Amlodipine and losartan potassium medicinal composition and preparation method thereof

A technology of losartan potassium and amlodipine, which is applied in the field of medicine, can solve the problems of synergy, accumulation, limited complementary effects, limited synergistic, cumulative, complementary effects, low overall level of blood drug concentration, etc., and achieve excellent dissolution performance, Improves bioavailability and prevents decomposition and deterioration

Active Publication Date: 2012-02-01
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In the prior art, amlodipine and amlodipine salts (such as amlodipine maleate, amlodipine besylate, amlodipine mesylate, etc.) are almost insoluble in water and are slowly absorbed in the human body. The peak blood drug concentration is reached within 6-12 hours, and the overall level of blood drug concentration is low, especially the initial blood drug concentration after administration is very low. The drug concentration reaches the peak blood concentration in 1 hour and 3-4 hours respectively, and the drug effect is fast. After the two drugs are administered at the same time, the time when they reach the peak blood concentration is far away, and the synergistic, cumulative and complementary effects very limited
For example, Chinese patent CN101472587A discloses a composition for preventing or treating cardiovascular diseases, which comprises amlodipine or a pharmaceutically acceptable salt thereof and losartan or a pharmaceutically acceptable salt thereof, the invention Improved the dissolution rate and stability of amlodipine and losartan potassium, but amlodipine is still slow to act, and the synergistic effect of the two is very limited
[0011] In addition, in order to improve the bioavailability of amlodipine salt, the prior art uses the amlo

Method used

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  • Amlodipine and losartan potassium medicinal composition and preparation method thereof
  • Amlodipine and losartan potassium medicinal composition and preparation method thereof
  • Amlodipine and losartan potassium medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Add 9g of amlodipine maleate, 21ml of ethanol, 42ml of dimethyl sulfoxide, and 7ml of deionized water into a 100ml reaction kettle, adjust the pH to 6 with triethylamine or acetic acid, stir for 30min, seal it, and place it in an oven at 125°C After 3 days, take out the reaction kettle, place the reaction kettle in a 40KHz ultrasonic field to cool down naturally, wait for the reaction kettle to cool down slowly to 70°C, open the reaction kettle, add 70°C deionized water dropwise, white crystalline powder precipitates, and cool to room temperature And turn off the ultrasonic wave, filter, wash with dichloromethane and ethanol, and dry in vacuum for 2 hours to obtain amlodipine maleate hydrate crystals. The particle size range of the crystal is 75-150 μm, mp: 178-180°C.

[0055] Adopt U.S. Perkin-Elmer company PE 2400II elemental analyzer, elemental analysis (%) calculated value is: C (52.22), H (5.84), Cl (6.42), N (5.08), O (30.44); Elemental analysis (%) ) found: C (5...

Embodiment 2

[0059] Add 9g of amlodipine maleate, 21ml of ethanol, 42ml of dimethyl sulfoxide, and 7ml of deionized water into a 100ml reaction kettle, adjust the pH to 6.5 with triethylamine or acetic acid, stir for 30min, seal it, and place it in an oven at 130°C After 3 days, the reactor was taken out, and the reactor was placed in a 40KHz ultrasonic field to cool down naturally. After the reactor was slowly cooled to 75°C, the reactor was opened, and deionized water at 75°C was added dropwise. White crystalline powder precipitated, and cooled to room temperature. And turn off the ultrasonic wave, filter, wash with dichloromethane and ethanol, and dry in vacuum for 3 hours to obtain amlodipine maleate hydrate crystals. The particle size range of the crystal is 75-150 μm, mp: 178-180°C.

[0060] Adopt U.S. Perkin-Elmer company PE 2400II elemental analyzer, elemental analysis (%) calculated value is: C (52.22), H (5.84), Cl (6.42), N (5.08), O (30.44); Elemental analysis (%) ) found: C (...

Embodiment 3

[0064] Ingredients as follows:

[0065]

[0066] 1000 pieces are made

[0067] Preparation:

[0068] Raw materials were crushed through 80-mesh sieve, microcrystalline cellulose and amlodipine maleate hydrate crystals were mixed, and then mixed with losartan potassium, pregelatinized starch, low-substituted hydroxypropyl cellulose, carboxymethyl The sodium starch is mixed evenly, and then mixed with magnesium stearate for 5 minutes, the intermediate is tested, and the composition chip is obtained by direct tableting; the film coating is obtained.

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Abstract

The invention relates to an amlodipine and losartan potassium medicinal composition, which comprises the following components calculated according to weight part: 2.5-10 parts of amlodipine, 20-100 parts of losartan potassium, 5-20 parts of pregelatinized starch, 20-60 parts of microcrystalline cellulose, 15-40 parts of low substitution hydroxypropyl cellulose, 1-8 parts of carboxymethyl starch sodium and 1-3 parts of magnesium stearate. The amlodipine is an amlodipine maleate hydrate crystal with a molecular formula of C24H29ClN2O9.1.5H2O. The amlodipine maleate in the medicinal composition can be used for stably releasing the medicinal effect within 24 hours and stably and quickly taking effect. The medicinal composition has strong synergism, accumulation and complementary action and high bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to amlodipine and its medicinal composition with losartan potassium and a preparation method thereof. Background technique [0002] Losartan potassium, Chinese alias: 2-butyl-4-chloro-5-(hydroxymethyl)-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl ] Potassium imidazole, English name: Losartan potassium, molecular formula: C22H22CIKN6OK, molecular weight: 461.01, structural formula is as follows: [0003] [0004] Losartan potassium is a new type of non-peptide angiotensin II receptor (AT1) antagonist, which can lower blood pressure, improve heart failure, and prevent and treat hypertension complicated by thickening of blood vessel walls and cardiac hypertrophy. It has the effect of maintaining the kidneys, increasing renal blood flow, glomerular filtration rate, increasing the excretion of urine, urinary sodium and uric acid, and reducing the secretion of adrenal ald...

Claims

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Application Information

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IPC IPC(8): A61K31/4178A61K9/28A61K47/12A61P13/12A61P9/00A61K31/4422A61P9/04A61K47/38A61K47/36A61P9/12
Inventor 钟正明罗韬马鹰军王小树
Owner HAINAN JINRUI PHARMA
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