Jun 26, 2007

Vitrification from solution in restricted space: formation and stabilization of amorphous nifedipine in a nanoporous silica xerogel carrier

International Journal of Pharmaceutics
Aljaz GodecJanko Jamnik

Abstract

The goal was to find thermodynamic criteria that must be satisfied in order to prevent formation of crystalline state of drugs within a confined space (e.g., nanopores of inorganic solid). Similarly, criteria that lead to stabilization of amorphous drug within such pores were investigated. In the theoretical part, the classical thermodynamics of nucleation is applied to the conditions of a restricted space. The theoretical findings are verified using porous silica as a carrier and nifedipine as a model drug. The amorphicity of the latter is checked using XRD and thermal analysis (DTA, DSC) in combination with BET measurements. It is shown that there exists a critical pore radius of a host below which the entrapped substance will solidify in an amorphous form. There also exists a critical pore radius below which the entrapped amorphous solid will not be able to crystallize. Specifically, incorporation of NIF into a silica xerogel with an average pore diameter of about 2.5 nm produces and stabilizes its amorphous form. Entrapment of drugs into solid nanoporous carriers could be regarded as a potentially useful and simple method for production and/or stabilization of non-crystalline forms of a wide range of drugs.

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Mentioned in this Paper

Embryo
Muscle Rigidity
Drug Carriers
Fluctuation
Ethanol
Nifedipine
Ethanol Measurement
Entire Embryo
Citricum acidum, citric acid, homeopathic preparation
Powder Diffraction

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