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US 10,238,634 B2Granted
Aqueous-based metronidazole gel formulations
AssigneeChemo Research, S.L.
InventorsMichael T. Nordsiek, Kodumudi S. Balaji
Life of this patent
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Abstract
The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.
Claims9
An intravaginal aqueous based gel composition comprising:
- a) metronidazole in a concentration of about 1.3% to about 1.5% by weight of the aqueous based gel composition;
- b) about 1% to about 3% by weight of the aqueous based gel composition of one or more mucoadhesive gelling polymers;
- c) about 30% to about 60% of water by weight of the aqueous based gel composition;
- and
- d) a ternary solvent system in a concentration of about 30% to about 60% by weight of the aqueous based gel composition, wherein the ternary solvent system comprises:
- i) one or more lower aromatic alcohols selected from the group consisting of benzyl alcohol, 2-methylbenzyl alcohol, phenoxyethanol, and mixtures thereof;
- ii) one or more lower alkylene diols selected from the group consisting of ethane-1,2-diol (ethylene glycol), propane-1,2-diol (propylene glycol), and mixtures thereof;
- and
- iii) one or more polyoxyalkylenes selected from the group consisting of polyoxyethylene (polyethylene glycol), polyoxypropylene, (polypropylene glycol) and mixtures thereof;
- said aqueous based gel composition exhibiting a viscosity ranging from about 200,000 mPa·s to about 400,000 mPa·s, measured at 25° C. using the controlled shear rate method, a Bohlin CVO 100 rheometer and the rheometer settings of Table 11 and having an aqueous phase with a pH ranging from about 3.0 to about 5.0.
7 more elements
A method of treating a subject with bacterial vaginosis, comprising administering intravaginally to the subject a single dose aqueous based metronidazole gel composition wherein the single dose aqueous based metronidazole gel composition is administered once a day for one, two or three days, and the single dose aqueous based metronidazole gel composition comprises:
- i) 60-70 mg of metronidazole in a concentration of about 1.3% to about 1.5% by weight of the aqueous based metronidazole gel composition;
- ii) about 30% to about 60% of water by weight of the single dose aqueous based metronidazole gel composition;
- iii) about 1% to about 3% by weight of the single dose aqueous based metronidazole gel composition of at least one mucoadhesive gelling polymer;
- and
- iv) about 30% to about 60% of a ternary solvent system by weight of the single dose aqueous based metronidazole gel composition, the ternary solvent system comprising:
- 1) one or more lower aromatic alcohols selected from the group consisting of benzyl alcohol, 2-methylbenzyl alcohol, phenoxyethanol, and mixtures thereof;
- 2) one or more lower alkylene diols selected from the group consisting of ethane-1,2-diol (ethylene glycol), propane-1,2-diol (propylene glycol), and mixtures thereof;
- and
- 3) one or more polyoxyalkylenes selected from the group consisting of polyoxyethylene (polyethylene glycol), polyoxypropylene, (polypropylene glycol) and mixtures thereof;
- wherein the single dose aqueous based metronidazole gel exhibits:
- a) a pH ranging from about 3.0 to about 5.0;
- and
- b) a viscosity of about 200,000 mPa·s to about 400,000 mPa·s at 25° C. using a controlled shear rate ramp method, a Bohlin CVO 100 rheometer and the rheometer settings of Table 11.
10 more elements
An intravaginal aqueous based gel composition comprising:
- a) metronidazole in a concentration of about 1.3% to about 1.5% by weight of the aqueous based gel composition;
- b) about 1% to about 3% by weight of the aqueous based gel composition of one or more mucoadhesive gelling polymers selected from the group consisting of hydroxyethylcellulose, a polycarbophil, and mixtures thereof;
- c) about 30% to about 60% of water by weight of the aqueous based gel composition;
- and
- d) a ternary solvent system in a concentration of about 30% to about 60% by weight of the aqueous based gel composition, wherein the ternary solvent system consists of:
- i) about 1.3% to about 2.5% by weight of the aqueous based gel composition of one or more lower aromatic alcohols selected from the group consisting of benzyl alcohol, 2-methylbenzyl alcohol, phenoxyethanol, and mixtures thereof;
- ii) about 3% to about 20% by weight of the aqueous based gel composition of one or more lower alkylene diols selected from the group consisting of ethane-1,2-diol (ethylene glycol), propane-1,2-diol (propylene glycol), and mixtures thereof;
- and
- iii) about 10% to about 50% by weight of the aqueous based gel composition of one or more polyoxyalkylenes selected from the group consisting of polyoxyethylene (polyethylene glycol), polyoxypropylene, (polypropylene glycol) and mixtures thereof;
- said aqueous based gel composition exhibiting a viscosity ranging from about 200,000 mPa·s to about 400,000 mPa·s, measured at 25° C. using a controlled shear rate method, a Bohlin CVO 100 rheometer and the rheometer settings of Table 11 and having an aqueous phase with a pH ranging from about 3.0 to about 5.0.
7 more elements
Dependencies are inferred from the claim text.