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1.
Eur J Pharm Sci ; 32(3): 216-22, 2007 Nov.
Article in English | MEDLINE | ID: mdl-17826966

ABSTRACT

The aim of the present paper was the use of mesoporous silicate MCM-41 to increase the dissolution rate of piroxicam, a non-steroidal anti-inflammatory drug-class II of the Biopharmaceutic Classification System. The inclusion/adsorption compound of piroxicam in MCM-41 was obtained with a drug loading of about 14%. X-ray powder diffraction and differential scanning calorimetry (DSC) revealed the presence of piroxicam not arranged in crystalline form and FT-IR spectroscopy showed the presence of light interactions (hydrogen bonds) between the silicate silanols and the drug. The decrease of Brunauer, Emmett and Teller (B.E.T.) specific surface area and pore volume between free MCM-41 and the inclusion/adsorption compound was a prove of the presence of piroxicam inside the mesopores. The inclusion compound was submitted to in vitro dissolution tests and a remarkable dissolution rate improvement was observed in comparison to the crystalline drug in all tested conditions. The dissolution profile at pH 1.2 was comparable to that of the marketed product Brexin, a formulation with rapid analgesic effect onset. The improvement of dissolution rate is due to both the lack of drug in the crystalline form and to the extremely large surface area of the siliceous support. Physical stability tests of the free drug and the inclusion/adsorption complex were conducted as well over one month storage at 40 degrees C at different relative humidity.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemistry , Drug Carriers , Piroxicam/chemistry , Silicon Dioxide/chemistry , Calorimetry, Differential Scanning , Chemistry, Pharmaceutical , Crystallography, X-Ray , Drug Compounding , Drug Stability , Drug Storage , Humidity , Hydrogen-Ion Concentration , Kinetics , Porosity , Solubility , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared , Surface Properties , Temperature , Thermogravimetry
2.
Protoplasma ; 227(2-4): 113-8, 2006 May.
Article in English | MEDLINE | ID: mdl-16736253

ABSTRACT

Nuclear DNA amounts were measured by Feulgen cytophotometry in Sorghum bicolor cv. 610 plants early exposed to 150 mM NaCl, a treatment known to induce an increased tolerance to salinity in plants carrying this genotype. In salt-treated plants, the percentages of 8C, 16C, and 32C nuclei in roots in the primary state of growth were 21.9%, 13.3%, and 4.3%, respectively. By contrast, in nonsalinized plants, only 3.5% of the nuclei had an 8C content and no higher DNA contents were observed. The salt treatment induced chromosome endoreduplication during the differentiation of cells in the root cortex, where 41.2% of the cells displayed a DNA content higher than 4C (versus 1.3% in control plants). No enhancement of endopolyploidy was observed in cells of the root vascular cylinder or the leaves of the salt-treated plants. In another S. bicolor genotype (DK 34-Alabama), noncompetent for salt adaptation, the same NaCl treatment did not induce chromosome endoreduplication in root cortex cells. Endopolyploidy may be considered as a part of the adaptive response of S. bicolor competent genotypes to salinity.


Subject(s)
Adaptation, Physiological/drug effects , Chromosomes, Plant/drug effects , Gene Duplication/drug effects , Sodium Chloride/pharmacology , Sorghum/drug effects , Sorghum/genetics , Cell Nucleus/metabolism , Chromosomes, Plant/genetics , DNA, Plant/metabolism , Plant Roots/drug effects
3.
Farmaco ; 56(5-7): 421-5, 2001.
Article in English | MEDLINE | ID: mdl-11482770

ABSTRACT

A microporous material obtained from kanemite, a layered polysilicate, was studied in order to investigate its feasibility of including drugs and then releasing them. Diphenydramine hydrochloride was chosen as a model drug. The preparation of the microporous material and its loading with the drug are described. As kanemite is able to intercalate anions between its layers, the intercalation compound of diphenydramine and kanemite was also prepared. Both the drug-loaded microporous material and the intercalation compound were submitted to dissolution tests at pH 7.5. The drug release profiles from these two different materials and from a physical mixture were compared.


Subject(s)
Excipients , Silicates/chemistry , Diphenhydramine/chemistry , Intercalating Agents/chemistry , Porosity , Solubility , Solvents , X-Ray Diffraction
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