Floating and sustained-release pellet, pharmaceutical composition containing pellet and preparation method of pharmaceutical composition

A technology of sustained-release pellets and compositions, which is applied in the direction of drug combinations, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problem of affecting the floating performance of gas generation, poor floating performance of preparations, and prolonged residence time in the stomach. problems, to achieve a reasonable drug release lag time, prolong the continuous floating time, and maintain the effect of blood drug concentration

Active Publication Date: 2015-01-21
AC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, this volume-expansion retention system has such disadvantages: the unit dosage form is prone to burst release, or individual preparations have poor floating performance and are quickly emptied by the stomach, which does not achieve the expected sustained and controlled release effect; and because the patient's gastric Individual differences in emptying rate often lead to uncertainty and lack of reproducibility in the prolongation of gastric residence time, so individual differences in drug release are large
However, due to the differences in the gastric environment between individuals, on an empty stomach and after meals, it often affects the gas production and floating performance of this type of floating preparation, thereby affecting its residence time in the stomach

Method used

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  • Floating and sustained-release pellet, pharmaceutical composition containing pellet and preparation method of pharmaceutical composition
  • Floating and sustained-release pellet, pharmaceutical composition containing pellet and preparation method of pharmaceutical composition
  • Floating and sustained-release pellet, pharmaceutical composition containing pellet and preparation method of pharmaceutical composition

Examples

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Embodiment 1

[0106] An embodiment of the floating slow-release pellets of the present invention, the structure of the floating slow-release pellets described in this embodiment is as attached figure 1 shown by the attached figure 1 It can be seen that the floating sustained-release pellets described in this example are sequentially composed of a drug-containing pellet core 1, a sustained-release coating layer 2, a bleaching aid layer 3 and a protective layer 4 from inside to outside, and the floating sustained-release pellets described in this example contain Components of the following masses:

[0107]

[0108] The floating sustained-release pellets described in this example are prepared by the following method:

[0109] (1) Preparation of pill cores: sieve pregabalin, fillers, blockers and binders, and then mix them uniformly in a three-dimensional mixer to obtain premixed powder; put the premixed powder in extrusion- In the spheronizer, add a wetting agent to obtain a 200-350 μm dr...

Embodiment 2

[0115] An embodiment of the floating slow-release pellets of the present invention, the structure of the floating slow-release pellets described in this embodiment is the same as in Example 1; in the preparation method of the floating slow-release pellets, the diluent used in step (2) is purified water , other preparation processes are all the same as in Example 1. The floating sustained-release pellets described in this embodiment contain the following components:

[0116]

[0117]

Embodiment 3

[0119] An embodiment of the floating slow-release pellets of the present invention, the structure and preparation method of the floating slow-release pellets described in this example are the same as in Example 2, and the floating slow-release pellets described in this example contain the following components:

[0120]

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Abstract

The invention discloses a Pregabalin gastric floating and sustained-release pellet. The pellet comprises a medicine-containing pellet core, a sustained-release coating layer and a floating supporting layer sequentially from inside to outside, wherein the external surface of the medicine-containing pellet core is wrapped by the sustained-release coating layer, and the external surface of the sustained-release coating layer is wrapped by the floating supporting layer; the medicine-containing pellet core contains a retarding agent, and the floating support layer contains a waxy material and a hydrophilic material. According to the Pregabalin gastric floating and sustained-release pellet disclosed by the invention, the risk that a medicine is suddenly released and is completely emptied can be lowered, and the bioavailability of the medicine and the adaptability of patient taking can be improved. Meanwhile, the invention further provides a pharmaceutical composition containing the gastric floating and sustained-release pellet and a preparation method of the pharmaceutical composition.

Description

technical field [0001] The invention relates to a sustained-release pellet, a pharmaceutical composition containing the pellet and a preparation method thereof, especially a gastric floating sustained-release pellet containing pregabalin, a pharmaceutical composition containing the pellet and its preparation method. Background technique [0002] Pregabalin, the molecular structural formula is as follows, its chemical name is (3S)-3-aminomethyl)-5-methylhexanoic acid, and its molecular formula is C 8 h 17 NO 2 , with a molecular weight of 159.23, white crystalline powder, easily soluble in water, alkaline and acidic aqueous solutions. [0003] [0004] Pregabalin is a new type of antiepileptic drug. Its molecular structure has a γ-aminobutyric acid structure. It is a new type of calcium ion channel regulator that can block voltage-dependent calcium channels and reduce the release of neurotransmitters. Therefore, it has antispasmodic effect. Pregabalin was successfully...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/197A61K9/26A61K9/56A61P25/08A61P25/02
Inventor 刘锋赖树挺周伟杰梁文伟
Owner AC PHARMA
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