National Organization of Drug Control and Research

Al Jīzah, Egypt

National Organization of Drug Control and Research

Al Jīzah, Egypt
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Abdel-Bar H.M.,National Organization of Drug Control and Research | Abdel-Reheem A.Y.,National Organization of Drug Control and Research | Awad G.A.S.,Ain Shams University | Mortada N.D.,Ain Shams University
Journal of Pharmacy and Pharmaceutical Sciences | Year: 2013

PURPOSE: The aim of the study was to target clonazepam, a CNS active drug, to the brain through the non-invasive intranasal (in) route using of nanocarriers with proven safety METHOD: in clonazepam nanocarriers were prepared by mixing isopropyl myristate, Tween 80, Cremophor EL or lecithin, polyethylene glycol 200, propylene glycol or ethanol in different ratios with water. in-vitro characterization of the nanocarriers was done by various methods including: polarized light microscopy, particle size determination, viscosity measurements and drug release studies. in-vivo study comparing intranasal and intravenous administration was performed. The drug targeting efficiency (DTE %) and direct nose to brain transport percentage (DTP %) were calculated and nasal integrity assessment was carried out. RESULTS: The obtained formulae had particle size below 100 nm favoring rapid direct nose to brain transport and the time for 100% drug release (T100%) depended on systems composition. Plasma Tmax of clonazepam nanostructured carriers varied from 10-30 min., while their brain Tmax did not exceed 10 min, in comparison with 30 min for iv solution. Although there was no significant difference (p>0.05) between the plasma AUC0-∞ of the different tested nanocarriers and intravenous one, the increase in brain AUC 0 -∞ of different nasal formulations in comparison to that of iv administration (3.6 -7.2 fold) confirms direct nose to brain transport via olfactory region. Furthermore, DTE and DTP% confirmed brain targeting of clonazepam following intranasal administration. CONCLUSION: The results confirmed that intranasal nanocarriers were proved to be safe alternative for iv clonazepam delivery with rapid nose to brain transport.


Nashwahgadallah M.,Princess NourahbintAbdelrahman University | Nashwahgadallah M.,National Organization of drug control and research
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2014

Objective: The main objective of current study is to develop and validate a selective HPLC method for determination of the studied drugs either in single or in mixture form. The method is rapid, precise, accurate and specific for the separation and determination of sitagliptin phosphate,metforminhydrochloride, and atorvastatin calcium in pure form and in pharmaceutical formulations in presence of quetiapine as an internal standard. Methods: This method is based on HPLC separation of the three drugs onHyperSil GOL column (150×4.6mm, 5μ). The mobile phase-A was prepared by mixing buffer (containing 1% of concentratednitric acid 65% and 2% of concentrated ammonia solution 28-32%, pH ≈8.5) and methanol in the ratio 30: 70. The flow rate is 1 ml/min, with isocratic elution and UV detection at 254nm. The retention time of each of sitagliptin phosphate, metformin hydrochloride, atorvastatin, quetiapine internal standard was found to be at3.384, 2.640, 4.837 or 6.000 min. respectively. Results: the proposed method was successfully applied for the quantitative determination of each of sitaglipitin, metformin and atorvastatin as single component or as combined mixture. The linear regression analysis data for calibration plots showed a good linear relationship over a concentration range of3.125-100 μg/ml for sitagliptin, 0.625-25 μg/ml for metformin, and 0.3125-10μg/mlfor atorvastatin. The mean values of the correlation coefficient, slope and intercept were 0.9976, 96.92 and +274.21 for sitagliptin,0.9995, 218.82 and +14.97 for metformin, 0.9994, 828.87 and + 81.95 for atorvastatin. The method was validated as per the ICH guidelines. The limit of detection (LOD) and limit of quantification (LOQ) was0.82 and 2.46 μg/ml for sitagliptin, 0.4 and 1.2 μg/ml for metformin,and 0.09 and 0.27 μg/ml for atorvastatin. Conclusion: The developed and validated HPLC method and the statistical analysis showed that the method is repeatable and selective for the estimation of the three studied drugs in presence of quetiapine as an internal standard.


