Granted Patent B2

US 12,569,505 · App. 19/210,719 · Granted Mar 10, 2026

Inventors: Jonathon Oliver Whitehouse (Herne Bay, GB); Md Mushfiq Hossain Akanda (Gillingham, GB); Edward Thomas (Faversham, GB); John Croall (Minster-on-sea, GB); Tammy Iyobosa Morrison (Rochester, GB)

Assignee: JAZZ PHARMACEUTICALS RESEARCH UK LIMITED

A61K31/658A61K9/1611A61K9/1617A61K9/4866A61K47/22

Abstract

Claims (35)

1 . A drug-containing particle comprising:

a. a drug substance comprising cannabidiol, wherein the cannabidiol is present at an amount ranging from about 15% to about 40% by weight based on the total weight of the drug-containing particle;

b. a porous solid carrier at an amount ranging from about 10% to about 60% by weight based on the total weight of the drug-containing particle;

c. a lipophilic material at an amount ranging from about 20% to about 35% by weight based on the total weight of the drug-containing particle; and

d. one or more antioxidants,

wherein the drug substance is adsorbed onto the porous solid carrier, wherein the porous solid carrier comprises a mesoporous silica or an amorphous silica, wherein the porous solid carrier has an average pore volume of about 1 mL/g to 2 mL/g; and wherein the lipophilic material comprises:

mono-, di- and triglyceride esters of C8-C18 fatty acids;

mono-, di-, and triglyceride esters of lauric and stearic acids and PEG-6 mono- and diesters of lauric and stearic acids; or

propylene glycol monocaprylate; or combinations thereof.

2 . The drug-containing particle of claim 1 , wherein the drug substance further comprises no more than about 0.5% by weight of active of cannabidiorcol (CBD-C1), no more than about 0.5% by weight of active of cannabidivarin (CBDV), or no more than about 0.2% by weight of active of cannabidibutol (CBD-C4).

3 . The drug-containing particle of claim 1 , wherein the cannabidiol is present in an amount ranging from about 20% to about 35% by weight based on the total weight of the drug-containing particle.

4 . The drug-containing particle of claim 1 , wherein the cannabidiol is present in non-crystalline form as measured by X-ray powder diffraction.

5 . The drug-containing particle of claim 1 , wherein the porous solid carrier comprises a mesoporous silica.

6 . The drug-containing particle of claim 1 , wherein the porous solid carrier is present in an amount ranging from about 30% to about 50% by weight based on the total weight of the drug-containing particle.

7 . The drug-containing particle of claim 1 , wherein the porous solid carrier has an average pore volume of about 1 mL/g to 1.9 mL/g.

8 . The drug-containing particle of claim 1 , wherein the porous solid carrier has an average surface area of about 250 m 2 /g to about 375 m 2 /g.

9 . The drug-containing particle of claim 1 , wherein the porous solid carrier has an average pore diameter of about 2 nm to about 50 nm.

10 . The drug-containing particle of claim 1 , wherein the porous solid carrier is a microparticle.

11 . The drug-containing particle of claim 1 , wherein the porous solid carrier has an average particle size of about 50 μm to about 150 μm.

12 . The drug-containing particle of claim 1 , wherein the porous solid carrier has a porosity of about 75% to about 99%.

13 . The drug-containing particle of claim 1 , wherein the lipophilic material comprises mono-, di- and triglyceride esters of C8-C18 fatty acids.

14 . The drug-containing particle of claim 1 , wherein the lipophilic material comprises mono-, di-, and triglyceride esters of lauric and stearic acids and PEG-6 mono- and diesters of lauric and stearic acids.

15 . The drug-containing particle of claim 1 , wherein the lipophilic material comprises propylene glycol monocaprylate.

16 . The drug-containing particle of claim 1 , wherein the lipophilic material comprises mono-, di-, and triglyceride esters of lauric and stearic acids and PEG-6 mono- and diesters of lauric and stearic acids, or propylene glycol monocaprylate.

17 . The drug-containing particle of claim 1 , wherein the one or more antioxidants comprises alpha-tocopherol, β-carotene, ascorbic acid, ascorbyl palmitate, lecithin, butylated hydroxyanisole, butylated hydroxytoluene, monothiolglycerol, propyl gallate, or a combination thereof.

18 . The drug-containing particle of claim 1 , wherein the one or more antioxidants comprises alpha-tocopherol.

19 . The drug-containing particle of claim 1 , wherein the amount of the one or more antioxidants ranges from about 0.05% to about 1.5% by weight based on the total weight of the drug-containing particle.

20 . The drug-containing particle of claim 1 , wherein the amount of the one or more antioxidants ranges from about 0.2% to about 1% by weight based on the total weight of the drug-containing particle.

21 . The drug containing particle of claim 1 , further comprising a chelating agent.

22 . The drug-containing particle of claim 21 , wherein the chelating agent comprises EDTA, citric acid, curcumin, or a combination thereof.

23 . The drug containing particle of claim 1 , wherein at least 50% of the cannabidiol is released from the drug-containing particle in 1 hour, as measured under USP 711 with a Type II apparatus at pH 6.8.

24 . A pharmaceutical composition comprising a plurality of the drug containing particles of claim 1 .

25 . The drug-containing particle of claim 1 , wherein the porous solid carrier has an average surface area of about 320 m 2 /g to about 375 m 2 /g.

26 . The drug-containing particle of claim 1 , wherein the porous solid carrier has an average pore diameter of about 15 nm to about 30 nm.

27 . The drug-containing particle of claim 1 , wherein the porous solid carrier comprises mesoporous silica and has an average surface area of about 320 m 2 /g to about 375 m 2 /g and an average pore volume of about 1 mL/g to about 1.9 mL/g.

Assignments (3)

Continuity (4)

References Cited (400)