59 results about "Fexofenadine Hydrochloride" patented technology

The present invention is related to novel polymorph of Fexofenadine and Fexofenadine hydrochloride of formula 1 and process of preparation thereof. The present invention is also directed to provide pure novel polymorphs of Fexofenadine and its hydrochloride by a simple process which is cost effective, commercially viable and environment friendly.

The invention provides a preparation method of fexofenadine hydrochloride orally disintegrating tablets. Based on the advantages of the orally disintegrating tablet preparation formulation, the product not only overcomes the defects of poor disintegration, slow effect, low bioavailability and the like of the preparation formulations on sale in foreign countries, but also fills a gap in the domestic market, thus adapting to the demand of development of market situation. The medicine has important significance in keeping good health of the people and creating economical and social benefits. The product has simple and easy technique and easily obtained raw and auxiliary materials, is suitable for industrial production, and has good application prospect.

The invention provides a method for preparing a fexofenadine hydrochloride orally disintegrating tablet. The method comprises the following steps of: (1) providing component substances including fexofenadine hydrochloride, microcrystalline cellulose, sodium carboxymethyl starch, polyvidone and absolute ethyl alcohol in the mass ratio of 300:550:100:50:240; (2) adding the fexofenadine hydrochloride, microcrystalline cellulose, sodium carboxymethyl starch and polyvidone in the component substances, adding a mixture into a wet mixing pelletizer, and starting shearing and mixing, wherein the rotating speed of a stirring paddle is 504 revolutions per minute, the rotating speed of a pelletizing knife is 1,500 revolutions per minute, and the mixing time is 10 minutes; (3) adding absolute ethyl alcohol into a powdery mixture, and mixing continually under the condition that the rotating speed of a stirring paddle wheel is 756 revolutions per minute, the rotating speed of the pelletizing knife is 3,000 revolutions per minute to obtain wet particles; and (4) drying the obtained wet particles obtained in the step (3) in a half way.

The invention relates to a pharmaceutical composition with fexofenadine hydrochloride. The composition is composed of the following components: 1-12% of fexofenadine hydrochloride as an active ingredient, 1-10% of suspending aid, 5-85% of filler, 1-10% of sweetening agent, 0.01-10% of essence and a conventional amount of flow aid, wherein the composition exists in a form of a dry suspension. The fexofenadine hydrochloride suspension provided by the invention has the advantages of high dispersity, uniformity in distribution, rapidness in absorption, high bioavailability, good taste, stability and the like.

The present invention relates to a pharmaceutical formulation of fexofenadine hydrochloride in a solvent system suitable as a liquid fill composition. In another aspect, the invention also relates to a process for the preparation of the said pharmaceutical formulation and the use of said composition for the preparation of a drug for the treatment of allergic reactions in a patient.

The invention discloses a fexofenadine hydrochloride orally disintegrating tablet, which consists of fexofenadine hydrochloride, a composite disintegrating agent, a filling agent, a lubricating agent and a composite flavoring agent. The fexofenadine hydrochloride orally disintegrating tablet is characterized in that the composite disintegrating agent is a highly efficient disintegrating agent, the highly efficient disintegrating agent is added internally and externally; and the composite flavoring agent is also added internally and externally. The orally disintegrating tablet of the inventionhas more excellent quality, can completely disintegrate in the oral cavity within 30 seconds, and has no gravel sense and no bitterness, and the dissolution can be more than 80 percent when determining the dissolution with water as the medium for ten minutes.

The present invention is related to novel polymorph of Fexofenadine and Fexofenadine hydrochloride of formula 1 and process of preparation thereof. The present invention is also directed to provide pure novel polymorphs of Fexofenadine and its hydrochloride by a simple process which is cost effective, commercially viable and environment friendly.

Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.

The present invention is related to novel polymorph of Fexofenadine and Fexofenadine hydrochloride of formula 1 and process of preparation thereof. The present invention is also directed to provide pure novel polymorphs of Fexofenadine and its hydrochloride by a simple process which is cost effective, commercially viable and environment friendly.

