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Neostigmine bromide slow release preparation and its preparation method

A kind of bromine neostigmine and slow-release technology, which is applied in the field of bromine neostigmine sustained-release tablet and its preparation field, can solve the problems such as no research report of bromine neostigmine sustained-release tablet, and avoid instability Effect

Inactive Publication Date: 2012-12-26
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After consulting patents and literature, there is no research report on Bromyostigmine Sustained-release Tablets

Method used

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  • Neostigmine bromide slow release preparation and its preparation method
  • Neostigmine bromide slow release preparation and its preparation method
  • Neostigmine bromide slow release preparation and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] The tablet core is a skeleton tablet, including the following components, and its weight composition is as follows:

[0057] Neostigmine bromide 750 parts

[0058] HPMC K4M 2000 copies

[0059] Lactose 1000 parts

[0060] Magnesium stearate 3333 parts

[0061] Talc powder 145 parts

[0062] 125 parts of 95% ethanol solution

[0063] The prescription of coating solution I, coating solution I comprises following each component, and its weight composition is:

[0064] Cellulose acetate 250 parts

[0065] PEG6000 15 parts

[0066] Neostigmine Bromide 8 parts

[0067] Acetone 6667 parts

[0068] 1667 parts of absolute ethanol

[0069] The prescription of coating liquid II, coating liquid II comprises following each component, and its weight composition is:

[0070] 13 parts cellulose acetate

[0071] PEG6000 1 part

[0072] Acetone 417 parts

[0073] The preparation method comprises the following steps: (1) tablet core preparation: take by weighing neostigmine b...

Embodiment 2

[0076] The tablet core is a skeleton tablet, including the following components, and its weight composition is as follows:

[0077] Neostigmine bromide 700 parts

[0078] HPMC K15M 2000 copies

[0079] Lactose 1000 parts

[0080] Magnesium stearate 3000 parts

[0081] Talc powder 130 parts

[0082] 125 parts of 95% ethanol solution

[0083] The prescription of coating solution I, coating solution I comprises following each component, and its weight composition is:

[0084] Ethyl cellulose 250 parts

[0085] PEG4000 15 parts

[0086] Neostigmine Bromide 8 parts

[0087] The prescription of coating liquid II, coating liquid II comprises following each component, and its weight composition is:

[0088] 13 parts ethyl cellulose

[0089] PEG6000 1 part

[0090] Preparation method is basically the same as embodiment 1. The difference is that the coating is coated with an aqueous dispersion of the coating liquid.

Embodiment 3

[0092] The tablet core is a skeleton tablet, including the following components, and its weight composition is as follows:

[0093] Neostigmine bromide 650 parts

[0094] HPMC K100M 2000 copies

[0095] Lactose 1000 parts

[0096] Magnesium stearate 3000 parts

[0097] Talc powder 120 parts

[0098] 95% ethanol solution 110 parts

[0099] The prescription of coating solution I, coating solution I comprises following each component, and its weight composition is:

[0100] Cellulose acetate 210 parts

[0101] PEG6000 15 parts

[0102] Neostigmine bromide 5 parts

[0103] Acetone 6000 parts

[0104] 1500 parts of absolute ethanol

[0105] The prescription of coating liquid II, coating liquid II comprises following each component, and its weight composition is:

[0106] 13 parts cellulose acetate

[0107] PEG6000 1 part

[0108] Acetone 400 parts

[0109] Preparation method is basically the same as embodiment 1.

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Abstract

The present invention belongs to the technical field of medicinal preparation. The invention discloses a formula of a neostigmine bromide slow release preparation which can be taken once every day for treating myasthemia gravis, functional flatulence after being performed an operation and urinary retention, as well as its preparation method. The preparation is disclosed as a slow release tablet form composed of a skeleton core containing neostigmine bromide and the slow release preparation and a coating. The neostigmine bromide slow release preparation of the present invention is capable of overcoming the disadvantage of present medicament common tablets in the market, slowly releasing to keep stable blood and medicine concentration, acting for a longer period, possessing low toxicity andside effect and conveniently taking the preparation, and the slow release preparation keeps effective blood and medicine concentration for a long time, reduces the medicine taking frequency, raises the compliance of the patients and reduces the side-effect due to over peak concentration. The invention has the advantages of simple preparation technology, low cost, easy control and easy industrial production.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to bromiostigmine slow-release tablets and a preparation method thereof. Background technique [0002] Neostigmine bromide is a cholinesterase inhibitor, which can increase the concentration of acetylcholine at the nerve-muscle junction, effectively replace the molecules of non-depolarizing muscle relaxants from the posterior membrane, and make acetylcholine play the role of transmitter. Excitement conduction, thereby restoring muscle tension, is often used clinically to treat myasthenia gravis, postoperative functional flatulence and urinary retention. Oral peak time is 1 to 3 hours, and the average plasma half-life is 0.87 hours. The preparation on the domestic market is a common tablet of bromyostigmine, the specification is 15 mg per tablet, orally, and the usual dose is 15 mg (1 tablet) once. 3 times a day, the dosage of patients with myasthenia gravis depends on the condition. The drug...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K9/36A61K47/38A61K31/27A61P21/04A61P1/00A61P13/00
Inventor 张景勍罗文熊华蓉赵春景
Owner CHONGQING MEDICAL UNIVERSITY
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