Aqueous colloidal or size are up to the pharmaceutical composition of the aqueous suspension form of 100 μm of particle, it includes amphiphilic sulfonate/ester of hydrophilic cancer drug or sulfate/ester or is made of the amphiphilic of hydrophilic cancer drug sulfonate/ester or sulfate/ester, and the solubility in water or in aqueous body fluid is less than 0.1 weight %. The production method of the particle of powder type, preparation method and colloid and suspension is further disclosed, by giving liver cancer (especially entity liver cancer tumor) treatment method of pharmaceutical composition, and the method for designing composition according to the present invention.