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
CN110623927AInactive Publication Date: 2019-12-31江苏世博生物医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
江苏世博生物医药科技有限公司
Publication Date
2019-12-31
Estimated Expiration
Not applicable · inactive patent

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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.
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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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