43 results about "Salmeterol" patented technology

The tiotropium bromide inhalant is prepared through spray drying the mixture solution of tiotropium bromide and amino acid to form superfine powder, mixing with re-crystallized lactose, and capsulizing or preparing other proper preparation form. It is administrated with special device so that the dry medicine powder enters to the lung via respiratory tract to treat chronic obstructive diseases. The present invention has simple preparation process without organic solvent and preservative used, and the prepared powdered preparation has good flowability, accurate dosage, high effective part depositing amount and no irritation to mucous membrane. The preparation process of the present invention may be also used for preparing Salbutamol, salmeterol and other inhalant.

A method for treating respiratory disorders by administrating by inhalation an effective amount of a β₂-receptor agonist, an acceptable amount of a corticosteriod, and HFA 134a, to a patient in need thereof, is disclosed. Preferably, the β₂-receptor agonist is salmeterol or a physiologically acceptable salt thereof, and the corticosteriod is fluticasone propionate or a solvate thereof. The combination of salmeterol, fluticasone proprionate, and HFA 134a may lower the risk of cardiac arrhythmias, sudden death, or hypercorticism that are sometimes associated with the simultaneous administration of a β₂-receptor agonist and an anti-inflammatory corticosteroid.

The present invention relates to a kind of medicine composite for treating branchial asthma. The medicine composite consists of active component including salmeterol or its medicinal salt and budesonide in the molar ratio of 1 to 0.38-20, as well as non-active components including solvent, cosolvent, propellant, antioxidant, dilutent and lubricant. The present invention has large range of medicine dosage, long lasting period and high comprehensive effect, and may be prepared into various preparation forms.

The invention discloses a method for preparing an anti-asthmatic medicament of salmeterol. The method comprises the following steps of: adding paraxylene, parahydroxyphenylacrylic acid, formaldehyde and acid medium into a reactor, heating, cooling, filtering, washing and drying to obtain 3-hydroxymethyl-4-hydroxyl-phenylacrylic acid; adding the 3-hydroxymethyl-4-hydroxyl-phenylacrylic acid into the reactor, then adding oxyful, lipase and ethyl acetate to finally obtain 3-hydroxymethyl-4-hydroxyl-(beta-hydroxy)-phenylpropyl aldehyde, adding the 3-hydroxymethyl-4-hydroxyl-(beta-hydroxy)-phenylpropyl aldehyde and 6-(4-phenylbutoxy)hexylamine into the reactor, heating for reflowing, cooling, filtering, adding sodium borohydride in batches into filtrate, stirring at normal temperature, then evaporating to dryness, extracting, combining organic layers, drying, filtering and evaporating to dryness to obtain a solid, and separating by using the column chromatography to obtain the final product. The invention has novel and short synthetic route, convenient experiment operation, higher yield of the target product and lower production cost.

The invention discloses a method for synthesizing (R)-salmeterol. The method is implemented by taking p-hydroxy benzaldehyde as a raw material through the steps of carrying out a methylolation reaction on the p-hydroxy benzaldehyde so as to obtain prochiral aldehyde for protecting double hydroxide radicals in an acetal form; then, through taking (S)-BINOLAM.AlCl as a chiral catalyst, carrying out an asymmetric nucleophilic addition reaction so as to obtain a chiral cyanohydrin intermediate; and reducing the chiral cyanohydrin intermediate so as to obtain primary amine, reacting the primary amine with mesylate [6-(4 phenylbutoxy]hexane, and carrying out hydrolysis on the obtain product so as to remove protecting groups, thereby obtaining a final product (R)-salmeterol. In the invention, a chiral catalyst precursor (S)-BINOLAM can be reused; and the method has relatively high yield and relatively good enantioselectivity, and is short in synthetic route, simple and convenient in operation and low in cost.

The invention provides application of salmeterol in medicine for treating type 2 diabetes and insulin resistance. The salmeterol has effects of lowering blood sugar, resisting diabetes and increasing the cell glucose consumption of a 3T3-L1 insulin resistance model. Measuring of PPAR gamma protein expression quantity through an ELISA method shows that the salmeterol can increase the PPAR gamma protein expression quantity. The salmeterol has evident curative effect on the type 2 diabetes.

There is provided according to the invention a pharmaceutical aerosol formulation which comprises: (i) salmeterol or a pharmaceutically acceptable salt thereof and (ii) a hydrofluoroalkane (HFA) propellant, characterised in that the salmeterol or pharmaceutically acceptable salt thereof is completely dissolved in the formulation.

The invention relates to the technical field of preparation and application of chiral high-performance liquid chromatography column materials, and discloses preparation and application of beta-CD-D2 high-performance liquid chromatography chiral column material. A high-performance liquid chromatography chiral column is prepared from beta-CD-D2 and is used for splitting chiral medicine enantiomers. The preparation and the application of the beta-CD-D2 high-performance liquid chromatography chiral column material comprise the following steps: 1, constructing a chiral environment by using beta-CD-D2, bonding the chiral environment with high-performance liquid chromatography silica beads into a fixed phase filler, then preparing the fixed phase filler into a chiral column, and applying the chiral column into high-performance liquid chromatography; 2, finding out an optional formula and an optional condition by using a proper characterization means, and optimizing the method and the condition; 3, establishing a preparation method of a salmeterol single enantiomer by using the prepared beta-CD-D2 chiral column, and splitting a chiral compound by using a cyclodextrins derivative for the first time; and 4, splitting drugs by using the prepared beta-CD-D2 chiral column, and establishing a method for splitting and qualitatively and quantitatively analyzing seven chiral drugs including salmeterol, terbutaline, procaterol, cetirizine, lamivudine, cefuroxime and ceftriaxone.

