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Medicament composition comprising Enalapril quick-releasing part and felodipine slow-releasing part

A technology of enalapril and sustained-release part, which is applied in the directions of drug combination, drug delivery, medical preparations containing active ingredients, etc. Insignificant and other problems, to achieve the effect of strong patient compliance, less adverse reactions, and rapid stabilization of blood pressure

Active Publication Date: 2010-09-29
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
[0005] The two drugs have been widely used in the treatment of cardiovascular diseases. There are domestic reports on compositions and preparation methods containing dihydropyridine calcium antagonists and angiotensin-converting enzyme inhibitors (see CN101548973), but the patent uses The two kinds of excipients are used as the sustained-release matrix, and a more complicated process must be adopted. Organic solvents must be used in the coating process, which has high production costs and is not conducive to large-scale production and environmental protection.

Method used

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  • Medicament composition comprising Enalapril quick-releasing part and felodipine slow-releasing part
  • Medicament composition comprising Enalapril quick-releasing part and felodipine slow-releasing part
  • Medicament composition comprising Enalapril quick-releasing part and felodipine slow-releasing part

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: Enalapril and felodipine sustained-release tablets (1000 formulations)

[0042] Chip:

[0043] Felodipine 2.5g

[0044] HPMC65g

[0045] Lactose 200g

[0046] Talc powder 2g

[0047] 95% ethanol solution 180g

[0048] Immediate release coating layer prescription (for preparing coating solution):

[0049] Enalapril Maleate 2.5g

[0050] Opadry 50g

[0051] Purified water 1000g

[0052] Prescription of protective layer (prepared as coating solution):

[0053] Opadry 50g

[0054] Purified water 1000g

[0055] Preparation:

[0056] Felodipine and HPMC were passed through a 100-mesh sieve, and lactose and talcum powder were passed through a 80-mesh sieve. Raw materials (i.e. the drug felodipine) / excipients are mixed evenly, and then the soft material is made with an appropriate amount (that is, the amount given above) of ethanol solution, granulated with a 16-mesh sieve, dried, granulated with a 18-mesh sieve, added with talcum powder and mixed even...

Embodiment 2

[0057] Embodiment 2: Enalapril and felodipine sustained-release tablets (1000 formulations)

[0058] Chip:

[0059] Felodipine 5g

[0060] HPMC 50g

[0061] Lactose 100g

[0062] Microcrystalline Cellulose 55g

[0063] Magnesium Stearate 2g

[0064] Hydrogenated Castor Oil 5g

[0065] povidone k 30 6g

[0066] 95% ethanol solution 120g

[0067] Purified water 15g

[0068] Immediate release coating formulation:

[0069] Enalapril Maleate 5g

[0070] Opadry 10g

[0071] Purified water 200g

[0072] Protective Layer Prescription:

[0073] Opadry 10g

[0074] Purified water 200g

[0075] Preparation:

[0076] Felodipine and HPMC were passed through a 100-mesh sieve, and microcrystalline cellulose, lactose, povidone k30, and magnesium stearate were passed through a 80-mesh sieve. After the raw / excipient materials are mixed evenly, use an appropriate amount (that is, the amount given above) to make soft materials with ethanol solution, granulate with a 16-mesh sieve,...

Embodiment 3

[0077] Embodiment 3: Enalapril and felodipine sustained-release tablets (1000 formulations)

[0078] Chip:

[0079] Felodipine 10g

[0080] HPMC 80g

[0081] Lactose 60g

[0082] Microcrystalline Cellulose 70g

[0083] Silica 2g

[0084] Magnesium Stearate 1g

[0085] 95% ethanol solution 150g

[0086] Purified water 40g

[0087] Immediate release coating formulation:

[0088] Enalapril Maleate 10g

[0089] Opadry 20g

[0090] Purified water 400g

[0091] Protective Layer Prescription:

[0092] Opadry 5g

[0093] Purified water 200g

[0094] Preparation:

[0095] Felodipine and HPMC were passed through a 100-mesh sieve, and microcrystalline cellulose, lactose, silicon dioxide, and magnesium stearate were passed through a 80-mesh sieve. After the raw materials / auxiliary materials are evenly mixed, use an appropriate amount of ethanol solution to make a soft material, granulate with a 16-mesh sieve, dry, granulate with a 18-mesh sieve, add magnesium stearate and sil...

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PUM

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Abstract

The invention relates to a medicament composition preparation comprising an Enalapril quick-releasing part and a felodipine slow-releasing part. The medicament composition is a medical composition formed by mixing Enalapril and felodipine as medical active components with and pharmaceutically acceptable auxiliary materials. The composition preparation comprising comprises a slow-releasing part tablet core and a quick-releasing part coating, wherein the slow-releasing part tablet core is the felodipine, and the quick-releasing part coating is the Enalapril or Enalapril-acid addition salts. Thecomposition can rapidly stabilize blood pressure and permanently keep the blood pressure steady.

Description

technical field [0001] The invention relates to a pharmaceutical composition preparation for treating hypertension, in particular to an immediate-release part coating layer containing enalapril or enalapril-acid addition salt and a sustained-release part containing felodipine The pharmaceutical composition preparation of tablet core 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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K9/30A61P9/12A61K31/4422
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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