE 2 DIABETES MELLITUS
29
38
EN
Miral
Shehata
Biochemistry Department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
10.21608/ajps.2016.6888
https://ajps.journals.ekb.eg/article_6888.html
https://ajps.journals.ekb.eg/article_6888_8a28ec55c1091da7c6a44a4bc6b78c7d.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
DESIGN AND OPTIMIZATION OF CAPTOPRIL SUBLINGUAL TABLETS: ENHANCEMENT OF PHARMACOKINETIC PARAMETERS IN HUMAN
90
107
EN
Hossameldin
Kadry
Department of pharmaceutics and Industrial Pharmacy,
Faculty of Pharmacy, Al-Azhar University
Abdelsattar
Omar
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Alsulaymanyah, Jeddah 21589, Saudi Arabia.
Farag
. Sherbiny
Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, 11884, Egypt
Alaa
Zaky
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Nasr City, Cairo, Egypt.
10.21608/ajps.2016.6889
Oral mucous membrane of drug delivery is considered to be a promising alternative to the oral route. Sublingual route is a useful when rapid onset of action is desired than orally administered tablets. The objective of this study was to develop the sublingual tablet of captopril and improve its bioavailability. Captopril is the drug of choice in treatment of hypertension crisis or acute heart failure. Improvement of drug absorption and bioavailability was achieved by decreasing the pH of the mouth using citric acid. A 3<sup>2</sup> full factorial design was applied to optimize the formulations. Nine batches were prepared and evaluated to developing and optimizing sublingual tablets of water soluble drug (captopril). The optimization design was used to obtained the concentration of mixture superdisintegrants X<sub>1</sub> (crosscarmellose sodium, crosspovidone and sodium starch glycolate at 1:1:1 ratio) and using microcrystalline cellulose containing silicon dioxide (Prosolv-SMCC®) as a diluent (X<sub>2</sub>). Disintegration time and t<sub>90</sub> values used as dependent variables for optimization to obtain the desirable optimized formula. According to the results, the selected variables have a strong influence on disintegration time and T<sub>90</sub> of captopril sublingual tablets. The lowest disintegration time (13.04 sec) and t<sub>90</sub> (2.78 min) were showed by sublingual formulations composed of 7.82 % of superdisintegrants combination (X<sub>1</sub>) with 30.50 % of prosolv-SMCC (X<sub>2</sub>). So, this formula was chosen as the optimized formula. The F-optimized formula was compared with the marketed tablet pharmaburst® formula. It is clear from the result that the F-optimize formula had a very significant lower disintegration time than F-pharmaburst (12.2 and 16.3 sec respectively), and t<sub>90</sub> (3.2 and 5.0 minute respectively). The pharmacokinetic parameter for the F-optimized showed a significant (<em>P </em>≤ 0.05) increase in maximum plasma concentration from 180.0 to 286.5ng/mL, and a shortening of the time taken to reach maximum plasma concentration to 45 min in comparison with the marketed tablet. Finally, the F-optimize improved oral absorption of captopril sublingual and a subsequent acceleration of clinical effect, which is favored for hypertensive crises and cardiac disorders.
