Tacrolimus compositions and methods of use
AssigneeCn2 Therapeutics, Inc.
InventorFRANCIS E. O'DONNELL, Jr.
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Abstract
The subject invention pertains to tacrolimus compositions and a method for the treatment of symptoms of allergic conjunctivitis or keratoconjunctivitis, including, for example, ocular redness and ocular itchiness. The composition is preservative free and can be dispensed in a multidose container.
Claims29
A composition comprising tacrolimus according to Formula (I), Formula (II), Formula (III), or any combination thereof, a carrier, a viscosifier, a dispersant, an emollient, Hydroxypropyl-β-cyclodextrin, and a buffer, and excluding a preservative, wherein the tacrolimus is provided as a particle with a size of less than 5 μm, wherein the tacrolimus is sterilized by gamma irradiation, wherein the carrier comprises squalene at a concentration of about 1 to about 10% v/v, wherein the composition is formulated to be dispensed from a dropper or drip chamber in a single drop, wherein the single drop comprises an amount of tacrolimus of about 0.5 mg to about 0.8 mg, wherein the composition has a viscosity of 6.7 centipoise (cP) to about 25 cP, wherein the particle size of the composition is about 0.2 μm to about 0.9 μm, and wherein:
(canceled)
8-9. (canceled)
A method for synthesizing a product of interest, the method comprising:
- mixing tacrolimus into Solution I by overhead mixing;
- and
- diluting the tacrolimus and solution I suspension with solution II,
- wherein solution I comprises sodium phosphate monobasic monohydrate, dibasic sodium phosphate heptahydrate, and a dispersant;
- and solution II comprises a viscosifier, glycerin, sodium phosphate monobasic monohydrate, dibasic sodium phosphate heptahydrate, and a dispersant, and
- wherein the product of interest has a pH of about 7 to about 8 and a concentration of 0.1% tacrolimus and excludes a preservative.
A method for synthesizing a product of interest, the method comprising:
- mixing tacrolimus into solution I by overhead mixing;
- microfluidizing the tacrolimus and solution I mixture with compressed air;
- and
- diluting the tacrolimus and solution I suspension with solution II or solution II and additional solution I,
- wherein solution I comprises sodium phosphate monobasic monohydrate, dibasic sodium phosphate heptahydrate, and a dispersant;
- and solution II comprises a viscosifier, glycerin, sodium phosphate monobasic monohydrate, dibasic sodium phosphate heptahydrate, and a dispersant,
- wherein the product of interest has a pH of about 7 to about 8 and a concentration of 0.1% tacrolimus and excludes a preservative, and
- wherein microfluidizing comprises 20 passes of the tacrolimus suspension in solution I through a microfluidization instrument.
Dependencies are inferred from the claim text.