Matrix-type preparation containing mycophenolic acid or mycophenolic acid salt and coated tablet thereof

A technology of mycophenolate mofetil and mycophenolic acid, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, drug delivery, etc., can solve the problem of increasing the temperature of the substance and the increase in coating weight. Requirements, flammable and explosive problems, to achieve the effect of preventing precipitation and improving bioavailability

Inactive Publication Date: 2012-11-28
WUXI FORTUNE PHARMA
View PDF3 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the characteristics of volatile, flammable and explosive organic solvents, the risk factor of the coating process is high, and it will pollute the environment at the same time
Although the aqueous dispersion of enteric materials has been developed in recent years to avoid the use of organic solvents, the aqueous dispersion needs to increase the coating tempe

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Matrix-type preparation containing mycophenolic acid or mycophenolic acid salt and coated tablet thereof
  • Matrix-type preparation containing mycophenolic acid or mycophenolic acid salt and coated tablet thereof
  • Matrix-type preparation containing mycophenolic acid or mycophenolic acid salt and coated tablet thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] prescription:

[0047] Sodium mycophenolate mofetil 192.4 mg

[0048] Acrylic resin No. Ⅱ 5 mg

[0049] Lactose 30 mg

[0050] Microcrystalline Cellulose 30 mg

[0051] Sodium carboxymethyl starch 40 mg

[0052] Magnesium stearate 5 mg

[0053] Silica 10 mg

[0054]Preparation method: Take the prescription amount of polyacrylic acid resin No. Ⅱ and dissolve it in an appropriate amount of absolute ethanol to prepare 0.05 g·mL -1 The solution, set aside; take the prescription amount of mycophenolate sodium mofetil, silicon dioxide, microcrystalline cellulose, lactose, and appropriate amount of sodium carboxymethyl starch in a mortar, grind and mix evenly, slowly add the above polyacrylic acid resin II No. ethanol solution, keep grinding until uniform, continue to drop an appropriate amount of absolute ethanol to prepare soft material; the obtained soft material is passed through a 18-mesh sieve to make granules, and dried at 40°C for 2 h; the obtained dry granules a...

Embodiment 2

[0056] prescription

[0057] Sodium mycophenolate mofetil 384.7 mg

[0058] Acrylic resin No. 20 mg

[0059] Lactose 65 mg

[0060] Sodium carboxymethyl starch 50 mg

[0061] Magnesium stearate 7 mg

[0062] Silica 13 mg

[0063] Preparation method: Take the prescription amount of polyacrylic acid resin No. Ⅱ and dissolve it in an appropriate amount of absolute ethanol to prepare 0.05 g·mL -1 The solution, set aside; take the prescription amount of sodium mycophenolate mofetil, silicon dioxide, lactose, and appropriate amount of sodium carboxymethyl starch in a mortar, grind and mix evenly, slowly add the above-mentioned polyacrylic acid resin No. Ⅱ ethanol solution dropwise, keep After grinding until uniform, continue to drop an appropriate amount of absolute ethanol to prepare soft material; the obtained soft material is passed through a 18-mesh sieve to make granules, and placed in 40°C for 2 h to dry; the obtained dry granules are mixed with the remaining sodium carbo...

Embodiment 3

[0065] prescription

[0066] Sodium mycophenolate mofetil 384.7 mg

[0067] Polyvinyl phthalate 50 mg

[0068] Lactose 65 mg

[0069] Croscarmellose sodium 23 mg

[0070] Magnesium stearate 7 mg

[0071] Silica 13 mg

[0072] Preparation method: Dissolve the prescription amount of polyvinyl alcohol phthalate in an appropriate amount of absolute ethanol to prepare 0.05 g·mL -1 Put the solution of mycophenolate mofetil, silicon dioxide, and lactose in the mortar, grind and mix evenly, slowly add the above-mentioned ethanol solution of polyvinyl alcohol phthalate, keep grinding until uniform, and then continue to drop Add an appropriate amount of absolute ethanol to prepare the soft material; pass the obtained soft material through a 18-mesh sieve to make granules, and dry them at 40°C for 2 hours; after mixing the obtained dry granules with croscarmellose sodium and magnesium stearate, It is compressed into tablets on a single tablet press, with a hardness of 7~10 kgf.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Hardnessaaaaaaaaaa
Hardnessaaaaaaaaaa
Login to view more

Abstract

The invention discloses a matrix-type preparation containing mycophenolic acid or a mycophenolic acid salt and a coated tablet thereof, and belongs to the technical field of medicinal preparations. The matrix-type preparation and the coated tablet thereof contain mycophenolic acid or a mycophenolic acid salt, and one or more pharmaceutically acceptable enteric polymers, one or more filling agents, one or more disintegrating agents and one or more lubricants and/or one or more adhesives. The matrix-type preparation containing mycophenolic acid or a mycophenolic acid salt and the coated tablet thereof can convey a drug to an upper end of the intestinal tract and release the drug so that precipitation of the drug in the stomach is avoided and bioavailability is improved.

Description

technical field [0001] A skeleton preparation containing mycophenolic acid or mycophenolate and its coated tablet belong to the technical field of pharmaceutical preparations. Background technique [0002] The invention relates to a matrix preparation capable of delaying the release of mycophenolic acid or mycophenolic acid salt and its coated tablet, which can release the medicine at the upper end of the intestinal tract after oral administration. [0003] The structural formula shown in formula (1) is mycophenolate sodium, which is an inhibitor of hypoxanthine monophosphate dehydrogenase, and is used for the prevention of rejection in kidney transplant patients. The active ingredient in the body is mycophenolic acid. [0004] [0005] [0006] (1) [0007] Sodium mycophenolate mofetil is a white to moon white crystalline powder, highly soluble in neutral and alkaline media, but basically insoluble in acidic media such as 0.1M hydrochloric acid solution. [0008] Due...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/00A61K9/36A61K31/365A61P37/06
Inventor 徐建国李勇张莹朱培硕付静史佳栋李晓明朱云峰张文芳
Owner WUXI FORTUNE PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap