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Quick release agent of large-dose medicine and preparation method of quick release agent

An immediate-release preparation and large-dose technology, applied in the field of medicine, can solve the problems that the preparation is not suitable for patients to take, the preparation is difficult to produce and use, and the amount of active pharmaceutical ingredients is large. Beneficial for swallowing

Inactive Publication Date: 2016-07-20
NKD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Large doses of drugs exist in the preparation drug delivery system, and there are the following difficulties: 1. The amount of active ingredients of the drug itself is relatively large, and the characteristics of the preparation are mainly reflected in the properties of the active ingredients during the preparation molding process, which can often meet the requirements of the preparation. performance requirements
2. Usually the size of the preparation is large, and the preparation patients should not take it
Such preparations have difficulties in preparation production and use
[0003] If the active ingredient of a drug is greater than 1 gram, it is difficult to make a tablet or capsule according to traditional preparation technology, and it is even more difficult for drugs with poor water solubility. For example, the initial dosage form of AstraZeneca OLAPARIB needs to take 16 capsules per day
More excipients are needed to improve the defects of the active ingredients that are not conducive to the characteristics of the preparation, resulting in a larger final dosage volume, and at the same time, such tablets are prone to disintegration and dissolution, resulting in bioavailability problems

Method used

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  • Quick release agent of large-dose medicine and preparation method of quick release agent
  • Quick release agent of large-dose medicine and preparation method of quick release agent
  • Quick release agent of large-dose medicine and preparation method of quick release agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Preparation of highly hydrophilic auxiliary material matrix: 100 g of sorbitol was dissolved in 1 L of depurified water; (2) under continuous stirring, 150 g of povidone was slowly added to dissolve, and then 204 g of Tween was added to obtain a highly hydrophilic auxiliary material base.

[0052] Preparation of pharmaceutical powder: mycophenolate mofetil is pulverized by jet to particle size D 90 If it is less than 20 microns, add a total amount of 1% micronized silica gel, mix well, and set aside.

[0053] 3D printing: tablets are obtained by powder bond printing. The active ingredient content is 99%, and the tablet weight is 1010mg.

Embodiment 2

[0054] [Example 2] Preparation of sofosbuvir+velpatasvir+GS-9857 compound tablet

[0055] Preparation of highly hydrophilic adjuvant matrix: 100 g of sorbitol was dissolved in 1 L of 80% ethanol; (2) under continuous stirring, 50 g of hydroxypropyl cellulose was slowly added to dissolve, and then 2 g of Span was added to obtain a highly hydrophilic adjuvant matrix.

[0056] Pharmaceutical powder preparation: Three components are jet milled to particle size D 90 If it is less than 1nm, add an appropriate amount of highly hydrophilic auxiliary material matrix, mix evenly, and use it as a printing material for later use.

[0057] 3D printing: printing materials, tablets are obtained by direct printing. The active ingredient content is 98%, and the tablet weight is 1.2g.

Embodiment 3

[0058] [Example 3] Preparation of Capecitabine Tablets

[0059] Preparation of highly hydrophilic auxiliary material matrix: 200g mannitol alcohol is dissolved in 1L80% ethanol; (2) under continuous stirring, slowly add hypromellose 10g to dissolve, then add sodium lauryl sulfate 40g, obtain high Hydrophilic excipient matrix.

[0060] Pharmaceutical powder preparation: to particle size D 90 If it is less than 1 micron, add a total of 1% micronized silica gel and mix evenly, and set aside.

[0061] 3D printing: tablets are obtained by powder bond printing. The active ingredient content is 90%, and the tablet weight is 550mg.

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Abstract

The invention discloses a quick release agent of large-dose medicine.The quick release agent is composed of an active ingredient and a quick release matrix containing high-hydrophily auxiliary materials.The quick release matrix is prepared from, by weight, 10% to 30% of high-hydrophily auxiliary materials, 0.05% to 0.4% of surface active agent, 0.1% to 15% of high-molecular polymer and the balance solvent.The quick release agent can be fast disintegrated and dispersed in the oral cavity after being taken, and disintegration difficulty cannot be caused.Due to the specific quick release matrix and the 3D printing technology, the preparation can be formed by the large-dose medicine through few auxiliary materials, the medicine loading capacity is improved, the active ingredient can be released according to computer simulation, the production process is environmentally friendly, and bioavailability is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a 3D printing fast-release preparation of a large dose of medicine and a preparation method thereof. Background technique [0002] Large doses of drugs exist in the preparation drug delivery system, and there are the following difficulties: 1. The amount of active ingredients of the drug itself is relatively large, and the characteristics of the preparation are mainly reflected in the properties of the active ingredients during the preparation molding process, which can often meet the requirements of the preparation. performance requirements. 2. Usually the size of the preparation is relatively large, so patients should not take it. At present, it is mostly used, and it is divided into multiple small dosage unit preparations, and multiple tablets are taken at a time. Such formulations present difficulties in formulation production and use. [0003] If the active i...

Claims

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Application Information

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IPC IPC(8): A61K47/26A61K9/22B33Y10/00
CPCA61K47/26A61K9/0002A61K9/2018B33Y10/00
Inventor 尚丽霞陶秀梅黄蕾
Owner NKD PHARMA CO LTD
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