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Matrine sustained releasing agent and its preparing process

A technology of matrine and slow-release preparations, applied in the field of matrine slow-release preparations and its preparation technology, can solve the problems of enhanced drug toxicity, increased blood drug concentration, and low blood drug concentration, so as to reduce drug intake The number of times, the blood drug concentration is stable, and the effect of reducing toxic and side effects

Inactive Publication Date: 2003-09-03
宁夏元康投资有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, matrine preparations on the market mainly include injections, infusions, quick-release capsules and tablets. However, due to the excellent water solubility of matrine, it is not easy to control the release rate. Inside, the blood drug concentration is very low, and then released quickly, so that the blood drug concentration in the body suddenly rises, and an obvious peak appears, as shown in Table 1, thereby enhancing the toxic and side effects of the drug
At the same time, from the perspective of therapeutic compliance, patients often forget to take medicines during the day when ordinary preparations are taken three times a day, and taking medicines three times a day should be administered once every minute or hour in theory, but in practice it is very difficult. The time interval between the three times is short, and the time from taking the medicine at night to the morning is long, resulting in low blood drug concentration in the morning and early morning, and the drug's efficacy is not stable.
Therefore, the use of existing dosage forms is far from being suitable for clinical needs, and the development of sustained-release preparations once or twice a day is adapted to the needs of the current medical market.

Method used

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  • Matrine sustained releasing agent and its preparing process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] prescription:

[0042] Matrine 150g

[0043] 50g microcrystalline cellulose

[0044] 50g pregelatinized starch

[0045] Hydroxypropyl Methyl Cellulose 245g

[0046] Magnesium Stearate 4.9g

[0047] 80% 7 Alcohol Appropriate amount,

[0048] Preparation: Grind the prescribed amount of the drug, microcrystalline cellulose, pregelatinized starch, hydroxypropyl methylcellulose, and magnesium stearate, sieve, mix well, and use an appropriate amount of 80% ethanol as a wetting agent to soften Material, granulated with 20 mesh sieve, dried at 50±5°C for wet granules, sized with 18 mesh sieve, mixed with dry granules plus lubricant, and then compressed into tablets. Embodiment 2 prescription:

Embodiment 2

[0048] Preparation: Grind the prescribed amount of the drug, microcrystalline cellulose, pregelatinized starch, hydroxypropyl methylcellulose, and magnesium stearate, sieve, mix well, and use an appropriate amount of 80% ethanol as a wetting agent to soften Material, granulated with 20 mesh sieve, dried at 50±5°C for wet granules, sized with 18 mesh sieve, mixed with dry granules plus lubricant, and then compressed into tablets. Embodiment 2 prescription:

[0049] Matrine 60g

[0050] 30g microcrystalline cellulose

[0051] 20g pregelatinized starch

[0052] Sodium hydroxymethylcellulose 150g

[0053] Magnesium stearate 6 g

[0054] An appropriate amount of 80% ethanol, the preparation process is the same as in Example 1.

Embodiment 3

[0055] Embodiment 3 prescription:

[0056] Matrine 550g

[0057] 100g microcrystalline cellulose

[0058] 30g pregelatinized starch

[0059] Hydroxypropyl Methyl Cellulose 450g

[0060] Al-Mg raw powder 8g

[0061] An appropriate amount of 40% 7-alcohol, the preparation process is the same as in Example 1.

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Abstract

A slowly releasing kurarinol in the form of tablet is prepared from kurarinol, diluent, adhesive and lubricant through pulverizing, proportional mixing, adding alcohol to prepare soft material, sieving by 20 meshes, drying at 50+ / -5 deg.C, sieving by 18 meshes, mixing with lubricant, and tabletting. Its advantages are balanced concentration in blood, durable action and low by-effect.

Description

technical field [0001] The invention relates to a new pharmaceutical dosage form of matrine, in particular to a slow-release agent of matrine and a preparation process thereof. Background technique [0002] Kushensu is an active ingredient extracted from the traditional Chinese medicine Sophora alopecuroides L or Sophoraflavescens Ait, which contains more than 98% of oxymatrine. Pharmacological and clinical studies have shown that Kushen Ginseng has the functions of anti-tumor, antibacterial, anti-virus, improving liver function, preventing liver fibrosis, reducing transaminase, and improving immunity of the body. After taking matrine, the replication level of hepatitis B virus in the infected cells in the body decreased significantly Quantitative detection of genes), alanine aminotransferase and bilirubin in patients with chronic hepatitis B recovered to normal rate reached 81.6% and 69.9% respectively. Therefore, matrine has been identified as a key promotional engineerin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/4375A61P1/16A61P31/12
Inventor 何仲贵李磊杨亚军
Owner 宁夏元康投资有限公司