Compound anisodamine and neostigmine sustained-release tablet and preparation method thereof

A technology of anisodamine and neostigmine, applied in the field of compound anisodamine neostigmine sustained-release tablets and its preparation, can solve the problems of short half-life and inability to meet anti-inflammatory treatment, and reduce the peak concentration , large application value, and the effect of increased action time

Active Publication Date: 2016-09-21
无锡圆道医药科技研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the half-life of neostigmine methosulfate and 654-2 in the body is relatively short (the half-life of neostigmine methosulfate is 0.89 to 1.2 hours, and 654-2 is only 40 minutes), which cannot meet the needs of continuous anti-inflammatory treatment in the body. There are no research reports on compound sustained-release tablets of 654-2 and neostigmine at home and abroad

Method used

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  • Compound anisodamine and neostigmine sustained-release tablet and preparation method thereof
  • Compound anisodamine and neostigmine sustained-release tablet and preparation method thereof
  • Compound anisodamine and neostigmine sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1: Preparation of Compound Anisodamine Neostigmine Sustained Release Tablets

[0049] 1. The formula of sustained-release tablet (according to 1000 tablets): by weight, anisodamine 16.67 parts, neostigmine: 0.03 parts, HPMCK4M: 20 parts, magnesium stearate: 0.7 parts, polyvinylpyrrolidone K30: 15 parts, pregelatinized starch: 8 parts, microcrystalline cellulose: 39.6 parts.

[0050] 2. The preparation method of the sustained-release tablet:

[0051] (1) Raw material preparation: pass anisodamine, neostigmine, HPMC K4M, pregelatinized starch, and microcrystalline cellulose through a 100-mesh sieve for later use;

[0052] (2) Mixing: Mix the sieved anisodamine, neostigmine, HPMC K4M, pregelatinized starch, and microcrystalline cellulose for 30 minutes to make drug fine powder for later use;

[0053] (3) Wet granulation: Dissolve polyvinylpyrrolidone K30 in distilled water, mix with the above-mentioned drug fine powder, granulate with a 20-mesh nylon screen, a...

Embodiment 2

[0056] Embodiment 2: Preparation of Compound Anisodamine Neostigmine Sustained Release Tablets

[0057] 1. Prescription for sustained-release tablets (calculated as 1000 tablets): by weight, anisodamine: 16.67 parts, neostigmine: 0.03 parts, HPMCK4M: 15 parts, magnesium stearate: 0.7 parts, polyvinylpyrrolidone K30: 15 parts, pregelatinized starch: 8 parts, microcrystalline cellulose: 44.6 parts.

[0058] 2. The preparation method of the sustained-release tablet:

[0059] (1) Raw material preparation: pass anisodamine, neostigmine, HPMC K4M, pregelatinized starch, and microcrystalline cellulose through a 100-mesh sieve for later use;

[0060] (2) Mixing: Mix the sieved anisodamine, neostigmine, HPMC K4M, pregelatinized starch, and microcrystalline cellulose for 30 minutes to make drug fine powder for later use;

[0061] (3) Wet granulation: Dissolve polyvinylpyrrolidone K30 in distilled water, mix with the above-mentioned drug fine powder, granulate with a 20-mesh nylon scre...

Embodiment 3

[0064] Example 3: Research on the Dissolution of Anisodamine in Compound Anisodamine Neostigmine Sustained Release Tablets

[0065] Refer to the dissolution test method of anisodamine tablets ("Chinese Pharmacopoeia" 2015 edition), adopt the paddle method, use 900ml of 0.1mol / L hydrochloric acid solution as the dissolution medium, rotate at 50 rpm, and set the temperature at 37°C to measure the dissolution Dissolution after 1, 2, 4, 8, 10, 12 hours. The method is to take 10ml of the solution at each time point, filter, and supplement the dissolution medium with a 0.1mol / L hydrochloric acid solution with the same volume and temperature as the taken solution, accurately measure 20ul of the subsequent filtrate, inject it into the liquid chromatograph, and use octadecyl Silane-bonded silica gel was used as filler, 0.01mol / L potassium dihydrogen phosphate solution (containing 0.15% triethylamine, pH value adjusted to 6.5 with phosphoric acid)-methanol (70:30) was used as mobile phase...

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Abstract

The invention discloses a sustained-release tablet prepared by compounding anisodamine and neostigmine and a preparation method of the sustained-release tablet. The sustained-release tablet is prepared from the following components in parts by weight: 10-20 parts of the anisodamine, 0.01-1 part of the neostigmine, 5-50 parts of sustained-release matrix materials, 0.3-5 parts of a lubricant, 1-20 parts of an adhesive, 1-15 parts of a diluting agent, 1-50 parts of a disintegrating agents and 1-50 parts of a filling agent. The sustained-release tablet provided by the invention is smooth and steady in release; by taking the sustained-release tablet provided by the invention, dosing times are reduced, and cting time is increased; the compliance of a patient is improved; side effects caused by an overhigh peak concentrationh are lowered; the sustained-release tablet is simple in preparation process, relatively low in cost, easy to control and suitable for large-scale industrial production, and has relatively high application value.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a compound anisodamine neostigmine sustained-release tablet and a preparation method thereof. Background technique [0002] In recent years, foreign studies have found that the cholinergic anti-inflammatory pathway is a neurophysiological mechanism that regulates the immune system. The anti-inflammatory signal reaches the reticuloendothelial system such as the spleen, liver and gastrointestinal tract through the efferent fibers of the vagus nerve, and then the vagus nerve releases acetylcholine. Interact with the α7 nicotinic acetylcholine receptor (α7nAchR) on the surface of macrophages and other cytokine-secreting cells, inhibit the synthesis and release of inflammatory cytokines, control the inflammatory response, and prevent tissue damage. Our clinical studies and animal experiments in recent years have also confirmed that the simultaneous use of cholinesterase inhibitors (...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/46A61K31/27A61K9/22A61P29/00
CPCA61K9/0002A61K9/2054A61K9/2059A61K31/27A61K31/46
Inventor 顾万清周小莉
Owner 无锡圆道医药科技研究院有限公司
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