Preparation method of metoprolol tartrate sustained release preparation

A technology of metoprolol tartrate and sustained-release preparations, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of large amount of excipients, changes in drug release, and unfavorable oral administration, etc. problems, to achieve the effects of high production efficiency, moderate dosage of capsule material, and good sustained-release function

Inactive Publication Date: 2018-12-18
刘丽
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dosage forms produced by this technology have the risk of sudden release and changes in drug release during storage, and the amount of excipients is large, which is not conducive to oral administration

Method used

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  • Preparation method of metoprolol tartrate sustained release preparation
  • Preparation method of metoprolol tartrate sustained release preparation
  • Preparation method of metoprolol tartrate sustained release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 1) 100g metoprolol tartrate is dissolved in 160g95% ethanol to obtain metoprolol tartrate ethanol solution, which is referred to as solution A;

[0023] 2) Add 130g of hydroxypropyl β-cyclodextrin and 20g of mannitol to solution A to obtain solution B;

[0024] 3) Dissolve 120g of polylactic acid and 20g of polyethylene glycol 200 in 120g of acetone to obtain a solution of polylactic acid and polyethylene glycol 200, which is referred to as solution C;

[0025] 4) Mix solution B and solution C to obtain solution D;

[0026] 5) Transfer solution D to a magnetic stirrer, control the temperature of solution D at 15°C to 18°C, continuously stir solution D for 12 hours, then reduce the temperature of solution D to 0°C to 1°C within 2 hours and let it stand for 12 hours. Hours, keep the temperature of solution D at 0°C to 1°C during the standing period;

[0027] 6) Heat the solution D obtained in step 5, and stir continuously for 12 hours when the temperature of the solutio...

Embodiment 2

[0031] 1) 100g metoprolol tartrate is dissolved in 170g95% ethanol to obtain metoprolol tartrate ethanol solution, which is referred to as solution A;

[0032] 2) Add 140g of hydroxypropyl β-cyclodextrin and 25g of mannitol to solution A to obtain solution B;

[0033] 3) Dissolve 130g of polylactic acid and 30g of polyethylene glycol 200 in 130g of acetone to obtain a solution of polylactic acid and polyethylene glycol 200, which is referred to as solution C;

[0034] 4) Mix solution B and solution C to obtain solution D;

[0035] 5) Transfer solution D to a magnetic stirrer, control the temperature of solution D at 15°C to 18°C, continuously stir solution D for 12 hours, then reduce the temperature of solution D to 0°C to 1°C within 2 hours and let it stand for 12 hours. Hours, keep the temperature of solution D at 0°C to 1°C during the standing period;

[0036] 6) Heat the solution D obtained in step 5, and stir continuously for 12 hours when the temperature of the solutio...

Embodiment 3

[0040] 1) 100g metoprolol tartrate is dissolved in 180g95% ethanol to obtain metoprolol tartrate ethanol solution, which is referred to as solution A;

[0041] 2) Add 150g of hydroxypropyl β-cyclodextrin and 30g of mannitol to solution A to obtain solution B;

[0042] 3) Dissolve 150g of polylactic acid and 40g of polyethylene glycol 200 in 150g of acetone to obtain a solution of polylactic acid and polyethylene glycol 200, which is referred to as solution C;

[0043] 4) Mix solution B and solution C to obtain solution D;

[0044] 5) Transfer solution D to a magnetic stirrer, control the temperature of solution D at 15°C to 18°C, continuously stir solution D for 12 hours, then reduce the temperature of solution D to 0°C to 1°C within 2 hours and let it stand for 12 hours. Hours, keep the temperature of solution D at 0°C to 1°C during the standing period;

[0045]6) Heat the solution D obtained in step 5, and stir continuously for 12 hours when the temperature of the solution...

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Abstract

The invention provides a preparation method of a metoprolol tartrate sustained release preparation. The preparation method is characterized in that the metoprolol tartrate is dissolved in 95% ethanolto obtain a solution A, and hydroxypropyl beta-cyclodextrin and mannitol are added in the solution A to obtain a solution B; polylactic acid and polyethylene glycol 200 are dissolved in acetone to obtain a solution C, the solution B and the solution C are mixed to obtain a solution D, the solution D is transferred to a magnetic stirrer, the solution D is continuously stirred for 12 hours, the temperature of the solution D is lowered to 0 DEG C to 1 DEG C in 2 hours and the solution D is subjected to standing for 12 hours, and the temperature of the solution D is kept to 0 DEG C to 1 DEG C during a standing period; after standing for 12 hours, the solution D is heated, when the temperature of the solution D is increased to 15 DEG C to 18 DEG C, the solution D is continuously stirred, when the temperature of the solution D is controlled at 15 DEG C to 18 DEG C while stirring, after the material is continuously stirred for 12 hours, the metoprolol tartrate sustained release preparation isprepared by a low-temperature spray-drying method. The dosage of a capsule material is moderate, the drying temperature of the material is low, the obtained drug-loading preparation is uniform, the drug release is stable, and the metoprolol tartrate sustained release preparation has sustained release characteristics.

Description

Technical field: [0001] The invention relates to a pharmaceutical preparation of a drug-loaded polymer preparation, in particular to a preparation method of a metoprolol tartrate sustained-release preparation. Background technique: [0002] Hydroxypropyl β-cyclodextrin is an ideal injection solubilizer and pharmaceutical excipient in the pharmaceutical industry. It can improve the water solubility of insoluble drugs, increase the stability of drugs, improve the bioavailability of drugs, increase the curative effect of drugs or reduce the dosage, adjust or control the release speed of drugs, and reduce the toxic and side effects of drugs. It can be used as a carrier for oral drugs, injections, mucosal drug delivery systems (including nasal mucosa, rectum, cornea, etc.), transdermal drug delivery systems, and lipophilic targeted drugs. [0003] Polylactic acid is highly safe to the human body, has good biocompatibility and biodegradability, and is widely used in drug sustaine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/40A61K47/34A61K47/10A61K47/26A61K31/138A61P9/12A61P9/10
CPCA61K9/1652A61K9/1623A61K9/1641A61K9/1647A61K31/138
Inventor 刘丽
Owner 刘丽
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