Prior art — US Patent 10864199

The following prior art documents have been identified as cited against US patent 10864199:

Due to the absence of explicit claims for US10864199 in the provided patent text, the potential anticipation under 35 U.S.C. § 102 is assessed based on a comparison of the cited prior art's abstract/description with the general inventive concepts and advantages described in US10864199, such as extended release, improved bioavailability, reduced Cmax, increased Tmax, reduced variability, and specific pharmaceutical formulations involving tacrolimus or its analogues.

Here are the details for each cited patent:

1. WO2005020994A1 - Solid dispersions of tacrolimus

Full Citation: WO2005020994A1, "Solid dispersions of tacrolimus", published March 10, 2005.
Publication/Filing Date: Publication date: March 10, 2005. Priority date: August 27, 2003.
Brief Description: This international patent application describes solid dispersions comprising tacrolimus and/or its analogues, along with a hydrophilic or water-miscible vehicle. The invention aims to improve the bioavailability of tacrolimus by formulating it in a solid dispersion or solid solution.
Potential Anticipation: This reference potentially anticipates the inventive concept of US10864199 relating to compositions where tacrolimus is present as a solid dispersion or solid solution in a hydrophilic or water-miscible vehicle, specifically aiming for improved bioavailability. The US10864199 patent text explicitly references WO 2005/020994 by the same inventors relating to solid dispersions comprising tacrolimus, indicating a strong foundational relationship.

2. WO2005020993A1 - Tacrolimus formulations with improved bioavailability

Full Citation: WO2005020993A1, "Tacrolimus formulations with improved bioavailability", published March 10, 2005.
Publication/Filing Date: Publication date: March 10, 2005. Priority date: August 27, 2003.
Brief Description: This international patent application discloses pharmaceutical compositions of tacrolimus designed to enhance its bioavailability upon oral administration. The formulations are tested in animal models, demonstrating improved bioavailability compared to conventional tacrolimus products. The patent also describes various controlled release formulations.
Potential Anticipation: This document is highly relevant as US10864199 explicitly states that its inventors also tested different tacrolimus formulations in WO 2005/020993, demonstrating improved bioavailability compared to Prograf®. This suggests that the core inventive concept of achieving improved bioavailability for tacrolimus through specific formulations is at least partially anticipated or built upon this prior work.

3. WO2003004001A1 - Particulate material

Full Citation: WO2003004001A1, "Particulate material", published January 16, 2003.
Publication/Filing Date: Publication date: January 16, 2003. Priority date: July 9, 2001.
Brief Description: This international patent application describes a process for preparing particulate material by a controlled agglomeration method, involving spraying a first composition (comprising an active substance and a melted carrier) onto a second solid carrier medium. This method is noted as useful for incorporating relatively large amounts of oil or oily-like material in solid compositions.
Potential Anticipation: US10864199 describes a method of preparation for its pharmaceutical compositions that is "a particularly useful method... described in WO 03/004001", specifically mentioning the controlled agglomeration method involving spraying a melted first composition onto a second solid carrier. This directly anticipates the manufacturing process aspect described in US10864199.

4. US6468565B1 - Extended release pharmaceutical compositions

Full Citation: US6468565B1, "Extended release pharmaceutical compositions", granted October 22, 2002.
Publication/Filing Date: Publication date: October 22, 2002. Filing date: January 16, 2001.
Brief Description: This patent describes extended-release pharmaceutical compositions designed to provide controlled release of an active agent over an extended period. The compositions often involve a core matrix or coating for controlled release.
Potential Anticipation: This patent broadly anticipates the concept of extended-release pharmaceutical compositions for oral administration, which is a fundamental aspect of US10864199. Depending on the specific active agents and release profiles claimed in US6468565B1, it could potentially anticipate the general formulation strategy for achieving extended release, though not necessarily with tacrolimus or the specific pharmacokinetic improvements outlined in US10864199.

5. US6472429B1 - Controlled release pharmaceutical composition

Full Citation: US6472429B1, "Controlled release pharmaceutical composition", granted October 29, 2002.
Publication/Filing Date: Publication date: October 29, 2002. Filing date: July 19, 2001.
Brief Description: This patent details a controlled-release pharmaceutical composition comprising a drug, a water-insoluble or sparingly water-soluble polymer, and a water-soluble excipient. The composition aims to provide a prolonged release of the drug.
Potential Anticipation: Similar to US6468565B1, this patent generally anticipates the concept of a controlled-release pharmaceutical composition. If the composition's characteristics (e.g., use of specific polymers, release kinetics) overlap with the generic aspects of extended-release formulations in US10864199, it could be seen as anticipating broad elements of the invention.

