35 results about "Tulobuterol" patented technology

A tulobuterol adhesive patch which comprises (a) a substrate, (b) an acrylic pressure-sensitive adhesive layer containing tulobuterol which is a percutaneously absorbable drug and optionally further containing a plasticizer comprising an oleophilic oily matter, and (c) a release liner superposed on the adhesive layer, wherein the acrylic pressure-sensitive adhesive comprises a copolymer obtained by copolymerizing an acrylic monomer which is an acetoacetoxyalkyl (meth)acrylate with one or more other vinyl monomers. Due to the use of the copolymer, the tulobuterol adhesive patch is excellent in tulobuterol releasability from the pressure-sensitive adhesive layer and tulobuterol permeation through the skin, is reduced in skin irritation, and is highly safe.

The invention discloses a method for industrial production of tulobuterol. The method comprises the following steps of 1, preparation of an intermediate II, wherein chloroacetophenone and an oxidant containing DMSO are added into a reaction kettle in sequence, a reaction is carried out for 1-1.5 hours under the condition of heat preservation, stirring is conducted until the reaction is completelyfinished, and through quenching, extraction, washing and concentration, the intermediate II is prepared; 2, preparation of a crude tulobuterol product, wherein the intermediate II, tert-butylamine, analcohol solvent and sodium borohydride are added into the reaction kettle in sequence and stirred, the reaction temperature is controlled, stirring is conducted until the reaction is completely finished, after concentration, extraction, washing and drying with a drying agent, filtration is conducted, and a filtrate is concentrated and recrystallized to obtain the crude tulobuterol product I; 3, refining of the tulobuterol, wherein the crude tulobuterol product I, an organic solvent and activated carbon for refinement of injection are recrystallized to obtain the refined tulobuterol. The industrial production method is green in reaction and simple in step and causes little pollution to the environment, the purity of the product is up to 99.95% or above, and the tulobuterol contains few impurities.

The invention relates to a synthesis method for compound tulobuterol. The technical problems that potential safety hazards exist in an existing method, and cost is high are solved. The method includes the following steps of a, an olefination reaction, wherein 1-(2-chlorphenyl)-1-ethyl alcohol serves as an initial raw material, and in the presence of a catalyst and acid, a heating reaction is conducted to generate 2-chloro-styrene; b, a cyclization reaction, wherein 2-chloro-styrene serves as a raw material, and in the presence of alkali and an oxidizing agent, an epoxidation reaction is conducted to obtain 2-(2-chlorphenyl) ethylene oxide; c, a ring-opening reaction, wherein 2-(2-chlorphenyl) ethylene oxide serves as a raw material and reacts with tert-butylamine to obtain compound 1-(2-chlorphenyl)-2-tert-butylamino ethanol. The synthesis method can be used for preparing tulobuterol.

The invention discloses a method for synthesizing tulobuterol. According to the method, 1-(2-chlorophenyl)-2-bromoethanone (compound 3) and 1-(2-chlorophenyl)-2,2-dibromoethanone (compound 10) can besimultaneously utilized to synthesize the tulobuterol. In an original route, the compound 10 is a by-product of synthesis of the compound 3, and about 10-15% of the compound 10 is not fully utilized.The method provided by the invention can improve the synthesis yield of the tulobuterol, is simple to operate, is environmentally friendly, is low in cost and is suitable for industrial production.

The invention relates to a transdermal absorption preparation with anti-asthmatic drug tulobuterol and salt as active ingredients, in particular to a tulobuterol patch. The transdermal absorption preparation is capable of controlling release of the tulobuterol continuously and has long-term storage stability at the same time, and tulobuterol particles can not be formed on a drug layer.

The present invention provides a tulobuterol adhesive patch comprising (a) a support, (b) an acrylic pressure-sensitive adhesive layer containing the percutaneously absorbing drug tulobuterol and if necessary a lipophilic oily plasticizer, and (c) a release liner, laminated in that order, wherein the acrylic pressure-sensitive adhesive is a copolymer obtained by copolymerizing an acrylic monomer which is acetoacetoxyalkyl (meth) acrylate with one or more other vinyl monomers, to yield a tulobuterol adhesive patch with excellent release and skin permeability of tulobuterol from the pressure-sensitive adhesive layer, low skin irritation and excellent safety.

The invention discloses a tulobuterol patch and a preparation method thereof. The tulobuterol patch consists of a back lining layer, a medicine-carrying pressure-sensitive adhesive layer and an anti-adhesive layer, wherein the medicine-carrying pressure-sensitive adhesive layer has a double-layer structure; and in the double-layer structure, a mass ratio of one layer which contacts the back lining layer and the other layer which contacts the anti-adhesive layer is (1:3)-(3:1). The preparation method comprises the following steps of: dissolving tulobuterol and a pressure-sensitive adhesive auxiliary material in a good solvent; and during preparation, coating two layers, namely coating a first layer, placing at room temperature, so that the solvent is volatilized fully, and coating a second layer to obtain a percutaneous absorption-type tulobuterol patch. The preparation process for the tulobuterol percutaneous absorption preparation is simple and can be used for producing the tulobuterol patch; and by the prepared tulobuterol patch, medicines can be released slowly at a constant speed, so the tulobuterol patch meets the requirements of preparations for treating asthma diseases.

