30 results about "Olopatadin" patented technology

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 provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.

The present invention relates to a novel process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

The invention provides an improved preparation method of 4-(2-carboxybenzyloxy) phenylacetic acid. 6, 11-dihydro-11-oxo-dibenz (b, e) oxepin-2-acetic acid which is a raw material for producing the anti-allergic drug of olopatatadine can be obtained through a cyclization reaction of the 4-(2-carboxybenzyloxy) phenylacetic acid.

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 pediatric human subject) 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.

The invention discloses olopatadine α-methyl compound, its preparation method and application, and belongs to the technical field of medicine. The present invention discovers for the first time an impurity compound in the olopatadine medicine—olopatadine alpha methyl compound, and its standard product can be used for qualitative analysis and quantitative detection of the impurity in the olopatadine hydrochloride medicine. At the same time, the present invention also provides a cream based on the compound. The compound can be used as an active component in cream products that mainly treats the main symptoms, and is mainly used for skin diseases such as mosquito bites.

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 invention provides a post-treatment purification method of olopatadine hydrochloride. The method comprises the steps of 1) washing a reaction liquid crude product with a sodium chloride solution to remove bromide ions so as to obtain an olopatadine hydrochloride salt-containing crude product; (2) dissolving the olopatadine hydrochloride salt-containing crude product prepared in the step (1) into a mixed solvent of dichloromethane, glacial acetic acid, acetic acid and alcohols, and carrying out desalting treatment so as to obtain an olopatadine hydrochloride crude product; and (3) recrystallizing the olopatadine hydrochloride crude product obtained in the step (2), wherein a solvent adopted for recrystallization is a mixed solvent of dimethyl sulfoxide and isopropyl ether. The target product olopatadine hydrochloride obtained through the method is extremely low in inorganic salt content, meanwhile, the preparation yield and the product purity of olopatadine hydrochloride are greatlyimproved, the production cost is reduced, and the method is suitable for industrial production.

The present invention provides an olopatadine composition, which comprises olopatadine, pyruvate and / or pyruvate, osmotic pressure regulator, metal ion complexing agent, preservative, pH regulator and purified water. The composition of the invention can improve the stability of the olopatadine, reduce the irritation to the nasal mucosa, accelerate the repair of the nasal mucosa, relieve nasal symptoms and improve the drug safety of the olopatadine.

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.

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.

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

The present invention relates to an ophthalmic composition, which comprises ganciclovir and olopatadine; wherein, the mass ratio of ganciclovir to olopatadine is (2‑6):1. The present invention also relates to a preparation method of an ophthalmic composition, comprising: step S1, mixing ganciclovir, olopatadine, an osmotic pressure regulator, a pH regulator and water for injection at a temperature of 90-100°C , to obtain a mixed solution; step S2, at a temperature of 70-80° C., adding a solubilizer, a preservative and water for injection to the mixed solution to obtain the ophthalmic composition. In addition, the present invention also relates to the application of the ophthalmic composition in the preparation of medicines for treating keratitis. The eye drops containing the ophthalmic composition provided by the invention not only have good anti-inflammatory and anti-viral effects, but also can avoid adverse reaction symptoms such as eyelid edema, conjunctival hyperemia, pain and burning sensation in patients with long-term use.

The invention provides a post-treatment purification method of olopatadine hydrochloride. The method of the present invention comprises the following steps: step 1): washing the crude product of the reaction solution through sodium chloride solution to remove bromide ions, and obtaining the crude product of olopatadine hydrochloride containing salt; step 2): washing the crude product of olopatadine hydrochloride obtained in step 1) The salt-containing crude product is dissolved in a mixed solvent of dichloromethane, glacial acetic acid and alcohols for desalination treatment to obtain the crude product of olopatadine hydrochloride; step 3): the crude product of olopatadine hydrochloride obtained in step 2) The product is recrystallized, wherein the solvent used for recrystallization is a mixed solvent of dimethyl sulfoxide and isopropyl ether. The target product olopatadine hydrochloride obtained by the method of the present invention has extremely low inorganic salt content, and at the same time greatly improves the preparation yield and product purity of the olopatadine hydrochloride, reduces production costs, and is suitable for industrial production.

The invention relates to the field of drug synthesis, in particular to a preparation method of olopatadine hydrochloride, which comprises the following steps: adding [3-(dimethylamino) propyl] triphenylphosphonium bromide hydrobromide into tetrahydrofuran, sodium hydride and dimethyl sulfoxide, keeping the temperature, stirring, adding 11-oxo-6, 11-dihydrodibenzo [b, e] oxepin-2-acetic acid, stirring until a reaction system becomes black brown turbid liquid, and ending the reaction; quenching the reaction liquid by using a mixed solution of purified water and tetrahydrofuran, post-treating a water phase by using a mixed solvent of hydrochloric acid and n-butyl alcohol, carrying out vacuum concentration on a post-treated aqueous solution, crystallizing a concentrated solution by using n-butyl alcohol, filtering and drying to obtain a crude olopatadine hydrochloride product, separating out a solid in water and a sodium hydroxide solution, and filtering and drying to obtain olopatadine; and adding the olopatadine into hydrochloric acid while stirring by acetone to form white turbid liquid, continuously stirring, filtering and drying to obtain the olopatadine hydrochloride. The prepared olopatadine hydrochloride is high in yield, and short in reaction path.