RU-2026112150-A - PHARMACEUTICAL COMPOSITIONS

Inventors

• ЧУ, Кевин Сэм
• ДЖОУНС, Клинтон Фрэнк
• МУНДРА, Дипак Балкришна
• ПАНЬ, Жэньнань
• ФИЛИП, Остин
• АЛИДОРИ, Симоне
• Гупта, Маниш К.
• Саха, Пратик
• ТАСКАР, Пранджал Самир

Assignees

• ВИИВ ХЭЛСКЭАР ЮКЕЙ (НО.3) ЛИМИТЕД

Dates

Publication Date

20260505

Application Date

20240925

Priority Date

20230927

Claims (20)

1. 1. A pharmaceutical composition containing:
2. cabotegravir;
3. a wetting agent, wherein the wetting agent is polysorbate 80 (PS80);
4. a stabilizer, wherein the stabilizer is sodium carboxymethylcellulose (SMC); and
5. tonicity regulator, where the tonicity regulator is mannitol;
6. wherein cabotegravir is present as particles having a mass median diameter (X50) of 2.5 μm to 10 μm (inclusive).
7. 2. The pharmaceutical composition according to claim 1, wherein cabotegravir is present in the form of particles having a mass median diameter (X50) greater than or equal to 3 μm and less than or equal to 8.5 μm.
8. 3. The pharmaceutical composition according to claim 1 or 2, wherein the cabotegravir particles have an X50 value greater than or equal to 3.5 μm and less than or equal to 8.0 μm, and wherein the cabotegravir particles have an X90 value greater than or equal to 7.0 μm and less than or equal to 18.0 μm.
9. 4. The pharmaceutical composition of any one of claims 1-3, wherein cabotegravir is present in an amount of from about 350 mg to about 1650 mg.
10. 5. The pharmaceutical composition according to any one of claims 1-4, wherein cabotegravir is present in an amount of about 800 mg.
11. 6. The pharmaceutical composition according to any one of claims 1-4, wherein cabotegravir is present in an amount of about 1600 mg.
12. 7. The pharmaceutical composition of any one of claims 1-6, wherein the weight ratio of the wetting agent to cabotegravir is in the range of from about 1:100 to about 1:150;
13. wherein the weight ratio of stabilizer to cabotegravir is in the range of from about 1:70 to about 1:120; and
14. wherein the mass ratio of the tonicity regulator to cabotegravir is in the range of from about 1:8 to about 1:25.
15. 8. The pharmaceutical composition according to any one of claims 1-7, wherein the mass ratio of cabotegravir:PS80:sodium CMC:mannitol is approximately 100:1:1.25:8.75.
16. 9. The pharmaceutical composition according to any one of claims 1-7, wherein the mass ratio of cabotegravir:PS80:sodium CMC:mannitol is approximately 400:3:3.7:25.9.
17. 10. A pharmaceutical composition according to any one of claims 1-9, wherein the pharmaceutical composition is presented in the form of a lyophilized powder.
18. 11. The pharmaceutical composition of any one of claims 1-10, wherein the concentration of cabotegravir is in the range of from about 300 mg/ml to about 650 mg/ml.
19. 12. The pharmaceutical composition according to claim 11, wherein the concentration of cabotegravir is approximately 400 mg/ml.
20. 13. The pharmaceutical composition of claim 11, wherein the concentration of cabotegravir is approximately 533 mg/ml.