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Gabapentin stomach retention sustained-release composition

A slow-release composition, gabapentin technology, applied in the direction of drug combination, medical preparations of non-active ingredients, pill delivery, etc., can solve the problems of reduced bioavailability and incomplete absorption, so as to reduce dosage and frequency and improve curative effect , Simple and feasible operation

Inactive Publication Date: 2008-02-13
珠海天翼医药技术开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When the dose increases, the bioavailability decreases instead, because when the dose is large, the drug will exceed the carrier's absorption capacity, causing part of the drug to flow into the lower digestive tract and incomplete absorption

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment one: every 1000 gabapentin sustained-release tablets contain the following substances:

[0022] Gabapentin 400.0g main ingredient

[0023] Ethyl cellulose 120.0g insoluble matrix material

[0024] Crospovidone 120.0g insoluble matrix material

[0025] Lactose 16.0g Filler

[0026] PVP 10.0g binder

[0027] Magnesium stearate 0.5g Lubricant

[0028] HPMC 250.0g Hydrophilic framework material

[0029] Weigh the prescription amount, mix evenly, and compress into tablets.

[0030] After testing, the release range of gabapentin gastric retention sustained-release tablets is 10-40% of the labeled amount within 1 hour; 40-70% of the labeled amount within 2 hours; and 40-70% of the labeled amount within 4 hours. The amount is greater than 65% of the labeled amount.

Embodiment 2

[0031] Embodiment two: every 1000 gabapentin gastric retention sustained-release tablets contain the following substances:

[0032] Bezafibrate 600.0g main ingredient

[0033] Acrylic resin 130.0g insoluble matrix material

[0034] Croscarmellose Sodium 120.0g Insoluble Skeleton Material

[0035] Starch 30.0g Filling agent

[0036] Talc 10.0g Lubricant

[0037] Kabham 200.0g Hydrophilic framework material

[0038] The method is the same as above.

[0039] After testing, the release range of the release rate is 10-40% of the labeled amount within 1 hour; 40-70% of the labeled amount within 2 hours; 70% of the labeled amount within 4 hours. %.

Embodiment 3

[0040] Embodiment three: every 1000 gabapentin gastric retention sustained-release tablets contain the following substances:

[0041] Gabapentin 800.0g main ingredient

[0042] Sodium cellulose phthalate 160.0g Insoluble framework material

[0043] Calcium carboxymethylcellulose 130.0g insoluble framework material

[0044] Microcrystalline Cellulose 20.0g Bulking

[0045] Kabham 165.0g Hydrophilic framework material

[0046] Talc 32.5g Lubricant

[0047] HPMC 210.0g Hydrophilic framework material

[0048] The method is the same as above.

[0049] After testing, the slow-release pellets are packed into hard capsules.

[0050] After testing, the release range of the release rate is 10-40% of the labeled amount within 1 hour; 40-70% of the labeled amount within 2 hours; 70% of the labeled amount within 4 hours. %.

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PUM

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Abstract

A Gabapentin slow-release compound for gastric retention is a slow-release drug delivery system for gastric retention, which comprises the Gabapentin served as the active component and the slow-release skeleton material with slow-release property and the other excipient with pharmaceutical approval. The composition proportion (weight ratio) is as following. The ratio of slow-release skeleton material to the other excellent with pharmaceutical approval is from one to 0.2 till 2 to 0.0 till 2. The compound can stay in the stomach for more than 2 hours. The compound is also capable of controlling the drug release, reducing the administration times, reducing toxic and side effects and improving the treatment effect.

Description

Technical field: [0001] The invention relates to a pharmaceutical preparation in the field of oral positioning drug release, and mainly refers to a gabapentin gastric retention slow-release composition and its prescription and preparation process. Background technique: [0002] Gabapentin is a synthetic amino acid that has obvious antiepileptic effects and is effective for partial seizures and secondary generalized tonic-clonic seizures. It is easily absorbed after oral administration, and reaches the peak concentration within 2 to 3 hours. Since the absorption of gabapentin must have amino acids as carriers, and amino acids are mainly concentrated in the upper gastrointestinal tract (duodenum), and the amount of carriers in the lower gastrointestinal tract is very small, and its drug absorption site is mainly in the duodenum. When a small dose of ordinary tablet (100 mg) is taken orally, the bioavailability is close to 100%, and when a single dose of 300 mg is taken orally...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K31/195A61K47/34A61K47/38A61P25/08A61K47/10A61K47/32A61K47/36
Inventor 张晓明杨岗曾万溪
Owner 珠海天翼医药技术开发有限公司
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