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Pharmaceutical composition of amlodipine and telmisartan and preparation method of pharmaceutical composition

A technology of telmisartan and amlodipine, which is applied in the field of medicine, can solve the problems of reducing the bioavailability of pharmaceutical compositions, high degree of equipment dependence, and high difficulty of control, and achieve enhanced bioavailability, obvious antihypertensive effect, Accelerated absorption effect

Active Publication Date: 2012-01-25
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] WO2006048208, CN101052381, and CN102058591 disclose double-layer tablets containing telmisartan and amlodipine. Telmisartan and amlodipine are separated into different sheets. This preparation method is complex and requires a lot of equipment. High degree of dependence, the entire tableting process needs to control the pressure of the first sheet and the second sheet separately, and the control range is small, so the control is difficult and the tableting yield is low.
In addition, due to the large investment in hardware such as equipment, the production cost of the method is directly high.
And unresolved amlodipine drug slow onset of action, and the time gap between the peak blood concentration of telmisartan, the synergy is weak, which reduces the bioavailability of the medicinal composition in the human body
[0010] In order to ensure the bioavailability of telmisartan, the telmisartan preparation must include alkaline material components, and when amlodipine maleate is in an alkaline environment, the ester bond in the molecule is unstable, so it is directly combined with The method of excipient mixing cannot be applied to the combination preparation of telmisartan and amlodipine maleate

Method used

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  • Pharmaceutical composition of amlodipine and telmisartan and preparation method of pharmaceutical composition
  • Pharmaceutical composition of amlodipine and telmisartan and preparation method of pharmaceutical composition
  • Pharmaceutical composition of amlodipine and telmisartan and preparation method of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] 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.

[0049] Adopt U.S. Perkin-Elmer company PE2400II 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 (52.2...

Embodiment 2

[0053] 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.

[0054] Adopt U.S. Perkin-Elmer company PE2400II 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 (52....

Embodiment 3

[0058] The raw and auxiliary materials are respectively crushed through an 80-mesh sieve, 40 parts by weight of telmisartan, 0.1 parts by weight of sodium bicarbonate, 20 parts by weight of microcrystalline cellulose, 28 parts by weight of hydroxypropyl cellulose and 38 parts by weight of lactose are added to water to make a soft material , centrifuged to make pellets, dried in a fluidized bed dryer, film-coated to make telmisartan pellets, intermediate inspection; and then according to the following prescription ingredients:

[0059]

[0060] 1000 pieces are made

[0061] Mix microcrystalline cellulose and amlodipine maleate hydrate crystals, then mix them with telmisartan pellets, compressible starch, low-substituted hydroxypropyl cellulose, and cross-linked polyvinylpyrrolidone, and then mix them with Magnesium stearate was mixed for 5 minutes, the intermediate was inspected, and the tablet was obtained.

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Abstract

The invention relates to a pharmaceutical composition of amlodipine and telmisartan; the pharmaceutical composition comprises amlodipine, telmisartan and a pharmaceutically acceptable carrier; the pharmaceutical composition contains 2.5-10 parts by weight of amlodipine and 20-80 parts by weight of telmisartan; the amlodipine is an amlodipine maleate hydrate crystal. The molecular formula of the amlodipine maleate hydrate crystal is C24H29C1N2O91.5H2O. The amlodipine in the pharmaceutical composition acts quickly and stably, and the pharmaceutical effect can be stably released within 24 h; andthe pharmaceutical composition has strong cooperation, accumulation and complementation, and high bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a crystal of amlodipine maleate hydrate, a pharmaceutical composition thereof with telmisartan and a preparation method thereof. Background technique [0002] Telmisartan, Chinese alias: 4-{[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-yl]methyl}link Phenyl-2-carboxylic acid, molecular formula: C 33 h 30 N 4 o 2 , molecular weight: 514.62. Telmisartan is a new type of antihypertensive drug, which is a specific angiotensin II receptor (AT type I) antagonist. Telmisartan substitutes for the angiotensin II receptor and binds with high affinity to the AT I receptor subtype (the known site of action of angiotensin II). Telmisartan does not have any partial agonist effect at the ATI receptor site, and Telmisartan selectively binds to the ATI receptor, and the binding effect is long-lasting. Telmisartan has no affinity for other receptors, includin...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K31/4184A61P9/12
Inventor 罗韬钟正明马鹰军王小树
Owner HAINAN JINRUI PHARMA
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