32 results about "Olopatadine" patented technology

Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the nose are disclosed. The aqueous formulations contain approximately 0.6% (w / v) of olopatadine.

The present invention is an ophthalmic composition containing a relatively high concentration of olopatadine. The composition is typically an ophthalmic aqueous solution containing relatively high concentrations of olopatadine solubilized within the solution. The composition is preferably capable of providing enhanced relief from symptoms of ocular allergic conjunctivitis, particularly late phase symptoms of ocular allergic conjunctivitis.

Olopatadine can be obtained by means of a process comprising hydrolysis of a compound of general formula (II), wherein Y is OR1, wherein R1 is C1-C7 alkyl, C3-C7 cycloalkyl, aryl, arylalkyl, or heterocycle; or NR2R3, wherein R2 and R3, independently from each other, are C1-C7 alkyl, aryl, arylalkyl, or R2 and R3 together with the nitrogen atom to which they are bound form a heterocycle of 3 to 7 members, obtained by means of a process comprising reacting the corresponding ester or amide of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid with a suitable Wittig reagent, in the presence of a base in a reaction medium comprising an organic solvent.

The present invention relates to a stable fixed dose aqueous pharmaceutical composition (e.g., contained in a container) for nasal administration to a human, comprising mometasone or its salt, olopatadine or its salt. The composition may further include a hydrocolloid. The invention also relates to a process for preparing the pharmaceutical composition, and the use of the pharmaceutical composition in the treatment of rhinitis in a subject.

The present invention relates to a stable fixed dose aqueous pharmaceutical composition (e.g., contained in a container) for nasal administration to a human, comprising mometasone or its salt, olopatadine or its salt. The composition may further include a hydrocolloid. The invention also relates to a process for preparing the pharmaceutical composition, and the use of the pharmaceutical composition in the treatment of rhinitis in a subject.

The present invention relates to a method of treating allergic rhinitis in a subject (e.g., a human) in need thereof comprising nasally administering to the subject an effective amount of a fixed-dose pharmaceutical composition comprising mometasone or its salt and olopatadine or its salt.

Olopatadine can be obtained by means of a process comprising hydrolysis of a compound of general formula (II), wherein Y is OR1, wherein R1 is C1-C7 alkyl, C3-C7 cycloalkyl, aryl, arylalkyl, or heterocycle; or NR2R3, wherein R2 and R3, independently from each other, are C1-C7 alkyl, aryl, arylalkyl, or R2 and R3 together with the nitrogen atom to which they are bound form a heterocycle of 3 to 7 members, obtained by means of a process comprising reacting the corresponding ester or amide of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid with a suitable Wittig reagent, in the presence of a base in a reaction medium comprising an organic solvent.

The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises olopatadine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising olopatadine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby casing transfer of a therapeutically effective amount of olopatadine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops.

An aqueous ophthalmic solution containing a relatively high concentration of olopatadine in solubilized form is provided. The solution comprises a combination of at least two non-ionic surfactants and is essentially devoid of cyclodextrins. The solution is useful for providing enhanced relief from symptoms of ocular allergic disorders (e.g. conjunctivitis).

The invention discloses a pharmaceutical composition of olopatadine or salts of olopatadine for treating allergic conjunctivitis, and a preparation method thereof. The composition mainly comprises the olopatadine or the salts of the olopatadine, and polycarbophil or polycarbophil salt or carbomer. The preparation method comprises firstly fully swelling the polycarbophil or the polycarbophil salt or the carbomer with a proper amount of pure water, and secondly adding the olopatadine or the salts of the olopatadine and other accessories.

The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer.

The invention discloses a preparation method of o-hydroxyl Olopatadine. The preparation method comprises the following steps: (1) performing a hydroxyl protection reaction on o-hydroxyl Isoxepac to obtain a compound shown in the general formula (I); (2) performing a Wittig reaction between the compound shown in the general formula (I) and [3-(dimethylamino)propyl]triphenylphosphine bromide hydrobromide to obtain a compound shown in the general formula (II); and (3) performing a protecting group removal reaction on the compound shown in the general formula (II) to obtain the o-hydroxyl Olopatadine, wherein the definition of R1 is specified in the specification. Moreover, the invention also discloses an intermediate compound for preparing o-hydroxyl Olopatadine.

The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer.

Stable formulations of Olopatadine, methods of making such formulations and methods of treatment using such formulations are provided.

The present invention refers to a new “one-pot” process for the preparation of olopatadine via intermediates of formula (III).

The present invention relates to a stable fixed dose aqueous pharmaceutical composition (e.g., contained in a container) for nasal administration to a human, comprising mometasone or its salt, olopatadine or its salt. The composition may further include a hydrocolloid. The invention also relates to a process for preparing the pharmaceutical composition, and the use of the pharmaceutical composition in the treatment of rhinitis in a subject.