Combination and uses and treatments thereof

Patent metadata

Field	Value
Publication number	US-12011506-B2
Application number	US-201816621309-A
Country	US
Kind code	B2
Filing date	Jun 27, 2018
Priority date	Jun 30, 2017
Publication date	Jun 18, 2024
Grant date	Jun 18, 2024

Abstract

Methods are provided for treating or preventing human immunodeficiency virus-1 (HIV-1) or human immunodeficiency virus-2 (HIV-2) in a virologically suppressed patient in need thereof comprising switching the patient from an antiretroviral treatment regimen comprising at least three antiretroviral agents to a treatment regimen comprising only two antiretroviral agents. In one aspect the two treatment regimen consists of dolutegravir, rilpivirine and at least one pharmaceutically acceptable excipient, diluent or carrier. In another aspect of the invention, there is provided a multilayer tablet comprising dolutegravir or a pharmaceutically acceptable salt thereof and rilpivirine or a pharmaceutically acceptable salt thereof.

First claim

We claim:

1. A bilayer tablet comprising
a) a first layer comprising dolutegravir sodium; and
b) a second layer comprising rilpivirine hydrochloride;
wherein said first layer and said second layer are in direct contact, and wherein the first layer consists of:

Ingredient
Mass (mg)

Intragranular

Dolutegravir sodium
52.62

D-mannitol
145.38

Microcrystalline cellulose
60.00

Povidone K29/32
15.00

Sodium starch glycolate
15.00

Purified water
q.s.

Extragranular

Sodium starch glycolate
6.00

Sodium stearyl fumarate
6.00

and the second layer consists of:

Ingredient
Mass (mg)

Intragranular

Rilpivirine hydrochloride
27.50

Lactose monohydrate
55.145

Croscarmellose sodium
1.10

Povidone K30
3.25

Polysorbate 20
0.35

Purified water
q.s.

Extragranular

D-mannitol
57.755

Silicified microcrystalline cellulose
40.00

Sodium starch glycolate
12.90

Magnesium stearate
2.00.

2. The bilayer tablet of claim 1 wherein the bilayer tablet further comprises a coating.

3. The bilayer tablet of claim 2 , wherein the coating comprises polyvinyl alcohol, titanium dioxide, macrogol/PEG, talc, yellow and red iron oxide.

4. The bilayer tablet of claim 2 , wherein the bilayer tablet comprises about 1 mg to about 30 mg of the coating.

5. The bilayer tablet of claim 2 , wherein the bilayer tablet comprises about 0.2% to about 6% w/w of the coating.

6. The bilayer tablet of claim 5 , wherein the bilayer tablet comprises about 2% to about 4% w/w of the coating.

7. The bilayer tablet of claim 5 , wherein the bilayer tablet comprises about 3% w/w of the coating.

8. The tablet of claim 2 , the multilayer tablet comprises about 15 mg of the film coating.

Assignees

• Viiv Healthcare Co
• Janssen Sciences Ireland Unlimited Co
• Janssen Sciences Ireland Uc

Inventors

• Campbell Kenneth Churchill
• Delaet Urbain Alfons C
• Goodrich James M
• Guaquière Juliette Segolène
• Laughery Thomas
• Limet Dominique J
• Pottage John C
• Renou Ludovic Sylvain Marc
• Scott Trevor R
• Seiler Christian
• Woodward Mary

Classifications

• A61K31/5365

  ortho- or peri-condensed with heterocyclic ring systems · CPC title

• A61K31/505 Primary

  Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim · CPC title

• A61K9/28

  Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} · CPC title

• A61K9/2095

  Tabletting processes · CPC title

• A61P31/18

  for HIV · CPC title