51 results about "Metoprolol Succinate" patented technology

Belonging to the field of pharmaceutical chemistry, the invention specifically relates to a method for preparing (S)-metoprolol succinate. The method comprises the steps of: pumping hydroxyphenylethyl methyl ether and (R)-chloropropylene oxide into a reaction vessel, and during the reaction process, pumping a reaction feed liquid into an external circulating dewatering system loaded with a dewatering agent for circulating dewatering, reacting the prepared (S)-3-[4-(2-methoxyethyl) phenoxyl]-1, 2-epoxypropane with isopropylamine so as to obtain an (S)-metoprolol base; mixing the (S)-metoprolol base with succinic acid, thus obtaining (S)-metoprolol succinate. During the first step of reaction in the invention, water generated in the reaction process can be effectively removed through the external circulating dewatering device, and the loss of (S)-3-[4-(2-methoxyethyl) phenoxyl]-1, 2-epoxypropane is reduced, thus realizing simple and fast production of low energy consumption. By the method of the invention, the conversion rate of the first step product (S)-3-[4-(2-methoxyethyl) phenoxyl]-1, 2-epoxypropane is over 90%, the final yield of (S)-metoprolol succinate is greater than 75%, and the utilization rate of the reaction substrate is obviously enhanced.

The invention provides a method for determining the content of residual isopropylamine in metroprolol succinate bulk pharmaceutical chemicals, and relates to the field of pharmaceutical chemicals. According to the method, a chromatographic column taking carboxylic acid cation exchange resin as filler is adopted for an ion chromatograph, and a mixed solution of acetone of methanesulfonic acid and water acts as leacheate, so as to prepare an electrical conductivity detector for detection. The method provided by the invention can effectively control the residual amount of isopropylamine in metroprolol succinate bulk pharmaceutical chemicals, and has the characteristics of good specificity, high precision and accuracy in determination.

This disclosure provides an extended-release capsule dosage form of metoprolol succinate in the form of coated discrete units, wherein said capsule dosage form is bioequivalent to the marketed Toprol-XL® tablet. The extended-release capsule dosage form comprising coated discrete units can be sprinkled onto food to ease administration to patients who have difficulty swallowing tablets or capsules.

The invention discloses a slow-release pellet preparation containing metoprolol succinate and hydrochlorothiazide and a preparation method thereof. The slow-release pellets of metoprolol succinate and the quick-release pellets of hydrochlorothiazide are mixed according to a prescribed dosage ratio and then filled. Made in hard capsules. Metoprolol succinate sustained-release pellets release continuously for 24 hours and take once a day to maintain a lasting antihypertensive effect. Hydrochlorothiazide immediate-release pellets are quickly absorbed to achieve diuretic and antihypertensive effects. The combination of the two makes the antihypertensive effect effective The additive effect can reduce the toxic and side effects of the drug, reduce the number of times of taking the drug, achieve a sustained and stable antihypertensive effect in the body, and improve the patient's compliance. At the same time, the sustained-release pellet preparation is composed of thousands of pellets with uniform particle size , the breakage of individual pellets will not lead to the sudden release of the entire preparation, which is safer than sustained-release tablets, less irritating to the gastrointestinal tract, and more stable blood drug concentration, effectively improving clinical effectiveness and safety.