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Medicinal composition comprising quick-release pellets containing Enalapril or Enalapril-acid addition salt and slow-release pellets containing Felodipine

A technology of enalapril and acid addition salts, which is applied in drug combinations, medical preparations containing active ingredients, drug delivery, etc., can solve the problem of no obvious advantage in target organ protection, insignificant curative effect, and no enalamic effect. Issues related to literature and patent reports of prifelodipine sustained-release pellets to achieve the effect of low-toxicity administration, uniform release, and rapid blood pressure stabilization

Active Publication Date: 2011-11-23
白云山威灵药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Enalapril was first developed by Merck Company of the United States, and it was launched in the Federal Republic of Germany in 1984. It was once one of the best-selling prescription drugs in the European and American markets, but sales began to decline after 2001. The main reasons are: The patent expires, countries imitate one after another, new products of the same kind appear continuously, and there are some problems: (1) The antihypertensive curative effect has a certain limit, and a large number of literature reports have a total effective rate of only about 60%, and 40% are ineffective or have no significant curative effect; ( 2) There is no obvious advantage in target organ protection
[0007] Through the search, there are no related literature and patent reports about enalapril and felodipine sustained-release pellets

Method used

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  • Medicinal composition comprising quick-release pellets containing Enalapril or Enalapril-acid addition salt and slow-release pellets containing Felodipine
  • Medicinal composition comprising quick-release pellets containing Enalapril or Enalapril-acid addition salt and slow-release pellets containing Felodipine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Enalapril and Felodipine Maleate Sustained-release Pellet Capsules (1000 formulations)

[0049] Ball core:

[0050] Felodipine 5g

[0051] Enalapril Maleate 5g

[0052] Microcrystalline Cellulose 160g

[0053] HPMC 30g

[0054] Purified water 200g

[0055] Sustained release coating ingredients (coating solution):

[0056] Ethylcellulose aqueous dispersion 250g

[0057] Add purified water to 1000ml

[0058] Ordinary outer coating ingredients (ordinary coating solution):

[0059] Opadry 15g

[0060] Add purified water to 1000ml

[0061] (1) Felodipine pills are prepared: Felodipine, microcrystalline cellulose, and HPMC are passed through an 80-mesh sieve respectively, and felodipine is mixed with 100g microcrystalline cellulose and 35g HPMC, and the soft material is added to the purified water system. Extrude strips with a 20-mesh aperture and a length of about 3-5cm, adjust the rotation speed of the bottom turntable to 800-1000rpm, round for about 3-5...

Embodiment 2

[0065] Example 2 Enalapril, Felodipine Maleate Sustained-release Pellet Capsules (1000 formulations)

[0066] Ball core:

[0067] Felodipine 2.5g

[0068] Enalapril Maleate 25g

[0069] Sucrose 50g

[0070] Microcrystalline Cellulose 400g

[0071] HPMC 10g

[0072] Purified water 300g

[0073] Sustained release coating ingredients (coating solution):

[0074] Ethylcellulose aqueous dispersion 250g

[0075] Add purified water to 1000ml

[0076] Ordinary outer coating ingredients (ordinary coating solution):

[0077] Opadry 15g

[0078] Add purified water to 1000ml

[0079] Preparation:

[0080] (1) Preparation of blank cores: Prepare blank cores by centrifugal granulation: take 300g of microcrystalline cellulose and place them in a centrifugal granulator, use purified water as a binder to prepare mother cores, dry, and sieve for 50- 60-mesh pellet core for standby;

[0081](2) Felodipine pills were prepared by loading blank pellet cores: Felodipine and 40 g of mic...

Embodiment 3

[0085] Example 3 Enalapril, Felodipine Maleate Sustained-release Pellet Capsules (1000 formulations)

[0086] Ball core:

[0087] Felodipine 25g

[0088] Enalapril Maleate 2.5g

[0089] Octadecanol 60g

[0090] PVP 12g

[0091] Microcrystalline Cellulose 150g

[0092] 0.5% HPMC aqueous solution 200g

[0093] Ordinary outer coating ingredients (ordinary coating solution):

[0094] Opadry 10g

[0095] Purified water 450g

[0096] (1) Felodipine sustained-release pellets are prepared: Felodipine is passed through an 80 mesh sieve, added to molten stearyl alcohol and stirred evenly, then added PVP and mixed uniformly, cooled and solidified, and ground into fine powder, and mixed with 60g microcrystalline cellulose Mix evenly, use 0.5% HPMC aqueous solution to make soft materials, extrude strips with a diameter of 14-20 mesh and a length of about 3-5 cm, adjust the rotation speed of the bottom turntable to 800-1000 rpm, roll into a ball for about 3-5 minutes, dry, and set a...

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PUM

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Abstract

The invention relates to a medicinal composition containing Enalapril or Enalapril-acid addition salt and Felodipine, prepared by putting slow-release pellets containing Felodipine and quick-release pellets containing Enalapril or Enalapril-acid addition salt in capsules. Each dosage unit of the medicinal composition contains 2.5-25mg of Enalapril maleate and 2.5-25mg of Felodipine. The medicinal composition can stabilize blood pressure quickly, and keep effective blood concentration for 24 hours, with increasing patient compliance. The medicinal composition is administered only once a day.

Description

technical field [0001] The present invention relates to a pharmaceutical composition preparation for treating hypertension, in particular to an immediate-release pellet containing enalapril or enalapril-acid addition salt and a sustained-release pellet containing felodipine The pharmaceutical composition preparation of the pill part belongs to the technical field of medicine. Background technique [0002] Enalapril is an angiotensin-converting enzyme (ACE) inhibitor. After oral administration, it is hydrolyzed into dicarboxylic acid enalaprilat in the liver, which strongly inhibits angiotensin-converting enzyme, reduces the content of angiotensin II, and causes systemic vascular Diastole, blood pressure drops. The usual dose is 5-10 mg, and it must be injected intravenously in order to speed up the onset time. The medicine treats moderate or severe hypertension, and the dose must be increased to 80mg / day, and only about 60% of hypertensive patients can be effective when us...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K31/40A61K9/52A61P9/12
Inventor 朱少璇廖颂明卢丹王健松邹瑜邢盛
Owner 白云山威灵药业有限公司
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