Immunosuppressant formulations

A solid phase pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and an active pharmaceutical ingredient (“API”) which is a compound of formula A1 or A2 or a pharmacologically acceptable salt, solvate or hydrate thereof, wherein the API is not exposed to a basic compound:

• wherein
• A is COOR5, OPO(OR5)2, PO(OR5)2, SO2OR5, POR5OR5 or 1H-tetrazol-5-yl, R5 being H or an ester-forming group;
• W is a bond, C1-3alkylene or C2-3alkenylene;
• Y is C6-10aryl or C3-10heteroaryl, optionally substituted by 1 to 3 radicals selected from halogen, NO2, C1-6alkyl, C1-6alkoxy;
• halo-substituted C1-6alkyl and halo-substituted C1-6alkoxy;
• Z is chosen from:
• wherein the asterisks of Z indicate the point of attachment between —C(R3)(R4)— and A of Formula Ia or Ib, respectively;
• R6 is chosen from hydrogen and C1-6alkyl;
• and J1 and J2 are independently methylene or a heteroatom chosen from S, O and NRS;
• wherein R5 is chosen from hydrogen and C1-6alkyl;
• and any alkylene of Z can be further substituted by one to three radicals chosen from halo, hydroxy, C1-6alkyl;
• or R6 can be attached to a carbon atom of Y to form a 5-7 member ring;
• R1 is C6-10aryl or C3-9heteroaryl, optionally substituted by C1-6alkyl, C6-10aryl, C6-10arylC1-4alkyl, C3-9heteroaryl, C3-9heteroarylC1-4alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-4alkyl, C3-8heterocycloalkyl or C3-8heterocycloalkylC1-4alkyl;
• wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R1 may be substituted by 1 to 5 groups selected from halogen, C1-6 alkyl, C1-6alkoxy and halo substituted-C1-6alkyl or —C1-6alkoxy;
• R2 is H, C1-6alkyl, halo substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl;
• and
• each of R3 or R4, independently, is H, halogen, OH, C1-6alkyl, C1-6alkoxy or halo substituted C1-6alkyl or C1-6alkoxy.