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Oral tigecycline enteric-coated microsphere and preparation method thereof

A technology of tigecycline and microspheres, which is applied to the active ingredients of tetracycline, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of inactivation, easy degradation by gastric juice, and inconvenient use, so as to promote repair, Prolonged disintegration time and ease of use

Pending Publication Date: 2020-05-19
赛隆药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The growth factor used to repair the mucous membrane is a polypeptide, which is easily degraded by gastric juice and loses its activity when it is taken directly orally. Therefore, it is often used as an external drug, which is inconvenient to use

Method used

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  • Oral tigecycline enteric-coated microsphere and preparation method thereof
  • Oral tigecycline enteric-coated microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A kind of oral tigecycline enteric-coated microspheres, comprising the following parts:

[0030] The first microspheres, including:

[0031] The first core: tigecycline 10mg, microcrystalline cellulose 80mg, magnesium lauryl sulfate 10mg;

[0032] The first jersey: Tolu balsam 3.2mg, crospovidone 0.5mg, chitosan 96.3mg;

[0033] First coating: acrylic resin;

[0034] a second microsphere comprising:

[0035] Second core: hEGF 1mg, microcrystalline cellulose 90mg, mannitol 9mg;

[0036] Second jersey: Tolu balsam 6.4mg, crospovidone 1mg, chitosan 92.6mg;

[0037] Second coating: 80% acrylic resin + 20% peach gum.

[0038] The enteric-coated microspheres are prepared by the following method:

[0039] S1: Weigh tigecycline, microcrystalline cellulose and magnesium lauryl sulfate in proportion and mix them, extrude and dry to obtain the first ball core; weigh tolu balsam, crospovidone and shell Polysaccharides are mixed to make the first jersey liquid; the first jers...

Embodiment 2

[0045] A kind of oral tigecycline enteric-coated microspheres, comprising the following parts:

[0046] The first microspheres, including:

[0047] The first core: tigecycline 5mg, microcrystalline cellulose 70mg, magnesium lauryl sulfate 25mg;

[0048] The first jersey: Tolu balsam 3.8mg, crospovidone 1.6mg, chitosan 94.6mg;

[0049] First coating: acrylic resin;

[0050] a second microsphere comprising:

[0051] Second core: hEGF 0.5mg, microcrystalline cellulose 75mg, mannitol 24.5mg;

[0052] Second jersey: Tolu balsam 7.6mg, crospovidone 3.2mg, chitosan 89.2mg;

[0053] Second coating: 75% acrylic resin + 25% peach gum.

[0054] The preparation method of the enteric microspheres is the same as in Example 1.

Embodiment 3

[0056] A kind of oral tigecycline enteric-coated microspheres, comprising the following parts:

[0057] The first microspheres, including:

[0058] The first core: tigecycline 10mg, microcrystalline cellulose 80mg, magnesium lauryl sulfate 10mg;

[0059] The first jersey: Tolu balsam 3.2mg, crospovidone 0.5mg, chitosan 96.3mg, heparin sodium 0.5mg, leucine 2mg;

[0060] First coating: acrylic resin;

[0061] a second microsphere comprising:

[0062] Second core: hEGF 1mg, microcrystalline cellulose 90mg, mannitol 9mg;

[0063] Second jersey: Tolu balsam 6.4mg, crospovidone 1mg, chitosan 92.6mg;

[0064] Second coating: 80% acrylic resin + 20% peach gum.

[0065] The enteric-coated microspheres are prepared by the following method:

[0066] S1: Weigh tigecycline, microcrystalline cellulose and magnesium lauryl sulfate in proportion, mix them, extrude and dry them to obtain the first ball core; weigh tolu balsam, crospovidone, shell Polysaccharide, heparin sodium and leuc...

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Abstract

The present invention provides an oral tigecycline enteric-coated microsphere and a preparation method thereof. The enteric-coated microsphere contains tigecycline and growth factors at the same time,firstly, an enteric coating prevents the microsphere from disintegrating in gastric juice and enables the microsphere to completely enter the small intestine for swelling and releasing, thereby avoiding an influence of strong acid environment of the gastric juice on bioavailability of the tigecycline; staying and disintegrating time of a second microsphere in the intestinal tract are prolonged byadjusting components and dosage of a second spherical coating or a second coating, so that the growth factors can be released after the tigecycline, after the tigecycline kills infected bacteria, andthen the growth factors promote repair of mucosa at a damaged part, thereby effectively relieving symptoms and promoting wound healing. During the preparation, the first microsphere and the second microsphere are first prepared respectively, then capsule shells, etc. are used for encapsulation according to a proportion, the two effective components are combined into one medicine and the two effective components can also be released respectively, so that the oral tigecycline enteric-coated microsphere is convenient to use.

Description

technical field [0001] The invention belongs to the technical field of industrial pharmacy, and in particular relates to a preparation method of oral tigecycline enteric-coated microspheres. Background technique [0002] Tigecycline is a broad-spectrum tetracycline antibiotic, which can overcome the tetracycline resistance caused by bacterial efflux and ribosome protection, and maintain good antibacterial activity against common pathogenic bacteria or multi-drug resistant bacteria. The last line of defense in the control of clinical multidrug-resistant or pan-drug-resistant bacterial infections. When mucosal parts such as the digestive tract and respiratory tract are damaged, bacteria can easily enter the body and cause infection; at the same time, bacterial infection can further aggravate mucosal damage. Therefore, in the process of using antibiotics to resist bacteria, and at the same time repair the mucosal damage, the effect of treatment will be greatly improved. The g...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K31/65A61K38/18A61P31/04A61P17/02
CPCA61K31/65A61K9/5084A61K38/1808A61P31/04A61P17/02A61K2300/00
Inventor 李剑峰周文
Owner 赛隆药业集团股份有限公司