Abdel-Bar H.M.,University of Sadat CityMenoufia | el Basset Sanad R.A.,National Organization of Drug Control and Research
Biomedicine and Pharmacotherapy | Year: 2017

Resveratrol (RSV) is a natural polyphenolic compound with high affinity to hepatocytes. It has numerous benefits as anticancer, antioxidant, immunomodulatory and cardioprotective actions. Nevertheless, RSV therapeutic applications are hindered by its low solubility, light sensitivity and extensive first-pass metabolism. Cubosomes are colloidally stable dispersed liquid crystalline nanoparticles. The incorporation of RSV into cubosomes could overcome some of its physicochemical limitations. A Design-Expert® software was applied to optimize cubosomes in terms of particle size and encapsulation efficiency (EE%). The used model proved its suitability in predicting optimum cubosomal size. The prepared cubosomes showed an enhanced HepG2 cytotoxicity except at particle size of ≈20 nm. Different endocytic pathways mechanisms as macropinocytosis, clathrin-mediated endocytosis and caveolae-mediated endocytosis were identified in the cellular uptake of RSV cubosomes depending on particle size. Caveolae-mediated transport was shown to have a significant effect on RSV cubosomes internalization efficiency and cytotoxicity. © 2017 Elsevier Masson SAS


Eissa S.,Ain Shams University | Shabayek M.I.,National Organization of Drug Control and Research | Ismail M.F.,Cairo University | El-Allawy R.M.,National Organization of Drug Control and Research | Hamdy M.A.,Cairo University
IUBMB Life | Year: 2010

Bladder carcinoma is an important worldwide health problem. Both cystoscopy and urine cytology used in detecting bladder cancer suffer from drawbacks where cystoscopy is an invasive method and urine cytology shows low sensitivity in low-grade tumors. This study validates easier and less time-consuming techniques for the estimation of survivin and TIMP-2 in urine of bladder cancer patients to evaluate them in comparison with cytology. This study includes malignant (bladder cancer patients, n = 42), benign (patients with bilharzial cystitis, n = 22) and healthy (n = 21) groups. The studied groups were subjected to cystoscopic examination, detection of bilharzial antibodies, urine cytology, and estimation of urinary survivin by qualitative RT-nested PCR and TIMP-2 by ELISA. Significantly higher positivity rates of urinary survivin and TIMP-2 were observed in the malignant group compared with benign and healthy groups. On associating the two urinary markers with different clinicopathological factors, only TIMP-2 exerted significantly higher positivity rate in invasive stage (100%) than superficial stage (82.3%). Survivin showed 78.6% sensitivity, 95.3% specificity, 94.3% PPV, 82% NPV, and 87% accuracy. When combined with urine cytology, the sensitivity increased to 83.3%. While on applying the cutoff value of urinary TIMP-2 (<639.5 pg/mg protein), it showed 93% sensitivity, 83.7% specificity, 85% PPV, 92.3% NPV, and 88.2% accuracy. When combined with urine cytology, the TIMP-2 sensitivity remained 93%. On combining cytology with both urinary survivin and TIMP-2, the highest sensitivity was reached (98%). Survivin and TIMP-2 can be considered as potentially useful urine markers in early detection of bladder cancer. © 2010 IUBMB.


Hegazy M.A.E.-M.,Cairo University | Eissa M.S.,Egyptian Russian University | Abd El-Sattar O.I.,National Organization of Drug Control and Research | Abd El-Kawy M.,Cairo University
Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy | Year: 2014

Linezolid (LIN) is determined in the presence of its alkaline (ALK) and oxidative (OXD) degradation products without preliminary separation based on ultraviolet spectrophotometry using two-way chemometric methods; principal component regression (PCR) and partial least-squares (PLS), and three-way chemometric methods; parallel factor analysis (PARAFAC) and multi-way partial least squares (N-PLS). A training set of mixtures containing LIN, ALK and OXD; was prepared in the concentration ranges of 12-18, 2.4-3.6 and 1.2-1.8 μg mL-1, respectively according to a multilevel multifactor experimental design. The multivariate calibrations were obtained by measuring the zero-order absorbance from 220 to 320 nm using the training set. The validation of the multivariate methods was realized by analyzing their synthetic mixtures. The capabilities of the chemometric analysis methods for the analysis of real samples were evaluated by determination of LIN in its pharmaceutical preparation with satisfactory results. The accuracy of the methods, evaluated through the root mean square error of prediction (RMSEP), was 0.058, 0.026, 0.101 and 0.026 for LIN using PCR, PLS, PARAFAC and N-PLS, respectively. Protolytic equilibria of LIN and its degradation products were evaluated using the corresponding absorption spectra-pH data obtained with PARAFAC. The obtained pKa values of LIN, ALK and OXD are 5.70, 8.90 and 6.15, respectively. The results obtained were statistically compared to that of a reported HPLC method, and there was no significant difference between the proposed methods and the reported method regarding both accuracy and precision. © 2014 Elsevier Ltd. All rights reserved.


