35 results about "Trandolapril" patented technology

A stable pharmaceutical composition comprising about 1 wt. % to about 80 wt. % of an ACE inhibitor or a pharmaceutical acceptable salt thereof, about 1 wt. % to about 70 wt. % of an alkali or alkaline earth metal carbonate, and about 1 wt. % to about 80 wt. % of hydroxypropyl cellulose, wherein the ACE inhibitor is selected from the group consisting of quinapril, enalapril, spirapril, ramipril, perindopril, indolapril, lisinopril, alacepril, trandolapril, benazapril, libenzapril, delapril, cilazapril and combinations thereof; wherein the formation of an internal cyclization product, and / or ester hydrolysis product, and / or oxidation product, has been reduced or eliminated, and the weight percents are based on the total weight of the pharmaceutical composition. The stabilized pharmaceutical compositions of the invention exhibit a number of advantages as follows: (i) the ACE inhibitor or a pharmaceutical acceptable salt thereof present in the compositions is preserved from degradation; (ii) the compositions exhibit extended shelf-life under normal storage conditions; (iii) the effect of moisture on the compositions is minimized; (iv) the compositions exhibit minimal, if any, discoloration over a significant period of time; and (v) the compositions exhibit minimal, if any, instability when employed in the presence of colorants.

The invention relates to a medicinal composition containing trandolapril taste-masking composition and a preparation technique thereof. The medicinal composition has the following characteristics that: flavoring agent in the trandolapril taste-masking composition is selected from gelatin, mannitol and aspartame, the medicinal composition is in the form of powder or particles, consequently, the stability of preparation is good, bitter taste is masked, taste is good, disintegration is quick, absorption is quick, and carrying is convenient.

The invention relates to a synthetic method for trandolapril key intermediate (2S, 3aR and 7as)-octahydro-1H-indole-2-carboxylic acid. The method comprises the following steps: obtaining a pair of cis 1, 2-cyclohexane dimethyl acid mono-methyl ester after refluxing hexahydrophthalic anhydride by methanol, splitting the cis 1, 2-cyclohexane dimethyl acid mono-methyl ester by (-) N, N-dimethyl amino diol to obtain 1, 2-cyclohexane dimethyl acid mono-methyl ester of (1R, cis) and (1S, cis) respectively; refluxing (1R, cis)-1, 2-cyclohexane dimethyl acid mono-methyl ester obtained by reclaiming mother liquor in hydrochloric acid to obtain cyclohexane o-dioctyl phthalate, and cyclizing the cyclohexane o-dioctyl phthalate to obtain an initial raw material of the hexahydrophthalic anhydride; and circulating the processes unceasingly to improve the impurity of the (1R, cis)-1, 2-cyclohexane dimethyl acid mono-methyl ester, and then directly entering a follow-up synthesizing process. The process effectively solves the problems of treatment of (1S, cis) 1, 2-cyclohexane dimethyl acid mono-methyl ester after racemization of (d1)1, 2-cyclohexane dimethyl acid mono-methyl ester and yield of (1R, cis)-1, 2-cyclohexane dimethyl acid mono-methyl ester, improves utilization efficiency of raw materials, reduces cost of products, is more suitable for industrialized production, can effectively improve follow-up reaction efficiency, and saves energy of a system.

A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.

The invention discloses a preparation method of an isomer of a trandolapril intermediate, and in particular discloses a preparation method of the isomer of the trandolapril intermediate which is shown in a formula C and is acquired by using (R,S,S)-octahydroindole-2-carboxylic acid (shown in a formula A) as an initial raw material with the content of more than 90 percent, performing configuration turning and upper benzyl protection to obtain isomer mixtures C and D of the corresponding trandolapril intermediate and performing separation again. According to the technical scheme, the formula A is subjected to configuration turning, and the content of a compound of the formula B is obviously increased, so that the isomers of the subsequent other intermediates are greatly prepared, and the compound is used for preparing medicines for resisting cardiovascular disease and controlling the quality of the medicines.