US2018289688A1PendingUtilityA1
Pharmaceutical composition for topical application
Est. expiryNov 21, 2028(~2.3 yrs left)· nominal 20-yr term from priority
A61K 31/4545A61P 11/02A61K 9/0043A61K 31/4353A61K 31/435A61K 9/08
43
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Claims
Abstract
A pharmaceutical composition comprises a solution having a pH of from 5 to 7.5, including loratadine and/or desloratadine. The composition is suitable for treatment of e.g. allergic rhinitis and allergic conjunctivitis.
Claims
exact text as granted — not AI-modifiedWe claim:
1 . A pharmaceutical composition comprising an aqueous solution having a pH of from 5 to 7.5 comprising:
Component
Amount (wt %)
a) At least one antihistamine selected
0.02-0.1
from Loratadine and Desloratadine and
their pharmaceutically acceptable salts
b) At least one polyethylene glycol with
5.0-15.0
a molecular weight of from 100 to 600
g/mole
c) Propylene glycol
5.0-15.0
d) At least one non-ionic ethylene
1.0-10.0
oxide/propylene oxide (EO/PO) block
copolymer with weight average
molecular weight (Mw) from 10,000 to
15,000
e) polyoxyethylene (20) sorbitan
0.5-5.0
monolaurate and/or polyoxyethylene
(20) sorbitan monooleate
f) Stabilizer
0.05-0.5
Other optional additives
<20
Water
Balance to 100.0%
2 . The pharmaceutical composition as claimed in claim 1 , which comprises an aqueous solution having a pH from 5 to 7.5 comprising:
Component
Amount (wt %)
Loratadine or a pharmaceutically
0.02-0.1
acceptable salt thereof
At least one polyethylene glycol with a
5.0-15.0
molecular weight of from 100 to 600
g/mole
Propylene glycol (co-solvent)
5.0-15.0
At least one non-ionic EO/PO block
1.0-10.0
copolymer with weight average
molecular weight (Mw) from 10,000 to
15,000
polyoxyethylene (20) sorbitan
0.5-5.0
monolaurate and/or polyoxyethylene
(20) sorbitan monooleate
Stabilizer
0.05-0.5
Other optional additives
<20
Water
Balance to 100.0%
3 . The pharmaceutical composition as claimed in claim 2 , which comprises an aqueous solution having a pH from 5 to 7 consisting of:
Component
Amount (wt %)
Loratadine or a pharmaceutically
0.06
acceptable salt thereof
PEG 400
10.0
Propylene glycol
10.0
At least one non-ionic EO/PO block
5.0
copolymer with weight average
molecular weight (Mw) of about 12,500
Polysorbate 80
1.8
Na 2 EDTA
0.1
Water
Balance to 100.0%
4 . The pharmaceutical composition as claimed in claim 1 , which comprises an aqueous solution having a pH from 5 to 7.5 comprising:
Component
Amount (wt %)
Desloratadine or a pharmaceutically
0.02-0.1
acceptable salt thereof
At least one polyethylene glycol with a
5.0-15.0
molecular weight of from 100 to 600
g/mole
Propylene glycol
5.0-15.0
At least one non-ionic EO/PO block
1.0-10.0
copolymer with weight average
molecular weight (Mw) from 10,000 to
15,000
polyoxyethylene (20) sorbitan
0.5-5.0
monolaurate and/or polyoxyethylene
(20) sorbitan monooleate
Stabilizer
0.05-0.5
Other optional additives
<20
Water
Balance to 100.0%
5 . The pharmaceutical composition as claimed in claim 4 , which comprises an aqueous solution having a pH from 5 to 7 consisting of:
Component
Amount (wt %)
Desloratadine or a pharmaceutically
0.6
acceptable salt thereof
PEG 400
10.0
Propylene glycol
10.0
At least one non-ionic EO/PO block
5.0
copolymer with weight average
molecular weight (Mw) of about 12,500
Polysorbate 80
1.8
Na 2 EDTA
0.1
Water
Balance to 100.0%
6 . A method for reducing histamine production wherein said method comprises nasally administering, to a subject in need of reduced histamine production, a pharmaceutical composition of claim 1 .
7 . The method, according to claim 6 , wherein said composition is an aqueous solution that consists of:
a) an antihistamine in an amount between 0.02% and 0.1% of the total weight of the composition (wt %), the antihistamine being selected from the group consisting of loratadine, desloratadine, and pharmaceutically acceptable salts thereof; b) polyethylene glycol with a molecular weight between 100 to 600 g/mole in an amount from 5.0 to 15.0 wt %; c) a propylene glycol, in an amount from 5.0 to 15.0 wt % ; d) a non-ionic block copolymer, wherein the block copolymer is an ethylene oxide and propylene oxide block copolymer, and wherein the block copolymer is present in an amount from 1.0 to 10.0 wt %; and e) a polyoxyethylene sorbitan monolaurate and/or monooleate, wherein the polyoxyethylene sorbitan monolaurate and/or monooleate is present in an amount from 0.5 to
5 . 0 wt % and wherein the composition is in an aqueous solution having a pH of from 5 to 7.5.
8 . A method for relieving allergy symptoms wherein said method comprises nasally administering, to a subject in need of such relief, a pharmaceutical composition of claim 1 .
9 . The method, according to claim 8 , wherein said composition is an aqueous solution that consists of:
a) an antihistamine in an amount between 0.02% and 0.1% of the total weight of the composition (wt %), the antihistamine being selected from the group consisting of loratadine, desloratadine, and pharmaceutically acceptable salts thereof; b) polyethylene glycol with a molecular weight between 100 to 600 g/mole in an amount from 5.0 to 15.0 wt %; c) a propylene glycol, in an amount from 5.0 to 15.0 wt % ; d) a non-ionic block copolymer, wherein the block copolymer is an ethylene oxide and propylene oxide block copolymer, and wherein the block copolymer is present in an amount from 1.0 to 10.0 wt %; and e) a polyoxyethylene sorbitan monolaurate and/or monooleate, wherein the polyoxyethylene sorbitan monolaurate and/or monooleate is present in an amount from 0.5 to 5.0 wt % and wherein the composition is in an aqueous solution having a pH of from 5 to 7.5.Join the waitlist — get patent alerts
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