bioavailability,oral absorption,sublingual tablets,Response surface design,captopril,crosscarmellose sodium,crosspovidone,sodium starch glycolate,Superdisintegrant
https://ajps.journals.ekb.eg/article_6889.html
https://ajps.journals.ekb.eg/article_6889_cf05b08aa06a5f74c8f548b52ae94ab3.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
SONOCHEMISTRY (APPLICATIONS OF ULTRASOUND IN CHEMICAL SYNTHESIS AND REACTIONS): A REVIEW PART I
108
122
EN
Menshawy
. Mohamed
Department of Pharmaceutical Chemistry, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box- 173, Al-Kharj 11942, Saudi Arabia. /bDepartment of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt
10.21608/ajps.2016.6890
<span>Sonochemistry is a powerful and green approach which is being used to accelerate synthesis of organic compounds, and involves the use of ultrasound technique to promote chemical reactions. Ultrasound is the part of the sonic spectrum, which ranges from about 20 KHz to 10 MHz. A large number of organic reactions can be carried out under ultrasonic irradiation in high yields, short reaction times, and mild conditions. Ultrasonic irradiation of liquids causes high energy chemical reactions to occur, often with the emission of light. The origin of sonochemistry and sonoluminescence is acoustic cavitation which is the formation, growth, and implosive collapse of bubbles. The collapse of bubbles caused by cavitation produces intense local heating and high pressures, with very short lifetimes (Hot spots). These hot-spots have an equivalent temperatures of roughly 5,000 K, pressures of about 1,000 atm, and increase reactivity by nearly million-fold using the radical mechanism. A variety of devices have been used for ultrasonic irradiation of solutions. </span>
Acoustic cavitation,Ultrasound,sonoluminescence,name reactions
https://ajps.journals.ekb.eg/article_6890.html
https://ajps.journals.ekb.eg/article_6890_898f5445b610dbeaac14afe2a58ccc69.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
PROTECTIVE EFFECT OF L-CARNITINE AGAINST CISPLATIN-INDUCED TESTICULAR TOXICITY IN RATS
123
142
EN
Ahmed
Eid
Department of Pharmacology, National Organization for Drug Control and Research (NODCAR), Giza, Egypt
10.21608/ajps.2016.6891
Testicular damage is one of the most deleterious effects whenever cisplatin (CIS) is employed in cancer chemotherapy. Oxidative stress has been proven to be involved in CIS induced toxicity. Thus, the current study explored the possible protective effect of L-carnitine (L-CAR) against cisplatin-induced testicular damage in rats. L-carnitine (500 mg/kg/day; i.p.) was injected for 15 days, whereas cisplatin (10 mg/kg; i.p.) was injected as a single dose at the 12<sup>th</sup> day to induce testicular damage in adult male Sprague-Dawley rats. In the current study, CIS reduced the reproductive organs weight, sperm count, sperm motility and serum testosterone level beside a marked increase in the incidence of sperm abnormalities. In addition, it significantly increased malondialdehyde (MDA) and nitric oxide (NO) along with a marked decrease in testis reduced glutathione (GSH) content and superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) activities. At the same time, CIS administration resulted in marked elevation in tumor necrosis factor-α (TNF-α) production and nuclear factor-kabba B (NF-κB) expression. These results were confirmed by histopathological examination. Treatment with L-CAR markedly attenuated cisplatin-induced injury by suppression of oxidative/nitrosative stress and inflammation, amendment of antioxidant defenses, as well as improvement of steroidogenesis, spermatogenesis and testicular histological features. This study suggests a novel therapeutic application for L-carnitine as a protective agent against cisplatin-induced testicular toxicity through its promising anti-inflammatory and antioxidant capacities.
Cisplatin,L-carnitine,Inflammation,Oxidative Stress,Testicular damage
https://ajps.journals.ekb.eg/article_6891.html
https://ajps.journals.ekb.eg/article_6891_6b1f1b9b87543896d7ba332dc823ae40.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
FORMULATION AND OPTIMIZATION OF VARDENAFIL HYDROCHLORIDE ORAL DISINTEGRATING TABLETS: EFFECT OF SUPERDISINTEGRANTS
39
57
EN
hamdy
Mourad
The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo, Egypt
Hossameldin
Kadry
Department of pharmaceutics and Industrial Pharmacy,
Faculty of Pharmacy, Al-Azhar University
10.21608/ajps.2016.6892
One of the fruitful results of oral technological advancement in dosage forms is the orally disintegrating tablets (ODTs) as they disintegrate rapidly in the mouth and do not require water for administration. This work employed mixture design approach for developing and optimizing oral disintegrating tablets of a slightly water soluble drug, vardenafil hydrochloride. Three component mixture design was used to optimize the type and concentration of superdisntegrants, crosscarmellose sodium (X<sub>1</sub>), crosspovidone (X<sub>2</sub>) and sodium starch glycolate (X<sub>3</sub>) using water soluble dextrates (Emdex<sup>®</sup>) as a filler. Disintegration time, wetting time and t<sub>90</sub> values for all formulations ranged from 33.69 to 208.68 s, 40.42 to 209.83 s and 80.04 to 484.63 s, respectively. According to the results, the selected variables have a strong influence on disintegration time, wetting time and t<sub>90</sub> of the ODTs. The lowest disintegration time, wetting time and t<sub>90</sub> were showed by ODTs formula composed of 1.72 % of crosscarmellose in combination with 4.28 % of crosspovidone. So, this formula was chosen as the optimized formula. Stability studies also showed that the optimized formula was stable under accelerated conditions. And, by comparing the selected formula with Prosolv<sup>®</sup> ODT G2 as a ready ODT system, it showed faster disintegration time and higher dissolution rate. Hence, the best superdisintegrants to be used with the water soluble dextrates are crosspovidone in combination with crosscarmellose sodium.