6. US6387918B1 - FK506-like compounds

Full Citation: US6387918B1, "FK506-like compounds", granted May 14, 2002.
Publication/Filing Date: Publication date: May 14, 2002. Filing date: January 18, 2001.
Brief Description: This patent describes novel FK506-like compounds and their use as immunosuppressants. FK506 is another name for tacrolimus.
Potential Anticipation: US10864199 explicitly cites US6387918 for disclosing analogues of tacrolimus. This patent is relevant for the active substance itself or its analogues, rather than the extended-release formulation technology. It would anticipate aspects of US10864199 that claim the use of tacrolimus or its pharmaceutically active analogues broadly, but not necessarily the specific formulation or pharmacokinetic profile improvements.

7. WO2000050007A1 - Self-emulsifying pharmaceutical formulation

Full Citation: WO2000050007A1, "Self-emulsifying pharmaceutical formulation", published August 31, 2000.
Publication/Filing Date: Publication date: August 31, 2000. Priority date: February 25, 1999.
Brief Description: This international patent application describes self-emulsifying pharmaceutical formulations containing an active agent, particularly amphiphilic surfactants, to improve the bioavailability of poorly water-soluble drugs.
Potential Anticipation: US10864199 mentions the inclusion of surfactants, specifically referencing "amphiphillic surfactants as those disclosed in WO 00/50007 in the name of Lipocine, Inc." This directly anticipates the use of certain surfactant types in tacrolimus formulations to aid solubility and potentially improve absorption.

8. WO9949863A1 - Pharmaceutical preparation containing tacrolimus

Full Citation: WO9949863A1, "Pharmaceutical preparation containing tacrolimus", published October 7, 1999.
Publication/Filing Date: Publication date: October 7, 1999. Priority date: March 31, 1998.
Brief Description: This international patent application describes pharmaceutical preparations containing tacrolimus, focusing on formulations that improve stability and bioavailability. It is relevant to the fast-release conventional product Prograf®.
Potential Anticipation: US10864199 explicitly refers to WO99/49863 as describing the formulation of the fast release conventional product Prograf®, owned by Fujisawa Pharmaceutical Co. This document serves as a baseline or comparison point for the improved bioavailability and pharmacokinetic profiles claimed by US10864199, rather than directly anticipating the extended-release features. However, it does anticipate the use of tacrolimus in pharmaceutical preparations and might contain elements of excipients or general formulation strategies that US10864199 builds upon or differentiates itself from.

9. WO9940902A1 - Controlled release pharmaceutical preparations for oral administration

Full Citation: WO9940902A1, "Controlled release pharmaceutical preparations for oral administration", published August 19, 1999.
Publication/Filing Date: Publication date: August 19, 1999. Priority date: February 12, 1998.
Brief Description: This international patent application describes controlled-release pharmaceutical preparations intended for oral administration, aiming to provide a prolonged therapeutic effect.
Potential Anticipation: This broadly anticipates the concept of controlled-release oral pharmaceutical preparations. The general goal of providing prolonged release is shared with US10864199. Specifics of the formulation, active ingredient, and achieved pharmacokinetic benefits would determine the degree of anticipation.

10. US5980942A - Sustained release oral dosage formulation comprising a highly water soluble drug

Full Citation: US5980942A, "Sustained release oral dosage formulation comprising a highly water soluble drug", granted November 9, 1999.
Publication/Filing Date: Publication date: November 9, 1999. Filing date: February 28, 1997.
Brief Description: This patent describes sustained-release oral dosage formulations, particularly for highly water-soluble drugs, using a specific combination of release-controlling polymers.
Potential Anticipation: While US10864199 deals with tacrolimus, which is practically insoluble in water, the general principles of sustained-release oral dosage formulations and the use of release-controlling polymers could be broadly anticipated by this patent.

11. US5891472A - Controlled release pharmaceutical preparations for oral administration

Full Citation: US5891472A, "Controlled release pharmaceutical preparations for oral administration", granted April 6, 1999.
Publication/Filing Date: Publication date: April 6, 1999. Filing date: October 23, 1996.
Brief Description: This patent describes controlled-release oral pharmaceutical preparations, which may involve matrix systems or coated particles to achieve prolonged drug release.
Potential Anticipation: Similar to WO9940902A1 and US6468565B1, this patent broadly anticipates the concept of controlled-release oral pharmaceutical preparations.

