PURPOSE: To provide the clathrate compound of benzodiazepine derivative in cyclodextrin, having the original activity of the benzodiazepine derivative and improved solubility in water, and useful as a tranquillizer, etc., by including a benzodiazepine derivative in cyclodextrin.
CONSTITUTION: The objective compound is prepared by including the benzodiazepine derivtive of formula (R1 is H, alkyl, cycloalkyl, or dialkylaminoalkyl; X is =CH2 or =C=O; Y is halogen or nitro; R2 is H or hydroxyl; R3 is phenyl, halogenated phenyl or pyridyl) (e.g. diazepam, etc.) in a cyclodextrin (preferably γ-cyclodextrin) by solution method or kneading method.
EFFECT: The improvement in the physiological usefulness can be expected.
USE: Medicine having muscle relaxing and narcotic activities.
ODAGIRI MASAKI
NAKANO SADAHIRO
