Preserved etherified cyclodextrin derivatives containing liquid aqueous pharmaceutical composition

Preserved etherified cyclodextrin derivatives containing liquid aqueous pharmaceutical composition

  • CN 105,377,235 A
  • Filed: 07/16/2014
  • Published: 03/02/2016
  • Est. Priority Date: 07/19/2013
  • Status: Active Application
First Claim
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1. an antiseptical liquid waterborne pharmaceutical composition, it comprises following:

  • The cyclodextrin derivative of-one or more etherificates;

    -one or more waterborne-type preservations;

    Be preferably selected from sorbic acid or its salt, preferred sodium sorbate, potassium sorbate, calcium sorbate;

    Benzoic acid or its salt, preferred sodium benzoate;

    Benzalkonium chloride;

    Benzethonium chloride;

    Cetylpyridinium chloride;

    Sodium pyrosulfite;

    Sodium acetate;

    P-Hydroxybenzoate and salt thereof, preferred methyl parahydroxybenzoate, ethylparaben, propyl p-hydroxybenzoate, butyl p-hydroxybenzoate, nipabutyl sodium;

    Or its combination;

    More preferably sorbic acid or its salt is selected from, preferred sodium sorbate, potassium sorbate, calcium sorbate;

    Benzoic acid or its salt, preferred sodium benzoate;

    Benzalkonium chloride;

    Benzethonium chloride;

    Cetylpyridinium chloride;

    Sodium pyrosulfite;

    Sodium acetate;

    Or its combination;

    With-at least one pharmaceutically active compound, its be insoluble in water, be very insoluble in water or water-fast;

    Wherein preferably, the dissolubility of described at least one pharmaceutically active compound in the scope of 15-25 DEG C in water is defined as follows;

    If must use more than 100mL water/g of compound, then described at least one pharmaceutically active compound is insoluble in water;

    If must use more than 1,000mL water/g of compound, then it is very insoluble in water;

    Carry out dissolved compound and if must use more than 10,000mL water/g of compound, then it is water-fast, andPreferred prerequisite is corticosteroid, particularly prednisolone and its prodrug prednisone acetate dragon, and fluoroquinolones, particularly ciprofloxacin, Gatifloxacin, Moxifloxacin, sitafloxacin, lomefloxacin, grepafloxacin, Gemifloxacin, norfloxacin, ofloxacin, levofloxacin and trovafloxacin, independently of one another from be insoluble in water, be very insoluble in water or be excluded water-fast pharmaceutically active compound.

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