Current Issue : July - September Volume : 2018 Issue Number : 3 Articles : 5 Articles
Omeprazole (OME) is employed for treating ulcer in children, but is unstable and exhibits\nfirst pass metabolism via the oral route. This study aimed to stabilize OME within mucoadhesive\nmetolose (MET) films by combining cyclodextrins (CD) and L-arginine (L-arg) as stabilizing excipients\nand functionally characterizing for potential delivery via the buccal mucosa of paediatric patients.\nPolymeric solutions at a concentration of 1% w/w were obtained by dispersing the required weight of\nmetolose in 20% v/v ethanol as solvent at a temperature of 40 ââ??¦C using polyethylene glycol (PEG 400)\n(0.5% w/w) as plasticizer. The films were obtained by drying the resulting polymer solutions at in an\noven at 40 ââ??¦C. Textural (tensile and mucoadhesion) properties, physical form (differential scanning\ncalorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy),\nresidual moisture content (thermogravimetric analysis (TGA)) and surface morphology (scanning\nelectron microscopy (SEM)) were investigated. Optimized formulations containing OME, CDs (Ã?² or\nÃ?³) and L-arg (1:1:1) were selected to investigate the stabilization of the drug. The DSC, XRD, and\nFTIR showed possible molecular dispersion of OME in metolose film matrix. Plasticized MET films\ncontaining OME:Ã?²CD:L-arg 1:1:1 were optimum in terms of transparency and ease of handling and\ntherefore further functionally characterized (hydration, mucoadhesion, in vitro drug dissolution\nand long term stability studies). The optimized formulation showed sustained drug release that\nwas modelled by Korsmeyerââ?¬â??Peppas equation, while the OME showed stability under ambient\ntemperature conditions for 28 days. The optimized OME loaded MET films stabilized with Ã?²CD\nand L-arg have potential for use as paediatric mucoadhesive buccal delivery system, which avoids\ndegradation in the stomach acid as well as first pass metabolism in the liver....
As coprocessed excipients (CPE) gain a lot of focus recently, this article compares three commercially available CPE of Avicel brand,\nnamely, CE 15, DG, and HFE 102. Comparison is based on measured physical properties of coprocessed mixtures, respectively,\nflow properties, pycnometric density, mean particle size, specific surface area, moisture content, hygroscopicity, solubility, pH\nleaching, electrostatic charge, SEMimages, and DSC. Tablets were made employing three pressure sets. Viscoelastic properties and\nejection force were assessed during compression, as well as pycnometric density, mass uniformity, height, tensile strength, friability,\ndisintegration, andwetting times.Avicel CE 15 is of mid-range flowproperties, contains mid-size and nonspherical particles, and has\nhigh hygroscopicity, growing negative charge, best lubricity, lowest tensile strength, and mid-long disintegration times. Avicel DG\npossesses the worst flow properties, small asymmetrical particles, lowest hygroscopicity, stable charge, intermediate lubricity, and\ntensile strength and exhibits fast disintegration of tablets. Finally, Avicel HFE 102 has the best flow properties, large symmetrical\nparticles, and middle hygroscopicity and its charge fluctuates throughout blending. It also exhibits inferior lubricity, the highest\ntensile strength, and slow disintegration of tablets. Generally, it is impossible to select the best CPE, as their different properties fit\nversatile needs of countless manufacturers and final products....
The presented work describes the formulation and characterization of modified\nrelease glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model\nBCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by\nmelting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under\nstandard and biorelevant conditions, were compared to those obtained from commercially\navailable formulations containing nifedipine such as modified release (MR) tablets and\nosmotic release oral system (OROS). The results indicate that the dissolution profiles of the\nGSDFs with nifedipine are neither affected by the pH of the dissolution media, type and\nconcentration of surfactants, nor by simulated mechanical stress of biorelevant intensity.\nFurthermore, it was found that the dissolution profiles of the novel dosage forms were similar\nto the profiles obtained from the nifedipine OROS. The formulation of GSDFs is relatively\nsimple, and the dosage forms were found to have favorable dissolution characteristics....
Encapsulation protects iron from degradation or oxidation possibilities due to its\nencapsulation material. Glucomannan (GM) is a neutral polysaccharide consist of D-mannose\nand D-glucose connected with -1,4 linkage. Deactylation transforms solubility of glucomannan\nas well as its gel structure. These properties support for excipient application. The aim of this\nwork was to determine performance of deacetylated glucomannan as iron matrix. Deacetylation\nwas conducted heterogeneously. Deacetylation did not change the backbone of GM. Higher\nalkali concentration has better ability to encapsulate iron. Extended deacetylation time and alkali\nconcentration affect insignificantly on the performance of encapsulation to protect iron from\noxidation. The release of iron from the matrix influences by deacetylation degree....
Degradation of triamcinolone acetonide (TCA) in an ointment was investigated.\nTCA appeared to be concentrated in propylene glycol (PG) which in turn is dispersed\nin a lanolin-petrolatum mixture. Two predominant degradation products were identified: a\n21-aldehyde and a 17-carboxylic acid. The 21-aldehyde is formed after TCA is oxidized by\nO2, a reaction that is catalyzed by trace metals. Logically, the content of trace metals has a\nprofound effect on the degradation rate. It was shown that trace metals are extracted from\nlanolin and petrolatum by PG, increasing the concentration in PG. In accordance with these\nfindings, TCA degrades faster in PG that is present in the ointment formulation than in\nregular PG. The 21-aldehyde was confirmed to be a primary degradation product, while the\n17-carboxylic acid was identified as a secondary degradation product. Based on the\nmechanism of degradation, the ointment can be stabilized by the addition of sodium\nmetabisulfite which was shown to reside also in the PG phase within the ointment....
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