39 results about "Olopatadine Hydrochloride" patented technology

The invention discloses a novel olopatadine hydrochloride eye drop and a preparation method thereof. The preparation method of the eye drop disclosed by the invention comprises the steps of: dissolving olopatadine hydrochloride and relevant accessories in water; adding a swelled sodium hyaluronate aqueous solution to the liquid medicine and then uniformly stirring; adding a sufficient amount of water; and finally, filtering and dispensing so as to obtain the eye drop. According to the novel olopatadine hydrochloride eye drop and the preparation method thereof, the defects of the current olopatadine hydrochloride eye drop are overcome; the residence time of the medicine on ocular surface is prolonged by the physical thickening and moisturizing lubrication effects of sodium hyaluronate; and furthermore, the medicine seldom flows into mouth and nasal cavity so as to reduce medicine loss and avoid bitterness from the olopatadine hydrochloride eye drop, and therefore, compliance of patients is increased and clinical curative effect is ensured.

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 invention discloses a preparation method of olopatadine hydrochloride. The preparation method comprises the following steps of preparing olopatadine hydrochloride crude products, preparing olopatadine freebase and preparing olopatadine hydrochloride. According to the preparation method of olopatadine hydrochloride, the key steps are upgraded, and the preparation method has the following advantages that 1, reaction steps are reduced, the loss is reduced, and the production efficiency is improved; 2, generation of hydrogen is reduced, and potential safety hazards are reduced; 3, the processing difficulty is reduced while ensuring the quality and yield unchanged; 4, a reaction temperature is optimized, a low-temperature harsh reaction is eliminated, and the dependence on equipment is reduced; 5, an original separate heterogeneous removal step is eliminated; and 6, the yield is high and the quality is good.

The invention discloses an externally applied composition and a preparation thereof, in particular an olopatadine hydrochloride containing externally applied composition and cream thereof. The composition contains olopatadine hydrochloride. The olopatadine hydrochloride containing externally applied composition directly acts on an affected part, the local medicament concentration of skin at an itching part is increased, and the effects of resisting histamine and stabilizing mast cells are achieved; adverse reaction of oral administration is avoided; the administration dosage can be selected according to the area of a diseased part, and the olopatadine hydrochloride containing externally applied composition is convenient to use and carry and high in stability; efficacy tests show that the composition has remarkable treatment effects on pruritic dermatosis; a process for the cream is simple, easy and low in cost.

The invention discloses a novel method for preparing olopatadine hydrochloride. The method comprises the steps as follows: (1) high-activity zinc and 3-bromo-N,N-dimethylpropylamine form an organic zinc reagent (I); (2) the organic zinc reagent is eliminated after electrophilic substitution with isoxepac (II) to form olopatadine (III); (3) the olopatadine with higher purity is obtained through recrystalization of the olopatadine, wherein structural formulas of the organic zinc reagent (I), the isoxepac (II) and the olopatadine (III) are as follows.

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

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 invention belongs to the field of analytical chemistry, and particularly relates to a method for separating and determining isoxepac and related substances of isoxepac by an HPLC (High PerformanceLiquid Chromatography) method. A chromatographic column adopted by the method disclosed by the invention adopts octylsilane-bonded silica gel as filler, a mobile phase A and a mobile phase B are adopted to carry out gradient elution, and detection is carried out in a detector; the related substances include one or more of A-G; the mobile phase A is potassium hexafluorophosphate solution, and themobile phase B is organic solvent. The method can effectively separate the seven impurities and other individual impurity in isoxepac and quantitatively determine the existence levels. The method hasthe advantages of high separation degree, high specificity, high sensitivity and accuracy, and is of a great significance in the control of the quality of isoxepac and olopatadine hydrochloride.

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 invention belongs to the technical field of medicine, and provides an olopatadine hydrochloride nasal spray and a preparation method thereof. The nasal spray is composed of olopatadine hydrochloride, water-soluble chitosan, chitosan quaternary ammonium salt, hydroxyl Propyl-β-cyclodextrin, osmotic pressure regulator, buffer, pH regulator and purified water. The olopatadine hydrochloride nasal spray provided by the present invention prolongs the residence time of olopatadine hydrochloride in the nasal cavity, improves the bioavailability of olopatadine hydrochloride, in addition, improves the stability of the product and reduces the The incidence of adverse reactions such as bitter taste, nosebleeds, and sore throat has low irritation to the nasal mucosa, and the side effects are small, which improves the safety of nasal medication.