Oral disintegrating tablets,mixture design,vardenafil hydrochloride,dextrates (Emdex),Prosolv ODT,crosscarmellose sodium,crosspovidone,sodium starch glycolate
https://ajps.journals.ekb.eg/article_6892.html
https://ajps.journals.ekb.eg/article_6892_7bc1a8f3d1f3b4ad216d04b2179e51d7.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
DESIGN, SYNTHESIS AND IN VITRO EVALUATION OF ANTIBACTERIAL AND ANTIADHESIVE POTENTIALS OF SOME SUBSTITUTED IMIDAZOLONES DERIVATIVES OF CINNAMALDEHYDE
58
72
EN
Abdelsattar
Omar
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Alsulaymanyah, Jeddah 21589, Saudi Arabia.
10.21608/ajps.2016.6893
<em>The cells of microorganisms often stick together and adhere to biotic and inert surfaces to form coats (biofilms) that are impenetrable and often highly resistant to antibiotics, as well as being</em><em>adaptive to immune responses of the host. The aim of this study is to develop drugs that are able to prevent cell adhesion and/or penetrate biofilm layer and reach the bacteria to render them harmless. </em><em>trans</em><em>-Cinnamaldehyde, found in oils and cinnamon barks, and curcumin found in turmeric have been found to hold such pharmacologic properties. The newly developed product hybrids were evaluated for their ability to exert </em><em>in vitro</em><em> antibacterial activity as well as their potential as bacterial anti-adhesive agents on several different bacteria. </em>In summary, we have developed several novel compounds that show both antibacterial and anti-adhesive properties. Although the compounds are not as potent as the positive controls, they serve as lead for further structural modification to develop more potent derivatives.
Synthesis,Antibacterial,Bacterial Anti-adhesive,Biofilm,imidazolone,Cinnamaldehyde
https://ajps.journals.ekb.eg/article_6893.html
https://ajps.journals.ekb.eg/article_6893_57489c5b65b43b06fbcc59048f75961e.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
SYNTHESIS, BIOLOGICAL EVALUATION AND BINDING STUDIES OF NEW FLAVONE DERIVATIVES AS ADENOSINE A2B RECEPTOR ANTAGONISTS
73
89
EN
Farag
Sherbiny
Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, 11884, Egypt
10.21608/ajps.2016.6894
A series of eleven flavone derivatives were synthesized. The synthesized compounds were characterized structurally by various techniques using spectral analyses. All of the synthesized compounds were subjected to MTT proliferation assay to investigate their in-<em>vitro</em> cytotoxic activity. Among all the studied compounds, compounds, VIi, VIh, VId and VIk revealed moderate growth inhibitory effect towards the MDA-MB 231 cell line compared to the reference, doxorubicin. These compounds showed cytotoxicity activity with IC<sub>50</sub> values ranging from 43.7 to 138 µM in MDA-MB 231 cell line. The results of cytotoxic activity revealed that flavone derivatives with N-aryl acetamide substituted at the 3-position of flavone backbone have better cytotoxic activity. Moreover, the highest activity was observed with compound VIi that has oxy-N-pyriden-2-yl acetamide substituent at the 3-position of flavone backbone followed by compound VIh with IC<sub>50</sub> values of 43.7 and 50 μM, respectively. The biological activity results were elucidated by molecular docking studies using the homology model of the human adenosine A<sub>2B</sub> receptor. As a result, the present study has highlighted that the bicyclic moiety of the compounds attached to hydrogen bond donor-acceptor capability and π-π stacking is an attractive scaffold for obtaining cytotoxic activity.