The invention provides a method for determining salmeterol, indacaterol and olodaterol in pork. The method includes the following steps: step 1, preparing samples; step 2, extracting to-be-detected samples; step 3, determining detection conditions of a liquid chromatography-tandem mass spectrometer and performing detection; step 4, drawing standard working curves; step 5, according to liquid chromatograms of to-be-detected solutions in the S2, calculating the contents of the olodaterol, the indacaterol and the salmeterol in the pork. The method has the advantages that the salmeterol, the indacaterol and the olodaterol in the pork are simultaneously determined for the first time, and the blank in current detection of the salmeterol, the indacaterol and the olodaterol in the pork is filled up; ion response values are high, sensitivity is high, detection limits are low, qualitativeness, quantitativeness, accuracy, rapidness, high efficiency and sensitivity are truly realized, and the method can serve as a reliable measure to detect the three drugs in the pork.

The invention relates to a preparing method of salmeterol and fluticasone super fine particles. The preparing method comprises the steps of dissolving the raw materials for preparing the super fine particles into a solvent to prepare a solution, and then adding the solution into a spray dryer to be subjected to spray drying, so that the salmeterol and fluticasone super fine particles are prepared, wherein the raw materials comprise salmeterol, fluticasone propionate and auxiliaries, the volume added quantity of the solution is 10%-30% of the total capacity of the spray dryer, and the mass concentration of the solution is 5%-10%. According to the preparing method of the salmeterol and fluticasone super fine particles, the salmeterol and fluticasone dry particles are finer, uniformity is better, and distribution of the two medicines is more reasonable.

The invention discloses a salmeterol lipid complex and a preparation method thereof. The complex comprises salmeterol, a lipid material, a buffer solution and the like. The lipid complex can compriseone or more lipids. In addition, the invention further discloses the ratio of the high-activity compound salmeterol to the lipids in the complex. The encapsulation efficiency of the salmeterol lipid complex can be increased, and in combination with a pharmaceutically acceptable vector or an optional medicament formula, the complex can prevent or treat related diseases, and has the characteristicsof good stability, high targeting property, low toxic and side effects and the like. The preparation method involved in the invention is simple, and is high in operability, and industrialized production is easy to implement.

The invention discloses a salmeterol transdermal patch, which contains salmeterol and its salts, a pressure-sensitive adhesive, a penetration enhancer, a solvent, and contains 0.05% to 0.1% of salmeterol and its salts, Sensitive glue 74.9%~98.5%, penetration enhancer 0.5~10%, solvent 1%~15%. It has excellent properties in transdermal absorption rate, mechanical properties and preparation process, and is used for the prevention and treatment of asthma.

The invention relates to a combination consisting of inhalation/oral roflumilast or a pharmaceutically acceptable salt thereof and inhalation salmeterol or a pharmaceutically acceptable salt thereof. The medicinal composition product is administrated synchronously, sequentially or separately, and is applied to treatment or preventive treatment of respiratory diseases or symptoms thereof, particularly treatment of diseases accompanied with obstruction or inflammation such as chronic obstructive pulmonary disease (COPD) or asthma.

The invention discloses a preparation method of salmeterol. The method includes the following steps: carrying out a condensation reaction on a compound 2 and a compound 3 under an alkaline condition to obtain an intermediate 4; carrying out acidic hydrolysis to obtain an intermediate 5, and reducing the intermediate 5 to obtain an intermediate 6; and removing a benzyl group from the intermediate 6 by using palladium on carbon (Pd/C) to obtain a salmeterol base. The preparation method has the advantages of mild reaction conditions, simple post-treatment, low cost, high yield high product purity, and easiness in realization of industrialization.

Pharmaceutical composition for inhalation, containing as active ingredient effective amounts of salmeterol or a physiologically salt of salmeterol or a solvate thereof, and budesonide or a therapeutically salt of budesonide or a solvate thereof, wherein the molecular ratio of salmeterol component to budesonide component is in the range 1:2 to 1:50, together with a pharmaceutically acceptable carrier.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a salmeteroxinamic acid ester microparticle for inhalation and a preparation method thereof, and the salmeteroxinamic acid ester microparticle for inhalation comprises the following components: salmeteroxinamic acid ester and a co-crushing agent in a mass ratio of 1: (10-70). The preparation method comprises the following steps: firstly, according to the mass ratio, mixing salmeteroxamic acid ester with the co-crushing agent for 0.5-1 hour; smashing the mixture obtained in the step 1) in a self-airflow smashing mode, wherein the smashing pressure is 0.6 Mpa, the feeding speed is 0.5 g/min, and obtaining the salmeteroxinamic acid ester particles for inhalation. Compared with independent crushing, the method provided by the invention has the advantages of higher feeding speed and higher product yield, powder blockage in the crushing cavity and the airflow channel is avoided, and the obtained product has smaller particle size.