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1. WO2011003853 - PROCESS FOR DRYING OF BIBW2992, OF ITS SALTS AND OF SOLID PHARMACEUTICAL FORMULATIONS COMPRISING THIS ACTIVE INGREDIENT

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[ EN ]

CLAIMS

1. A process for drying of BIBW 2992 or a salt thereof, comprising drying with a gas which is inert towards BIBW 2992 or the salt thereof at the drying conditions and which has a relative humidity (rh) of not more than 15 %, at a temperature below 400C.

2. A process for drying of a pharmaceutical formulation comprising BIBW 2992 or a salt thereof as the active product ingredient (API) and at least one further excipient, with a gas which is inert towards the ingredients of the pharmaceutical formulation at the drying conditions, and which has a relative humidity of not more than 15 % at a temperature below 400C.

3. A process according to one of claims 1 or 2, wherein the BIBW 2992 salt is selected from the hydrochloride, hydrobromide, hydroiodide, hydrosulphate, hydrophosphate, hydromethanesulphonate, hydronitrate, hydromaleate, hydroacetate, hydrobenzoate, hydrocitrate, hydrofumarate, hydrotartrate, hydrolactate, hydroxalate, hydrosuccinate, hydrobenzoate and hydro-p-toluenesulphonate, preferably the hydrochloride, hydrobromide, hydrosulphate, hydrophosphate, hydromaleate, hydrofumarate and hydromethanesulphonate.

4. A process according to one of claims 1 or 2, wherein the BIBW 2992 salt is the dimaleate (BIBW 2992 MA2).

5. A process according to any of claims 1 to 4, wherein the gas has a relative humidity of not more than 12 % rh and a temperature in the range of 20 to 400C, preferably below 300C.

6. A process according to any of claims 1 to 5, wherein the gas is inert gas, dried compressed or constantly supply dried air, nitrogen or carbon dioxide.

7. A process according to any of claims 1 to 6, wherein BIBW 2992 or the salt thereof is placed in a container having an inlet and an outlet opening for the supply and removal of the gas and the gas is supplied as a continuous flow-through of dried compressed air or by a continuous flow generated by ventilators.

8. The process according to claim 7, wherein the gas is supplied as a continuous flow-through of dried compressed air with a pressure at the outlet of approximately 0.5 to 3 bar.

9. The process according to claim 7, wherein the gas is supplied as a continuous flow generated by ventilators (e.g using a Munters® device) providing an air flow rate of 20 - 1000 ncm/h.

10. The process according to any of claims 1 to 9, performed for at least 8 hours.

11. A pharmaceutical composition comprising BIBW 2992 or a salt thereof as the active product ingredient (API) and at least one further excipient, characterized by a water activity of the formulation of not more than 0.20, preferably of not more than 0.17, or, most preferred, of not more than 0.15.

12. A pharmaceutical composition comprising BIBW 2992 or a salt thereof as the active product ingredient (API) and at least one further excipient, characterized by a water content (Karl-Fischer) of not more than 4.2 %, preferably of not more than 4.0 %, particularly of not more than 3.8 %, or, most preferred, of not more than 3.7 %.

13. The pharmaceutical composition of claim 11 or 12, selected from intermediate blends for further processing, oral powders, oral granules, pellets, uncoated tablets and filmcoated tablets.