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Fundamental aspects of solid dispersion technology for poorly soluble drugs.

Huang Y, Dai WG - Acta Pharm Sin B (2013)

Bottom Line: The solid dispersion has become an established solubilization technology for poorly water soluble drugs.Since a solid dispersion is basically a drug-polymer two-component system, the drug-polymer interaction is the determining factor in its design and performance.In this review, we summarize our current understanding of solid dispersions both in the solid state and in dissolution, emphasizing the fundamental aspects of this important technology.

View Article: PubMed Central - PubMed

Affiliation: Key Laboratory of Advanced Materials (MOE), Department of Chemical Engineering, Tsinghua University, Beijing 100084, China.

ABSTRACT
The solid dispersion has become an established solubilization technology for poorly water soluble drugs. Since a solid dispersion is basically a drug-polymer two-component system, the drug-polymer interaction is the determining factor in its design and performance. In this review, we summarize our current understanding of solid dispersions both in the solid state and in dissolution, emphasizing the fundamental aspects of this important technology.

No MeSH data available.


The three possible structures of a drug/polymer solid dispersion where hexagonal symbols represent drug molecules and curvy lines represent polymer chains. (A) The ideal structure of a solid dispersion where the drug is molecularly dispersed in the polymer matrix; (B) a drug–polymer system in which crystalline drug formation has occurred and (C) a drug–polymer system containing amorphous drug-rich domains dispersed in the polymer matrix.
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f0005: The three possible structures of a drug/polymer solid dispersion where hexagonal symbols represent drug molecules and curvy lines represent polymer chains. (A) The ideal structure of a solid dispersion where the drug is molecularly dispersed in the polymer matrix; (B) a drug–polymer system in which crystalline drug formation has occurred and (C) a drug–polymer system containing amorphous drug-rich domains dispersed in the polymer matrix.

Mentions: Historically, the term “solid dispersion” was defined as a dispersion of drug in a solid matrix where the matrix was either a small molecule or polymer. The dispersed state has included many forms such as eutectic mixtures, crystalline/glass solutions, and amorphous/crystalline suspensions7,8. Taking account of its currently most-used form (Table 1), a solid dispersion can now be more narrowly defined as dispersion of drug in an amorphous polymer matrix where the drug is preferably in the molecularly dispersed state (i.e. as a glass solution to use the old term, Fig. 1A). The following discussion is limited to systems that fit this more limited definition.


Fundamental aspects of solid dispersion technology for poorly soluble drugs.

Huang Y, Dai WG - Acta Pharm Sin B (2013)

The three possible structures of a drug/polymer solid dispersion where hexagonal symbols represent drug molecules and curvy lines represent polymer chains. (A) The ideal structure of a solid dispersion where the drug is molecularly dispersed in the polymer matrix; (B) a drug–polymer system in which crystalline drug formation has occurred and (C) a drug–polymer system containing amorphous drug-rich domains dispersed in the polymer matrix.
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4590721&req=5

f0005: The three possible structures of a drug/polymer solid dispersion where hexagonal symbols represent drug molecules and curvy lines represent polymer chains. (A) The ideal structure of a solid dispersion where the drug is molecularly dispersed in the polymer matrix; (B) a drug–polymer system in which crystalline drug formation has occurred and (C) a drug–polymer system containing amorphous drug-rich domains dispersed in the polymer matrix.
Mentions: Historically, the term “solid dispersion” was defined as a dispersion of drug in a solid matrix where the matrix was either a small molecule or polymer. The dispersed state has included many forms such as eutectic mixtures, crystalline/glass solutions, and amorphous/crystalline suspensions7,8. Taking account of its currently most-used form (Table 1), a solid dispersion can now be more narrowly defined as dispersion of drug in an amorphous polymer matrix where the drug is preferably in the molecularly dispersed state (i.e. as a glass solution to use the old term, Fig. 1A). The following discussion is limited to systems that fit this more limited definition.

Bottom Line: The solid dispersion has become an established solubilization technology for poorly water soluble drugs.Since a solid dispersion is basically a drug-polymer two-component system, the drug-polymer interaction is the determining factor in its design and performance.In this review, we summarize our current understanding of solid dispersions both in the solid state and in dissolution, emphasizing the fundamental aspects of this important technology.

View Article: PubMed Central - PubMed

Affiliation: Key Laboratory of Advanced Materials (MOE), Department of Chemical Engineering, Tsinghua University, Beijing 100084, China.

ABSTRACT
The solid dispersion has become an established solubilization technology for poorly water soluble drugs. Since a solid dispersion is basically a drug-polymer two-component system, the drug-polymer interaction is the determining factor in its design and performance. In this review, we summarize our current understanding of solid dispersions both in the solid state and in dissolution, emphasizing the fundamental aspects of this important technology.

No MeSH data available.