12. WO9706791A1 - Pharmaceutical compositions containing 2-substituted cephalosporins

Full Citation: WO9706791A1, "Pharmaceutical compositions containing 2-substituted cephalosporins", published February 27, 1997.
Publication/Filing Date: Publication date: February 27, 1997. Priority date: August 19, 1995.
Brief Description: This international patent application describes pharmaceutical compositions containing 2-substituted cephalosporins, which are a class of antibiotics.
Potential Anticipation: This document is unlikely to directly anticipate any core inventive concepts of US10864199, as it concerns a completely different active pharmaceutical ingredient (cephalosporins vs. tacrolimus). It might be cited for very general formulation techniques or excipients common across pharmaceutical compositions, but not for the specific extended-release tacrolimus formulation or its pharmacokinetic advantages.

13. US5554388A - Controlled-release composition of FK506

Full Citation: US5554388A, "Controlled-release composition of FK506", granted September 10, 1996.
Publication/Filing Date: Publication date: September 10, 1996. Filing date: February 15, 1995.
Brief Description: This patent specifically describes a controlled-release composition for FK506 (tacrolimus), which is directly relevant to US10864199. It aims to achieve sustained release of tacrolimus.
Potential Anticipation: This patent is highly significant as it directly addresses controlled-release formulations of tacrolimus (FK506). It potentially anticipates the broad concept of an extended-release tacrolimus oral dosage form for immunosuppressive treatment. The novelty of US10864199 would then lie in the specific extended release profile, improved bioavailability parameters (e.g., lower Cmax, higher AUC, reduced variability, sustained Cmin), formulation components, or methods that differentiate it from the teaching of US5554388A.

14. US5503848A - Controlled-release pharmaceutical compositions

Full Citation: US5503848A, "Controlled-release pharmaceutical compositions", granted April 2, 1996.
Publication/Filing Date: Publication date: April 2, 1996. Filing date: May 11, 1994.
Brief Description: This patent describes controlled-release pharmaceutical compositions, often involving a matrix system, to provide a sustained therapeutic effect.
Potential Anticipation: This broadly anticipates the general concept of controlled-release pharmaceutical compositions, similar to other general controlled-release patents cited.

15. US5260082A - ENTERIC DOSAGE FORMS

Full Citation: US5260082A, "ENTERIC DOSAGE FORMS", granted November 9, 1993.
Publication/Filing Date: Publication date: November 9, 1993. Filing date: April 1, 1992.
Brief Description: This patent describes enteric dosage forms designed to prevent drug release in the stomach and release it in the intestines, often using pH-sensitive coatings.
Potential Anticipation: US10864199 mentions that its release "may be pH dependent, i.e., the release predominantly takes place after passage of the stomach," and that "Such a pH dependent release is mainly provided by means of enteric coating material." This patent directly anticipates the use of enteric coatings for delayed, pH-dependent release.

16. US5202128A - Extended-release compositions

Full Citation: US5202128A, "Extended-release compositions", granted April 13, 1993.
Publication/Filing Date: Publication date: April 13, 1993. Filing date: August 14, 1992.
Brief Description: This patent describes extended-release compositions, often involving matrix systems, for prolonged drug delivery.
Potential Anticipation: This broadly anticipates the general concept of extended-release compositions, similar to other general controlled-release patents cited.

17. US5128143A - Enteric-coated sustained-release pharmaceutical compositions

Full Citation: US5128143A, "Enteric-coated sustained-release pharmaceutical compositions", granted July 7, 1992.
Publication/Filing Date: Publication date: July 7, 1992. Filing date: February 13, 1991.
Brief Description: This patent describes pharmaceutical compositions combining enteric coating with sustained-release mechanisms.
Potential Anticipation: This patent combines the concepts of enteric coating and sustained release, both of which are discussed in US10864199 as potential mechanisms for achieving its desired release profile. Thus, it potentially anticipates aspects relating to combined delayed and extended release.

