| abstract |
PROBLEM TO BE SOLVED: To provide a method for amorphizing efonidipine hydrochloride. SOLUTION: A mixture of efonidipine hydrochloride (I), hydroxypropylmethylcellulose acetate succinate and optionally a heat stabilizer is added to a mixture of 85-85%. 14 After heat treatment at 0 ° C or after A step of performing mechanochemical treatment at 0 to 140 ° C, dipping treatment in a solution containing water, impregnation treatment with a solution containing water, or contact treatment with a steam-containing gas is included. By performing the step B or by subjecting the mixture to steam treatment under high pressure at 100 to 140 ° C., a solid dispersion of efonidipine hydrochloride having high intestinal absorbability can be obtained as a solid dispersion in an amorphous state. . Further, by using high-frequency heating in the above step A, a solid dispersion of efonidipine hydrochloride having a high intestinal absorbability can be obtained as a solid dispersion in an amorphous state without using the step B. This manufacturing method has a remarkable manufacturing advantage that it does not require the use of an organic solvent. Embedded image |