Adenosine A2B Antagonists,Flavone Derivatives,antitumor activity,Molecular Docking Studies
https://ajps.journals.ekb.eg/article_6894.html
https://ajps.journals.ekb.eg/article_6894_07c039483bf5f0f43144875c98abd17f.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
BIOLOGICAL STUDIES ON ACTIVE COMPOUNDS FROM TRICHODERMA VIRIDE.
143
159
EN
mohamed
Mourad
The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo, Egypt.
10.21608/ajps.2016.6895
There has been some evidence to date suggesting that <em>Trichoderma</em> species. had several biological activities. To test antibacterial and antifungal activity, the secondary metabolites obtained by culturing the fungi <em>Trichoderma</em> <em>viride</em> RCMB 017002 on YES broth for 21 days were extracted using chloroform/methanol solvent system then screened by agar well diffusion method. Two fungal metabolites were isolated and purified from the chloroform/methanol (2:1) extract of <em>Trichoderma viride</em> broth culture using column chromatography. The chemical structures of the separated metabolites were elucidated using the spectroscopic methods FTIR, <sup>1</sup>HNMR and EI-MS analyses. The first compound was benzene diamine derivative produced from fraction 10 and showed good inhibitory activity against the tested bacteria, and tumor (against HepG2 & MCF-7) cells. Also, compound 1 showed moderate antiviral activity against herpes simplex type 1 virus along with no antifungal activities. However, compound 2 was with the known compound, 6-pentyl-α-pyrone that produced from fraction 17<br /> with broad spectrum antimicrobial activity as well as moderate antitumor activities and weak antiviral activity.This report demonstrates the biological activities of new fungal metabolites from <em>Trichoderma viride</em> as potential drug that need further studies and development.
Trichoderma viride,secondary metabolites,spectroscopic methods,Antibacterial,Antifungal,antiviral and antitumor
https://ajps.journals.ekb.eg/article_6895.html
https://ajps.journals.ekb.eg/article_6895_cf871e61fa073618c3a886d59c3d6487.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
EFFECT OF DIFFERENT DOSES OF PINOCEMBRIN ON CARBON TETRACHLORIDE-INDUCED HEPATOTOXICITY IN RATS
160
168
EN
Marwa
Said
Pharmacist at Central Administration for Pharmaceutical Affairs, Ministry of Health, Cairo, Egypt.
10.21608/ajps.2016.6896
Pinocembrin (PIN), a flavanone found abundantly in honey and propolis, has been reported to have many benefits and medicinal properties. However, its protective effects against carbon tetrachloride (CCl<sub>4</sub>) induced hepatotoxicity have not been clarified. The aim of the present study was to investigate the potential hepatoprotective dose of PIN on CCl<sub>4</sub> treated rats. PIN was screened at different doses (10, 20 and 40 mg/kg/day) orally for 7 days, against a single dose of CCl<sub>4</sub> (1 ml/kg, 1:1 mixture with corn oil, i.p.). PIN protected against CCl<sub>4</sub>-induced increase in hepatic transaminases, total cholesterol and histopathological changes. The dose of 20 mg/kg PIN was selected for further assessment to address the PIN hepatoprotective mechanisms.
Pinocembrin,Carbon tetrachloride,Liver fibrosis
https://ajps.journals.ekb.eg/article_6896.html
https://ajps.journals.ekb.eg/article_6896_981a1d607c4740a0caf29de70cae152e.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
INVESTIGATION OF THE POSSIBLE NEUROPROTECTIVE EFFECT OF AN ESTROGEN RECEPTOR BETA AGONIST AGAINST ROTENONE-INDUCED PARKINSON’S DISEASE IN RATS
169
180
EN
Rania
Salama
Pharmacology Department, Faculty of Pharmacy, Misr International University (MIU), Cairo, Egypt
10.21608/ajps.2016.6897
Parkinson's disease (PD) is the second most common neurodegenerative disorder. Androst-5-ene-3β, 17β-diol (ADIOL), an estrogen receptor (ER) β agonist, was found to induce a transrepressive mechanism, which selectively amend the extent of neuroinflammation and, in turn, neurodegeneration; nevertheless, its effect on PD has not yet been revealed. In consequence, our study was designed to examine the possible neuroprotective effect of ADIOL against a rotenone (ROT)-induced PD in rats. Reduction in the nuclear factor-kappa B (NF-κB) levels and the expression of down-stream inflammatory mediators was detected in the SN upon pre-treatment with ADIOL at the dose of 0.35 mg/kg/day. Likewise, light microscopy (LM) examination showed improvement in the number of viable neurons in the SN pars compacta (SNpc). In conclusion,the current study confirmed the ability of ADIOL to reduce neuroinflammation and, in turn, neurodegeneration process as well as motor impairment in PD.
