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A kind of oral sustained-release antihypertensive composition

A technology of composition and sustained release agent, which is applied in the field of antihypertensive compound drugs, and can solve the problem of high treatment cost

Inactive Publication Date: 2012-02-08
北京化药科创医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, bevanolol and enalapril that exist in the market are both unilateral antihypertensive preparations, and the times of taking are both twice a day. For a good effect of controlling blood pressure drop, two different preparation units need to be taken at the same time. When taking it, the dosage of each preparation must be kept in mind at all times, which brings a lot of inconvenience to the patient. Taking it twice a day costs a lot of money. higher

Method used

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  • A kind of oral sustained-release antihypertensive composition
  • A kind of oral sustained-release antihypertensive composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Prescription of bevanolol sustained-release tablets (content per tablet)

[0039] Bevanolol 100.0mg

[0040] Hydroxypropyl methylcellulose 105.0mg

[0041] Starch 100.0mg

[0042] Povidone 18.0mg

[0043] Stearic acid 7.0mg

[0044] Micro Silica Gel 2.0g

[0045] 70% ethanol appropriate amount

[0046] Total weight 332mg

[0047] Enalapril immediate-release tablet prescription (content per tablet)

[0048] Enalapril 2.5mg

[0049] Cross-linked polyvinylpyrrolidone 30mg

[0050] Microcrystalline Cellulose 55mg

[0051] Povidone 10mg

[0052] Micro silica gel 2.5mg

[0053] 70% ethanol appropriate amount

[0054] Total weight 100mg

[0055] Take bevanolol and enalapril and pass through a 100-mesh sieve respectively, starch, microcrystalline cellulose, hydroxypropyl methylcellulose, povidone and stearic acid respectively pass through a 100-mesh sieve, set aside, prepare 1000 samples Prescription amount, take the prescription amount of bevanolol, hydroxypropyl...

Embodiment 2

[0057] The operation of Example 1 was repeated except that the amounts of the components were changed to obtain compressed bilayer tablets.

[0058] Prescription of bevanolol sustained-release tablets (content per tablet)

[0059] Bevanolol hydrochloride 50.0mg, ethyl cellulose 80.0mg, lactose 150.0mg, povidone 18.0mg, magnesium stearate 2.0g, acetone amount, total weight 300.0mg

[0060] Enalapril immediate-release tablets

[0061] Enalapril maleate 5.0 mg, low-substituted hydroxypropyl cellulose 40.0 mg, lactose 40.0 mg, povidone 8 mg, magnesium stearate 2.0 mg, 70% ethanol in appropriate amount, total weight 100.0 mg.

Embodiment 3

[0063] The operation of Example 1 was repeated except that the amounts of the components were changed to obtain compressed bilayer tablets.

[0064] Prescription of bevanolol sustained-release tablets (content per tablet)

[0065] Bevanolol Hydrochloride 200.0mg, Xanthan Gum 100.0mg, Stearic Acid 10.0mg, Magnesium Stearate 2.0g, 30% ethanol in proper amount, total weight 312.0mg

[0066] Enalapril immediate-release tablets

[0067] Enalapril maleate 2.5mg, polyvinylpyrrolidone 50.0mg, lactose 40.0mg, povidone 6.5mg, magnesium stearate 1.0mg, 70% ethanol amount, total weight 100.0mg.

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PUM

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Abstract

The present invention relates to an antihypertensive compound preparation consisting of bevanolol or its pharmaceutically acceptable salt and enalapril or its pharmaceutically acceptable salt, wherein in the prepared preparation, enalapril or its pharmaceutically acceptable The salt is the immediate-release part, and the bevanolol or its pharmaceutically acceptable salt is the sustained-release part. The compound preparation of the present invention has a strong and long-lasting antihypertensive effect on patients with moderate to severe hypertension, and is convenient for patients to take and has an accurate dose.

Description

technical field [0001] The invention relates to a compound antihypertensive drug, which belongs to the technical field of pharmaceutical preparations. Background technique [0002] Bevanolol and enalapril are currently commonly used drugs for the treatment of hypertension, and their respective mechanisms of action are different. Bevantolol (bevantolol) is a relatively new fat-soluble selective β1-receptor blocker developed by the Warner-Lambert Company of the United States. It has no intrinsic sympathomimetic activity because it can block α-receptors and calcium ions channels, and thus have a mild vasodilator effect. The bioavailability of bevanolol is 60%, the peak time is about 1-2 hours, and the plasma half-life is about 1.5 hours, and its metabolite 4-hydroxyl bevanolol has antihypertensive activity (McNeil JJ, Drummer OH , Anderson AI, et al. Pharmacokinetics and concentration-effect relationships of bevantolol (CI-775) in normal volunteers [J]. JCandiovasc Pharmacol,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/40A61K31/138A61P9/12A61K9/24A61K9/52
Inventor 关屹闫冬
Owner 北京化药科创医药科技发展有限公司
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