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Nintedanib nano lipid carrier with high bioavailability and preparation method thereof

A nano-lipid carrier, nintedanib technology, applied in liposome delivery, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of low oral bioavailability of nintedanib

Inactive Publication Date: 2019-12-31
江苏世博生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problem of low oral bioavailability of nintedanib, aiming at the above-mentioned prior art, the present invention provides a curcumin nano-lipid carrier with high bioavailability, and a preparation method thereof

Method used

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  • Nintedanib nano lipid carrier with high bioavailability and preparation method thereof
  • Nintedanib nano lipid carrier with high bioavailability and preparation method thereof
  • Nintedanib nano lipid carrier with high bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Weigh 1250 mg of glyceryl monooleate and 625 mg of glyceryl tricaprylate into a small beaker, place it in a water bath at 67°C, and stir at 600 rpm / min to melt. Add Tween-80660mg and continue to stir for 5 min. Add 50mg nintedanib and continue to stir for 1 hour to obtain the medicated oil phase. Take an appropriate amount of distilled water, add 225mg Tween-80, and preheat at the same temperature to obtain the water phase. Slowly add the water phase to the oil phase and continue stirring for 3 minutes. The nintedanib nano lipid carrier with high bioavailability of the present invention is obtained by sonicating at 30% power for 13 minutes and solidifying in an ice bath for 6 minutes.

[0031] Results: The particle size of the high bioavailability nintedanib nanolipid carrier was 145.4±3.1nm. The encapsulation rate is 87.5%, and the drug loading is 5mg / ml.

Embodiment 2

[0033] Referring to the preparation method of Example 1, the difference is that the solid lipid materials are not selected from glyceryl trilaurate, glyceryl monostearate, and glyceryl behenate.

[0034] Table 1 The effect of solid lipids on the high bioavailability nintedanib lipid carrier (n=3)

[0035]

[0036]

Embodiment 3

[0038] Referring to the preparation method of Example 1, the difference is that the liquid lipid materials were selected as caprylic acid capric acid triglyceride, medium chain oil, polyglyceryl oleate, oleic acid, soybean oil, and caprylic acid capric acid polyethylene glycol. Glycerides.

[0039] Table 2 The effect of liquid lipids on the high bioavailability nintedanib lipid carrier (n=3)

[0040]

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Abstract

The invention discloses a nintedanib nano-lipid carrier with high bioavailability and a preparation method thereof. The nano lipid carrier comprises nintedanib, a solid lipid material, a liquid lipidmaterial, a surfactant and an absorption promoter. The preparation scheme comprises the following steps: heating solid and liquid lipids in a water bath at a certain temperature, and stirring until the solid and liquid lipids are molten; and adding a surfactant, and continuously stirring for 5 minutes; adding nintedanib, and stirring for 1h to obtain a drug-containing oil phase; adding part or allof the surfactant into a water phase, preheating at the same temperature, and adding the water phase into the drug-containing oil phase while stirring; after probe ultrasonic treatment, performing ice-water bath curing, and obtaining the product. The prepared nintedanib nano lipid carrier is simple in scheme, free of organic solvents, high in drug loading capacity, uniform in particle size and particle size distribution and good in stability, intake of nintedanib by small intestine epithelial cells can be remarkably increased, and in-vivo bioavailability is effectively improved.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations and biomedicine technology, in particular to a nintedanib nano lipid carrier with high bioavailability and a preparation method thereof. Background technique [0002] Idiopathic pulmonary interstitial fibrosis (IPF) is a type of disease with unknown etiology, characterized by progressive dyspnea and deterioration of lung function. At present, there is no definite and effective treatment method for IPF other than lung transplantation. Without lung transplantation, the 3-year and 5-year mortality rates are 50% and 80%, respectively. [0003] Nintanib is a triple tyrosine kinase inhibitor and growth factor antagonist. It is used to treat idiopathic pulmonary fibrosis that can only be treated by lung transplantation in the medical community. It is a new research result in the treatment of IPF. Nintedanib is a p-gp substrate and has a first pass effect. It has poor solubility in the small intestin...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/496A61P11/00
CPCA61K9/1277A61K31/12A61K31/496A61P11/00
Inventor 何海冰
Owner 江苏世博生物医药科技有限公司
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