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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 Flory interaction parameter of drug molecules and polymer segments χ represents the energy difference between the inter-species (i.e., drug–polymer) contact interaction (right) and the average self-contact interactions (drug–drug and polymer–polymer) (left).
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f0020: The Flory interaction parameter of drug molecules and polymer segments χ represents the energy difference between the inter-species (i.e., drug–polymer) contact interaction (right) and the average self-contact interactions (drug–drug and polymer–polymer) (left).

Mentions: A drug–polymer phase diagram can be constructed using the Flory–Huggins polymer solution theory9,14. Taking the volume of a drug molecule as the unit lattice volume, the free energy change associated with mixing a polymer and small molecule is given by27(3)ΔGΚT=ϕlnϕ+(1−ϕ)mln(1−ϕ)+χϕ(1−ϕ)where K is the Boltzmann constant, T is the absolute temperature, ϕ is the volume fraction of drug in the solid dispersion (i.e., the drug loading), m is the volume ratio between polymer and drug, and χ is the Flory drug–polymer interaction parameter representing the difference between the drug–polymer contact interaction (Fig. 4, right) and the average self-contact interactions of drug–drug and polymer–polymer (Fig. 4, left). For example, hydrogen-bond formation between drug and polymer chains [e.g., in the fenbufen/poly(vinylpyrrolidone) pair] may make it more energetically favorable for the drug and polymer to interact with each other rather than with themselves, resulting a negative interaction parameter.


Fundamental aspects of solid dispersion technology for poorly soluble drugs.

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

The Flory interaction parameter of drug molecules and polymer segments χ represents the energy difference between the inter-species (i.e., drug–polymer) contact interaction (right) and the average self-contact interactions (drug–drug and polymer–polymer) (left).
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0020: The Flory interaction parameter of drug molecules and polymer segments χ represents the energy difference between the inter-species (i.e., drug–polymer) contact interaction (right) and the average self-contact interactions (drug–drug and polymer–polymer) (left).
Mentions: A drug–polymer phase diagram can be constructed using the Flory–Huggins polymer solution theory9,14. Taking the volume of a drug molecule as the unit lattice volume, the free energy change associated with mixing a polymer and small molecule is given by27(3)ΔGΚT=ϕlnϕ+(1−ϕ)mln(1−ϕ)+χϕ(1−ϕ)where K is the Boltzmann constant, T is the absolute temperature, ϕ is the volume fraction of drug in the solid dispersion (i.e., the drug loading), m is the volume ratio between polymer and drug, and χ is the Flory drug–polymer interaction parameter representing the difference between the drug–polymer contact interaction (Fig. 4, right) and the average self-contact interactions of drug–drug and polymer–polymer (Fig. 4, left). For example, hydrogen-bond formation between drug and polymer chains [e.g., in the fenbufen/poly(vinylpyrrolidone) pair] may make it more energetically favorable for the drug and polymer to interact with each other rather than with themselves, resulting a negative interaction parameter.

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.