Hegazy M.A.-M.,Cairo University | Eissa M.S.,Egyptian Russian University | Abd El-Sattar O.I.,National Organization of Drug Control and Research | Abd El-Kawy M.M.,Cairo University
Journal of Pharmaceutical Analysis | Year: 2014

Simple, accurate, sensitive and validated UV spectrophotometric and chemometric methods were developed for the determination of imidapril hydrochloride (IMD) in the presence of both its alkaline (AKN) and oxidative (OXI) degradation products and in its pharmaceutical formulation. Method A is the fourth derivative spectra (D4) which allows the determination of IMD in the presence of both AKN and OXD, in pure form and in tablets by measuring the peak amplitude at 243.0 nm. Methods B, C and D, manipulating ratio spectra, were also developed. Method B is the double divisor-ratio difference spectrophotometric one (DD-RD) by computing the difference between the amplitudes of IMD ratio spectra at 232 and 256.3 nm. Method C is the double divisor-first derivative of ratio spectra method (DD-DR1) at 243.2 nm, while method D is the mean centering of ratio spectra (MCR) at 288.0 nm. Methods A, B, C and D could successfully determine IMD in a concentration range of 4.0-32.0 μg/mL. Methods E and F are principal component regression (PCR) and partial least-squares (PLS), respectively, for the simultaneous determination of IMD in the presence of both AKN and OXI, in pure form and in its tablets. The developed methods have the advantage of simultaneous determination of the cited components without any pre-treatment. The accuracy, precision and linearity ranges of the developed methods were determined. The results obtained were statistically compared with those of a reported HPLC method, and there was no significant difference between the proposed methods and the reported method regarding both accuracy and precision. © 2013 Xi'an Jiaotong University.


Mahmoud D.B.,National Organization of Drug Control and Research | Shukr M.H.,National Organization of Drug Control and Research | Bendas E.R.,Cairo University
International Journal of Pharmaceutics | Year: 2014

The current investigation was aimed to improve the solubility of poorly soluble drug, cilostazol (CLZ). Self-nanoemulsifying drug delivery system (SNEDDS) composed of oil, surfactant and co-surfactant for both oral and parenteral administration of CLZ was formulated. The components for SNEDDS were identified by solubility studies, and pseudo-ternary phase diagrams were plotted to identify the efficient self-emulsification regions. The optimum formula, composed of Capryol 90 as an oil phase, Cremophor EL as a surfactant, and Transcutol HP as a co-surfactant in a ratio of 19.8:30.5:49.7 by weight, was able to solubilize CLZ 2000 times higher than its solubility in water. This formula was able to form grade "A" nanoemulsion when diluted with water, resulted in emulsification time of 50 ± 1.1 s, particle size of 14.3 nm, PDI of 0.5 and % transmittance was 97.40% ± 0.65. It showed excellent in vitro dissolution of 93.1% and 81.5% after 5 min in 0.3% sodium lauryl sulphate solution and phosphate buffer pH 6.4, respectively when compared with the marketed tablet formulation and drug suspension as the tablets showed only 44.3% and 9.9% while CLZ suspension showed 33.9% and 8.8% in 0.3% sodium lauryl sulphate solution and phosphate buffer pH 6.4, respectively. It was found to be robust to dilution, thermodynamically stable with low viscosity values of 14.20 ± 0.35 cP. In vivo study revealed significant increase in bioavailability of CLZ in rabbits to 3.94 fold compared with the marketed tablet formulation after oral administration. This formula could be sterilized by autoclaving and did not cause significant hemolysis to human blood which indicates its safety for intravenous administration with a 1.12 fold increase in bioavailability compared with its oral administration. Our study illustrated the potential use of SNEDDS of poorly soluble CLZ orally, and its successful administration of parenterally when required in acute cases of myocardial and cerebral infarction. © 2014 Elsevier B.V. All rights reserved.


