Spray Congealing: An Emerging Technology to Prepare Solid Dispersions with Enhanced Oral Bioavailability of Poorly Water Soluble Drugs

被引:40
|
作者
Bertoni, Serena [1 ]
Albertini, Beatrice [1 ]
Passerini, Nadia [1 ]
机构
[1] Univ Bologna, Dept Pharm & BioTechnol, Via S Donato 19-2, I-40127 Bologna, Italy
来源
MOLECULES | 2019年 / 24卷 / 19期
关键词
spray chilling; spray cooling; microparticles; solubility enhancement; dissolution rate; polyethylene glycol; poloxamer; Gelucire((R)); IN-VITRO MODELS; POLOXAMER; 407; MICROSPHERES; MECHANOCHEMICAL ACTIVATION; PHARMACEUTICAL COCRYSTALS; AMORPHOUS DISPERSIONS; VIVO PERFORMANCE; GELUCIRE; 50/13; PART II; MICROPARTICLES; DISSOLUTION;
D O I
10.3390/molecules24193471
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The low and variable oral bioavailability of poorly water soluble drugs remains a major concern for the pharmaceutical industry. Spray congealing is an emerging technology for the production of solid dispersion to enhance the bioavailability of poorly soluble drugs by using low-melting hydrophilic excipients. The main advantages are the absence of solvents and the possibility to obtain spherical free-flowing microparticles (MPs) by a relatively inexpensive, simple, and one-step process. This review aims to fully describe the composition, structure, physico-chemical properties, and characterization techniques of spray congealed-formulations. Moreover, the influence of these properties on the MPs performance in terms of solubility and dissolution enhancement are examined. Following, an overview of the different spray congealed systems developed to increase the oral drug bioavailability is provided, with a focus on the mechanisms underpinning the bioavailability enhancement. Finally, this work gives specific insights on the main factors to be considered for the rational formulation, manufacturing, and characterization of spray congealed solid dispersions.
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页数:21
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