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Sorafenib drug lipid nanosuspension and preparation method thereof

A nano-suspension, sorafenib technology, applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of low oral bioavailability, poor water solubility, obvious absorption effects, etc., to achieve Good biocompatibility and safety, simple prescription, and improved absorption in the body

Active Publication Date: 2019-01-15
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In order to improve its solubility in water, it is clinically made into tosylate, but the water solubility is still poor, the oral bioavailability is low, less than 10%, and the diet has a significant impact on its absorption
[0008] In addition, from basic research to clinical application of nanosuspensions, there are still many difficulties in whether the improvement of its bioavailability, drug safety and effectiveness can be realized.

Method used

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  • Sorafenib drug lipid nanosuspension and preparation method thereof
  • Sorafenib drug lipid nanosuspension and preparation method thereof
  • Sorafenib drug lipid nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] The screening of stabilizer in the preparation of embodiment 1 Sorafenib nanosuspension

[0063] The basic prescription of Sorafenib nano-suspension is: phospholipid concentration is 10mg / mL; drug-to-lipid ratio is 1:10; auxiliary stabilizer dosage is 1%; organic phase water phase volume ratio is 1:10; 5mL / min; magnetic stirring speed 800r / min; ice bath.

[0064] The basic prescription was optimized by single factor investigation, and the auxiliary stabilizer of Sorafenib lipid nanosuspension was screened. The particle size and particle size distribution were the main factors to be investigated, and its shape and uniformity were observed to examine its formulation and process. , and the results are shown in Table 1.

[0065] Table 1 The impact of the type of auxiliary stabilizer on the particle size and potential of Sorafenib lipid nanosuspension

[0066]

[0067] It can be seen from Table 1 that when Tween-80 is used as an auxiliary stabilizer, the obtained partic...

Embodiment 2

[0071] The preparation of embodiment 2 Sorafenib lipid nanosuspension--nanoprecipitation method

[0072] Weigh 9 mg of sorafenib and 75 mg of phospholipids in 1 mL of methanol as the methanol phase; dissolve Tween-80 in water to obtain a 1.5% (g / 100 mL) Tween solution as the water phase. Under the condition of magnetic stirring in an ice bath, the methanol phase was slowly added dropwise at a rate of 5mL / min into the 10mL water phase. After the dropwise addition, the methanol was evaporated to obtain a lipid nanosuspension of Sorafenib.

[0073] The above-mentioned prepared Sorafenib lipid nanosuspension has an average particle diameter of 164.5nm, a polydispersity coefficient of 0.202, a drug loading of 10.8%, potential-11.2mV, and a particle size distribution of figure 1 shown.

[0074] Get an appropriate amount of Sorafenib lipid nanosuspension prepared above, drop it on the copper grid, carry out negative staining with 2% phosphotungstic acid, observe under the transmissi...

Embodiment 3

[0075] Preparation of Example 3 Sorafenib Lipid Nanosuspension--High Pressure Homogenization

[0076] Accurately weigh 250 mg of phospholipids and Tween-80 and add them to 50 mL of distilled water (the concentration of Tween-80 is 1.0% (g / 100 mL)) to dissolve to form a dispersion medium (solution A). Add 25 mg of sorafenib and disperse uniformly by ultrasonic to obtain suspension B. Continue to use high-speed shearing machine 20000r / min high-speed shearing for 3min to prepare suspension C. Then suspension C is adopted high-pressure homogeneous method, circulates 5 times at 200bar respectively, 1000bar circulates 15 times, makes Sorafenib lipid nanosuspension, average particle diameter is 178.6nm, polydispersity coefficient 0.199, loaded The dose is 11.2%, and the potential is -10.2mV.

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Abstract

The invention discloses a sorafenib medicinal lipid nanosuspension and a preparation method of the sorafenib medicinal lipid nanosuspension. The sorafenib medicinal lipid nanosuspension is prepared by adopting a nanoprecipitation method or / and a high-pressure homogenization method, wherein phospholipids and tween-80 are taken as stabilizers. The prepared sorafenib lipid nanosuspension is good in biocompatibility, high in drug loading capacity, and small in grain diameter; freeze-drying can be realized only by adding a small amount of freeze-drying protective additive; the freeze-dried product is good in reconstruction property; for the prepared sorafenib lipid nanosuspension, the in-vivo tissue distribution of the medicine can be improved, the distribution of the medicine in the liver and tumor can be obviously enhanced, and thus the anti-tumor effect of the sorafenib lipid nanosuspension can be obviously enhanced; the preparation condition is mild, simple and controllable, and thus the development prospect is wide.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a sorafenib drug lipid nanosuspension and a preparation method thereof. Background technique [0002] Cancer is a major disease that threatens human health and life. Liver cancer is one of the five most common cancers in the world, and its death rate ranks third among all cancers, second only to lung cancer and gastric cancer. Most patients with advanced liver cancer lack effective systemic treatment measures, and drug therapy plays an irreplaceable role in the treatment of liver cancer. In recent years, molecular targeted drugs have achieved remarkable therapeutic effects in clinical practice, and have received close attention from researchers. [0003] Sorafenib is a new type of diaryl urea and oral multi-target molecular targeted drug, which has created a milestone in the systemic treatment of liver cancer. Sorafenib, as a multi-target multi-kinase small...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K9/19A61K47/24A61K47/26A61K31/44A61P35/00
CPCA61K9/10A61K9/19A61K31/44A61K47/24A61K47/26
Inventor 张娜杨绍梅张波苏志会肖亚男王天琪
Owner SHANDONG UNIV
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