18. US5019397A - Controlled release pharmaceutical compositions

Full Citation: US5019397A, "Controlled release pharmaceutical compositions", granted May 28, 1991.
Publication/Filing Date: Publication date: May 28, 1991. Filing date: April 17, 1989.
Brief Description: This patent describes various controlled-release pharmaceutical compositions designed for prolonged drug delivery.
Potential Anticipation: This broadly anticipates the general concept of controlled-release pharmaceutical compositions.

19. US4871549A - Dosage forms for providing biphasic release

Full Citation: US4871549A, "Dosage forms for providing biphasic release", granted October 3, 1989.
Publication/Filing Date: Publication date: October 3, 1989. Filing date: January 17, 1986.
Brief Description: This patent describes dosage forms that provide a biphasic release profile (e.g., immediate release followed by sustained release).
Potential Anticipation: While US10864199 focuses on extended release, the general concept of tailoring release profiles, including initial release characteristics, could be broadly anticipated by this patent.

20. EP-A-0 184 162 - Preparation of tacrolimus

Full Citation: EP-A-0 184 162 (European Patent Application), "Macrolide Compounds and Process for Their Production and Use", published June 11, 1986. (Equivalent to US4894366A)
Publication/Filing Date: Publication date: June 11, 1986. Filing date: October 22, 1985.
Brief Description: This European patent application describes the preparation of tacrolimus (FK506) itself.
Potential Anticipation: US10864199 explicitly states, "The preparation of tacrolimus is described in EP-A-0 184 162". This patent anticipates the method of synthesizing the active pharmaceutical ingredient, tacrolimus, but not the specific extended-release formulations or their pharmacokinetic advantages.

21. US4606909A - PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION

Full Citation: US4606909A, "PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION", granted August 19, 1986.
Publication/Filing Date: Publication date: August 19, 1986. Filing date: June 20, 1985.
Brief Description: This patent describes general pharmaceutical compositions for oral administration.
Potential Anticipation: This is a very broad citation, likely anticipating the general concept of pharmaceutical compositions for oral administration, but not the specific extended-release features, active ingredient (tacrolimus), or pharmacokinetic benefits.

22. US4476107A - Controlled release pharmaceutical compositions

Full Citation: US4476107A, "Controlled release pharmaceutical compositions", granted October 9, 1984.
Publication/Filing Date: Publication date: October 9, 1984. Filing date: September 1, 1982.
Brief Description: This patent describes early forms of controlled-release pharmaceutical compositions using various matrix materials.
Potential Anticipation: This broadly anticipates the general concept and basic mechanisms of controlled-release pharmaceutical compositions, providing a foundation upon which later, more specific extended-release technologies (like those for tacrolimus) were developed.

23. EP-A-0 444 659 - Analogues of tacrolimus

Full Citation: EP-A-0 444 659 (European Patent Application), "Macrolactam compounds, their preparation and use", published September 4, 1991. (Equivalent to US5250678A)
Publication/Filing Date: Publication date: September 4, 1991. Filing date: February 28, 1991.
Brief Description: This European patent application discloses various macrolactam compounds, including analogues of tacrolimus, with immunosuppressive properties.
Potential Anticipation: US10864199 explicitly states that "analogues of tacrolimus are disclosed e.g. in EP-A-0 444 659". Similar to US6387918B1, this patent anticipates the existence and chemical structure of certain tacrolimus analogues, which are defined as part of the active substance in US10864199, but not the specific extended-release formulation or its pharmacokinetic advantages.

Summary of Most Relevant Prior Art:

The most relevant prior art documents appear to be those directly related to tacrolimus formulations or methods that US10864199 explicitly builds upon or differentiates itself from:

US5554388A (Controlled-release composition of FK506): Directly addresses controlled-release formulations of tacrolimus.
WO2005020993A1 (Tacrolimus formulations with improved bioavailability) and WO2005020994A1 (Solid dispersions of tacrolimus): These are by the same inventors and are explicitly referenced in US10864199 as foundational for improved bioavailability and solid dispersion technology.
WO2003004001A1 (Particulate material): Explicitly referenced for the manufacturing process of the particulate material.
WO9949863A1 (Pharmaceutical preparation containing tacrolimus): Describes the conventional Prograf® formulation, which US10864199 aims to improve upon.
EP-A-0 184 162 and EP-A-0 444 659: These anticipate the existence and preparation of tacrolimus and its analogues, respectively, which are the active ingredients of US10864199.

Other patents provide more general background on controlled-release technologies or pharmaceutical excipients that are not specific to tacrolimus.