30 results about "Risedronic acid" patented technology

Provided is a novel method of making bisphosphonic acids, e.g. risedronic acid, including the step of combining a carboxylic acid, phoshorous acid, and a halophosphorous compound in the presence of a diluent that is an aromatic hydrocarbon or a silicone fluid. When the diluent is an aromatic hydrocarbon, a inert support or ortho-phosphoric acid codiluent is advantageously included.

Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of risedronic acid or a pharmaceutically acceptable salt thereof, in high yield and purity.

The present invention relates to an industrially advantageous process of making bisphosphonic acid or its salt in particular risedronic acid, [1-hydroxy-2(3-pyridinyl)ethylidene]bisphosphonic acid, having formula-(I) or its salts in high purity and high yields.

The present invention relates to an industrially advantageous process of making bisphosphonic acid or its salt in particular risedronic acid, [1-hydroxy-2(3-pyridinyl)ethylidene]bisphosphonic acid, having formula-(I) or its salts in high purity and high yields.

The disclosure provides a method for quantitatively determining risedronate in a urine sample by adding an internal standard to the urine sample, applying the urine sample to a polymeric water-wettable reverse-phased sorbent preconditioned with methanol, washing the sorbent with TEA in water and formic acid in methanol, eluting risedronate with a mixture of methanol and water containing EDTA under vacuum, evaporating the eluted solution and reconstituting with a mixture of methanol and NH4OH buffer and analyzing the sample with a LC-MS / MS system.

It is intended to provide a preventive agent or a therapeutic agent for a disease caused by abnormal bone metabolism, particularly for osteoporosis, which is more effective than ever before. By combined application of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)-phenoxy]pentoxy}-benzamidine or a salt thereof and one or more compounds selected from the group consisting of etidronic acid, clodronic acid, pamidronic acid, tiludronic acid, risedronic acid, minodronic acid, ibandronic acid, zoledronic acid, and salts thereof, a higher bone resorption inhibitory action compared with the administration of a single compound is exhibited, and an excellent preventive effect and therapeutic effect for a disease caused by abnormal bone metabolism, particularly for osteoporosis can be obtained.

The invention discloses a preparation method of risedronate sodium. The preparation method comprises the following steps of: (1) dissociating 3-pyridinecarboxylicacid chloride in 3-pyridinecarboxylicacid chloride hydrochloride; (2) reacting 3-pyridinecarboxylicacid chloride with diazomethane to generate a diazoketone compound represented by a formula (I); (3) generating 3-pyridylacetic acid under the common action of a catalyst and water; (4) adding hydrochloric acid, separating an organic phase from an inorganic phase, and evaporating and concentrating the inorganic phase to obtain 3-pyridylacetic acid hydrochloride; (5) converting 3-pyridylacetic acid hydrochloride into risedronic acid in the presence of phosphorus trichloride and phosphorous acid; and (6) reacting risedronic acid with sodium hydroxide solution to generate risedronate sodium. The preparation method of risedronate sodium disclosed by the invention has the advantages of being few in reaction step, short in reaction time, simple in post-treatment and higher in product yield.

The invention discloses a solid-phase microextraction-high performance liquid chromatography online combined detection method for zoledronic acid and risedronic acid. In the present invention, the hydroxyapatite functional monolithic column is firstly prepared by the in-situ mineralization method, and then the monolithic column is used as the solid phase microextraction monolithic column, combined with the solid phase microextraction-high performance liquid chromatography online system, to establish a Solid-phase microextraction-high performance liquid chromatography online detection method for zoledronic acid and risedronic acid. The invention utilizes the specific electrostatic interaction between the hydroxyapatite on the surface of the monolithic column and the P-C-P structure of the analysis object to realize the efficient extraction and enrichment of zoledronic acid and risedronic acid, and eliminate The interference of impurities in the sample matrix on the analytical detection. The method of the invention is simple, the technique is ingenious, the required instruments are highly popular, and it is easy to popularize, and can realize efficient extraction and enrichment of trace amounts of zoledronic acid and risedronic acid in complex actual samples, and meet the relevant high-sensitivity detection requirements.

The present invention relates to pharmaceutical compositions for preventing or treating osteoporosis, which comprise bisphosphonate-based compounds such as risedronic acids or the salts thereof, ibandronic acids or the salts thereof, or the like, and high-dose cholecalciferol, and which are to be administered once a month. The present invention also relates to pharmaceutical compositions for preventing or treating osteoporosis to be administered once a month, comprising: (a) cholecalciferol-containing granules obtained by adsorbing, to microcrystalline cellulose, the solution obtained by dissolving, into ethanol or an aqueous ethanol solution: (i) 24,000 to 50,000 IUs of cholecalciferol; (ii) one or more first stabilizers selected from among tocopheryl acetate, butylated hydroxytoluene and butylated hydroxyanisole; and iii) a binder; (b) mannitol as a second stabilizer; and (c) risedronic acids or the salts thereof or ibandronic acids or the salts thereof.