THERAPEUTIC COMPOSITIONS FOR INTRANASAL ADMINISTRATION OF KETOROLAC
Therapeutic compositions, particularly sprayable aqueous compositions, comprise ketorolac or a pharmaceutically acceptable salt, in combination with a local anesthetic, such as lidocaine hydrochloride. The compositions are nasally administered to a subject in need thereof to treat pain or inflammation and have the benefit of reduced stinging and improved efficacy, compared to known nasally administered compositions.
1 . A composition for nasal administration to a patient, the composition comprises a therapeutically effective amount of a compound 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, of a formula
an optically active form thereof, a racemic mixture, or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable diluent and about 5 to 6% w/v of lidocaine, or a pharmaceutically acceptable salt thereof.
2 . The composition of claim 1 , wherein the pharmaceutically acceptable salt of the compound is ketorolac tromethamine as a racemic mixture.
3 . The composition of claim 1 , wherein the composition comprises 25 mg-225 mg of said compound dissolved per mL, wherein the diluent is water and the composition is liquid and sprayable.
4 . The composition of claim 3 , wherein the composition comprises 50-200 mg of said compound per mL.
5 . The composition of claim 1 , wherein a chelator is present.
6 . The composition of claim 1 , wherein the composition comprises about 2.5-22.5% w/v of said compound dissolved in the diluent, which is water.
7 . The composition of claim 6 , wherein the composition comprises about 15% w/v of said compound.
8 . The composition of claim 1 , wherein the composition is in a single-dose form for administration to a single patient, wherein the composition is a sprayable liquid and the diluent is water.
9 . The composition of claim 1 , wherein the composition is in a multi-dose formulation, wherein the composition is a sprayable liquid and the diluent is water.
10 . The composition of claim 1 , wherein the composition is in a form of an aqueous solution.
11 . The composition of claim 1 , wherein said pharmaceutically acceptable salt of lidocaine is lidocaine hydrochloride.
12 . (canceled)
13 . (canceled)
14 . The composition of claim 1 , wherein said composition is contained in a vessel equipped with a device for spraying the composition into the nasal passage of a subject, wherein the composition is an aqueous solution.
15 . The composition of claim 14 , wherein the vessel holds about 50 to 2000 microliters (μL).
16 . The composition of claim 1 , wherein the pH of the composition is about 6 to 7.5.
17 . (canceled)
18 . The composition of claim 1 , wherein
(1) water is the sole diluent,
(2) the compound is racemic ketorolac tromethamine dissolved at about 2.5-22.5% w/v,
(3) pharmaceutically acceptable salt of lidocaine is lidocaine hydrochloride dissolved at about 5-6% w/v, and
(4) the pH of the composition is adjusted to 7.2 and a chelator is present.
19 . The composition of claim 18 , wherein the compound is present at a level of about 15% w/v, potassium phosphate is a pH buffer, and the chelator is sodium EDTA.
20 . A method for treating pain or inflammation in a subject in need of such treatment, which comprises intranasally administering to the subject the composition of claim 1 .
21 . The method of claim 20 , wherein the method is for treating pain.
22 . The method of claim 21 , wherein the pain is the a result of a trauma inflicted on the subject.
23 . The method of claim 21 , wherein the pain is a result of a medical operation performed on the subject.
24 . The method of claim 21 , wherein the pain is pathological.
25 . The method of claim 21 , wherein the pain is neuropathic.
26 . The method of claim 21 , wherein the pain is migraine or other headache pain.
27 .- 29 . (canceled)
30 . A composition, wherein
(1) water is a sole diluent,
(2) a racemic ketorolac tromethamine dissolved at about 15% w/v,
(3) a lidocaine hydrochloride dissolved at about 5-6% w/v,
(4) a pH of the composition buffered to 7.2 using potassium phosphate and
(5) sodium EDTA.