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Nux-vomica seed slow-released preparation and proless for preparing same

A technology of sustained-release preparations and Nuxe chinensis, applied in anti-inflammatory agents, pharmaceutical formulas, non-central analgesics, etc., can solve problems such as narrow safety range, achieve definite curative effect, simple preparation method, and less side effects

Inactive Publication Date: 2004-03-24
安徽省新药研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nuxychnium powder with different mesh numbers was used to investigate the release rate. The alkaloids were released in about 20 to 30 minutes, and the speed of release had little to do with the degree of pulverization of the powder (see Figure 1). The toxicity to the heart and central nervous system is more obvious, because its maximum effective dose E max and the minimum lethal dose L min The distance between them is small, and the safety range of this product is narrow

Method used

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  • Nux-vomica seed slow-released preparation and proless for preparing same
  • Nux-vomica seed slow-released preparation and proless for preparing same
  • Nux-vomica seed slow-released preparation and proless for preparing same

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0034] Example 1, preparation of Nuxychnium sustained-release tablet

[0035] (1) Take the following raw materials

[0036] Appropriate amount of alkaloid extract (each tablet contains strychnine gmg)

[0037] Hypromellose 150g

[0038] Sodium Carboxymethyl Cellulose 50g

[0039] Talc powder 100g

[0040] Lactose 50g

[0041] Stearic acid 30g

[0042] A total of 1000 pieces were made

[0043] (2) Production process

[0044] Grind Nuxychee into medium powder, add an appropriate amount of ammonia water, add 3 to 5 times the amount of chloroform, soak for 24 hours, and use a fat extractor to reflux extract for 3 to 5 hours; after the extract is concentrated to a suitable volume, add 3→ After extracting three times with 100% sulfuric acid, adjust the pH of the acid solution to 9-10, add chloroform for extraction three times, evaporate the chloroform to dryness, and obtain alkaloid powder; Mix blocker, diluent, etc., add wetting agent appropriate...

example 2

[0045] Example 2, preparation of Nuxychnium sustained-release granules

[0046] After the formula and technology of example 1 are used to make dry granules, granulate with 10 mesh and 14 mesh sieves, keep the part that can cross 10 mesh sieves and cannot cross 14 mesh sieves, after adding an appropriate amount of talcum powder, coating (coating material) 2% ethyl cellulose ethanol solution), the granules are prepared, packaged, and obtained. The finished product is tested for release rate, and the results are shown in the attached table.

[0047] The obtained slow-release granules can be mixed with corresponding quick-release granules prepared from other Chinese and Western medicine quick-release components to prepare compound sustained-release granules.

example 3

[0048] Example 3, preparation of nuxychnium sustained-release pellets and sustained-release capsules

[0049] (1) Take the following ball core raw materials

[0050] Alkaloid extract appropriate amount (each dose contains strychnine 8mg)

[0051] Hypromellose 50g

[0052] Starch 250g

[0053] (2) Take the following coating liquid raw materials

[0054] Ethyl cellulose 20 g

[0055] Polyethylene glycol 5 grams

[0056] Talc powder 50g

[0057] 95% ethanol 1000ml

[0058] Made a total of 1000 doses

[0059]The preparation method of sustained-release pellets: take an appropriate amount of extract powder (approximately equivalent to 8 grams of strychnine), add 20 milliliters of 95% ethanol, and ultrasonically dissolve it completely to obtain a spare solution; weigh 250 grams of starch, hydroxy Add 50 grams of propyl methylcellulose, after mixing evenly in equal amounts, use the spare solution as a wetting agent to make a soft material, p...

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PUM

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Abstract

The present invention adopts the proper extraction method to obtain nux vomica extract, adds retarding agent and diluting agent or utilizes modern coating technique to make the sustained release medication of nux vomica and its compound preparation, including slow-release tablet, slow-release granules, slow-release micropill and compound slow-release preparation. After the effective component of nux vomica is slowly released, it not only can improve compliance of patient, but also can retain proper therapeutic concentration and can reduce its toxic side effect.

Description

technical field [0001] The present invention relates to a kind of traditional Chinese medicine preparation and preparation method, specifically Nuxychnium sustained-release preparation and preparation method Background technique [0002] Acute LD of strychnine, strychnine and strychnine contained in the seeds of Nuxychnium fed to mice 50 3.27, 233.0 and 234.5mg / kg respectively; mice ip acute LD 50 1.53, 69.0 and 77.76 mg / kg respectively; LD of strychnine given to mice iv 50 8mg / kg. Adults who take 5-10mg of strychnine at one time can cause poisoning, and 30mg can cause death; 200mg / kg of strychnine suspension is administered to mice three times a day for 14 consecutive days, which can cause heart failure in mice. , liver, kidney and other organs have varying degrees of damage; it has been reported that diphtheria was treated with nuxychonzi, and poisoning was caused when the total dose reached 50.54mg; some people died or took it after taking Jiuzhuanhuishengdan (the main...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/52A61P15/00A61P29/00A61P43/00
Inventor 陈旭张继稳黄小枫
Owner 安徽省新药研究院
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