https://ajps.journals.ekb.eg/article_6897.html
https://ajps.journals.ekb.eg/article_6897_17fed9c023692084ca5c3d7527e91d1a.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
PHARMACOLOGICAL EFFECTS OF GEMFIBROZIL ON SOME CARDIOVASCULAR PREPARATIONS OF EXPERIMENTAL ANIMALS
181
197
EN
Enass
Ouda
Assistant Professor of Pharmacology Faculty of Medicine (Girls) – Al-Azhar University
10.21608/ajps.2016.6914
Gemfibrozil (member of fibrates) is Peroxisome proliferator activated receptors (PPAR-α) agonist which improves lipid profiles particulary very low density lipoprotein and high density lipoprotein in patients with dyslipidemia.<strong>Objective:</strong> Studying the pharmacological effects of Gemfibrozil on some cardiovascular preparations of experimental animals. <strong>Materials and Methods:</strong> The experiments were conducted to study the effect of different doses of gemfibrozil on isolated perfused rabbit heart & coronary flow, isolated rabbit aortic spiral strip and mean arterial blood pressure of anaesthetized cats. Each experiment was done on six preparations. <strong>Results: <em>In-vitro study:</em> </strong>onisolated perfused rabbit heart, gemfibrozil (25-800µg/ml) produced a dose-dependent reduction on the amplitude of myocardial contractions. The inhibitory effect of gemfibrozil (100µg/ml) was not abolished after complete blockade of nicotinic and muscarinic receptors while it was completely abolished after inhibition of nitric oxide synthase by N-methyl L-arginine. On the other hand the stimulatory effects of calcium gluconate, isoprenaline, histamine and serotonin were not abolished after administration of gemfibrozil (100µg/ml). On coronary flow of isolated perfused rabbit heart, gemfibrozil (25-800μg/ml) produced also a dose-dependent reduction of coronary flow. On isolated spiral aortic strips of rabbit , gemfibrozil produced dose-dependent significant reduction on nor-epinpherine (NE) induced contraction. <strong><em>In-vivo study</em></strong> gemfibrozil produced a dose-dependent significant reduction in mean arterial blood pressure (MABP) of anaesthetized cats. <strong>Conclusion:</strong> Gemfibrozil produced a negative inotropic effect through nitric oxide release with a decrease in coronary flow. It also reduced NE- induced contractions of aortic spiral strips with reduction in mean arterial blood pressure. So it must me used cauciously in cases of heart failure, but it could be beneficial in hypertensive patient with atherosclerosis.
Gemfibrozil,Isolated Prefused Rabbit Heart,Aortic Spiral Strips Anaesthetized cats
https://ajps.journals.ekb.eg/article_6914.html
https://ajps.journals.ekb.eg/article_6914_78c9ff08c79377ab292783857971bec1.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
PHARMACOKINETIC EVALUATION OF A CHRONOTHERAPEUTIC SYSTEM LOADED WITH AN ANTIASTHMATIC DRUG AS AN ORAL DRUG DELIVERY SYSTEM
198
206
EN
Rasha
Elbatanony
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt.
10.21608/ajps.2016.6915
Recent studies proved that the symptoms of bronchial asthma follow the circadian rhythms and become worse in the early morning. In such cases, conventional sustained-release treatment regimens are inappropriate for the delivery of antiasthmatic drugs as they cannot be administrated just prior to the worsening of the symptoms. The current work aimed to explore the pharmacokinetics of a model antiasthmatic drug following oral administration of a chronotherapeutic system in six healthy volunteers. A sensitive and selective chromatoghraphic method was used to determine drug concentration in human plasma. A standard calibration curve of the drug over the concentration range of 0.15 - 80 µg/ml was prepared in human plasma. Anhydrous caffeine was used as an internal standard. The protocol of the studies was approved by the Research Ethics Committee for clinical studies at Faculty of Pharmacy, Cairo University, Egypt. Following oral administration of the treatments, the pharmacokinetic parameters of the drug including C<sub>max </sub>(µg/ml), T<sub>max</sub> (h), MRT<sub>(0– ∞)</sub>, (h), AUC<sub>0–24 </sub>(µg h/ml) and AUC<sub>0–∞</sub> (µg h/ml) were derived from the individual plasma concentration time curves. The data were statistically analyzed using two-way ANOVA at <em>P</em> < 0.05. The results confirmed that the drug reached C<sub>max</sub> rapidly within two hours following a definite lag time; confirming the potential of the developed chronotherapeutic system in promoting the drug absorption at its site of action at the required time.
