PHARMACEUTICAL COMPOSITIONS FOR INTRAOCULAR ADMINISTRATION AND METHODS FOR FABRICATING THEREOF
Pharmaceutical compositions for intraocular injection are described, the compositions consisting essentially of a therapeutically effective quantity of an anti-bacterial agent (such as moxifloxacin), a therapeutically effective quantity of an anti-inflammatory agent (such as triamcinolone), at least one pharmaceutically acceptable excipient and a pharmaceutically acceptable carrier. Methods for fabricating the compositions and using them for intraocular injections are also described.
1 . A pharmaceutical composition for intraocular injection, comprising:
(a) a therapeutic component consisting essentially of:
(a1) a therapeutically effective quantity of an anti-bacterial agent independently selected from the group consisting of quinolone, a fluorinated quinolone and pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof; and
(a2) a therapeutically effective quantity of an anti-inflammatory agent independently selected from the group consisting of corticosteroids and pharmaceutically acceptable salts, hydrates, solvates, ethers, esters, acetals and ketals thereof;
(b) optionally, at least one pharmaceutically acceptable excipient suitable for intraocular injection; and
(c) optionally, a pharmaceutically acceptable carrier therefor suitable for intraocular injection.
2 . The pharmaceutical composition of claim 1 , wherein the anti-bacterial agent is a fluorinated quinolone.
3 . The pharmaceutical composition of claim 2 , wherein the fluorinated quinolone is selected from the group consisting of moxifloxacin and gatifloxacin.
4 . The pharmaceutical composition of claim 2 , wherein the fluorinated quinolone is moxifloxacin.
5 . The pharmaceutical composition of claim 1 , wherein the anti-bacterial agent is a fluorinated quinolone having the chemical structure (A):
6 . The pharmaceutical composition of claim 1 , wherein the corticosteroid is selected from the group consisting of triamcinolone, triamcinolone acetonide, triamcinolone diacetate, triamcinolone benetonide, triamcinolone furetonide, triamcinolone hexacetonide, betamethasone acetate, dexamethasone, fluorometholone, fluocinolone acetonide and a combination thereof.
7 . The pharmaceutical composition of claim 1 , wherein the corticosteroid is triamcinolone.
8 . The pharmaceutical composition of claim 1 , wherein the corticosteroid has the chemical structure (B):
9 . The pharmaceutical composition of claim 1 , wherein:
(a) the anti-bacterial agent is moxifloxacin; and
(b) the corticosteroid is triamcinolone or a derivative thereof.
10 . The pharmaceutical composition of claim 1 , wherein the excipient is a solubilizing and suspending agent selected from the group consisting of non-ionic polyoxyethlene-polyoxypropylene block copolymers.
11 . The pharmaceutical composition of claim 10 , wherein the excipient is Poloxamer 407®.
12 . The pharmaceutical composition of claim 1 , comprising:
(a) moxifloxacin at a concentration of about 1.0 mg/mL;
(b) triamcinolone acetonide at a concentration of about 15.0 mg/mL; and
(c) Poloxamer 407® at a concentration of about 1.0 mass %.
13 . The pharmaceutical composition of claim 1 , further comprising a therapeutically effective quantity of an antibiotic selected from the group consisting of vancomycin, teicoplanin, telavancin, decaplanin, ramoplanin, gentamicin, tobramycin, amikacin, cefuroxime, polymyxin B sulfate, trimethoprim, and a combination thereof.
14 . The pharmaceutical composition of claim 13 , wherein the antibiotic is vancomycin.
15 . A method for preparing a pharmaceutical composition for intraocular injection comprising combining components (a), (b) and (c) of claim 1 , to obtain the pharmaceutical composition thereby.
16 . The method of claim 15 , wherein the anti-bacterial agent is a fluorinated quinolone.
17 . The method of claim 16 , wherein the fluorinated quinolone is moxifloxacin.
18 . The method of claim 15 , wherein the corticosteroid is triamcinolone.
19 . The method of claim 14 , wherein:
(a) the anti-bacterial agent is moxifloxacin; and
(b) the corticosteroid is triamcinolone or a derivative thereof.
20 . The method of claim 14 , wherein the excipient is a solubilizing and suspending agent selected from the group comprising non-ionic poly(oxyethlene-co-oxypropylene).
21 . The method of claim 20 , wherein the excipient is Poloxamer 407®.
22 . The method of claim 20 , further comprising a therapeutically effective quantity of vancomycin.
23 . The method of claim 15 , wherein the anti-bacterial agent, the anti-inflammatory agent, the excipient and the carrier are combined in a one-batch formulation method.
24 . A method for treating an ophthalmological disease, condition or pathology in a mammalian subject in need of such treatment comprising delivery to the subject the composition of claim 1 , wherein the method of delivery is selected from the group consisting of intravitreal injection, intraocular intracameral injection, intra-lesional injection, intra-articular injection, subconjunctival injection, sub-tenon injection, delivery via eye drops, delivery via spray and intra-canalicular delivery, to treat the ophthalmological disease, condition or pathology thereby.
25 . The method of claim 24 , wherein the intravitreal injection is selected from the group consisting of a transzonular injection and a non-transzonular injection.
26 . The method of claim 24 , wherein the mammalian subject is selected from the group consisting of a human, a cats, a dog, another pet, a wild animal and a farm animal.
27 . A method for treating an ophthalmological disease, condition or pathology in a mammalian subject in need of such treatment comprising intravitreally transzonularly injecting the subject with the composition of claim 9 , to treat the ophthalmological disease, condition or pathology thereby.
28 . A method for treating an ophthalmological disease, condition or pathology in a mammalian subject in need of such treatment comprising intraocularly injecting the subject with a composition comprising
(a) a therapeutically effective quantity of moxifloxacin;
(b) a therapeutically effective quantity of triamcinolone acetonide; and
(c) a quantity of Poloxamer 407®,
to treat the ophthalmological disease, condition or pathology thereby.
29 . A method for treating an ophthalmological disease, condition or pathology in a mammalian subject in need of such treatment comprising intravitreally transzonularly injecting the subject with the composition of claim 12 , to treat the ophthalmological disease, condition or pathology thereby.
30 . The method of claim 31 , wherein the injecting is intravitreal and transzonular.
31 . The method of claim 31 , wherein the injecting is intraoperative.
32 . A pharmaceutical kit, comprising a sealed container containing the pharmaceutical composition of claim 1 and an instruction for the use of the composition enclosed with the container.
33 . A method for treating an ophthalmological disease, condition or pathology in a mammalian subject in need of such treatment comprising:
(a) intravitreally transzonularly injecting the subject with an anti-bacterial agent of claim 1 ; and
(b) intravitreally transzonularly injecting the subject with an anti-inflammatory agent of claim 1 ,
to treat the ophthalmological disease, condition or pathology thereby.