Drug release from liquisolid systems: speed it up, slow it down

被引:84
作者
Nokhodchi, Ali [1 ,2 ]
Hentzschel, Christina M. [3 ]
Leopold, Claudia S. [3 ]
机构
[1] Univ Kent, Medway Sch Pharm, Chem & Drug Delivery Grp, Chatham ME4 4TB, Kent, England
[2] Univ Greenwich, Medway Sch Pharm, Chem & Drug Delivery Grp, Chatham ME4 4TB, Kent, England
[3] Univ Hamburg, Inst Pharm, Dept Pharmaceut Technol, D-20146 Hamburg, Germany
关键词
compactibility; co-solvent; dissolution enhancement; flowability; liquisolid technology; solubility; sustained release; DISSOLUTION RATE ENHANCEMENT; POORLY SOLUBLE DRUGS; IN-VITRO; SOLID DISPERSIONS; SUSTAINED-RELEASE; WATER; INDOMETHACIN; TABLET; FORMULATION; BEHAVIOR;
D O I
10.1517/17425247.2011.548801
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
Introduction: Today, the properties of many new chemical entities have shifted towards higher molecular weights and this in turn increases the lipophilicity hence decreasing aqueous solubility. The low solubility of drugs usually has in vivo consequences such as low bioavailability, increased chance of food effect and incomplete release from the dosage form. Areas covered: The present review discusses the advantages of the liquisolid technology in formulation design of poorly water soluble drugs for dissolution enhancement and highly water soluble drugs for slow release pattern. Expert opinion: With the advent of high throughput screening and combinatorial chemistry, it has been shown that most of the new chemical entities have a high lipophilicity and poor aqueous solubility, hence poor bioavailability. In order to improve the bioavailability, the release rate of these drugs should be enhanced. Although there are multiple technologies to tackle this issue, they are not cost effective due to the involvement of sophisticated machinery, advanced preparation techniques and complicated technology. As the liquisolid technology uses a similar production process as the conventional tablets, this technology to improve the release rate of poorly water soluble drugs will be cost effective. This technology also has the capability to slow down drug release and allows preparing sustained release tablets with zero order drug release pattern. The excipients required for this technology are conventional and commonly available in the market. The technology is in the early stages of its development with extensive research currently focused on. It is envisaged that the liquisolid compacts could play a major role in the next generation of tablets.
引用
收藏
页码:191 / 205
页数:15
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