Ksiksi T.,United Arab Emirates University | Hamza A.A.,United Arab Emirates University | Hamza A.A.,National Organization of Drug Control and Research
Molecules | Year: 2012

Acridocarpus orientalis (AO) is a traditional medicinal plant used for treatment of inflammatory diseases that may have potential in cancer treatment. In the present study, the aqueous ethanolic crude extract of Acridocarpus aerial parts obtained from Al Ain and Oman were evaluated for their antioxidant capability, polyphenolic content, anti-lipoxygenase and anti-histone deacetylase (HDAC) properties. The total antioxidant capacity was estimated by the FRAP, DPPH, ABTS and β-carotene bleaching assays. Acridocarpus-Al Ain exhibited the highest polyphenol content (184.24 mg gallic acid/g) and the best antioxidant activity (1.1, 1.04, 1.14 mmol ascorbic acid equivalent/g in the FRAP, ABTS and DPPH assays, respectively). Additionally, the same extract showed significant anti-inflammatory properties via lipoxygenase (LOX) inhibitory activity (IC 50 = 50.58 μg/mL). Acridocarpus-Al Ain also showed the strongest histone deacetylase (HDACs) inhibitory activity (IC 50 = 93.28 μg/mL). The results reported here suggest that there was a significant influence of location and the plant may be considered a good source of compounds with antioxidant, anti-LOX and HDAC properties for therapeutic, nutraceutical and functional food applications. © 2012 by the authors.


Hamza A.A.,United Arab Emirates University | Hamza A.A.,National Organization of Drug Control and Research
Food and Chemical Toxicology | Year: 2010

This study was carried out to evaluate the effect of Moringa oleifera Lam (Moringa) seed extract on liver fibrosis. Liver fibrosis was induced by the oral administration of 20% carbon tetrachloride (CCl4), twice weekly and for 8 weeks. Simultaneously, M. oleifera Lam seed extract (1 g/kg) was orally administered daily. The biochemical and histological results showed that Moringa reduced liver damage as well as symptoms of liver fibrosis. The administration of Moringa seed extract decreased the CCl4-induced elevation of serum aminotransferase activities and globulin level. The elevations of hepatic hydroxyproline content and myeloperoxidase activity were also reduced by Moringa treatment. Furthermore, the immunohistochemical study showed that Moringa markedly reduced the numbers of smooth muscle α-actin-positive cells and the accumulation of collagens I and III in liver. Moringa seed extract showed significant inhibitory effect on 1,1-diphenyl-2-picrylhydrazyl free radical, as well as strong reducing antioxidant power. The activity of superoxide dismutase as well as the content of both malondialdehyde and protein carbonyl, which are oxidative stress markers, were reversed after treatment with Moringa. Finally, these results suggested that Moringa seed extract can act against CCl4-induced liver injury and fibrosis in rats by a mechanism related to its antioxidant properties, anti-inflammatory effect and its ability to attenuate the hepatic stellate cells activation. © 2009 Elsevier Ltd. All rights reserved.


Mohamed N.G.,National Organization of Drug Control and Research | Mohamed M.S.,National Organization of Drug Control and Research
Journal of the Chilean Chemical Society | Year: 2010

Spectrophotometric procedures are presented for the determination of the antiparkinsonism drug entacapone. The first method based on the formation of a coloured complex of entacapone with ferric chloride in ethanolic solutions. The coloured product is quantified spectrophotometrically at 665nm. The other Spectrophotometric method determine entacapone in presence of levodopa and carbidopa (which formulated with entacapone in stalevo tablets) by measuring the UV absorbance of entacapone either in zero order at 391nm or in the first order by measuring the amplitude between 360nm and 402nm without any interference from levodopa and carbidopa. HPLC method is described for the separation and determination of entacapone, levodopa and carbidopa on Luna CN 150 × 4.6 column with UV detection at 390nm for entacapone and at 280nm for both levodopa and carbidopa. © 2010.

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