Process for formulation of antibiotic compounds

  • US 6,486,150 B2
  • Filed: 04/27/2001
  • Issued: 11/26/2002
  • Est. Priority Date: 10/29/1999
  • Status: Expired due to Term
First Claim
Patent Images

1. A process for preparing a final formulation product of a compound of formula I, embedded imageor its pharmaceutically acceptable salt, or hydrate wherein,R1 is:

  • (a) 1-hydroxyethyl, (b) 1-fluoroethyl, or (c) hydroxymethyl;

    R2 and R3 are independently;

    (a) hydrogen, or (b) (C1-C6)-alkyl;

    R4, R5, and R6 are independently (a) hydrogen (b) (C1-C6)-alkyl, or (c) alkali-metal or alkali earth-metal wherein the alkali-metal or alkali earth-metal is sodium, potassium, lithium, cesium, rubidium, barium, calcium or magnesium; and

    R7 and R8 are independently;

    (a) hydrogen, (b) halo, (c) cyano, (d) (C1-C6)-alkyl, (e) nitro, (f) hydroxy, (g) carboxy, (h) (C1-C6)-alkoxy, (i) (C1-C6)-alkoxycarbonyl, (j) aminosulphonyl, (k) (C1-C6)-alkylaminosulphonyl, (l) di-(C1-C6)-alkylaminosulphonyl, (m) carbamoyl, (n) (C1-C6)-alkylcarbamoyl, (o) di-(C1-C6)-alkylcarbamoyl, (p) trifluoromethyl, (q) sulphonic acid, (r) amino, (s) (C1-C6)-alkylamino, (t) di-(C1-C6)-alkylmino, (u) (C1-C6)-alkanoylamino, (v) (C1-C6)-alkanoyl(N-(C1-C6)-alkyl)amino, (w) (C1-C6)-alkanesulphonamido, or (x) (C1-C6)-alkyl-S(O)n wherein n is 0-2;

    comprising the steps of;

    (1) charging a solution of carbon dioxide source having a pH range of about 6.0 to about 12.0 into a reaction vessel;

    (2) adding an effective amount of a mole ratio of a base and an active ingredient into the reaction vessel containing the solution of carbon dioxide source to maintain pH at about 6.0 to about 9.0 and a temperature range of about −

    C. to about 15°


    (3) lyophilizing the solution of Step (2) to yield the final formulation product of a compound of formula I with less than about 10% of moisture content.

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