Patent application EP19382298A (EP), filed 2019-04-16
Publication number: EP3725298A1
Title: STABLE AND PRESERVED PHARMACEUTICAL COMPOSITIONS OF BILASTINE
Abstract: [0001]    The invention relates to an aqueous pharmaceutical composition comprising:
a) bilastine, or a pharmaceutically acceptable salt or solvate thereof,
b) benzalkonium chloride, in combination with at least one further preservative selected from the group comprising phenylethyl alcohol, benzyl alcohol, sodium benzoate, chlorbutanol, phenoxyethanol, cetrimide and 2-(ethylmercuriomercapto)benzoic acid sodium salt,
c) a suspending agent, and
d) 2-hydroxypropyl-β-cyclodextrin;
wherein the pH of the aqueous pharmaceutical composition is between 3.5 and 5.5.
[0002]    The invention also relates to said compositions for use in the treatment and/or prevention of a disorder or disease susceptible to amelioration by antagonism of H<1> histamine receptor and/or of a corticosteroid-responsive disease through nasal administration.
[0003]    The invention also relates to a process for preparing the aqueous pharmaceutical composition above mentioned.
IPC codes: A61K  31/   454            A I
A61K  31/    58            A I
A61K  47/    10            A I
A61K  47/    12            A I
A61K  47/    18            A I
A61K  47/    24            A I
A61K  47/    38            A I
A61K  47/    40            A I
A61K  47/    69            A I
A61K   9/    00            A I
A61K   9/    08            A I
Claims: number: 1
text: An aqueous pharmaceutical composition comprising:
number: 2
text: The aqueous pharmaceutical composition according to claim 1, further comprising e) mometasone or a pharmaceutically acceptable derivative thereof selected from an ester, ether and ketonide derivative, and wherein the content of 2-hydroxypropyl-β-cyclodextrin is less than 8.5 wt%.
number: 3
text: The aqueous pharmaceutical composition according to any one of claims 1 or 2, wherein the content of bilastine or a pharmaceutically acceptable salt or solvate thereof is comprised between 0.2 wt% and 0.8 wt%.
number: 4
text: The aqueous pharmaceutical composition according to any one of claims 1 to 3, wherein the total content of preservative is comprised between 0.010 and 2 wt%, preferably between 0.010 and 0.6 wt%.
number: 5
text: The aqueous pharmaceutical composition according to any one of claims 1 to 4, wherein the content of 2-hydroxypropyl-β-cyclodextrin is comprised between 1 and 5 wt%.
number: 6
text: The aqueous pharmaceutical composition according to any one of claims 1 to 5, wherein the suspending agent is selected from cellulose and/or cellulose derivatives selected from cellulose ether derivatives wherein the hydroxyl groups of cellulose have been partially or fully substituted to provide cellulose ethers.
number: 7
text: A process for preparing an aqueous pharmaceutical composition according to any one of claims 1 to 6 comprising:
number: 8
text: The process according to claim 7, further comprising the step of:
b1) preparing a dispersion of mometasone, or a pharmaceutically acceptable derivative thereof selected from an ester, ether and ketonide derivative with a surfactant in purified water,
wherein the dispersion of step b1) is added to the mixture of step c), before the homogenizing step d), and wherein the content of 2-hydroxypropyl-3-cyclodextrin in step a) is less than 8.5 wt%.
number: 9
text: The process according to any one of claims 7 or 8, wherein the aqueous solution of 2-hydroxypropyl-β-cyclodextrin is an aqueous solution wherein the content of 2-hydroxypropyl-β-cyclodextrin is comprised between 1 and 5 wt%.
number: 10
text: An aqueous pharmaceutical composition according to any one of claims 1 to 6, for use as a medicament.
number: 11
text: An aqueous pharmaceutical composition according to any one of claims 1 to 6, for use in the treatment and/or prevention of a disorder or disease susceptible to amelioration by antagonism of H<1> histamine receptor and/or of a corticosteroid-responsive disease.
number: 12
text: The aqueous pharmaceutical composition for use according to claim 11, wherein the disorder or disease susceptible to amelioration by antagonism of H1 histamine receptor is an allergic disorder or disease selected from rhinitis, conjunctivitis and rhinoconjunctivitis.
number: 13
text: The aqueous pharmaceutical composition for use according to claim 11, wherein the corticosteroid-responsive disease is selected from asthma, allergic and non-allergic rhinitis, non-malignant proliferative and inflammatory diseases.
number: 14
text: The aqueous pharmaceutical composition for use according to any one of claims 10 to 13 wherein the aqueous pharmaceutical composition is intranasally administered.
number: 15
text: A nasal spray device comprising the aqueous pharmaceutical composition according to any one of claims 1 to 6.
Office action: search_report, dated 2020-10-21
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Final disposition: pending (2020-10-21)