The invention discloses olopatadine hydrochloride dispersible tablets, a preparation method thereof and a quality control method thereof. The olopatadine hydrochloride dispersible tablets contain olopatadine hydrochloride serving as a main medicament and a disintegrating agent, a filler, a binding agent and a lubricating agent which serve as auxiliary materials. A wet-method is adopted for granulation and tabletting, and an internal disintegrating agent addition method is adopted. The olopatadine hydrochloride dispersible tablets have the advantages of excellent dispersion state, short disintegrating time, quick medicament digestion, convenient administration, low production cost, no special equipment, convenient and stable carrying and transport and the like.

The invention relates to the field of pharmaceutical preparations, and particularly provides a novel olopatadine hydrochloride eye drop. The olopatadine hydrochloride eye drop comprises olopatadine hydrochloride, a buffer agent, an osmotic pressure regulator, a preservative, a pH regulator and a solvent.

The invention discloses traditional Chinese and western medicine compound eye drops for treating bacterial coronitis and a preparation method thereof, belonging to the technical field of medicines. The eye drops comprise the following raw materials: japanese calystegia, mud snail, marsh horsetail herb, betel leaf, angelica sinensis, zornia gibbosa, semen thlaspi, leaf of Chinese loropetalum, incised spleenwort, three-coloured amaranth seed, smallfruit fig resin, cannalike dona rhizome, common vetch, olopatadine hydrochloride, carbachol and norfloxacin. The eye drops disclosed by the invention adopt a therapeutic method of combining traditional Chinese medicine and western medicine, have excellent treatment effects compared with those of generally pure traditional Chinese and western medicine, take the effects of clearing away heat and toxic materials, diminishing inflammation and sterilizing, improving eyesight and relieving opacity, relieving swelling and pain and tonifying liver and nourishing kidney as treatment principles, can improve the effects of the traditional Chinese medicinal components and western medicine at the highest efficiency and improve medicinal effects, are externally and directly dripped into eyes so as to kill bacteria and realize high antibacterial property, can directly reach lesions, are convenient to use and good in absorption effect, do not have any bad and toxic or side effect, and have good effects of treating decreased eyesight, chemosis and the like caused by bacterial coronitis.

The invention discloses an externally applied composition and a preparation thereof, in particular an olopatadine hydrochloride containing externally applied composition and cream thereof. The composition contains olopatadine hydrochloride. The olopatadine hydrochloride containing externally applied composition directly acts on an affected part, the local medicament concentration of skin at an itching part is increased, and the effects of resisting histamine and stabilizing mast cells are achieved; adverse reaction of oral administration is avoided; the administration dosage can be selected according to the area of a diseased part, and the olopatadine hydrochloride containing externally applied composition is convenient to use and carry and high in stability; efficacy tests show that the composition has remarkable treatment effects on pruritic dermatosis; a process for the cream is simple, easy and low in cost.

The invention discloses a multistage filtering device for preparation of olopatadine hydrochloride eye drops, and relates to the technical field of eye drop preparation equipment. The multistage filtering device for preparation of olopatadine hydrochloride eye drops comprises a cylinder body and a filter element, the top of the cylinder body is movably connected with a cylinder cover, the bottom of the cylinder cover is fixedly connected with positioning pins, positioning grooves are formed in the top of the cylinder body, the positioning pins are inserted into the positioning grooves, sealing grooves are formed in the top of the cylinder body and the bottom of the cylinder cover, and the inner walls of the sealing grooves are movably connected with the surfaces of sealing strips. By arranging movable plates, round rods, fixed blocks and cams, the problems that in the prior art, when a common multistage filtering device for preparing olopatadine hydrochloride eye drops is used and a polyethersulfone membrane filter element is replaced, due to the fact that the number of bolts for fixing the cylinder cover is large, the cylinder cover is inconvenient to disassemble and assemble, and accordingly the filter element is inconvenient to replace are solved.