DRUG SOLUBILIZERS TO AID PHARMACOLOGISTS - AMORPHOUS CYCLODEXTRIN DERIVATIVES
DRUG SOLUBILIZERS TO AID PHARMACOLOGISTS - AMORPHOUS CYCLODEXTRIN DERIVATIVES
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DOI：
10.1016/0024-3205(88)90150-6
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发表时间：
1988-01-01
期刊：
影响因子：
6.1
通讯作者：
NYE, JS
中科院分区：
文献类型：
--
作者：
PITHA, J;IRIE, T;NYE, JS
晶体的转换。度量。-或。gamma。-环糊精转化为水溶性衍生物的无定形混合物，产生无毒的增溶剂，通过形成包合物溶解药物。从这些类型的化合物中，环糊精的2-羟丙基醚目前已经进行了研究，并确定了这些化合物在(a)膜制剂受体结合试验、(b)体外细胞和(c)小鼠肠外使用中的安全使用范围。所研究的药物的溶解量与所用增溶剂的浓度成线性比例，并且在水介质稀释时不沉淀。这些增溶剂可以大大促进新的，水不溶性潜在药物的药理学评价。
Conversion of crystalline .alpha.-, .beta.-, or .gamma.-cyclodextrins into amorphous mixtures of water soluble derivatives yields non-toxic solubilizers which dissolve drugs through the formation of inclusion complexes. From these types of compounds 2-hydroxypropyl ethers of cyclodextrins have presently been investigated and the ranges for the safe use in working with (a) receptor binding assays on membrane preparations, (b) cells in vitro, and (c) parenteral use in mice were established for these compounds. The drugs which were investigated were dissolved in amounts linearly proportionate to the concentration of the solubilizers used and did not precipitate upon dilution by aqueous media. These solubilizers may considerably facilitate pharmacological evaluation of new, water insoluble potential drugs.