PubMed · 11838817
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Deepak Agrawal. 2002. Vasospasm.. https://pubmed.ncbi.nlm.nih.gov/11838817/
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Conditions under which poly(ethyl acrylate, methyl methacrylate) 2:1 (poly(EA-MMA), Eudragit NE) forms a stable matrix were investigated in tablets with diclofenac sodium (DS) as an active substance. DS was granulated with the aqueous polymer dispersion. Granules and/or tablets were cured under various temperature and humidity conditions. A six position rotating disk (200 rpm) apparatus was used for the release studies conducted in 37 degrees C acid then phosphate buffer (0.4 M) pH 6.8 or buffer only as the dissolution media. Morphological characteristics of the tablet surface were observed under SEM. Changes in tablet structure upon curing were evaluated through changes in tablet mechanical characteristics. Modulus of rupture, Young's modulus, AUC, AUC( max), where AUC=AUC( max), were determined by the three-point bending test. Some poorly cured tablets dose-dumped when placed directly into buffer but not if first placed in acid and then buffer. A higher content of polymer in the matrix, led to formation of a stronger polymer network upon higher curing temperature and/or longer curing duration, whereas relative humidity had a minor effect.
Given the major role of elevated blood pressure in the pathogenesis of both stroke and coronary heart disease, one of the biggest challenges facing public health authorities and medical practitioners is the control of hypertension worldwide, both in individual patients and at the population level. The prevalence of hypertension increases with age and is nearly 60% in people aged 65 - 74 years. With increasing age, polymorbidity and polypharmacy usually contribute to an increasingly complex approach to manage the respective clinical conditions, including the treatment of hypertension. All subgroups of calcium channel blockers are effective and well-tolerated in lowering blood pressure. They are of demonstrated benefit for the prevention of stroke in elderly patients with systolic hypertension. Calcium channel blockers are particularly recommended for elderly patients with systolic hypertension and for black patients. The nifedipine gastrointestinal therapeutic system (GITS) formulation provides a once-daily dosing regimen with a continuous and slow release of the drug, resulting in a smooth plasma concentration/time profile. The INSIGHT study established that nifedipine GITS decreased mortality and morbidity at the same level as standard diuretic treatment in hypertensive patients with additional risk factors. A subgroup analysis showed that the long-term protective effects of nifedipine GITS extended to hypertensive patients with diabetes mellitus and with previous myocardial infarction. Two substudies of INSIGHT showed that nifedipine slowed the progression of atherosclerosis in carotid arteries (intima-media thickness) and coronary arteries (coronary calcium) as compared to diuretic.
Human serum albumin (HSA) was encapsulated as a model protein in microspheres of biodegradable and biocompatible polymers by the water-in-oil-in-water (w/o/w) emulsion solvent extraction/evaporation (double emulsion) technique for purpose of controlled release. To improve the properties and control the rate of drug release of the delivery vehicle, materials with different hydrophobicity from that of their conventional counterparts, such as poly(lactide-co-ethylene glycol) (PELA) in place of poly(lactide-co-glycolide) (PLGA) as the polymer matrix, ethyl acetate/acetone in place of dichloride methane (DCM) as the (co)solvent and d-alpha tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) as the additive, were used to prepare the microspheres. It has been found that PELA microspheres, compared with PLGA ones, were slightly smaller in size if prepared at identical emulsification strength. They had more porous surface and internal structure, higher encapsulation efficiency (EE) and more rapid in vitro release rate. Furthermore, the physical properties of the microspheres were also affected by the presence of solvents and additives and their properties. Our results suggest that these materials could have interesting potential applications in preparation of polymeric microspheres for controlled protein release.