European patent- improved daptomycin injectable, page-4

Claims (9)
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1. A stable, lyophilized formulation comprising antibacterial agent daptomycin as active and tocopheryl phosphate hydrolysate.
2. A formulation comprising antibacterial agent daptomycin as active and tocopheryl phosphate hydrolysate mixture (TPM).
3. A stable, lyophilized formulation obtainable by lyophilizing a composition comprising antibacterial agent daptomycin as active and tocopheryl phosphate hydrolysate mixture (TPM).
4. The daptomycin formulation according to any one of claims 1 to 3, wherein the daptomycin is in the range of 350-500 mg.
5. The daptomycin formulation according to claim 2 or 3, wherein the tocopheryl phosphate hydrolysate mixture (TPM) comprises 0.5% tocopheryl phosphate hydrolysate, 1.7% ethanol, a pH adjuster 0.1 M NaOH and water.
6. A process for preparation of stable lyophilized formulation of daptomycin comprising:
   i) dissolving tocopheryl phosphate hydrolysate mixture (TPM) under continuous stirring in absolute ethanol (dehydrated), followed by addition of this solution to water for injection at the temperature between 2-8°C;
   ii) dissolving daptomycin under continuous stirring in solution of step (i) followed by adjusting the pH to 3.5-5.0 with sodium hydroxide solution and making volume up to 100%;
   iii) filtering solution of step (ii) and filling into sterilised vials and lyophilizing.
7. The process according to claim 6, wherein the tocopheryl phosphate mixture (TPM) comprises 0.5% tocopheryl phosphate hydrolysate, 1.7 % ethanol, a pH adjuster 0.1 M NaOH and water.
8. A stable, lyophilized formulation