Medicament carrier for releasing medicament in sustained-release way

Abstract

The invention discloses a medicament carrier for releasing a medicament in a sustained-release way. The medicament carrier comprises (a) an aliphatic additive of which the melting points in vivo and vitro are higher than 37 DEG C, (b) water-soluble, low-viscosity and non-irritating additive particles, (c) a water-swellable and water-insoluble acidic (or alkaline) polymer, (d) an alkaline (or acidic) substance, (e) a water-soluble surfactant and (f) a medicament. The medicament carrier has high medicament release properties, a good anti-salt poisoning effect and high medicament release uniformity, so that the medicament can be released in a sustained way or the problem about end-release is solved; the medicament carrier has low mucous membrane irritation and high biocompatibility; and the medicament safety problems such as medicament burst release and dose pour release are not easily caused.

Description

technical field

[0001] The invention relates to a medicine carrier for sustained release of medicine. More specifically, the present invention relates to a drug carrier for sustained-release drug with improved properties, the drug carrier includes aliphatic additives with in vivo and in vitro melting points greater than 37°C, water-soluble low-viscosity additive particles, water Swellable water-insoluble acidic (or basic) polymer, basic (or basic) excipient (material), water-soluble surfactant and drug. technical background

[0002] Sustained-release preparations such as sustained-release suppositories, especially those with oily materials as the main sustained-release material, often exhibit the so-called "terminal release" problem, that is, the release of the drug is fast in the early stage, gradually slows down in the middle stage, and slows down in the later stage. Often, a part of the drug remains in the matrix within the specified (or expected) action time, and the ex...

Examples

Embodiment 1

[0236]

[0237] Note: a1, the main performance parameters of this particle are shown in Table 1;

[0238] b1, the preparation method of the sodium polyacrylate particles: see the preparation method of the acidic (or alkaline) water-insoluble and swellable polymer (particle) in the comparative example below.

Embodiment 2

[0240]

[0241] Note: a2, the main performance parameters of this particle are shown in Table 1;

[0242] b2, the preparation method of the polylysine citrate particles: see the preparation method of the acidic (or alkaline) water-insoluble and swellable polymer (particle) in the comparative example below.

Embodiment 3

[0244]

[0245] Note: a3, the main performance parameters of this particle are shown in Table 1;

[0246] b3, the preparation method of the sodium polyacrylate particles: see the preparation method of the acidic (or alkaline) water-insoluble and swellable polymer (particle) in the comparative example below.

technical field

[0001] The invention relates to a medicine carrier for sustained release of medicine. More specifically, the present invention relates to a drug carrier for sustained-release drug with improved properties, the drug carrier includes aliphatic additives with in vivo and in vitro melting points greater than 37°C, water-soluble low-viscosity additive particles, water Swellable water-insoluble acidic (or basic) polymer, basic (or basic) excipient (material), water-soluble surfactant and drug. technical background

[0002] Sustained-release preparations such as sustained-release suppositories, especially those with oily materials as the main sustained-release material, often exhibit the so-called "terminal release" problem, that is, the release of the drug is fast in the early stage, gradually slows down in the middle stage, and slows down in the later stage. Often, a part of the drug remains in the matrix within the specified (or expected) action time, and the ex...

Examples

Embodiment 1

[0236]

[0237] Note: a1, the main performance parameters of this particle are shown in Table 1;

[0238] b1, the preparation method of the sodium polyacrylate particles: see the preparation method of the acidic (or alkaline) water-insoluble and swellable polymer (particle) in the comparative example below.

Embodiment 2

[0240]

[0241] Note: a2, the main performance parameters of this particle are shown in Table 1;

[0242] b2, the preparation method of the polylysine citrate particles: see the preparation method of the acidic (or alkaline) water-insoluble and swellable polymer (particle) in the comparative example below.

Embodiment 3

[0244]

[0245] Note: a3, the main performance parameters of this particle are shown in Table 1;

[0246] b3, the preparation method of the sodium polyacrylate particles: see the preparation method of the acidic (or alkaline) water-insoluble and swellable polymer (particle) in the comparative example below.

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