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

Stable lenvatinib pharmaceutical composition and preparation method thereof

A technology of lenvatinib and its composition, which is applied in the field of lenvatinib pharmaceutical composition and its preparation, can solve the problems of dissolution hysteresis, easy decomposition, unstable chemical properties, etc., and achieve low loss of volatile components and inhibit Effects of Growth and Enzyme Action

Inactive Publication Date: 2017-04-05
TIANJIN HANKANG PHARMA BIOTECH
View PDF0 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Lenvatinib has hygroscopicity, its chemical properties are unstable under humidification and heating conditions, and it is easy to decompose, and the surface of the drug is prone to gelation, and the dissolution lag is caused by moisture absorption

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
  • Stable lenvatinib pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The prescription composition of Lenvatinib Tablets Lenvatinib 10g

[0029] Hydroxypropyl-α-CD 30g

[0030] Starch slurry 50g

[0031] Povidone 36g

[0032] Lactose 90g

[0033] Talc powder 4g

[0034] Makes 1000 pieces

[0035] Specific preparation method:

[0036] a. Weigh the prescribed amount of hydroxypropyl-α-CD cyclodextrin and dissolve it in pure water, weigh the prescribed amount of lenvatinib and add it to the dissolved cyclodextrin, and stir until the solution is clear and transparent to form lenvatinib cyclodextrin Inclusion compound, freeze-dried, pre-frozen at -40°C, 85Pa, vacuumed at -20°C, dried at 100 Pa, 20°C to obtain freeze-dried mixture Ⅰ;

[0037] b. Crush the freeze-dried mixture I, pass through a 100-mesh sieve, add starch slurry, povidone, and lactose according to the prescription ratio, mix for more than 5 minutes, then add talcum powder, and mix for more than 1 minute to obtain mixture II;

[0038] c. Put the mixture II into a dry granul...

Embodiment 2

[0049] Lenvatinib 10g

[0050] Hydroxypropyl-γ-CD 50g

[0051] Hypromellose 40g

[0052] Sodium carboxymethyl starch 20g

[0053] Mannitol 76g

[0054] Magnesium Stearate 4g

[0055] Specific preparation method:

[0056] a. Weigh the prescribed amount of hydroxypropyl-γ-CD cyclodextrin and dissolve it in pure water, weigh the prescribed amount of lenvatinib and add it to the dissolved cyclodextrin, stir until the solution is clear and transparent, and form lenvatinib cyclodextrin Inclusion compound, freeze-dried, pre-frozen at -30°C, vacuumed at 75 Pa, -20°C, dried at 90 Pa, 20°C to obtain freeze-dried mixture I;

[0057] b. Crush the freeze-dried mixture I, pass through a 100-mesh sieve, add hydroxypropyl cellulose, mannitol, and sodium carboxymethyl starch according to the prescription ratio, mix for more than 5 minutes, then add magnesium stearate, and mix for more than 1 minute, Obtain mixture II;

[0058] d. Put mixture II in a dry granulator to granulate, add the re...

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
hardnessaaaaaaaaaa
Login to View More

Abstract

The invention discloses a stable lenvatinib pharmaceutical composition and a preparation method thereof. The pharmaceutical composition consists of a cyclodextrin inclusion of an active ingredient lenvatinib and other pharmaceutically acceptable carriers; and the pharmaceutical composition is prepared by virtue of a freeze-drying dry granulation process by strictly controlling temperature and humidity in a preparation process. According to the lenvatinib pharmaceutical composition and the preparation method thereof, the lenvatinib is included in cyclodextrin, and meanwhile the preparation process of freeze-drying and dry granulation is adopted, so that the shortcomings of the lenvatinib, as a main drug, which is capable of absorbing moisture quite easily and quite poor in stability and cannot be prepared into an oral preparation, can be greatly overcome, and meanwhile, influence on disintegration and the dissolution of ingredients of the main drug can be avoided; and the finished lenvatinib pharmaceutical composition, which is not a coated tablet, can avoid the shortcoming of a conventional coated tablet which is relatively slow in dissolution.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral lenvatinib pharmaceutical composition and a preparation method thereof. Background technique [0002] Lenvatinib (E7080) is a multi-target inhibitor, most effective on VEGFR2(KDR) / VEGFR3(Flt-4), less effective on VEGFR1 / Flt-1, more effective on VEGFR2 / 3 than FGFR1, PDGFRα / β selectivity is about 10 times higher. E7080 potently inhibits angiogenesis and also significantly inhibits VEGF / KDR and SCF / KIT signaling pathways. According to in vitro receptor tyrosine and ser / threonine kinase assays, E7080 inhibits Flt-1, KDR, and Flt-4. Besides these kinases, E7080 also inhibits FGFR1 and PDGFR tyrosine kinases. [0003] The FDA approved lenvatinib for the treatment of patients with aggressive, differentiated thyroid cancer (DTC) whose disease has progressed despite radioactive iodine therapy (radioiodine-refractory disease). [0004] Lenvatinib ...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/47A61K47/69A61P35/00
Inventor 严洁
Owner TIANJIN HANKANG PHARMA BIOTECH
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