The invention discloses a tulobuterol-containing aquogel patch, which comprises tulobuterol, a macromolecular framework material, a crosslinker, a crosslinking regulator, a humectant and distilled water, wherein the crosslinker is a combination of more than two organic acids; and at least one organic acid is tartaric acid and at least the other organic acid is selected from citric acid, gluconic acid, lactic acid, malic acid and malicaicd. The invention also discloses a method for preparing the tulobuterol-containing aquogel patch. The tulobuterol-containing aquogel patch and the preparation method of the invention make the cohesion of aquogel matrix so stable that the matrix avoids cloth penetration, hardening and other phenomena; the patch is proper in viscosity and insusceptible to falling off after being adhered and can be stripped without causing pains; and the method is controllable in gel time and can meet requirements for industrial large-scale production.

The invention discloses an immune-electrochemistry sensor for detecting seven beta-adrenergic receptor agonists, and a manufacture method and application of the immune-electrochemistry sensor. The immune-electrochemistry sensor comprises a substrate glass electrode, and a film layer and a detection layer which sequentially coat the surface of the substrate glass electrode, wherein the material of the detection is a beta-agonist general hapten 4-(4-(2-terttert-butylamino) 1-ethoxy) phenylbutyric acid solution. The method comprises the following steps: firstly dispensing graphene / chitosan dispersion liquid on the surface of the clean substrate glass electrode, drying to form a film formation layer, dispensing the 4-(4-(2-terttert-butylamino) 1-ethoxy) phenylbutyric acid solution on the surface of the film layer, and then drying. The sensor is based on the cross immunoreactions of a beta-agonist broad specificity antibody on various beta-agonists, and can realize the detection of seven beta-agonists including clenbuterol, salbutamol, mabuterol, brombuterol, cimbuterol, tulobuterol and terbutaline.

The invention discloses a tulobuterol transdermal patch and a preparation method thereof. The patch comprises a medicine storage layer, the medicine storage layer comprises a first adhesive layer containing amorphous tulobuterol; and a second adhesive layer which is arranged below the first adhesive layer, is in contact with the first adhesive layer and comprises tulobuterol crystals, wherein the solubility of tulobuterol of the first adhesive layer is 2-8 times that of tulobuterol of the second adhesive layer. The medicine storage layer adopts a mixed matrix composed of a polyacrylate pressure-sensitive adhesive and an acrylate-rubber copolymer adhesive according to a specific content, the solubility of the tulobuterol medicine in the matrix can be enhanced, and the tulobuterol medicine exists in the first adhesive layer in an amorphous supersaturated state, so that the initial transdermal rate of the tulobuterol medicine can be remarkably enhanced; the tulobuterol crystals of the second adhesive layer are used for timely supplementing released medicines, so that the initial transdermal rate is remarkably improved, and meanwhile, long-time (48-72 hours) continuous approximate constant-speed transdermal administration is maintained.

The present invention discloses a transcutaneous plaster containing tulobuterol, its preparation method and application. The pressure-sensitive adhesive used by said invention is a hot-melt pressure-sensitive adhesive whose melting point is 50-250 deg.C. the described hot-melt pressure-sensitive adhesive is an adhesive made up by using thermoplastic polymer as main raw material, and hs the hot-melting and pressure-sensitive double characteristics. Said product contains no organic solvent, and its coating speed is quick, and its cost is low.

The present invention provides an adhesive skin patch that permits excellent and prolonged percutaneous absorption of tulobuterol and that can be stably applied to the skin for a long period of time with less skin irritation. The adhesive skin patch comprises a base material and a medicated layer provided on one surface of the base material. The medicated layer contains 1 to 30% by weight of a resolvent, 40 to 98% by weight of a pressure-sensitive adhesive, and tulobuterol. The resolvent contains an aliphatic alcohol having a branched-chain structure or a double bond in its C8 to C30 carbon chain. The pressure-sensitive adhesive is a copolymer obtained by copolymerizing monomers containing 70% by weight or more of an alkyl(meth)acrylate whose alkyl group has 6 to 20 carbon atoms.

The invention provides a tulobuterol crystal form and a preparation method thereof. The preparation method comprises the following steps of: dissolving tulobuterol in ethyl acetate and other good solvents, dropwisely adding n-heptane and other poor solvents into the system, filtering, taking the filter cake, and drying the filter cake to obtain the tulobuterol crystal form crystal. The crystal form is high in purity and good in stability, has superiority in process production, and is suitable for long-term storage in the preparation process.