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Aescin b enteric-coated sustained-release pellets and preparation method thereof

A technology of aescin and sustained-release pellets, which can be used in microcapsules, pharmaceutical formulas, medical preparations of non-active ingredients, etc., and can solve problems such as gastrointestinal discomfort, difficult quality control, and complex components of sodium aescinate

Active Publication Date: 2021-05-04
WUHAN AIMIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the short half-life of sodium aescinate, the number of times of taking it is high, and it needs to be taken 2-3 times a day. At the same time, because the composition of sodium aescinate is complex and contains a variety of other saponins, the quality of this product is difficult to control, and gastrointestinal problems often occur. Road discomfort and other adverse reactions

Method used

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  • Aescin b enteric-coated sustained-release pellets and preparation method thereof
  • Aescin b enteric-coated sustained-release pellets and preparation method thereof
  • Aescin b enteric-coated sustained-release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1. Prepare the sustained-release pellet core, the prescription is as follows:

[0027] ingredients effect Dosage (g) ％ Aescin B active ingredient 150 15 lactose filler 500 50 Hydroxypropylmethylcellulose Slow-release matrix material 240 24 carbomer Slow-release matrix material 60 6 polyethylene glycol 4000 porogen 50 5

[0028] 1) Weigh lactose, hydroxypropyl methylcellulose, carbomer, and polyethylene glycol 4000, pass through a 100-mesh sieve, and mix well;

[0029] 2) Weigh aescin B, dissolve it with 40% ethanol, add it to the above powder and stir to make a soft material;

[0030] 3) Extrude the soft material at a speed of 50r / min through a sieve with a diameter of 0.5mm in the extruder, then roll it in a spheronizer at a speed of 600r / min for 10min, and finally dry it at 50°C for 3h. After sieving, take 20-30 mesh pellets.

[0031] 2. Preparation of enteric-coated sustained-release pellets:

[0032] ...

Embodiment 2

[0036] 1. Prepare the sustained-release pellet core, the prescription is as follows:

[0037] ingredients effect Dosage (g) ％ Aescin B active ingredient 100 10 microcrystalline cellulose filler 400 40 Hydroxypropylmethylcellulose Slow-release matrix material 400 40 polyethylene glycol 4000 porogen 100 10

[0038] 1) Weigh microcrystalline cellulose, hydroxypropyl methylcellulose, and polyethylene glycol 4000, pass through a 100-mesh sieve, and mix uniformly;

[0039] 2) Weigh aescin B, dissolve it with 50% ethanol, add it to the above powder and stir to make a soft material;

[0040] 3) Extrude the soft material through a 0.4mm sieve in the extruder at a speed of 30r / min, then roll it in a spheronizer at a speed of 1000r / min for 5min, and finally dry it at 45°C for 5h. After sieving, take 20-30 mesh pellets.

[0041] 2. Preparation of enteric-coated sustained-release pellets:

[0042] 1) Prepare the coating material, the...

Embodiment 3

[0046] 1. Prepare the sustained-release pellet core, the prescription is as follows:

[0047] ingredients effect Dosage (g) ％ Aescin B active ingredient 120 12 sucrose filler 250 25 dextrin filler 50 5 carbomer Slow-release matrix material 500 50 polyethylene glycol 6000 porogen 80 8

[0048] 1) Weigh sucrose, dextrin, carbomer, and polyethylene glycol 6000, pass through a 100-mesh sieve, and mix well;

[0049] 2) Weigh aescin B, dissolve it with 50% ethanol, add it to the above powder and stir to make a soft material;

[0050] 3) The soft material is extruded in the extruder at a speed of 60r / min through a sieve with a hole diameter of 0.5mm, then rolled in a spheronizer at a speed of 400r / min for 12min, and finally dried at 60°C for 1h. After sieving, take 20-30 mesh pellets.

[0051] 2. Preparation of enteric-coated sustained-release pellets:

[0052] 1) Prepare the coating material, the prescription is as fo...

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Abstract

The invention discloses a escin B enteric-coated sustained-release pellet, belonging to the field of pharmaceutical preparations, which consists of a sustained-release pellet core and an enteric coating material coated on the sustained-release pellet core. The release pellet core is composed of the following components by weight: escin B 10-20%, filler 30-60%, slow-release matrix material 20-50%, and porogen 2-10%. The invention cannot be absorbed in the stomach, but can only be absorbed in the intestinal tract, thereby reducing the irritation to the stomach, reducing adverse reactions, improving bioavailability and reducing the number of administrations.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a escin B enteric-coated sustained-release pellet and a preparation method thereof. Background technique [0002] Sodium aescinin is a sodium aescinate salt extracted from the dried mature seeds of Aesculus Wilsonii Rehd. Sodium aescinate can reduce the increase of pathological capillary permeability, increase venous tension, reduce the exudation of inflammatory substances, have anti-inflammation, detumescence, pain relief, improve blood circulation, and promote the recovery of acute closed soft tissue injury. It is proved that the main active ingredients in aescin are aescin B, B, C, D, wherein aescin B and B are β-type aescin, and the two are isomers of each other, molecular formula: C 55 h 85 o 24 Na has a molecular weight of 1153.24 and a half-life of 1.5 hours. [0003] Sodium aescinate tablets currently on the market are mainly used clinically for ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/58A61K31/704A61K47/38A61K47/32A61P29/00A61P7/10
CPCA61K9/0002A61K9/5026A61K31/704A61K47/32A61K47/38
Inventor 石召华叶利春张晓存沈倩颖吴灯江强
Owner WUHAN AIMIN PHARMA