Cefaclor film-controlled sustained-release pellets and capsules

A technology of slow-release pellets and pellets, which is applied in the direction of medical preparations of non-active ingredients, organic active ingredients, pharmaceutical formulations, etc., and can solve the problems of membrane aging and release decline

Active Publication Date: 2017-07-11
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to solve the problem of release decline caused by film aging of cefaclor film-controlled sustained-release pellets prepared by water dispersion coating, the present invention provides a film-controlled film-controlled pellet that can maintain stable release performance throughout the validity period. Cefaclor sustained-release pellet capsules are characterized in that the core of the pellets contains sodium carboxymethyl starch with high water-swellability, and the sustained-release coating film is deformed by water swelling, thereby offsetting the aging of the film

Method used

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  • Cefaclor film-controlled sustained-release pellets and capsules
  • Cefaclor film-controlled sustained-release pellets and capsules
  • Cefaclor film-controlled sustained-release pellets and capsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The cefaclor sustained-release pellet capsule of embodiment 1 common ball core

[0030] 1. Prescription

[0031] 1. Pill core prescription (1000 capsules)

[0032]

[0033] 2. Prescription of sustained-release film coating solution

[0034]

[0035] 3. 00el ordinary stomach-soluble gelatin capsule shell 1000 capsules

[0036] Second, the preparation process:

[0037] 1. Ball core preparation process:

[0038] (1) Pass cefaclor through a 60-mesh sieve.

[0039] (2) Weigh the cefaclor, microcrystalline cellulose PH101 and lactose in the prescribed amount, put them in a wet granulator and mix them evenly.

[0040] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft material;

[0041] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0042] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

[0043] (6) Sieve, and take ball cores between 16 and 30 mesh.

[...

Embodiment 2

[0067] Example 2 Cefaclor Sustained-release Pellet Capsules Containing 5% Carboxymethyl Starch Sodium

[0068] 1. Prescription

[0069] 1. Pill core prescription (1000 capsules)

[0070]

[0071] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0072] 3. 00el ordinary stomach-soluble gelatin capsule shell 1000 capsules

[0073] Second, the preparation process:

[0074] 1. Ball core preparation process:

[0075] (1) Cefaclor is passed through a 60-mesh sieve;

[0076] (2) Take cefaclor, microcrystalline cellulose PH101, lactose, carboxymethyl starch sodium of prescription quantity, put in the wet granulator and mix uniformly;

[0077] (3) make soft material with 2% carboxymethylcellulose sodium 10% ethanol solution;

[0078] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0079] (5) Put it on the spheronizer for spheronization, the spheronization speed is 900~1000rpm, and dry in the fl...

Embodiment 3

[0098] Example 3 Cefaclor Sustained-release Pellet Capsules Containing 10% Carboxymethyl Starch Sodium

[0099] 1. Prescription

[0100] 1. Pill core prescription (1000 capsules)

[0101]

[0102] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0103] 3. 00el ordinary stomach-soluble gelatin capsule shell 1000 capsules

[0104] Second, the preparation process:

[0105] 1. Ball core preparation process: the same as in Example 2

[0106] 2. Preparation process of sustained-release film coating solution:

[0107] Same as Example 1

[0108] 3. Coating (sustained release film):

[0109] The ball core is placed in a fluidized bed for coating, and the weight gain of the coating film is controlled, and the weight gain of the coating is 26.5% and 30.7%.

[0110] 4, heat treatment: with embodiment 1

[0111] 5. Pellet filling: same as Example 1

[0112] 3. Release, content determination and results

[0113] Measuring method: see table 5 with...

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PUM

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Abstract

The invention relates to a cefaclor film-controlled sustained-release pellet capsule, the sustained-release film of the pellet adopts the mixture of water dispersion Eurdragit RL 30D:Eurdragit RS 30D=4:1 (weight ratio) as the film-forming material, the pellet The core contains high-expandability sodium carboxymethyl starch, and the commonly used excipients of pharmaceutically acceptable sustained-release pellets. The excipients are preferably microcrystalline cellulose and lactose, wherein the sodium carboxymethyl starch in the ball core is It accounts for 5-20% of the weight of the ball core. The sustained-release coating film comprises a mixture of water dispersion film-forming materials Eurdragit RL 30D and Eurdragit RS 30D, a plasticizer triethyl citrate and an anti-sticking agent talc, and the ratio is preferably Eurdragit RL 30D: Eurdragit RS 30D: citric acid Triethyl ester: talcum powder = 24:6:2:4, and the coating weight gain is preferably 23-40%. Because the ball core contains sodium carboxymethyl starch, which has high water swelling property, it will swell obviously after absorbing water, resulting in the expansion of the slow-release coating film, the thickness becomes thinner, the pore size of the water-permeable micropores becomes larger, and the permeability becomes better. , which compensates for the decrease in permeability caused by membrane aging, so that the release rate in the middle and late stages is basically constant, and the residue in the end stage is small, which can always maintain a stable release performance within the validity period.

Description

technical field [0001] The invention relates to a cefaclor membrane-controlled sustained-release pellet capsule, in particular to a cefaclor membrane-controlled sustained-release pellet capsule whose core contains sodium carboxymethyl starch, belonging to the field of pharmaceutical preparations. Background technique [0002] Cefaclor is a cephalosporin antibiotic, which plays an antibacterial effect by inhibiting the synthesis of bacterial cell walls and has bactericidal properties. It can quickly sterilize bacteria at low concentrations, and is used for respiratory system, urinary system, otolaryngology, skin and soft tissue infections caused by sensitive bacteria. [0003] Cefaclor is slightly soluble in water, and the earliest common preparation on the market needs to be taken 3 times a day, the blood concentration fluctuates greatly, the peak concentration is too high, and the adverse reactions are serious. [0004] Cefaclor Sustained Release Tablets (trade name: Cefac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K9/16A61K31/545A61K47/36A61P31/04
Inventor 姜庆伟狄媛吕玉珠唐亚坤刘俊轶
Owner 北京天衡药物研究院有限公司
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