Floating type pellets in stomach and preparation method thereof

A gastric flotation and pellet technology, which is applied in the field of medicine, can solve the problems of negative impact on flotation performance, high blood drug concentration in patients, enhanced tensile strength, etc. Effect

Active Publication Date: 2008-10-22
特康药业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantages are: 1. The pressure of tablet pressing also affects the floating performance. Excessive pressure will increase the tensile strength of the tablet and reduce the porosity, which will have a ne

Method used

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  • Floating type pellets in stomach and preparation method thereof
  • Floating type pellets in stomach and preparation method thereof
  • Floating type pellets in stomach and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Expandable polystyrene beads (particle size 1800-300um) are softened when placed in a batch pre-expansion machine and heated by steam to above 92°C. Adjust the pre-expansion temperature, steam pressure and feed amount to volatilize the blowing agent The volume of the escaped particles slowly expands to 20 times, and then the foam particles are allowed to fall freely into the aging chamber made of mesh anti-static gauze for 8 hours. Enter the fluidized bed for drying to obtain pellet cores with a particle size of 500-800um. Then sieve according to the needs, and sieve out the pellet core of 700um-800um; its density is about 0.05g / cm 3 Then it is put into the fluidized bed and sprayed with stomach-dissolving coating liquid, which can further increase the particle diameter and density of the pellet core and make the appearance smoother.

[0022] Ball core prescription:

[0023]

[0024] drug coating solution

[0025]

[0026] protective coating solution

[0027] ...

Embodiment 2

[0045] Expandable polystyrene beads (particle size 180-300um) are softened when placed in a batch pre-expansion machine and heated by steam to above 92°C. Adjust the pre-expansion temperature, steam pressure and feed amount to volatilize the blowing agent The volume of the escaped particles slowly expands to 20 times, and then the foam particles are allowed to fall freely into the aging chamber made of mesh anti-static gauze for 8 hours. Enter the fluidized bed for drying to obtain pellet cores with a particle size of 500-800um. Then sieve according to the needs, and sieve out the pellet core of 700um-800um; its density is about 0.05g / cm 3

[0046] Ball core prescription:

[0047]

[0048] drug coating solution

[0049]

[0050] protective coating solution

[0051]

[0052] Sustained release layer coating solution

[0053]

[0054] 1. Preparation of drug coating solution

[0055] Weigh Povidone K30 according to the prescribed amount and dissolve it in 455ml w...

Embodiment 3

[0069] Ball core preparation:

[0070] Expandable polystyrene beads (particle size 180-300um) are softened when placed in a batch pre-expansion machine and heated by steam to above 92°C. Adjust the pre-expansion temperature, steam pressure and feed amount to volatilize the blowing agent The volume of the escaped particles slowly expands to 20 times, and then the foam particles are allowed to fall freely into the aging chamber made of mesh anti-static gauze for 8 hours. Enter the fluidized bed for drying to obtain pellet cores with a particle size of 500-800um. Then sieve according to the needs, and sieve out the pellet core of 700um-800um; its density is about 0.05g / cm 3 Then it is put into the fluidized bed and sprayed with stomach-dissolving coating liquid, which can further increase the particle diameter and density of the pellet core and make the appearance smoother.

[0071] above core

[0072]

[0073] drug coating solution

[0074]

[0075] protective coating ...

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Abstract

The invention relates to the technical field of medicine, in particular to a stomach floating type pellet and a preparation method thereof. The stomach floating type pellet comprises a pellet core, a drug layer and a sustained-release layer; the density of the pellet is smaller than 1g/cm<3>, so that the drug can float in the stomach, sustainably release the drug ingredients; stomach floating type capsules can be prepared by loading the pellets into capsules. The preparation type is suitable for drugs mainly absorbed in the stomach, in particular to the drugs that are absorbed better in the stomach than in the enteric canal. When the drugs are prepared into stomach floating type pellets or stomach floating type capsules, compared with ordinary preparation, the times of administration is reduced and the relatively stable blood concentration of the drugs is kept in vivo, thus ensuring the sustained release of the drugs, improving the bioavailability and reducing the dosage. At the same time, as the stomach floating type pellet is a granose system, the drug release behavior is the collective behavior of each pellet, so that coating failure of a plurality of pellets can not lead to failure of the whole dosage, thus having higher safety. The sustained-release pellet is prepared by adopting general technique and is easy for realizing industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a floating micropill in the stomach and a preparation method thereof. Background technique [0002] For those drugs or nutrients that are only well absorbed in the stomach and need to act locally in the stomach and have an absorption window in the duodenum, the general immediate-release preparations are discharged into the intestinal tract due to rapid disintegration in the stomach, Difficult to get maximum absorption. For this type of drug, the residence time of the drug in the stomach can be prolonged after being prepared as a floating preparation in the stomach, and the effects of these substances can be brought into full play to the greatest extent. Tosssounian and Sheth were the first to describe in detail gastric floating formulations, which they called "bioeffective formulations". The gastric floating preparation [gastric floating (buayant) preparation] desi...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K47/10A61K47/44A61K47/32A61K47/38A61K9/34A61K9/48A61K45/00A61K47/14A61K47/42
Inventor 王雷波
Owner 特康药业集团有限公司
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