Claims for Patent: 9,956,171

Summary for Patent: 9,956,171

Title:	Liquid inhalation formulation comprising RPL554
Abstract:	The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation which comprises a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof. Also described is a liquid pharmaceutical composition according to the invention for use in the treatment of the human or animal body.
Inventor(s):	Spargo Peter Lionel, French Edward James, Haywood Phillip A.
Assignee:	VERONA PHARMA PLC
Application Number:	US15509943
Patent Claims:	2. A liquid pharmaceutical composition according to claim 1 , wherein the particles of RPL554 have a particle size distribution with a Dv50 value of from about 0.7 μm to about 2.5 μm.3. A liquid pharmaceutical composition according to claim 1 , wherein the concentration of particles of RPL554 in the liquid pharmaceutical composition is from about 0.01 mg/mL to about 40 mg/mL.4. A liquid pharmaceutical composition according to claim 1 , wherein the composition has a pH of from about 6 to about 8.5. A liquid pharmaceutical composition according to which further comprises one or more surfactants.6. A liquid pharmaceutical composition according to claim 5 , wherein the one or more surfactants are selected from one or more non-ionic surfactants.7. A liquid pharmaceutical composition according to claim 6 , wherein the one or more surfactants are selected from polyoxyethylene glycol sorbitan alkyl esters and sorbitan alkyl esters.8. A liquid pharmaceutical composition according to which further comprises one or more buffers.9. A liquid pharmaceutical composition according to claim 8 , wherein the one or more buffers are selected from citrate or phosphate buffers.10. A liquid pharmaceutical composition according to claim 1 , which composition comprises:(a) the particles of RLP554 at a concentration of from about 0.01 mg/mL to about 40 mg/mL;(b) one or more surfactants at a concentration of from about 0.01 mg/mL to about 5 mg/mL; and(c) a buffer at a concentration of from about 5 mg/mL to about 20 mg/mL.11. A liquid pharmaceutical composition according to claim 1 , wherein the composition further comprises a tonicity adjuster claim 1 , optionally wherein the tonicity adjuster is sodium chloride.12. A liquid pharmaceutical composition according to claim 1 , wherein the diluent is water.13. A liquid pharmaceutical composition according to claim 1 , which composition comprises:(a) the particles of RLP554 at a concentration of 0.01 mg/mL to 30 mg/mL;(b) a polyoxyethylene glycol sorbitan alkyl ester at a concentration of from 0.1 mg/mL to 2 mg/mL;(c) a sorbitan alkyl ester at a concentration of from 0.01 mg/mL to 0.1 mg/mL;(d) a first phosphate buffer component at a concentration of from 5 mg/mL to 10 mg/mL;(e) a second phosphate buffer component at a concentration of from 5 mg/mL to 10 mg/mL; and(f) a tonicity adjuster at a concentration of from 2 mg/mL to 8 mg/mL.14. A liquid pharmaceutical composition according to claim 1 , which composition comprises:(a) the particles of RLP554 at a concentration of 0.05 mg/mL to 25 mg/mL;(b) polyoxyethylene (20) sorbitan monolaurate (Polysorbate 20, Tween 20) at a concentration of from 0.1 mg/mL to 2 mg/mL;(c) sorbitan monolaurate (Span 20) at a concentration of from 0.01 mg/mL to 0.1 mg/mL;(d) monosodium phosphate monohydrate at a concentration of from 5 mg/mL to 10 mg/mL;(e) dibasic sodium phosphate anhydrous at a concentration of from 5 mg/mL to 10 mg/mL; and(f) sodium chloride at a concentration of from 2 mg/mL to 8 mg/mL.15. A liquid pharmaceutical composition according to which is suitable for administration by nebulizer.16. A nebulizer comprising a composition according to .17. A method of treating a disease or condition selected from asthma claim 1 , allergic asthma claim 1 , hay fever claim 1 , allergic rhinitis claim 1 , bronchitis claim 1 , emphysema claim 1 , bronchiectasis claim 1 , chronic obstructive pulmonary disease (COPD) claim 1 , adult respiratory distress syndrome (ARDS) claim 1 , steroid resistant asthma claim 1 , severe asthma claim 1 , paediatric asthma claim 1 , cystic fibrosis claim 1 , lung fibrosis claim 1 , pulmonary fibrosis claim 1 , interstitial lung disease claim 1 , skin disorders claim 1 , atopic dermatitis claim 1 , psoriasis claim 1 , ocular inflammation claim 1 , cerebral ischaemia claim 1 , inflammatory diseases and auto-immune diseases in a subject claim 1 , which method comprises administering to said subject an effective amount of a liquid pharmaceutical composition according to .18. A method of treating a disease or condition according to claim 17 , wherein the disease or condition is chronic obstructive pulmonary disease (COPD).