Method for preparing adhesive pellets by extrusion and spheronization

A technology of extrusion spheronization and pellets, which is applied in the direction of medical preparations of non-active ingredients, devices for making drugs into special physical or taking forms, and pharmaceutical formulations, which can solve the problem of adhesion of adhesives and pellets. Adhesion performance and toughness reduction, poor roundness of pills and other problems, to achieve the effect of improved adhesion performance, prolonged residence time, and good roundness

Inactive Publication Date: 2011-04-13
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The method described in the above-mentioned patent application obtains micropills, although it also has a certain adhesion effect, there are still the following deficiencies according to the research of the inventor: 1. The adhesive agent is mixed with the active ingredient to make a soft material, and after extrusion-spheronization- During the drying process, a large amount of heat is released and hydration disperses, and the adhesive performance and toughness of the prepared pellets are significantly reduced; 2. The adhesive becomes particularly sticky after being hot-melted, and many spikes are formed on the surface of the soft material during the extrusion process. The roundness of the pill after rounding is also obviously poor

Method used

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  • Method for preparing adhesive pellets by extrusion and spheronization
  • Method for preparing adhesive pellets by extrusion and spheronization

Examples

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example 1

[0019] Present embodiment is a kind of preparation method of leech adhesion pellet, and this method is as follows:

[0020] 1) Take 5g of dry powder of leech extract, add 145g of microcrystalline cellulose and 5g of lactose, and mix uniformly by the method of equal increments, pass through a 100-mesh sieve, add 100mL of water to prepare a soft material and place it in an extrusion-spheronizer to extrude The technological parameters of speed 20rpm, spheronization speed 200rpm and spheronization time 5min were extruded and spheronized, then dried at 50°C for 18h, and passed through a 30-mesh sieve to obtain leech-loaded pellets.

[0021] 2) Place the obtained pellets in a coating pan, add powder mixed with 5 g of hypromellose and 95 g of microcrystalline cellulose, spray with an appropriate amount of water to moisten, and adopt a powder layer coating method at 70°C Wrap the powder on the surface of the pellets loaded with leeches, and then place them in an oven at 40° C. and dry...

example 2

[0023] This embodiment is a preparation method of matrine adhered pellets, the method is as follows:

[0024] 1) Take 10g of matrine, add 100g of microcrystalline cellulose, 5g of lactose, and 5g of starch, mix uniformly by the method of equal increments, pass through a 100-mesh sieve, add 190mL of water to prepare a soft material, put it in an extrusion-spheronizer, and The technological parameters of extrusion speed 25rpm, spheronization speed 250rpm and spheronization time 7min were extruded and spheronized, then dried at 50°C for 20h, and passed through a 30-mesh sieve to obtain matrine-loaded pellets.

[0025] 2) Place the obtained pellets in a coating pan, add powder mixed with 3 g of carbomer and 55 g of microcrystalline cellulose, spray it with an appropriate amount of water to moisten it, and apply a powder layer coating method at 70° C. The above-mentioned powder was wrapped on the surface of the matrine-loaded pellets, and then dried in an oven at 40° C. for 12 hour...

example 3

[0027] Present embodiment is a kind of preparation method of metronidazole adhesion pellet, and the method is as follows:

[0028] 1) Take 7.5g of metronidazole, add 95g of microcrystalline cellulose, 2.5g of lactose, and 2.5g of starch, mix uniformly by using the method of equal increments, pass through a 100-mesh sieve, add 75mL of water to prepare a soft material and place it in an extrusion-spheronizer In the process, extrude and spheronize with the technological parameters of extrusion speed 15rpm, spheronization speed 150rpm and spheronization time 3min, then dry at 50°C for 20h, and pass through a 30-mesh sieve to obtain pellets loaded with metronidazole.

[0029] 2) Put the obtained micropellets in a coating pan, add 2.5g of hypromellose, 2.5g of carbomer and 90g of microcrystalline cellulose powder, spray with an appropriate amount of water to moisten, and put them under the condition of 70°C The powder was coated on the surface of the metronidazole-loaded pellets by ...

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Abstract

The invention relates to a medicinal preparation characterized by a special physical shape, in particular to a method for preparing adhesive pellets by extrusion and spheronization, which comprises the following steps: (1) sieving a medicament and a filler with a 100-mesh sieve and uniformly mixing the medicament and the filler according to a medicament to filler weigh ratio of 1-2:10-30, adding an adhesive in an amount which is 0.5 to 30 times the weight of the added medicament to prepare a soft material, extruding, spheronizing, drying and sieving with a 24-to-40-mesh sieve, and obtaining the medicament-loaded pellets; or dissolving the medicament in the adhesive in an amount which is 0.5 to 30 times the weight of the medicament, adding the filler according to a medicament to filler weigh ratio of 1-2:10-30 to prepare the soft material, extruding spheronizing, drying and sieving with the 24-to-40-mesh sieve and obtaining the medicament-loaded pellets; and (2), placing the medicament-loaded pellets in a coating pan, adding powdered adhesive according to a medicament to adhesive weigh ratio of 1-2:10-20, wetting by spraying a proper amount of water or ethanol at concentration of 40 to 60 percent, coating the adhesive on the outer layer of the medicinal pellets at the temperature of 65 to 80 DEG C by a powder lamination coating process, placing the pellets in an oven at 40 DEG C and drying the pellets for 12 hours.

Description

technical field [0001] The invention relates to a pharmaceutical preparation characterized by a special physical shape, in particular to an adhesive pellet for positioning drug delivery. Background technique [0002] Pellets (pills) refer to small spherical oral dosage forms with a diameter of 1-2.5 mm. Using different prescriptions, the pellets can be made into quick-release, sustained-release or controlled-release pellets, which can be used directly, or in capsules or compressed into tablets. In recent years, with the development of modern micropill preparation technology, more and more micropills are used in long-acting and controlled release preparations; the current preparation methods of micropills can be generally classified into the following categories: extrusion spheronization, centrifugal Granulation method, solution / suspension layering method, powder layering method, spray drying method, compression into ball method, spherical crystallization technology and high...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/38A61J3/00
Inventor 关世侠彭灿
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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