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High drug-loaded p-aminosalicylic acid sustained-release pellets and its enteric-coated preparation

A technology of p-aminosalicylic acid and sustained-release pellets, which is applied in the field of para-aminosalicylic acid sustained-release enteric-coated oral preparations, high-drug-loading sustained-release pellets and their preparation fields, can solve the waste of raw materials, strips Problems such as poor deformation ability and weak strips can reduce production costs, improve formability, and save energy.

Active Publication Date: 2015-08-26
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] (1) The material cannot be extruded smoothly through the extruder to form a strip; or
[0022] (2) Although the extruder can extrude the material, the strips obtained are not strong and have a jagged shape. When the strips are rounded, they are easily broken by centrifugal force and cannot be made into pellets; or
[0023] (3) The extruder can extrude the material, and the obtained strips are strong, but the toughness is very poor, and the deformation ability of the strips is poor when rounded, and the obtained pellets are mostly dumbbell-shaped or short cylindrical, and cannot be spherical
[0024] The above three situations will directly cause waste of raw materials or directly affect the efficacy of finished products

Method used

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  • High drug-loaded p-aminosalicylic acid sustained-release pellets and its enteric-coated preparation
  • High drug-loaded p-aminosalicylic acid sustained-release pellets and its enteric-coated preparation
  • High drug-loaded p-aminosalicylic acid sustained-release pellets and its enteric-coated preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] 1. Pellet C

[0077] Material

Proportion(%)

Weight (g)

p-aminosalicylic acid

70.0

350.0

microcrystalline cellulose

25.0

125.0

Croscarmellose Sodium

3.0

15.0

Hypromellose

2.0

10.0

total

100.0

500.0

[0078] After weighing p-aminosalicylic acid, microcrystalline cellulose, croscarmellose sodium and hydroxypropylmethyl cellulose and mixing them uniformly through a 80-mesh sieve according to the formula, add 300g of purified water (the soft material made by this material) The maximum amount that can be added) makes soft materials. Prepare drug-containing micropills by the method of Comparative Example 1 to obtain micropills C.

[0079] 2. Preparation C

[0080] Configure the coating liquid by the coating formula of comparative example 1, and get 16~24 mesh pellets C 200g after coating by the method of comparative example 1, fill in the medicinal composi...

Embodiment 2

[0082] 1. Pellet D (changed the proportion of water-absorbing material and the type of binder)

[0083] Material

[0084] According to the formula, p-aminosalicylic acid, microcrystalline cellulose, croscarmellose sodium and carboxymethyl cellulose sodium were weighed through an 80-mesh sieve and mixed evenly, and then 350 g of purified water was added to make a soft material. Prepare drug-containing micropills by the method of Example 1, and obtain micropills D.

[0085] 2. Preparation D (the coating formula has been changed)

[0086] Material

[0087] Weigh the polyacrylic resin II according to the formula, add 315g of 95% ethanol, dissolve it completely in a water bath at 60°C, add triethyl citrate and talcum powder, and stir evenly to obtain an enteric coating solution. Take 16-24 mesh pellets D 200g and place them in a multi-functional granulation coating machine, adjust the air volume and spray speed, control the temperature for coating at 35-39°C,...

Embodiment 3

[0089] 1. Pellet E (change the proportion of water-absorbing material and the type of binder)

[0090] Material

[0091] Take p-aminosalicylic acid, microcrystalline cellulose, croscarmellose sodium and polyvinylpyrrolidone according to the formula and mix them uniformly, then add 350 g of purified water to make a soft material. Prepare drug-containing micropills by the method of Comparative Example 1, and obtain micropills E.

[0092] 2. Preparation E (change the coating formula)

[0093] Material

[0094] Weigh Eudragit L100 according to the formula, add 315g of 95% ethanol, dissolve it completely in a water bath at 60°C, add triethyl citrate and talcum powder, and stir evenly to obtain an enteric coating solution. Take 16-24 mesh pellets E 200g and place them in a multi-functional granulation coating machine, adjust the air volume and spray speed, control the temperature for coating at 35-39°C, stop coating when the coating weight increases by 10%, 35...

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Abstract

The invention finds that the plasticity of a material can be enhanced and the problem of poor forming property of a pellet with a high drug-loading rate is solved when a highly-hydrophilic material generally serving as a disintegrating agent in a medicament is used for preparing a sustained-release pellet with high drug-loading rate. In the invention, an applicable highly-hydrophilic material is screened by breaking free from convention, reasonable using amount is researched, the contradiction between sustained release and disintegration of a medicament is avoided, a high-quality pellet is prepared, and a preparation has a sustained release function simultaneously. The invention provides a formula of a para-aminosalicylic acid sustained-release pellet with high drug-loading rate and a preparation process thereof, and provides an enteric-coated oral preparation prepared from the sustained-release pellet.

Description

technical field [0001] The invention relates to the application of strong water-absorbing materials to improve the formability of micro-pills in the preparation of high-loaded sustained-release micro-pills. The invention also relates to high-loaded sustained-release pellets containing strong water-absorbing materials and a preparation method thereof, and p-aminosalicylic acid sustained-release enteric-coated oral preparations prepared from the pellets. Background technique [0002] One, have the following technical problems in the preparation of p-aminosalicylic acid oral preparations: [0003] 1. It is necessary to make a preparation with high drug loading, because it needs to be administered orally in a large dose, and it is necessary to overcome the inconvenience of swallowing caused by the large dose [0004] Para-aminosalicylic acid is an anti-tuberculosis drug discovered in the 1940s. This drug can enhance the activity of isoniazid and streptomycin, so it is widely us...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/606A61K47/36A61K47/38A61P31/06
Inventor 熊伟袁媛
Owner CHONGQING HUAPONT PHARMA
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