Concentrated methotrexate solutions

Abstract

Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 25 mg/ml. The invention also relates to a ready-made syringe and a carpule containing such a pharmaceutical solution formulation, as well as a pen injector comprising such a carpule and/or a ready-made syringe.

1 . A ready-made syringe, comprising a pharmaceutical solution formulation of methotexate with a concentration of more than 30 mg/ml in a pharmaceutically acceptable solvent for subcutaneous administration. 
     
     
         2 . The ready-made syringe according to  claim 1 , wherein the methotrexate is present at a concentration of more than 30 mg/ml to 100 mg/ml. 
     
     
         3 . The ready-made syringe according to  claim 2 , wherein the methotrexate is present at a concentration of about 50 mg/ml. 
     
     
         4 . The ready-made syringe according to  claim 1 , comprising a dosage of 5 to 40 mg of methotrexate. 
     
     
         5 . The ready-made syringe according to  claim 1 , comprising a dosage selected from 5.0, 7.5, 10.0, 12.5, 15.0, 17.5, 20.0, 22.5, 25.0, 27.5, 30.0, 32.5, 35.0, 37.5 or 40.0 mg of methotrexate. 
     
     
         6 . The ready-made syringe according to  claim 1 , wherein the pharmaceutically acceptable solvent is selected from water, water for injection purposes, water comprising isotonization additives and sodium chloride solution. 
     
     
         7 . The ready-made syringe according to  claim 6 , wherein the sodium chloride solution comprises isotonic sodium chloride solution 
     
     
         8 . The ready-made syringe according to  claim 1 , wherein the ready-made syringe is constructed to allow patient self-administration by a patient with limited fine motor skills 
     
     
         9 . A carpule, comprising a pharmaceutical solution formulation of methotrexate with a concentration of more 30 mg/ml in a pharmaceutically acceptable solvent for subcutaneous administration. 
     
     
         10 . The carpule according to  claim 9 , wherein the methotrexate is present at a concentration of more than 30 mg/ml to 100 mg/ml. 
     
     
         11 . The carpule according to  claim 10 , wherein the methotrexate is present at a concentration of about 50 mg/ml. 
     
     
         12 . The carpule according to  claim 9 , wherein the pharmaceutical solution formulation furthermore comprises a preservative. 
     
     
         13 . The carpule according to  claim 9 , wherein said carpule contains a total dosage amount of 5 to 5,000 mg. 
     
     
         14 . The carpule according to  claim 9 , wherein the corpule contains a total dosage amount of 7.5 to 300 mg of methotrexate. 
     
     
         15 . The carpule according to  claim 9 , wherein the pharmaceutically acceptable solvent is selected from water, water for injection purposes, water comprising isotonization additives and sodium chloride solution. 
     
     
         16 . The carpule according to  claim 15 , wherein the sodium chloride solution comprises isotonic sodium chloride solution 
     
     
         17 . A pen injector comprising the carpule according to  claim 9 . 
     
     
         18 . The pen injector according to  claim 17 , wherein the carpule and the pen injector are effective to provide administration of multiple applications of single dosages. 
     
     
         19 . The pen injector according to  claim 18 , wherein the single dosages per application can be adjusted to 5 to 40 mg each of methotrexate. 
     
     
         20 . The pen injector according to  claim 19 , wherein the single dosages per application can be adjusted to be selected from 5.0, 7.5, 10.0, 12.5, 15.0, 17.5, 20.0, 22.5, 25.0, 27.5, 30.0, 32.5, 35.0, 37.5 or 40.0 mg each of methotrexate