Drug sustained and controlled release microparticle preparation for treating intestinal diseases, and preparation method thereof

A technology for intestinal diseases and drugs, which is applied in the field of sustained and controlled release pellets or granule preparations and the preparation of the above slow and controlled release pellets or granule preparations. Compliance, reducing the number of doses taken, and ensuring the effect of uniformity

Active Publication Date: 2012-01-18
PIVOT PHARMA TECH SHANGHAI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the general preparation production process, it is difficult to ensure that the sustained-release polymer material is evenly mixed with the main drug and other excipients, thus easily affecting the release effect of the drug and affecting the quality of the drug
[0006] The Chinese patent whose patent number is CN00808889.6 also has the above-mentioned defects, and cannot achieve the purpose of intestinal localized release; and improving the drug loading capacity; and the content disclosed in the patent of CN200480010790.6

Method used

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  • Drug sustained and controlled release microparticle preparation for treating intestinal diseases, and preparation method thereof
  • Drug sustained and controlled release microparticle preparation for treating intestinal diseases, and preparation method thereof
  • Drug sustained and controlled release microparticle preparation for treating intestinal diseases, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Prescription with pill core:

[0040] 1 mesalazine 750g

[0041] 2 microcrystalline cellulose 195g

[0042] blank core

[0043] 3 povidone 45g

[0044] 4 water to taste

[0045] Preparation method of ball core: Take the above ingredients 1, 3, and 4 of the drug-containing pill core prescription and stir them evenly to prepare a suspension with a solid content of 10-20% for later use; put the blank core of component 2 into the coating equipment and preheat When the bed temperature is higher than 35°C, pump the suspension of the drug until the end, rinse the container and pipeline with a small amount of water, and dry to obtain a qualified immediate-release drug-containing pellet core.

[0046] Coating prescription:

[0047] 1 povidone 20.0g

[0048] 2 Talc powder 7.5g

[0049] 3 water 270g

[0050] 4 Ethyl cellulose 20.0g

[0051] 5 Talc powder 2.5g

[0052] 6 water 175g

[0053] 7 Methacrylic acid 215.0g

[0054] and methacrylic

[0055] Acid methy...

Embodiment 2

[0061] Prescription with pill core:

[0062] 1 mesalazine 750g

[0063] 2 microcrystalline cellulose 195g

[0064] 3 povidone 45g

[0065] 4 magnesium stearate 10g

[0066] 5 water as appropriate

[0067] Preparation method of pellet core: Take the above components and mix thoroughly, use different types of mixing equipment or high-shear wet granulator, and then add appropriate amount of water to prepare soft material. The obtained soft material is further extruded and granulated, and then spheronized with a spheronizer to obtain a wet pellet core of a suitable size. The pellet core is further dried and sieved to obtain a qualified drug-containing immediate-release pellet core.

[0068] Coating prescription:

[0069] 1 povidone 25.0g

[0070] 2 Talc powder 8.0g

[0071] 3 water 270g

[0072] 4 Ethylcellulose 16.9g

[0073] 5 Talc powder 4.1g

[0074] 6 water 185.0g

[0075] 7 Methacrylic acid 150g

[0076] and acrylic acid

[0077] Ester 1:1 Copolymer

[00...

Embodiment 3

[0085] Prescription with pill core:

[0086] 1 mesalazine 950g

[0087] 2 microcrystalline cellulose 40g

[0088] 3 hypromellose 5g

[0089] white

[0090] 4 magnesium stearate 5g

[0091] 5 water as appropriate

[0092] Preparation method of pellet core: Take the above components and mix thoroughly, use different types of mixing equipment or high-shear wet granulator, and then add appropriate amount of water to prepare soft material. The obtained soft material is further extruded and granulated, and then spheronized with a spheronizer to obtain a wet pellet core of a suitable size. The pellet core is further dried and sieved to obtain a qualified drug-containing immediate-release pellet core.

[0093] Coating prescription:

[0094] 1 povidone 15.0g

[0095] 2 Talc powder 7.5g

[0096] 3 water 210g

[0097] 4 Ethylcellulose 15.9g

[0098] 5 Talc powder 2.1g

[0099] 6 water 165g

[0100] 7 Methacrylic acid 250g

[0101] and methacrylic

[0102] Acid meth...

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Abstract

The present invention discloses a drug sustained and controlled release microparticle preparation for treating intestinal diseases. The preparation comprises: a pill core containing the drug, wherein the pill core contains 5-aminosalicylic acid and an assistant material; an isolation layer for providing a smooth and flat surface for the microparticle and preventing the drug from penetrating into a sustained release coating layer, wherein the penetration of the drug into the sustained release coating layer can affect the release effect, the used material of the isolation layer comprises one or a plurality of materials selected from a water-soluble polymer and an anti-adhesion agent; the sustained release coating layer for slowly releasing the drug, wherein different drug release levels can be achieved through adjusting the thickness of the sustained release coating layer, the used material of the sustained release coating layer mainly adopts a sustained-release material; an enteric-coating layer, the enteric-coating layer is provided for avoiding the early release of the drug in gastric juice, reducing stimulation of the main drug to stomach, increasing the local concentration of the drug in the lesion location, the used material of the enteric-coating layer mainly adopts a polymer enteric material. The invention further discloses a preparation method for the microparticle preparation. According to the present invention, the drug and the sustained release coating material are uniformly dispersed on the surface of the pellet, such that the problem of mixing uniformity of the assistant material and the main drug can be effectively solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a sustained and controlled release pellet or particle preparation of a drug (5-aminosalicylic acid) for treating intestinal diseases; Methods for controlled release of pellet or microparticle formulations. Background technique [0002] Mesalazine (ie, 5-aminosalicylic acid) is mainly used clinically for the treatment of Crohn's disease and ulcerative colitis. But its dosage is higher (up to 4g is often used in the prescription), and the stomach is stimulated to a certain extent, and the diseased part of the treatment is in the colon. Most oral products on the market are prepared by slow-release and controlled-release methods. Products to reduce the number of times of taking and the stimulation to the human body, and improve the curative effect. However, the technology involved in most products and inventions cannot achieve the expected purpose, mainly beca...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/606A61K47/32A61K47/34A61K47/36A61K47/38A61P1/04
CPCA61K47/34A61K31/606A61K9/2054A61K9/14A61K9/2846A61K9/5073A61K47/36A61K9/5047A61K9/2886A61K9/2077A61K47/32A61K47/38A61K9/5026A61K9/5078A61P1/04
Inventor 赵建成石宗丰慕晓军
Owner PIVOT PHARMA TECH SHANGHAI
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