Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Methotrexate oral disintegrating tablet and its preparation method

A technology for oral disintegrating tablets and methotrexate, which is applied in the field of pharmaceutical compositions containing methotrexate, and can solve the problems of slow disintegration speed, low dissolution rate, low bioavailability and the like

Inactive Publication Date: 2006-04-05
马晶
View PDF0 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The reasons for the low bioavailability of ordinary methotrexate tablets are related to the disadvantages of slow disintegration and low dissolution rate

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
  • Methotrexate oral disintegrating tablet and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Methotrexate 2.5g

[0050] Sodium carboxymethyl starch 13.5g

[0051] Microcrystalline Cellulose 42.5g

[0052] Mannitol 6.7g

[0053] Magnesium stearate 0.9g

[0054] Made into 1000 pieces

[0055] Methotrexate, microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate, and mannitol all pass through a 100-mesh sieve.

[0056] Weigh 2.5 grams of methotrexate, first mix it with 14 grams of carboxymethyl starch sodium in equal increments, then add 42 grams of microcrystalline cellulose and mix thoroughly, then mix it with 6.7 grams of mannitol and 0.9 grams of stearic acid Magnesium mix well. Detect the percentage content of methotrexate in the mixed powder, calculate the weight of the tablet, and press it into a tablet. In this way, 1000 orally disintegrating tablets of methotrexate can be compressed.

[0057] Its disintegration time is 28 seconds, and its dissolution rate is 91.9% in 15 minutes.

Embodiment 2

[0059] Methotrexate 5.0g

[0060] Sodium carboxymethyl starch 16g

[0061] Microcrystalline Cellulose 38g

[0062] Mannitol 7.8g

[0063] Magnesium stearate 1.2g

[0064] Made into 1000 pieces

[0065] Methotrexate, microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate, and mannitol all pass through a 100-mesh sieve.

[0066] Weigh 5.0 grams of methotrexate, first mix with 16 grams of sodium carboxymethyl starch in equal increments, then add 38 grams of microcrystalline cellulose and mix thoroughly, then successively add 7.8 grams of mannitol and 1.2 grams of magnesium stearate Mix well. Detect the percentage content of methotrexate in the mixed powder, calculate the weight of the tablet, and press it into a tablet. In this way, 1000 orally disintegrating tablets of methotrexate can be compressed.

[0067] Its disintegration time is 32 seconds, and its dissolution rate is 93.1% in 15 minutes.

Embodiment 3

[0069] Methotrexate 2.5g

[0070] Sodium carboxymethyl starch 13.5g

[0071] Microcrystalline Cellulose 37.5g

[0072] Mannitol 13g

[0073] Magnesium Stearate 1.1g

[0074] Made into 1000 pieces

[0075] Methotrexate, microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate, and mannitol all pass through a 100-mesh sieve.

[0076] Weigh 2.5 grams of methotrexate, first mix it with 13.5 grams of carboxymethyl starch sodium in equal increments, then add 37.5 grams of microcrystalline cellulose and mix thoroughly, then successively add 13 grams of mannitol and 1.1 grams of magnesium stearate Mix well. Detect the percentage content of methotrexate in the mixed powder, calculate the weight of the tablet, and press it into a tablet. In this way, 1000 orally disintegrating tablets of methotrexate can be compressed.

[0077] Its disintegration time is 35 seconds, and its dissolution rate is 92.9% in 15 minutes.

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

No PUM Login to View More

Abstract

The invention provides a methotrexate oral disintegrating tablet for rapid disintegrating in oral cavity without water, which is prepared by comminuting methotrexate, sodium carboxymethylstarch, crystalline cellulose, mannitol, magnesium stearate, passing through 100 mesh sieves, mixing homogeneously, and pelleting directly.

Description

Technical field: [0001] The invention relates to a pharmaceutical composition containing methotrexate, and relates to an improved technique for oral preparations of methotrexate. technical background: [0002] Methotrexate has been used clinically for decades, and it has been used to treat leukemia and antitumor drugs, including various types of acute leukemia, especially acute lymphoblastic leukemia, malignant lymphoma, non-Hodgkin's Lymphoma and mycosis fungoides, multiple myelopathy, head and neck cancer, lung cancer, various soft tissue sarcomas, psoriasis; breast cancer, ovarian cancer, cervical cancer, malignant mole, choriocarcinoma, testicular cancer, etc. . In recent years, methotrexate, as an immunosuppressant, has been widely used in the treatment of active rheumatoid arthritis and other autoimmune diseases. [0003] Methotrexate is poorly soluble in water, and its bioavailability in vivo is related to its dissolution characteristics in vitro. At present, the o...

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): A61K31/519A61K9/20A61P35/00
Inventor 马晶
Owner 马晶
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com