.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 6,884,433

« Back to Dashboard

Claims for Patent: 6,884,433

Title: Sustained release formulation 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 Japanes Pharmacopocia, the 13-th edition, Dissolution Test, No. 2 (Puddles 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 comprises a solid base which is a water-soluble or water-insoluble polymer. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. The formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune disease. In addition, a solid dispersion composition is provided. The solid dispersion comprises tacrolimus or its hydrate in a mixture containing water-soluble or water-insoluble polymer and an excipient.
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:10/412,281
Patent Claims: 1. A sustained-release formulation comprising a solid dispersion composition, wherein the solid dispersion composition comprises tacrolimus or its hydrate, in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.

2. The sustained-release formulation of claim 1, wherein the solid dispersion composition has a particle size equal to or smaller than 250 .mu.m.

3. The sustained-release formulation of claim 1, wherein the weight ratio of the water-soluble polymer to tacrolimus is 0.2-0.4:1, and the weight ratio of the water-insoluble polymer to tacrolimus is 0.1-5:1.

4. The sustained-release formulation of claim 3, wherein the weight ratio of the water-insoluble polymer to tacrolimus is 0.1-1:1.

5. The sustained-release formulation of claim 1, wherein the water-insoluble polymer is ethylcellulose.

6. The sustained-release formulation of claim 1 wherein the water-soluble polymer is hydroxypropylmethyl cellulose.

7. The sustained-release formulation of claim 1, wherein the excipient is lactose.

8. The sustained-release formulation of claim 7, wherein the weight ratio of lactose to tacrolimus is 2, 3 or 5:1.

9. The sustained-release formulation of claim 1, wherein the solid dispersion composition does not substantially contain any disintegrators.

10. The sustained-release formulation of claim 1, wherein tacrolimus or its hydrate is present as an amorphous state.

11. The sustained-release formulation of claim 2, wherein the weight ratio of the water-soluble polymer to tacrolimus is 0.2-0.4:1, and the weight ratio of the water-insoluble polymer to tacrolimus is 0.1-5:1.

12. The sustained-release formulation of claim 11, wherein the weight ratio of the water-insoluble polymer to tacrolimus is 0.1-1:1.

13. The sustained-release formulation of claim 6, wherein the water-insoluble polymer is ethylcellulose.

14. The sustained-release formulation of claim 13, wherein the excipient is lactose.

15. The sustained-release formulation of claim 1, wherein tacrolimus or its hydrate is present as an amorphous state in a mixture of ethylcellulose and hydroxypropylmethyl cellulose.

16. The sustained-release formulation of claim 15, wherein the weight ratio of the ethylcellulose to tacrolimus is 0.3:1, and the weight ratio of the hydroxypropylmethyl cellulose to tacrolimus is 0.3:1.

17. The sustained-release formulation of claim 16, wherein the excipient is lactose.

18. The sustained-release formulation of claim 17, wherein the weight ratio of lactose to tacrolimus is 2:1.

19. The sustained-release formulation of claim 18, wherein the solid dispersion composition has a particle size equal to or smaller than 212 .mu.m.

20. The sustained-release formulation of claim 3, wherein the water-insoluble polymer is ethylcellulose and the water soluble polymer is hydroxypropylmethyl cellulose.

21. The sustained-release formulation of claim 1, in a form of a powder, granule, tablet or capsule.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc