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Bevantolol hydrochloride orally disintegrating tablet

A technology of bevanolol hydrochloride and orally disintegrating tablets, which is applied in the field of bevanolol hydrochloride orally disintegrating tablets and its preparation, can solve the problem of not finding bevanolol hydrochloride orally disintegrating tablets and not being able to perform better Therapeutic effect, inability to play a quick-acting role, etc., to achieve the effect of improving bioavailability, good taste, and convenient administration

Active Publication Date: 2009-11-11
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

[0003] In the existing oral dosage form, it is ordinary tablet or capsule, and the method of taking it is 1 tablet at a time, twice a day, 100 mg each time, after oral administration of bevanolol, due to the first-pass effect, a part of It will be metabolized, resulting in a decrease in its bioavailability, which is about 60%, and its therapeutic effect cannot be better exerted, and when taking ordinary tablets or capsules, because of the long peak time, it cannot play a quick-acting effect
In addition, when taking ordinary tablets or capsules, it is necessary to use boiled water to deliver the medicine, which has certain difficulties for patients with dysphagia or inconvenient water intake, and is often very inconvenient; It can be used with the assistance of medical staff, which obviously cannot meet the needs of patients to take it by themselves, and the compliance is poor; for patients with high blood pressure or angina pectoris, they often hope to have a drug that is convenient to take and can reach the blood concentration in a short time and quickly recover. Therefore, it is particularly necessary to develop a preparation that reduces the first-pass effect as much as possible, has a rapid onset of action, and is beneficial to special populations and special environments.
[0004] However, in the prior art, there is no bevanolol hydrochloride orally disintegrating tablet

Method used

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  • Bevantolol hydrochloride orally disintegrating tablet
  • Bevantolol hydrochloride orally disintegrating tablet
  • Bevantolol hydrochloride orally disintegrating tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Recipe: 1000 tablets

[0048] Component Weight

[0049] Bevanolol Hydrochloride 50g

[0050] Citric acid 20g

[0051] Sodium bicarbonate 10g

[0052] Microcrystalline Cellulose 200g

[0053] Low-substituted hydroxypropyl cellulose 130g

[0054] Preparation process: Weigh bevanolol hydrochloride, citric acid, microcrystalline cellulose and 50 g of low-substituted hydroxypropyl cellulose according to the prescription, put them into a mixer and mix them evenly, add 7% ethanol solution as a binder, and stir Evenly, granulate with a 40-mesh sieve, ventilate and dry at 50°C±5°C, pass the dry granules through a 40-mesh sieve for granulation, add the remaining amount of low-substituted hydroxypropyl cellulose to the granules, mix well, take a sample for testing, and pass the test. Tablets, ready to use. After the finished product passes the inspection, it is double-aluminum packaged and assembled.

[0055] Test results of disintegration time limit of 6 samples in three b...

Embodiment 2

[0058] Recipe: 1000 tablets

[0059] Component Weight

[0060] Bevanolol Hydrochloride 100g

[0061] Citric acid 20g

[0062] Sodium bicarbonate 8g

[0063] Microcrystalline Cellulose 110g

[0064] Low-substituted hydroxypropyl cellulose 80g

[0065] Aspartame 40g

[0066] Micro Silica Gel 2g

[0067] Preparation process: Weigh bevanolol hydrochloride, citric acid, microcrystalline cellulose, and 40 g of low-substituted hydroxypropyl cellulose according to the prescription, put them into a mixer and mix them evenly, add 7% ethanol solution as a binder, Stir evenly, granulate with a 40-mesh sieve, ventilate and dry at 50°C±5°C, pass the dry granules through a 40-mesh sieve for granulation, add the remaining low-substituted hydroxypropyl cellulose and aspartame to the granules, and mix Evenly, add the micro silica gel into it, continue to mix, take a sample for testing, if it is qualified, press it into tablets, that is to say. After the finished product passes the inspe...

Embodiment 3

[0072] Recipe: 1000 tablets

[0073] Component Weight

[0074] Bevanolol Hydrochloride 200g

[0075] Citric acid 20g

[0076] Sodium bicarbonate 8g

[0077] Microcrystalline Cellulose 90g

[0078] Low-substituted hydroxypropyl cellulose 40g

[0079] Aspartame 20g

[0080] Micro Silica Gel 2g

[0081] Preparation process: Weigh bevanolol hydrochloride, citric acid, microcrystalline cellulose, and 20 g of low-substituted hydroxypropyl cellulose according to the prescription, put them into a mixer and mix them evenly, add 7% ethanol solution as a binder, Stir evenly, granulate with a 40-mesh sieve, ventilate and dry at 50°C±5°C, pass the dry granules through a 40-mesh sieve for granulation, add the remaining low-substituted hydroxypropyl cellulose and aspartame to the granules, and mix Evenly, add the micro silica gel into it, continue to mix, take a sample for testing, if it is qualified, press it into tablets, that is to say. After the finished product passes the inspec...

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Abstract

The invention relates to a bevantolol hydrochloride orally disintegrating tablet, which consists of a therapeutically effective amount of bevantolol hydrochloride, citric acid, sodium bicarbonate, microcrystalline cellulose, low-substituted hydroxypropyl cellulose and other pharmaceutically acceptable pharmaceutical excipients. The orally disintegrating tablet can be prepared by mixing the bevantolol hydrochloride, the citric acid, the microcrystalline cellulose and partial low-substituted hydroxypropyl cellulose evenly, taking 70 percent ethanol as an adhesive for pelletization, and then adding a residual amount of the low-substituted hydroxypropyl cellulose and other pharmaceutical excipients. The bevantolol hydrochloride orally disintegrating tablet can effectively solve the problem of low bioavailability of ordinary tablets due to first pass effect.

Description

technical field [0001] The invention relates to a bevanolol hydrochloride orally disintegrating tablet and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] β-blockers are the first-line drugs for the treatment of hypertension. Long-term treatment of hypertension with non-selective β-receptor blockers can cause dyslipidemia. Among selective β-receptor blockers, antihypertensive drugs that have little effect on blood lipids will receive more and more attention. 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 ha...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/138A61K47/38A61P9/12
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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