The present invention relates to pharmaceutical compositions of antihistamine-decongestant combination. Specifically the invention relates to bilayered tablet formulation comprising antihistaminic decongestant combination. More specifically present invention relates to the novel polymorph of fexofenadine or pharmaceutically accepted salts thereof, with at least one decongestant in the form of bilayered tablet. The preferred polymorphs are polymorph A and polymorph X of fexofenadine hydrochloride.

The invention discloses a fexofenadine hydrochloride tablet and a preparation method thereof. The preparation is prepared from solid dispersion and pharmaceutical acceptable auxiliary materials by the procedures of evenly mixing and directly tabletting, wherein the solid dispersion is obtained by dissolving fexofenadine hydrochloride and citric acid into ethanol, drying and removing ethanol. According to the tablet disclosed by the invention, the dosage of a disintegrating agent is reduced under the premise of ensuring that the drug is rapidly dissolved out; the production cost is reduced; meanwhile, the fexofenadine hydrochloride tablet is simple in preparation technology, and good in surface after accelerated inspection.

The present invention provides a fexofenadine hydrochloride oral disintegrating drug composition. The fexofenadine hydrochloride oral disintegrating drug composition has characteristics of good stability, high bioavailability, and cost reducing. With the fexofenadine hydrochloride oral disintegrating drug composition of the present invention, the industrialization is achieved, the good clinical application is provided, and the obvious advantage is provided.

The invention discloses a synthetic process of fexofenadine hydrochloride. The synthetic process of fexofenadine hydrochloride comprises the following steps of: with alpha, alpha-dimethyl phenylacetic acid as a raw material, carrying out an esterification reaction on alpha, alpha-dimethyl phenylacetic acid and absolute ethyl alcohol under the catalysis of a silica gel loaded phosphotungstic acid (PW12 / SiO2) solid acid catalyst to obtain alpha, alpha-dimethyl ethyl phenylacetate; carrying out Friedel-Grafts reaction on alpha, alpha-dimethyl ethyl phenylacetate and 4-chlorobutyryl chloride to obtain alpha, alpha-dimethyl-4-(4-chloro-1-oxo butyl) ethyl phenylacetate; reducing by virtue of sodium borohydride in 95% ethyl alcohol to obtain alpha, alpha-dimethyl-4-(4-chloro-1-hydroxyl butyl) ethyl phenylacetate; and carrying out N-alkylation reaction on alpha, alpha-dimethyl-4-(4-chloro-1-hydroxyl butyl) ethyl phenylacetate and alpha, alpha-dimethyl-4-piperidine methyl alcohol in DMF (dimethyl formamide) for 24 hours at the temperature of 80 DEG C to obtain alpha, alpha-dimethyl-4-[1-hydroxyl-4-[4-(hydroxyl diphenylmethyl)-1-piperidyl]-butyl] ethyl phenylacetate, and then carrying out alkali hydrolysis and salification by virtue of hydrochloric acid, so that fexofenadine hydrochloride is obtained. The synthetic process of fexofenadine hydrochloride is high in yield and low in cost, produces less pollution and is applicable to industrial mass production.

The invention relates to a composition of fexofenadine hydrochloride and microcrystalline cellulose. On the basis of totally manufacturing 1000 chips, the composition comprises the following components: 60 grams of the fexofenadine hydrochloride, 66 grams of the microcrystalline cellulose, 34 grams of starch, 10 grams of sodium carboxymethyl cellulose, proper quantity of 5-pecent povidone ethanolsolution, and 0.8 gram of magnesium stearate; and on the basis of totally coating 1000 film coats, the composition comprises the following components: 0.67 gram of hydroxypropyl methylcellulose, 0.33milliliter of propylene glycol, 800.33 milliliters of polysorbate, 0.67 gram of titanium dioxide, 26.7 milliliters of 95-percent ethanol and 6.67 milliliters of purified water. The method for preparing the composition comprises staged production steps. As both the microcrystalline cellulose and the starch have high fluidity and compressibility and can accelerate disintegration of tablets, the microcrystalline cellulose and the starch are selected and used on the basis of determining the used amount of the fexofenadine hydrochloride; and the sodium carboxymethyl cellulose is selected as a disintegrating agent, has higher disintegration and higher compressibility, and is an excellent disintegrating agent for the tablets.