Nintedanib self-microemulsion preparation and soft capsule thereof and preparation method

A technology for nintedanib and emulsion preparations, which is applied in the directions of capsule delivery, pharmaceutical formulation, emulsion delivery, etc., can solve the problem of difficulty in improving the bioavailability of such drugs, so as to improve the bioavailability, speed and degree of , the effect of obvious social benefit

Active Publication Date: 2017-09-22
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dosage form plays a decisive role in the absorption of this type of drug in the gastrointestinal tract. Traditional tablets are difficult to improve the bioavailability of this type of drug. Appropriate dosage form is the key to the successful development of this type of drug product

Method used

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  • Nintedanib self-microemulsion preparation and soft capsule thereof and preparation method
  • Nintedanib self-microemulsion preparation and soft capsule thereof and preparation method
  • Nintedanib self-microemulsion preparation and soft capsule thereof and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Propylene glycol monocaprylate (Capryol 90) is used as the oil phase, polyoxyethylene 40 hydrogenated castor oil (RH40) is used as the emulsifier, and propylene glycol (PG) is used as the co-emulsifier. Mix the emulsifier and co-emulsifier evenly in the weight ratio of 2:1, 1:1, 1:2, and then mix it with the oil phase in the weight ratio of 1:9, 2:8, 3:7, 4:6, 5:5 , 6:4, 7:3, 8:2, 9:1 mixed at 50r·min -1 Drop into water preheated to 37°C while stirring, and observe the state of microemulsion. Record the changes and states of the mixing system in different proportions, and limit the proportion of emulsifier to 20%-40%, the proportion of co-emulsifier to more than 20%-60%, and the proportion of oil phase to 10%-30%. These proportioning data draw the ternary phase diagram, and select the effective area of ​​the blank self-microemulsion and the effective area of ​​nintedanib self-microemulsion, see figure 1 Middle shaded part.

[0034] From figure 2 It can be seen tha...

Embodiment 2

[0037] Prescription of nintedanib self-microemulsion preparation with nintedanib concentration of 2%

[0038] Select raw materials according to the following proportions:

[0039]

[0040] Preparation method: Dissolve the prescribed amount of nintedanib in the prescribed amount of PG, add the prescribed amount of MCT and RH40, mix well, and obtain nintedanib self-microemulsion preparation.

[0041]The prepared nintedanib self-microemulsion preparation is a colorless uniform transparent liquid. Take the prepared nintedanib self-microemulsion preparation, dilute 100 times with water, measure the particle size, and the average particle size is 18.3nm. Take nintedanib self-microemulsion 5ml, at 50r min -1 Add 10 times the amount of water at 37°C under stirring, and the self-microemulsion stock solution can be completely emulsified within 1 minute, forming a transparent O / W type microemulsion with slightly bluish light, and at 50r·min -1 It remained stable for 8 hours under s...

Embodiment 3

[0043] Prescription of nintedanib self-microemulsion preparation with nintedanib concentration of 2.5%

[0044] Select raw materials according to the following proportions:

[0045]

[0046] Preparation method: Dissolve the prescribed amount of nintedanib in the prescribed amount of PG, add the prescribed amount of MCT and RH40, mix well, and obtain nintedanib self-microemulsion preparation.

[0047] The prepared nintedanib self-microemulsion preparation is a colorless uniform transparent liquid. Take the prepared nintedanib self-microemulsion preparation, dilute 100 times with water, measure the particle size, and the average particle size is 18.1nm. Take nintedanib self-microemulsion 5ml, at 50r min -1 Add 10 times the amount of water at 37°C under stirring, and the self-microemulsion stock solution can be completely emulsified within 1 minute, forming a transparent O / W type microemulsion with slightly bluish light, and at 50r·min -1 It remained stable for 8 hours unde...

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Abstract

The invention provides a Nintedanib self-microemulsion preparation and a soft capsule thereof and a preparation method. The concentration of nintedanib in the nintedanib self-microemulsion preparation is 2%-3% by mass; the proportion of oil phase in the nintedanib self-microemulsion preparation is 20%-40% (w / w); the proportion of co-emulsifier in the nintedanib self-microemulsion preparation is 20%-60% (w / w); the proportion of stabilizer in the nintedanib self-microemulsion preparation is 0-3% (w / w). by means of the self-microemulsion technology, the prepared Nintedanib self-microemulsion preparation is used to produce the soft Nintedanib self-microemulsion capsule. Since the Nintedanib self-microemulsion preparation can be quickly emulsified after encountering with gastrointestinal aqueous environment, the irritation generated after long contact of drugs and gastrointestinal tracts is reduced; meanwhile, the self-microemulsion drug delivery system can not only improve the dissolution rate of drugs, but increase the absorption rate and degree of drugs, and therefore, the bioavailability of drugs is higher.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparation research, and in particular relates to a nintedanib self-microemulsion preparation, a soft capsule made from it and a preparation method. Background technique [0002] In June 2014, Boehringer Ingelheim announced that the marketing authorization application for nintedanib ethanesulfonate for the treatment of idiopathic pulmonary fibrosis (IPF) was confirmed by the European Medicines Agency (EMA), and EMA was included in the accelerated approval list. On October 15, 2014, the US Food and Drug Administration FDA approved nintedanib ethanesulfonate (trade name: Ofev) a new oral drug for the treatment of idiopathic pulmonary fibrosis (IPF). [0003] The chemical name of nintedanib is (3Z)-2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazolyl)acetyl]amino]phenyl ]amino]benzylidene]-2-oxo-1H--methyl indole-6-carboxylate, its structural formula is: [0004] [0005] Based on the classificati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/48A61K47/14A61K47/44A61K47/10A61K47/32A61K47/26A61K47/22A61K31/496A61P11/00
CPCA61K9/1075A61K9/4858A61K9/4866A61K31/496A61K47/10A61K47/14A61K47/22A61K47/26A61K47/32A61K47/44
Inventor 许颖冯文骁何洮凤刘宏飞逯胜哲
Owner JIANGSU UNIV
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