Claims for Patent: 9,757,362

Summary for Patent: 9,757,362

Title:	Modified release compositions comprising tacrolimus
Abstract:	A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.
Inventor(s):	Holm; Per (Vanlose, DK), Norling; Tomas (Lyngby, DK)
Assignee:	VELOXIS PHARMACEUTICALS A/S (Copenhagen, DK)
Application Number:	14/855,624
Patent Claims:	1. A solid pharmaceutical composition comprising: (a) tacrolimus; (b) hydroxypropyl methylcellulose; (c) lactose; (d) polyethylene glycol 6000; (e) poloxamer 188; and (f) magnesium stearate. 2. The solid pharmaceutical composition of claim 1, wherein less than 20% w/w of the tacrolimus is released from the solid pharmaceutical composition within 0.5 hours, when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium. 3. The solid pharmaceutical composition of claim 1, wherein less than 20% w/w of the tacrolimus is released from the solid pharmaceutical composition within 3 hours, when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium. 4. The solid pharmaceutical composition of claim 2, wherein the weight ratio of polyethylene glycol 6000 to poloxamer 188 is between 1:3 and 10:1. 5. The solid pharmaceutical composition of claim 2, wherein the dosage form is a tablet. 6. The solid pharmaceutical composition of claim 1, wherein the composition releases at most 62% of the tacrolimus in the composition within 15 hours when subjected to an in vitro dissolution test using USP Paddle method at a rotation speed of 50 rpm in a 900 mL aqueous dissolution medium with 0.005% hydroxypropylcellulose which has been adjusted to pH 4.5. 7. The solid pharmaceutical composition of claim 1, wherein the dosage form is a tablet. 8. The solid pharmaceutical composition of claim 3, wherein the dosage form is a tablet.