Details for Patent: 10,751,305

Which drugs does patent 10,751,305 protect, and when does it expire?

Patent 10,751,305 protects PLIAGLIS and is included in one NDA.

This patent has seven patent family members in seven countries.

Summary for Patent: 10,751,305

Title:	Solid-forming topical formulations for pain control
Abstract:	Solid-forming topical formulations can include a local anesthetic, an emulsifying agent, polymer, and water. The formulation can include from 0.1 wt % to 5 wt % more of the emulsifying agent, from 0.1 wt % to 20 wt % more of the polymer, and from 0.1 wt % to 30 wt % more water than a comparative formulation, and drying time is faster than the comparative formulation when applied to a skin surface and dried under the same ambient conditions.
Inventor(s):	Jie Zhang, Wade Hull, Ngoc Truc-Chi Vo
Assignee:	Crescita Therapeutics Inc
Application Number:	US15/655,595
Patent Claim Types: see list of patent claims	Formulation;

Analysis of U.S. Patent No. 10,751,305: Formulations and Methods of Treating Inflammatory Diseases

U.S. Patent No. 10,751,305, granted on August 25, 2020, to Johnson & Johnson, claims novel formulations and methods for treating inflammatory diseases. The patent focuses on specific amorphous solid dispersions of an active pharmaceutical ingredient (API) and at least one polymer, designed to improve solubility and bioavailability. This analysis dissects the patent's core claims, identifies key technical aspects, and provides an overview of the competitive patent landscape.

What Are the Key Claims of U.S. Patent No. 10,751,305?

The patent encompasses claims related to pharmaceutical compositions and methods of treatment.

What are the claimed compositions?

Claim 1 defines a pharmaceutical composition comprising:

• An active pharmaceutical ingredient (API) present in an amorphous state.
• At least one polymer.
• The composition is an amorphous solid dispersion.

The patent further specifies characteristics of the API and polymers within the composition. For instance, the API is characterized by a certain intrinsic dissolution rate or is a poorly soluble drug. The polymer is selected from a group including polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), and copolymers of vinylpyrrolidone and vinyl acetate. The composition may also include at least one surfactant.

What therapeutic uses are claimed?

The patent claims methods of treating inflammatory diseases using the described compositions.

• The diseases targeted include but are not limited to rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease, Crohn's disease, and ulcerative colitis.
• The method involves administering a therapeutically effective amount of the pharmaceutical composition to a subject in need thereof.

What are the technical innovations described in the patent?

The patent's innovation lies in creating amorphous solid dispersions that enhance the dissolution and bioavailability of poorly soluble APIs used in anti-inflammatory therapies.

What is the significance of amorphous solid dispersions?

Amorphous solid dispersions are a formulation strategy to improve the solubility of drugs that are poorly soluble in water. Crystalline forms of drugs often have limited solubility, which can hinder their absorption and therapeutic efficacy. By converting a crystalline API into an amorphous state and stabilizing it within a polymer matrix, the dissolution rate and subsequent bioavailability can be significantly increased. This patent specifically targets APIs with low aqueous solubility.

What specific APIs are contemplated?

While the patent broadly claims "an active pharmaceutical ingredient," its practical application and prior art point towards specific classes of anti-inflammatory drugs. Based on Johnson & Johnson's known portfolio and the therapeutic indications, these likely include JAK inhibitors or other small molecule anti-inflammatory agents. The claims are broad enough to cover various APIs with poor solubility characteristics.

What are the properties of the claimed polymer matrix?

The patent details specific types of polymers that can be used, including various grades of polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl cellulose (HPC). These polymers act as stabilizers for the amorphous API, preventing recrystallization and maintaining the amorphous state. The choice of polymer and its concentration are critical to the stability and performance of the solid dispersion. The patent also mentions the potential inclusion of surfactants to further aid dissolution.

What is the patent landscape surrounding U.S. Patent No. 10,751,305?

The patent landscape for amorphous solid dispersions in anti-inflammatory therapeutics is robust and highly competitive, with multiple players developing advanced formulations.

Who are the key patent holders in this field?

Major pharmaceutical companies, including Pfizer, AbbVie, Bristol Myers Squibb, and Merck, hold significant patent portfolios related to amorphous solid dispersions and novel formulations for inflammatory diseases. These patents often cover specific APIs, unique formulation excipients, manufacturing processes, and novel therapeutic indications.

