|Title:||Low viscosity, highly flocculated triamcinolone acetonide suspensions for intravitreal injection|
|Abstract:||Triamcinolone acetonide suspension compositions are disclosed. The suspension compositions have a relatively low viscosity and are easy to extrude through a 27- or 30-gauge needle but are highly flocculated and easily redispersed. The compositions are particularly suitable for intravitreal injection.|
|Inventor(s):||Kabra; Bhagwati P. (Euless, TX), Sarkar; Ruma (Fort Worth, TX)|
|Assignee:||Alcon Research, Ltd. (Fort Worth, TX)|
1. An aqueous suspension composition particularly suited for injection into the eye, wherein the suspension composition does not contain a preservative, has a pH from
6-7.5, a viscosity of 2-12 cps, and a Degree of Flocculation of about 9.5 or greater, and wherein the suspension composition consists essentially of: a) 4% (w/v) triamcinolone acetonide having a mean volume diameter of 3-10 .mu.m; b) 0.5% (w/v) sodium
carboxymethylcellulose; c) 0.002-0.015% (w/v) polysorbate 80; d) one or more pharmaceutically acceptable chloride salts selected from the group consisting of sodium chloride, potassium chloride. calcium chloride, and magnesium chloride as
tonicity-adjusting agents in a total amount sufficient to cause the suspension composition to have an osmolality from 250-350 mOsm; e) a buffering agent; f) water for injection; and g) optionally a pH-adjusting agent.
2. The suspension composition of claim 1 wherein the sodium carboxymethylcellulose has a molecular weight such that a 2% (w/v) solution of the sodium carboxymethylcellulose in water at 25.degree. C. has a viscosity of 25-50 cps.
3. The suspension composition of claim 1 wherein the concentration of polysorbate 80 is 0.015% (w/v).
4. The suspension composition of claim 1 wherein the suspension composition comprises 0.4-0.6% (w/v) sodium chloride, 0.05-0.1% (w/v) potassium chloride, 0.04-0.06% (wlv) calcium chloride, and 0.01-0.04% (w/v) magnesium chloride.
5. The suspension composition of claim 1 wherein the buffering agent comprises sodium acetate and sodium citrate.
6. The suspension composition of claim 1 wherein the suspension composition has a viscosity of 2-9 cps.
7. The suspension composition of claim 6 wherein the suspension composition has a viscosity of 2-8 cps.