30 results about "Epinastine" patented technology

A method for treating allergic rhinitis, comprising topically administering to the nasal mucus membrane of a host in need of such treatment a solution comprising: epinastine, optionally in the form of its racemate, its enantiomers, or its pharmacologically acceptable acid addition salts, in a pharmacologically acceptable carrier.

The invention discloses a synthetic method of epinastine hydrochloride. The synthetic method comprises the following steps: enabling a substance A to react with a substance B to obtain a substance C; enabling the substance C to be subjected to ring closing reaction with polyphosphoric acid to obtain a substance D; enabling the substance D to react with a de-protection reagent to obtain a substance E; enabling the substance E to react with cyanogen bromide to obtain epinastine and then salifying with hydrochloric acids to obtain the epinastine hydrochloride. The synthetic method disclosed by the invention is easily-available in raw materials, mild in reaction conditions, low in energy consumption, low in production cost, simple to operate, short in preparation period and suitable for large-scale industrial production; the prepared epinastine hydrochloride is high in purity and relatively high in yield in each step of reaction.

The invention discloses a preparation method of an epinastine related substance and relates to the technical field of medicines. The preparation method comprises steps as follows: epinastine is takenas a raw material, an oxidizing agent, a catalyst and a reaction system solvent are added, the mixture is stirred uniformly, an organic solvent is added after the reaction ends, extraction, washing, drying and suction filtration under reduced pressure are sequentially performed, and the organic solvent is recovered. An epinastine impurity A with the purity up to 97% is obtained through oxidation preparation, separation and purification steps, and the method is simple in preparation process, low in cost and high in yield.

The invention provides a freeze-dried oral preparation containing ebiprazole and a preparation method thereof, belonging to the field of pharmaceutical preparations. The freeze-dried oral preparation includes medicinal dose of ebiprazole and other pharmaceutical auxiliary materials. The preparation method prepares raw materials and auxiliary materials into a freeze-dried oral preparation by adopting a freeze-drying method. The present invention fills the blank of ebiprazole in the technical field of freeze-dried preparations by preparing ebiprazole bulk drug into freeze-dried oral preparations, not only provides clinical patients with a variety of drug dosage forms, but also contains ebiprazole The lyophilized oral formulation of azole can disintegrate quickly, so that the ebiprazole can be quickly dissolved and absorbed by the patient, and the bioavailability is improved; at the same time, the lyophilized oral formulation can be disintegrated in the patient's mouth without water, so that Part of the drug can be absorbed through mucosal transport, thus realizing pregastric absorption, avoiding the stimulation and damage of the drug to the stomach, and improving the compliance of clinical patients.

The present invention provides a transdermal absorption preparation for preventing or treating allergic eye diseases, the preparation comprising epinatidine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye diseases, the method comprising applying a transdermal absorption preparation comprising epinatine or a salt thereof to the skin surface including the eyelid skin surface, whereby a therapeutically effective amount of epinatine Nadine or its salts are transferred from the formulation to the anterior part of the eye through the eyelid skin rather than the systemic blood stream. Compared with conventional preparations such as eye drops, the preparation of the present invention can exhibit long-acting pharmacological effects through a single application.

The invention discloses a method for synthesizing epinastine. The method comprises the following steps: (1) reacting 6-halomethylmorphanthridine with hexamine in an organic solvent, thereby obtaining a 6-halomethylmorphanthridine quaternary ammonium salt; (2) dissolving the 6-halomethylmorphanthridine quaternary ammonium salt in the organic solvent to carry out an acid hydrolysis reaction, thereby obtaining 6-halomethylmorphanthridine hydrochloride; (3) reducing the product 6-halomethylmorphanthridine hydrochloride obtained in the step (2) by using a reducing agent, thereby obtaining 6-aminomethyl-6,11-dihydro-5H-dibenzo[b,e]aza-cycloheptatrien; and (4) adding cyanogen bromide to carry out a ring-closure reaction, thereby obtaining the epinastine. According to the synthetic method disclosed by the invention, use of high-price and flammable lithium aluminum hydride or aluminum hydride is avoided, use of virulent sodium cyanide is avoided, and the security risk and production cost are effectively reduced. The method disclosed by the invention is simple in synthetic process, the reaction conditions are mild, the product is high in yield and high in purity, and industrial production is facilitated.

The invention discloses a new chemical synthesizing method of yipisidin, which comprises the following steps: ammonifying 6-chloromethyl-11-dihyrogen-dibenz [b,e] aza to generate 6-aminomethyl-11-dihydrogen-dibenz [b,e] aza; reducing the 6-aminomethyl-11-dihydrogen-dibenz [b,e] aza into 6-aminomethyl-6,11-dihydrogen-5H-dibenz [b,e] aza; generating the product through cyanogen bromide to loop. Theinvention simplifies the making method with little by-product, which improves the receiving rate by 69% with high purity (HPLC. 99. 0%) for industrial manufacturing.

The invention discloses a synthesis method of epinastine. The synthesis method is implemented by taking 2-aminobenzophenone as a raw material and comprises the following steps of: reacting the 2-aminobenzophenone with a silane agent to obtain 2-benzylaniline; then, carrying out acylation reaction on the 2-benzylaniline and 2-chloroacetyl chloride to obtain N-(2-benzyl phenyl)-2-chloroacetamide; carrying out acidamide dehydration and cyclization on the N-(2-benzyl phenyl)-2-chloroacetamide under the action of a dehydrating agent to obtain 6-(chloromethyl)-11H-dibenzo[b,e] azepine; carrying out azidation reaction on the 6-(chloromethyl)-11H-dibenzo[b,e] azepine to obtain 6-(azido-methytbiphenyl)-11H-dibenzo[b,e] azepine; carrying out reduction on the 6-(azido-methytbiphenyl)-11H-dibenzo[b,e] azepine to obtain 6-(aminomethyl)-6,11-dihydro-1H-dibenzo[b,e] azepine; and finally, carrying out cyclization on the 6-(aminomethyl)-6,11-dihydro-1H-dibenzo[b,e] azepine and cyanogen bromide to obtain the epinastine. The synthesis method disclosed by the invention avoids the application of expensive and flammable lithium aluminium hydride and aluminium hydride as well as hypertoxic sodium cyanide, so that the operation is safer in industrial production, and the cost is reduced. The method is simple in process and high in yield, requires mild conditions, and is suitable for industrialized production.

The invention provides a freeze-dried oral preparation containing ebiprazole and a preparation method thereof, belonging to the field of pharmaceutical preparations. The freeze-dried oral preparation includes a medicinal amount of ebiprazole and pharmaceutical auxiliary materials. The preparation method prepares raw materials and auxiliary materials into a freeze-dried oral preparation by adopting a freeze-drying method. The present invention fills the blank of ebiprazole in the technical field of freeze-dried preparations by preparing ebiprazole bulk drug into freeze-dried oral preparations, not only provides clinical patients with a variety of drug dosage forms, but also contains ebiprazole The lyophilized oral formulation of azole can disintegrate quickly, so that the ebiprazole can be quickly dissolved and absorbed by the patient, and the bioavailability is improved; at the same time, the lyophilized oral formulation can be disintegrated in the patient's mouth without water, so that Part of the drug can be absorbed through mucosal transport, thus realizing pregastric absorption, avoiding the stimulation and damage of the drug to the stomach, and improving the compliance of clinical patients.