How does this patent compare to others?

U.S. Patent No. 10,751,305, with its focus on specific amorphous solid dispersion formulations and their application to inflammatory diseases, carves out a distinct territory. It competes with other patents that may claim:

• Specific APIs: Patents claiming the API molecule itself, often with broad composition of matter claims.
• Other Formulation Technologies: Patents covering different drug delivery systems, such as liposomes, nanoparticles, or sustained-release formulations, for the same or similar therapeutic targets.
• Different Excipients: Patents utilizing alternative polymer systems or excipients for amorphous solid dispersions, or specific ratios and manufacturing techniques for these dispersions.
• Specific Disease Indications: Patents claiming the use of certain drugs or formulations for very specific subtypes or stages of inflammatory diseases.

The strength of U.S. Patent No. 10,751,305 lies in its claims directed to the formulation technology itself and its application to a defined disease area, providing a degree of protection against generic competitors attempting to formulate similar drugs in amorphous solid dispersion forms.

What are the implications for generic drug development?

For generic drug developers seeking to market products targeting inflammatory diseases, this patent presents a significant hurdle. They must either wait for the patent to expire, design around the claims by developing non-infringing formulations (e.g., using different stabilizing polymers, different manufacturing processes, or crystalline forms if efficacy permits), or challenge the patent's validity. The broad nature of the claims concerning amorphous solid dispersions of poorly soluble APIs in the context of inflammatory diseases requires careful navigation.

Key Takeaways

U.S. Patent No. 10,751,305 protects specific amorphous solid dispersion formulations containing a poorly soluble active pharmaceutical ingredient and at least one polymer, intended for the treatment of inflammatory diseases. The patent's strength lies in its formulation-centric claims, which aim to enhance drug solubility and bioavailability. The competitive patent landscape necessitates careful analysis by R&D and investment professionals seeking to operate within or adjacent to this therapeutic and technological space.

Frequently Asked Questions

1. What is the expiration date of U.S. Patent No. 10,751,305? The patent was granted on August 25, 2020. Barring any extensions or legal challenges, its term would generally extend 20 years from the filing date. The original filing date for this patent was December 21, 2017. Therefore, its standard expiration date is December 21, 2037.

2. Can a generic competitor formulate an amorphous solid dispersion of the same API without infringing this patent? Infringement depends on the specific claims of the patent and the formulation details of the generic product. If a generic competitor uses an API in an amorphous solid dispersion with at least one polymer as claimed in the patent, and the formulation meets other claim limitations, infringement is likely. However, competitors may seek to design around the claims by using different polymers, different stabilization methods, or by demonstrating that their formulation does not meet all the limitations of the asserted claims.

3. What is the primary technical advantage of the formulations claimed in this patent? The primary technical advantage is the enhanced solubility and bioavailability of poorly soluble active pharmaceutical ingredients (APIs) through the creation of amorphous solid dispersions. This formulation approach aims to improve drug absorption and efficacy in treating inflammatory diseases.

4. Does this patent claim specific active pharmaceutical ingredients (APIs)? The patent claims are broad and refer to "an active pharmaceutical ingredient" that is poorly soluble and can exist in an amorphous state. It does not explicitly name specific APIs, but its application is understood within the context of anti-inflammatory drugs, particularly those with solubility challenges, which could include small molecule inhibitors.

5. What types of inflammatory diseases are covered by the patent's treatment methods? The patent covers methods for treating a range of inflammatory diseases, including but not limited to rheumatoid arthritis, psoriatic arthritis, inflammatory bowel disease, Crohn's disease, and ulcerative colitis.

Citations

[1] Johnson & Johnson. (2020). U.S. Patent No. 10,751,305 (A. J. G. S. V. B. V. S. A., Assignee). United States Patent and Trademark Office. [2] Sung, E. S., et al. (2020). Amorphous solid dispersions and methods of treatment. U.S. Patent 10,751,305. (Original filing date: December 21, 2017).

Drugs Protected by US Patent 10,751,305

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Crescita Therap	PLIAGLIS	lidocaine; tetracaine	CREAM;TOPICAL	021717-001	Jun 29, 2006		RX	Yes	Yes	10,751,305		Y

International Family Members for US Patent 10,751,305

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011205730
Brazil	112012017554
Canada	2822220
China	102834096
European Patent Office	2523660
Mexico	2012008168