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Oral sustained release hypotensive composition

A composition and slow-release technology, which can be applied in the direction of drug combination, active ingredients of heterocyclic compounds, drug delivery, etc., can solve the problem of high treatment cost

Active Publication Date: 2009-12-02
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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  • Oral sustained release hypotensive composition
  • Oral sustained release hypotensive 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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Abstract

The invention relates to a hypotensive compound preparation consisting of bevantolol or pharmaceutical salt thereof and enalapril or pharmaceutical salt thereof, wherein in the preparation, the enalapril or the pharmaceutical salt thereof is a fast release part, and the bevantolol or the pharmaceutical salt thereof is a sustained release part. The compound preparation, for moderate and severe hypertension patients, has strong hypotensive effect, sustained action, convenient administration for patients, and accurate dosage.

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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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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