antiasthmatic drug,circadian rhythm,Pharmacokinetics,pulsatile drug delivery system
https://ajps.journals.ekb.eg/article_6915.html
https://ajps.journals.ekb.eg/article_6915_93924b9215e05d659f974d96299ba7f5.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
DESIGN AND SYNTHESIS OF PHTHALAZINE BASED DERIVATIVES AS POTENTIAL ANTICANCER AGENTS
207
236
EN
Salwa
Elmeligie
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt
10.21608/ajps.2016.6917
In an attempt to develop novel targeted anticancer agents, a series of novel substituted phthalazine derivatives has been designed and synthesized as inhibitors of vascular endothelial growth factor receptor (VEGFR) kinase enzyme in accordance to SAR studies of known VEGFR inhibitors<em>. </em>The designed compounds incorporated a biarylamide or biarylurea tail linked to a phthalazine scaffold via an amino or ether linkage or else incorporated an N-substituted piperazine motif at position 1 of the phthalazine core. The prepared compounds were evaluated for their enzymatic inhibition of VEGFR-2 kinase. Furthermore, three of the phthalazines bearing a biarylurea (<strong>6b, 6e &7b</strong>) exhibited excellent broad spectrum cell growth inhibition against NCI full 60 cell panel with GI<sub>50</sub> values between 0.15-5μM. In addition, docking studies were performed through docking of the investigated compounds into VEGFR-2 binding site in order to gain further insight into their binding affinities and binding interactions with the VEGFR-2 kinase.
Substituted phthalazines,Cytotoxic activity,Kinase inhibitors,VEGFR-2
https://ajps.journals.ekb.eg/article_6917.html
https://ajps.journals.ekb.eg/article_6917_04bfa87dabab595a102e822d137d1fd8.pdf
Al-Azhar University, Faculty of Pharmacy
Al-Azhar Journal of Pharmaceutical Sciences
1110-1644
2535-1958
53
1
2016
03
01
SCREENING THE HEPATOPROTECTIVE DOSE OF DEFERIPRONE AGAINST CONCANAVALIN A-INDUCED ACUTE HEPATOTOXICITY
237
247
EN
Dalia
El-Khouly
Pharmacology & Toxicology Department, Faculty of Pharmacy, Future University, Cairo, Egypt
10.21608/ajps.2016.6919
Iron overload is one of mechanisms by which hepatitis C virus causes oxidative stress that may contribute to fibrosis and carcinogenesis in the liver. Chronic hepatitis C (CHC) virus infection is a leading cause of progressive liver fibrosis, liver cirrhosis and hepatocellular carcinoma. Liver fibrosis with high mortality rate after diagnosis and limited successful treatment. The present study was designed to screen the potential hepatoprotective dose of deferiprone (DFP) and whether it can attenuate hepatotoxicity induced by concanavalin A (con A) in rats. Male Wister rats were randomized into 6 groups and treated with Con A (20 mg/kg, once, i.v) and/ordeferiprone (5, 10, 25 or 40 mg/kg/day, one hour before con A). Liver enzymes levels were assessed in addition to histopathological examination of liver tissues. DFP (5 mg/kg) pre-treatment restored liver enzymes toward normal values. Moreover, histopathological examination confirmed the protective effect of this dose of DFP.
: Hepatotoxicity – deferiprone – concanavalin A
https://ajps.journals.ekb.eg/article_6919.html
https://ajps.journals.ekb.eg/article_6919_19b15a68b86ab187e8e9f6ea71debfb7.pdf