Sustained release preparation of a macrolide compound like tacrolimus

Sustained release formulation of a macrolide compound, wherein the time (T63.2%) which is necessary to 63.2% of the maximum amount of macrolide compound is dissolved from 0.7 to 15 hours using a test solution which is 0.005% aqueous solution of hydroxypropyl of pulp adjusted to pH 4.5, wherein the macrolide compound is a tricyclic compound represented by the general formula (I) and a pharmaceutically acceptable salt thereof, wherein each of adjacent pairs of R 1 and R 2, R 3 and R 4, and R 5 and R 6 independently (a) is two adjacent hydrogen atoms, but R2 may also be alkyl groups, or (b) may form another bond formed between the carbon atoms to which they are attached; R 7 is hydrogen atom, hydroxy group, protected hydroxy or alkoxy group, or an oxo group together with R1; R 8 and R 9 are, independently, a hydrogen atom or a hydroxy group; R 10 is a hydrogen atom, alkyl group, alkyl substituted by one or more hydroxy groups, an alkenyl group, an alkenyl group substituted by one or more hydroxy groups, or alkyl substituted with an oxo group; X is an oxo group, (a hydrogen atom and a hydroxy group), (a hydrogen atom and a hydrogen atom), or a group represented by formula -CH 2 O-; Y is an oxo group, (a hydrogen atom and a hydroxy group), (a hydrogen atom and a hydrogen atom), or a group represented by the formula N-NR11R12 or N-OR13, R11 and R12 are, independently, a hydrogen atom, alkyl group, aryl group or a tosyl group; R 13, R 14, R 15, R 16, R 17, R 18, R 19, R 22 and R 23 are, independently, a hydrogen atom or alkyl group; R 24 is an optionally substituted ring system which may contain one or more heteroatoms; n is an integer 1 or 2; and Y with the above definitions R10 and R23 together with the carbon atom to which they are attached, may represent a saturated or unsaturated 5- or 6-membered heterocyclic ring containing nitrogen, sulfur and / or oxygen, optionally substituted by one or more groups selected from the group consisting of alkyl, hydroxy, alkoxy, benzyl, a group of formula "CH2 Si (C6H5), and alkyl groups substituted by one or more hydroxy groups, which forms a solid dispersion composition, wherein the macrolide compound (I) is present in amorphous form which is substantially insoluble in water, where a base is insoluble in water, comprised in the solid dispersion composition, selected from polymers insoluble in water or wax. Log contains 28 claims.