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Controlled Release Systems Containing Solid Dispersions: Strategies and Mechanisms

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ABSTRACT

In addition to a number of highly soluble drugs, most new chemical entities under development are poorly water-soluble drugs generally characterized by an insufficient dissolution rate and a small absorption window, leading to the low bioavailability. Controlled-release (CR) formulations have several potential advantages over conventional dosage forms, such as providing a uniform and prolonged therapeutic effect to improve patient compliance, reducing the frequency of dosing, minimizing the number of side effects, and reducing the strength of the required dose while increasing the effectiveness of the drug. Solid dispersions (SD) can be used to enhance the dissolution rate of poorly water-soluble drugs and to sustain the drug release by choosing an appropriate carrier. Thus, a CR-SD comprises both functions of SD and CR for poorly water-soluble drugs. Such CR dosage forms containing SD provide an immediately available dose for an immediate action followed by a gradual and continuous release of subsequent doses to maintain the plasma concentration of poorly water-soluble drugs over an extended period of time. This review aims to summarize all currently known aspects of controlled release systems containing solid dispersions, focusing on the preparation methods, mechanisms of action and characterization of physicochemical properties of the system.

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Abbreviations

AAS:

atomic absorption spectroscopy

AES:

atomic emission spectroscopy

CLSM:

confocal laser scanning microscopy

CR:

controlled release

CR-SD:

controlled-release solid dispersion

DSC:

differential scanning calorimetry

EC:

ethylcellulose

EPRI:

electron paramagnetic resonance imaging

FTIR:

fourier transformed infrared spectroscopy

HPMC:

hydroxypropyl methylcellulose

HEC:

hydroxyethyl cellulose

HPC:

hydroxypropyl cellulose

ICP spectrometry:

inductively coupled plasma spectrometry

IR-SD:

immediate-release solid dispersion

MRI:

magnetic resonance imaging

NIR imaging:

near infrared imaging

NMR:

nuclear magnetic resonance

NSESD:

non-self-emulsifying solid dispersion

PCS:

photon correlation spectroscopy

PEG:

polyethylene glycol

PEO:

polyethylene oxide

PVP:

polyvinyl pyrrolidone

pHM :

microenvironmental pH

PXRD:

powder X-ray diffraction

SD:

solid dispersion

SEM:

scanning electron microscopy

SESD:

self-emulsifying solid dispersion

TEM:

transmission electron microscopy

Tg :

glass transition temperature

TMDSC:

temperature modulated differential scanning calorimetry

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ACKNOWLEDGMENTS

This work was supported by the Ministry of Education, Science and Technology and by a grant from the Korean Health Technology R&D Project, Ministry for Health and Welfare (A092018).

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  1. Bioavailability Control Laboratory, College of Pharmacy, Kangwon National University, 1 University Road, Hyoja-Dong, Chuncheon, 200-701, Republic of Korea

    Phuong Ha-Lien Tran, Thao Truong-Dinh Tran, Jun Bom Park & Beom-Jin Lee

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Tran, P.HL., Tran, T.TD., Park, J.B. et al. Controlled Release Systems Containing Solid Dispersions: Strategies and Mechanisms. Pharm Res 28, 2353–2378 (2011). https://doi.org/10.1007/s11095-011-0449-y

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