# US 12,594,243 B2 · Pharmaceutical formulations

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- Number: US 12,594,243 B2
- Document ID: US12594243B2
- Status: Granted
- Kind: B2
- Application number: 18/501,714
- Filed: 2023-11-03
- Published: 2024-05-02
- Granted: 2026-04-07
- Earliest claimed: 2020-10-05
- Assignees: Theracosbio, LLC
- Applicants: Theracosbio, LLC
- Inventors: Feng Wang; Ankit Shrivastava; Rina Shah; Brian Seed; Vinay Patil; Michael J. Hadd; Fuxia Dong; Vipan Dhall; Chunfeng Dai; Joseph Ho-Lun Chau; Qiuhua Cai
- Web page: https://patentgrep.com/patent/US12594243B2

## CPC

- A61K 9/0065: {Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/0007: {Effervescent (A61K9/0065 takes precedence)}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/1611: {Inorganic compounds}
- A61K 9/1617: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone}
- A61K 9/501: {Inorganic compounds}
- A61K 9/5015: {Organic compounds, e.g. fats, sugars}
- A61K 9/5026: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 31/351: not condensed with another ring
- A61K 31/70: Carbohydrates; Sugars; Derivatives thereof (sorbitol A61K31/047)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The pharmacokinetic profile of the SGLT2 inhibitor bexagliflozin can be improved by formulating it as an extended release tablet. Compared with standard immediate-release dosage forms these tablets can permit a lower peak plasma concentration, Cmax, while maintaining plasma concentrations at therapeutic levels for a desired period. This can be used, for instance, to administer lower doses while still providing the same pharmacological effect.

## Claims

### Claim 1

A tablet comprising:
(a) 1-13% by weight of bexagliflozin;
(b) 30-35% by weight of glyceryl dibehenate;
(c) 16-20% by weight of polyethylene oxide having an average molecular weight of 900,000 g/mol;
(d) 11-13% by weight of lactose;
(e) 10-12% by weight of poloxamer 188;
(f) 18-20% by weight of microcrystalline cellulose;
(g) 1.0-1.5% by weight of colloidal silicon dioxide; and
(h) 1.5-2.5% by weight of magnesium stearate,
wherein the tablet provides a maximum bexagliflozin plasma concentration in a fasted human subject between 80-150 ng/mL.

### Claim 2

A tablet comprising:
(a) from 3 mg to 60 mg of bexagliflozin;
(b) from 50 mg to 75 mg of polyethylene oxide having an average molecular weight of 900,000 g/mol;
(c) from 100 mg to 140 mg of glyceryl dibehenate;
(d) from 40 mg to 50 mg of lactose;
(e) from 40 mg to 45 mg of poloxamer 188;
(f) from 60 mg to 80 mg of microcrystalline cellulose;
(g) from 4 mg to 5 mg of colloidal silicon dioxide; and
(h) from 6 mg to 9 mg of magnesium stearate,
wherein the tablet provides a maximum bexagliflozin plasma concentration in a fasted human subject between 80-150 ng/mL.

### Claim 3 (depends on 2)

The tablet of claim 2, comprising
(a) 20 mg of bexagliflozin;
(b) 65 mg of polyethylene oxide having an average molecular weight of 900,000 g/mol;
(c) 120 mg of glyceryl dibehenate powder;
(d) 45 mg of spray-dried lactose monohydrate;
(e) 42 mg of micronized poloxamer 188;
(f) 70 mg of microcrystalline cellulose;
(g) 4.5 mg of amorphous anhydrous colloidal silicon dioxide; and
(h) 7.5 mg of magnesium stearate.

### Claim 4 (depends on 2)

The tablet of claim 2 further comprising from 10 mg to 12 mg of a film coating comprising polyvinyl alcohol, titanium dioxide, and polyethylene glycol 3350.

### Claim 5 (depends on 3)

The tablet of claim 3 further comprising a film coating consisting of 11.22 mg of a mixture of polyvinyl alcohol, titanium dioxide, polyethylene glycol 3350, talc, disodium 2-[[4-[ethyl-[(3-sulfonatophenyl)methyl]amino]phenyl]-[4-[ethyl-[3-sulfonatophenyl)methyl]azaniumylidene]cyclohexa-2,5-dien-1-ylidene]methyl]benzenesulfonate, and indigo carmine.

### Claim 6 (depends on 2)

The tablet of claim 2, wherein the tablet releases 20-45% by weight of bexagliflozin after 3 hours, according to an in vitro dissolution test performed with a United States Pharmacopoeia Apparatus 1 at 50 rpm with 900 mL of 0.1 N HCl at 37±0.5° C.

### Claim 7 (depends on 2)

The tablet of claim 2, wherein the tablet releases 45-75% by weight of bexagliflozin after 5 hours, according to an in vitro dissolution test performed with a United States Pharmacopoeia Apparatus 1 at 50 rpm with 900 mL of 0.1 N HCl at 37±0.5° C.