Tigecycline composition for injection

Abstract

Disclosed is a tigecycline composition for injection, comprising the active component, tigecycline, and a propping agent. Also included is a stabilization agent. Also disclosed is a stable, pharmaceutically acceptable reconstitution liquid having freeze-dried tigecycline. The tigecycline composition for injection of the present invention has good redissolution, and can dissolve without intense shaking, thereby avoiding foams caused by intense shaking. Upon testing, the tigecycline composition and the tigecycline composition-diluted reconstitution liquid prepared in the present invention prove to have substantially lowered oxidation degradation and epimer generation and increased stability of the tigecycline preparation. Compared to the compositions currently in clinical use, the composition of the present invention can increase the treatment effect of tigecycline, avoid safety risks caused by lactose, is easy to produce and store, and has a clinical usage stability, satisfying the requirements for clinical medicine.

1 . A tigecycline composition for injection, characterized in that it comprises the active component tigecycline and a propping agent. 
     
     
         2 . The tigecycline composition for injection as claimed in  claim 1 , characterized in that said propping agent is selected from one or several of L-arginine, L-arginine hydrochloride, D-arginine, DL-arginine, and a salt formed by L, D or DL-arginine with an acid or alkali. 
     
     
         3 . The tigecycline composition for injection as claimed in  claim 1 , characterized in that said propping agent is L-arginine hydrochloride. 
     
     
         4 . The tigecycline composition for injection as claimed in any one of  claims 1  to  3 , characterized in that it further comprises a stabilizing agent. 
     
     
         5 . The tigecycline composition for injection as claimed in  claim 4 , characterized in that the weight ratio among components of the tigecycline composition for injection is:
 tigecycline 1.0, the propping agent 0.2-10, and the stabilizing agent 0-4.   
     
     
         6 . The tigecycline composition for injection as claimed in  claim 4 , characterized in that the weight ratio among components of the tigecycline composition for injection is: tigecycline 1.0, the propping agent 0.3-4, and the stabilizing agent 0-2. 
     
     
         7 . The tigecycline composition for injection as claimed in  claim 4 , characterized in that said stabilizing agent is sodium chloride. 
     
     
         8 . The tigecycline composition for injection as claimed in  claim 4 , characterized in that the pH value of the tigecycline composition for injection is additionally adjusted to 3.0-8.0 using a pH adjuster. 
     
     
         9 . The tigecycline composition for injection as claimed in  claim 4 , characterized in that the pH value of the tigecycline composition for injection is additionally adjusted to 4.0-6.0 using a pH adjuster. 
     
     
         10 . The tigecycline composition for injection as claimed in  claim 8 , characterized in that said pH adjuster is hydrochloric acid, sodium hydroxide or a mixture thereof. 
     
     
         11 . The tigecycline composition for injection as claimed in  claim 9 , characterized in that said pH adjuster is hydrochloric acid, sodium hydroxide or a mixture thereof. 
     
     
         12 . The tigecycline composition for injection as claimed in  claim 1 , characterized in that the amount of tigecycline is 50 mg. 
     
     
         13 . The tigecycline composition for injection as claimed in  claim 1 , characterized in that the tigecycline composition for injection is a solution for injection or a solid preparation for injection. 
     
     
         14 . The tigecycline composition for injection as claimed in  claim 13 , characterized in that said solid preparation for injection is a freeze-dried powder for injection. 
     
     
         15 . A stable and pharmaceutically acceptable reconstituted solution of freeze-dried tigecycline, characterized in that it is prepared by treating the freeze-dried powder of the tigecycline composition for injection as claimed in  claim 1  with a suitable amount of a pharmaceutically acceptable diluent. 
     
     
         16 . The reconstituted solution as claimed in  claim 15 , characterized in that said diluent is normal saline, 5% glucose solution or lactated Ringer's solution.