53 results about "Bilastine" patented technology

The invention belongs to the technical field of medicines, and relates to a bilastine pharmaceutical composition with good dissolution effect. The pharmaceutical composition comprises bilastine, a water-soluble excipient, a disintegrating agent, a lubricating agent and the like, wherein the bilastine is micronized, the grain size of 90% of the bilastine is controlled to 5 to 50 microns and is specifically preferable to 10 to 20 microns. A medicine prepared by the preparation method shows good dissolution effect, and therefore, the bioavailability of the medicine can be effectively improved.

The invention relates to a method for preparing bilastine. The method comprises the following steps: adding a compound I oxazolol to water, adding a phase transfer catalyst, p-toluenesulfonyl chlorideand sodium hydroxide, stirring and reacting all above substances, and performing filtration to obtain oxazolol sulfonate; adding the sulfonate to water, adding 2-(4-piperidinyl)-1-H-benzimidazole andthe phase transfer catalyst, adding sodium carbonate or potassium carbonate, heating the obtained suspension, performing a reaction for 3-5 h, filtering the obtained intermediate II, adding the intermediate II to a strong polar aprotic solvent, adding sodium hydroxide and the phase transfer catalyst, adding ethylene glycol monoethyl ether tosylate, stirring and reacting the obtained mixture at -20-60 DEG C, filtering the obtained reaction product, and washing the filtered reaction product with water to obtain an intermediate III; and adding the intermediate III to an aqueous solution of an organic acid, performing refluxing for 3-5 h, adding water, adding a strong alkali until saturation, refluxing the obtained solution for 3-5 h to generate a bilastine salt insoluble in the saturated alkaline solution, and performing extraction to obtain the bilastine. The method has the advantages of mild reaction conditions, simplicity in operation, greenness, environmental protection, high yield,and convenience in industrial production.

The invention discloses a preparation method of 2-(4-haloethyl) phenyl-2-methyl propionic ester and a synthesis method of bilastine, which comprises the following steps of: carrying out acylation reaction on 2, 2-dimethyl phenylacetate and halogen acetyl halides under the action of catalyst, to generate 2-(4-halogen acetyl) phenyl-2-methyl propionic ester; carrying out kishner-wolff-huang reduction reaction on the 2-(4-halogen acetyl) phenyl-2-methyl propionic ester, to reduce the carbonyl so as to generate the 2-(4-haloethyl) phenyl-2-methyl propionic ester; having condensation reaction with 1-ethoxy ethyl-2-pyridine-4-group benzimidazole by taking the 2-(4-haloethyl) phenyl-2-methyl propionic ester as a midbody to obtain esterified bilastine; and hydrolyzing, to generate the bilastine. The novel synthesis method of the bilastine provided by the invention can easily obtain raw materials, and is simple to operate, lower in cost, environment-friendly, and completely suitable for the industrial production.

The invention relates to a method for preparing a novel crystal form of bilastine. The method comprises the following steps: dissolving bilastine in a mixed solvent of an organic solvent and water, heating until all bilastine is dissolved, and cooling and crystallizing to obtain the novel crystal form of bilastine.

The invention provides an antiallergic nasal medicine composition with high moisture retention and preparation methods and applications thereof. The composition has high moisture retention and no irritation to a nasal mucosa. The composition comprises levocetirizine, azatadine, loratadine, ebastine, setastine, bilastine, clemastine, mizolastine, epinastine and moxifloxacin which are antiallergic medicine as main medicine, wherein the main medicine can be salts or free alkalis, sea salt as an osmotic pressure regulator, and a mixture of sodium hyaluronate and glycerin of different molecular weights as a moisturizing excipient. Plant essential oil can be contained in the composition. Preparations can be an aqueous solution, a cyclodextrin-coated suspension or a nanosuspension. Dosage forms include spray, aerosol and nose drops. Main indications include nasal dryness, runny nose, nasal itching, nasal obstruction and the like due to allergic rhinitis.

The invention belongs to the technical field of medicinal preparations, and particularly relates to a bilastine tablet capable of realizing direct powder compression adopting silicified microcrystalline cellulose, and a preparation method thereof. The tablet is prepared from the following components by weight percent: 1 to 10 percent of bilastine, 10 to 90 percent of silicified microcrystalline cellulose, 3 to 20 percent of a disintegrating agent, 0.5 to 5 percent of a lubricating agent, and 0 to 5 percent of a flow aid. According to the bilastine tablet and the preparation method thereof provided by the invention, the defects of poor fluidity and compressibility of the bilastine are overcome, a recipe and a technology of direct bilastine compression are realized, the preparation technology is simpler, the stability of the product quality is ensured, and the method is suitable for mass production.

The invention provides a preparation method of bilastine. Specifically the method comprises the following steps: oxidizing 4-hydroxyethyl phenyl methyl tert-butyrate to obtain 4-acetaldehyde phenyl methyl tert-butyrate, and carrying out a reductive amination reaction on the 4-acetaldehyde phenyl methyl tert-butyrate and a compound represented by a formula IV to obtain 4-[2-[1-(2-ethoxyethyl)benzimidazolyl]piperidyl]ethyl-phenyl methyl tert-butyrate (represented by a formula V); and hydrolyzing and acidifying the compound represented by the formula V to obtain bilastine. The method is high in yield, simple to operate and suitable for industrial production.

The invention discloses a preparation method of a bilastine oxide impurity. The preparation method comprises that bilastine undergoes a reaction in an alcohol solvent in the presence of an oxidizing agent to produce a bilastine oxide impurity in a high yield. The bilastine oxide impurity can be used for quality control of a bilastine bulk drug or its preparation and can be used as an impurity contrast.