Amoxicillin sustained release solid medicinal composition and preparation method thereof

A technology of amoxicillin and composition, applied in the field of amoxicillin sustained-release solid pharmaceutical composition and preparation thereof, can solve the problem of low initial release, inability to effectively prevent coating film adhesion, affecting drug onset time and curative effect, etc. problem, to achieve the effect of improving curative effect and ensuring effective blood drug concentration

Active Publication Date: 2012-04-04
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In the process of studying amoxicillin sustained-release preparations, the inventors found that the amoxicillin controlled-release tablets obtained according to the prescription process described in patents US6544555, US6669948, US6723341, WO2008069806A1, and WO2007067770A2 showed that the tablets disintegrated in vitro Afterwards, the pH-sensitive coated pellets adhered to each other, and the initial release rate in the delayed release part was significantly lower than that before tablet compression, which obviously affected the onset time and curative effect of the drug
[0009] In the process of studying the amoxicillin sustained-release preparation, the inventor found that the microparticles (tablets or pellets) were coated with acrylic resin and aggregated due to stickiness, thereby affecting the release rate of amoxicillin. If hydrophobic materials such as talcum powder, micropowder silica gel, magnesium stearate, etc. are directly mixed or suspended in an appropriate solvent and sprayed on the surface of tablets and pellets, it still cannot effectively prevent the adhesion between coating films However, it was unexpectedly found that spraying acrylic resin on the surface of the pH-sensitive coating film with a hydrophilic coating material can effectively prevent the adhesion between the coating films, thereby solving the problem of delayed release of amoxicillin controlled-release tablets. significantly lower

Method used

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  • Amoxicillin sustained release solid medicinal composition and preparation method thereof
  • Amoxicillin sustained release solid medicinal composition and preparation method thereof
  • Amoxicillin sustained release solid medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1 (comparative example):

[0075] (Each tablet contains 775 mg of amoxicillin, and the distribution ratio in each part is immediate release part: first delayed release part: second delayed release part=48:26:26)

[0076] 1. Quick release part:

[0077] Immediate release prescription:

[0078]

[0079] Preparation Process:

[0080] 1) Mix the amoxicillin, MCC and crospovidone (XL-10) evenly;

[0081] 2) Prepare 4% HPMC (E5) adhesive;

[0082] 3) Slowly add binder to prepare soft material, pass through a 30-mesh sieve to prepare granules, dry at 55°C, and pass through a 20-mesh sieve to granulate.

[0083] 2. Delayed release part:

[0084] Pill core prescription:

[0085]

[0086] Preparation Process:

[0087] 1) prepare 4% hydroxypropyl methylcellulose adhesive;

[0088] 2) Mix the amoxicillin and microcrystalline cellulose of the recipe quantity evenly;

[0089] 3) Dissolve polyoxyethylene (35) castor oil and polyethylene glycol 400 in an appropri...

Embodiment 2

[0124] Embodiment 2 (comparative example)

[0125] The formulation process of immediate-release, pellet core, and two kinds of delayed-release pH-sensitive coatings refers to Example 1, but the weight gain of the two kinds of delayed-release pH-sensitive coatings is 30%, wherein each tablet of the preparation contains 775 mg of amoxicillin, and in The distribution ratio of each part was immediate release part: first delayed release part: second delayed release part = 48:26:26.

Embodiment 3

[0127] Adopt the 85% alcohol solution of 4% hydroxypropyl methylcellulose to carry out isolation coating to two kinds of delayed-release pellets of embodiment 1, embodiment 2 respectively, coating weight gain is 0.5~2%, wherein this preparation is every The tablet contains 775 mg of amoxicillin, and the distribution ratio in each part is immediate-release part: first delayed-release part: second delayed-release part=48:26:26.

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Abstract

The invention relates to an amoxicillin sustained release solid medicinal composition and a preparation method thereof. The composition which comprises a fast release unit containing amoxicillin, a first delayed release unit containing amoxicillin, and a second delayed release unit containing amoxicillin is characterized in that: the two delayed release units are a micropill or a particle which comprises a pill core containing amoxicillin, an inner pH-sensitive coating material which is coated on the inner layer of the pill core, and an outer hydrophilic coating material which is coated on the outer layer of the pill core, wherein pH-sensitive coating materials of the first delayed release unit and the second delayed release unit are different; the pH of the pH-sensitive release point of the coating materials of the first delayed release unit is equal to or more than 5.0; and the pH of the pH-sensitive release point of the coating materials of the second delayed release unit is equal to or more than 6.0. The composition allows the release degree of the tableted amoxicillin pH-sensitive coating micropill in the initial release stage to be improved.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an amoxicillin sustained-release solid composition and a preparation method thereof. The composition comprises an amoxicillin-containing immediate-release unit, a first delayed-release unit containing amoxicillin and a The second delayed-release unit of cillin is characterized in that: the two delayed-release units are each composed of a pellet core containing amoxicillin, an inner layer pH-sensitive coating material coated on the surface of the pellet core, and an outer hydrophilic layer. Pellets or granules composed of coating materials, wherein the pH-sensitive coating materials of the first delayed-release unit and the second delayed-release unit are different, and the pH-sensitive release point pH of the coating material of the first delayed-release unit is ≥ 5.0, the pH-sensitive release point pH of the coating material of the second delayed-release unit is ≥ 6.0. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K9/48A61K31/43A61P31/04A61K31/424
Inventor 欧云国张涛万娟李霞
Owner CHONGQING PHARMA RES INST
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