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Claims for Patent: 6,576,259

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Claims for Patent: 6,576,259

Title: Sustained release formulations containing tacrolimus
Abstract:Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanese Pharmacopoeia, the 13-th edition, Dissolution Test, No. 2 (Puddle method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprise a solid base which is a water-soluble polymer and/or wax. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. Furthermore, the formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune diseases.
Inventor(s): Yamashita; Kazunari (Kyoto, JP), Hashimoto; Eiji (Wakayama, JP), Nomura; Yukihiro (Osaka, JP), Shimojo; Fumio (Hyogo, JP), Tamura; Shigeki (Osaka, JP), Hirose; Takeo (Kyoto, JP), Ueda; Satoshi (Hyogo, JP), Saitoh; Takashi (Osaka, JP), Ibuki; Rinta (Kyoto, JP), Ideno; Toshio (Osaka, JP)
Assignee: Fujisawa Pharmaceutical Co., Ltd. (Osaka, JP)
Application Number:09/978,025
Patent Claims: 1. A sustained-release formulation comprising tacrolimus or its hydrate, wherein the time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours, as measured according to the Japanese Pharmacopoeia, the 13-th edition, Dissolution Test, No. 2 (Puddle method, 50 rpm) using a test solution which is an aqueous 0.005% hydroxypropyl cellulose solution adjusted to pH 4.5.

2. The sustained-release formulation in claim 1, which comprises a solid dispersion composition, wherein the tacrolimus or its hydrate is present as an amorphous state in a solid base.

3. The sustained-release formulation in claim 2, which the solid dispersion composition is characterized by (1) lactose or calcium hydrogen phosphate is contained as an excipient and/or lubricant, (2) no disintegrator is contained, and (3) the particle size of the said solid dispersion composition is equal to or smaller than 350 .mu.m.

4. The sustained-release formulation in claim 2, in which the solid base is selected from a group consisting if water-soluble polymer and wax.

5. The sustained-release formulation in claim 2, in which the solid base is selected from a group consisting of 1) hydroxypropylmethyl cellulose, in a weight ratio to tacrolimus of 0.2-0.4 to 1, and 2) glycerin monostearate, polyglycerin fatty acid ester or sucrose fatty acid ester, in a weight ratio to tacrolimus of 0.2-20 to 1.

6. The sustained-release formulation in claim 2, which the solid dispersion composition is characterized by (1) tacrolimus or its hydrate is present as an amorphous state in hydroxypropylmethyl cellulose in a weight ratio to tacrolimus of 0.2-0.4 to 1, (2) lactose is contained as an excipient, (3) no disintegrators are contained, and (4) the particle size of the said solid dispersion composition is equal to or smaller than 250 .mu.m.

7. The sustained-release formulation in claim 1, in which tacrolimus or its hydrate is present as fine powder characterized by a particle diameter distribution within the range of 0.1 to 50 .mu.m and/or a mean particle diameter within the range of 0.2 to 20 .mu.m.

8. The sustained-release formulation in claim 1, in which the time (T63.2%) is 1.0 to 12 hours.

9. The sustained-release formulation in claim 1, in which the time (T63.2%) is 1.3 to 8.2 hours.

10. The sustained-release formulation in claim 1, in which the time (T63.2%) is 2 to 5 hours.

11. The sustained-release formulation in claim 1, which is in a form of powder, fine powder, granule, tablet or capsule.

12. A method for administering tacrolimus or its hydrate to a patient without the risk of an undesired effect caused by a transiently excessive concentration of tacrolimus and insuring an expression of pharmacological efficacy over a sufficiently extended period of time, by administering the sustained-release formulation of claim 1 once a day.

13. A method for treating or preventing rejection of organs or tissues by transplantation or autoimmune diseases, by administering an effective amount of the sustained-release formulation of claim 1 once a day, without the risk of an undesired effect caused by a transiently excessive concentration of tacrolimus and insuring an expression of pharmacological efficacy over a sufficiently extended period of time.
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