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Sorafenib solid lipid nanoparticles and preparation method thereof

A solid lipid nano and solid lipid technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, capsule delivery, etc., can solve the problems of difficult to completely remove organic solvents, high incidence of adverse reactions, low bioavailability, etc. problems, to achieve the effect of improving bioavailability, good liver targeting, and simple preparation process

Inactive Publication Date: 2016-02-17
NANCHANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] As the only clinical dosage form at present, sorafenib tosylate tablet has been widely used in the treatment of solid cancers such as liver cancer and kidney cancer. The inhibitory effect of this dosage form on solid tumors is obvious to all, but it still has many shortcomings : not only expensive, poor tolerance, and low bioavailability, but also the incidence of adverse reactions during the application process is as high as 80%, of which the third-grade adverse events include diarrhea (8%), hypertension (2%), hand-foot Skin reactions (8%) and abdominal pain (2%)
However, the solid lipid nanoparticles prepared by the solvent evaporation method are difficult to completely remove the organic solvent, and the residual organic solvent is likely to cause certain damage to the human body.

Method used

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  • Sorafenib solid lipid nanoparticles and preparation method thereof
  • Sorafenib solid lipid nanoparticles and preparation method thereof
  • Sorafenib solid lipid nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] The preparation of embodiment 1 Sorafenib solid lipid nanoparticles

[0043] The prescription is as follows:

[0044] Sorafenib 3mg

[0045] Glyceryl Behenate 50mg

[0046] Soy Lecithin 25mg

[0047] Poloxamer 18850mg

[0048] Absolute ethanol 0.5ml

[0049] Distilled water 10ml

[0050] Prepare Sorafenib solid lipid nanoparticles: step 1, accurately weigh each component of the prescription amount, dissolve Sorafenib in a small amount of organic solvent (absolute ethanol), and then mix with glyceryl behenate Mix with soybean lecithin, heat to 85°C to melt the lipid to obtain an oil phase; step 2, add poloxamer 188 to 10ml of distilled water, and heat to the same temperature as the oil phase to form a water phase; step 3, Pour the water phase into the oil phase, shear at 11,000 rpm for 3 min, and ultrasonically break at 300 W for 3 min to obtain Sorafenib solid lipid nanoparticles.

Embodiment 2

[0051] The preparation of embodiment 2 Sorafenib solid lipid nanoparticles

[0052] The prescription is as follows:

[0053] Sorafenib 5mg

[0054] Glyceryl Behenate 100mg

[0055] Soy Lecithin 25mg

[0056] Poloxamer 18850mg

[0057] Absolute ethanol 0.5ml

[0058] Distilled water 10ml

[0059] Prepare Sorafenib solid lipid nanoparticles: step 1, accurately weigh each component of the prescription amount, dissolve Sorafenib in a small amount of organic solvent (absolute ethanol), and then mix with glyceryl behenate Mix with soybean lecithin, heat to 85°C to melt the lipid to obtain an oil phase; step 2, add poloxamer 188 to 10ml of distilled water, and heat to the same temperature as the oil phase to form a water phase; step 3, Pour the water phase into the oil phase, shear at 11,000 rpm for 3 min, and ultrasonically break at 300 W for 3 min to obtain Sorafenib solid lipid nanoparticles.

Embodiment 3

[0060] The preparation of embodiment 3 Sorafenib solid lipid nanoparticles

[0061] The prescription is as follows:

[0062] Sorafenib 5mg

[0063] Glyceryl Behenate 100mg

[0064] Soy Lecithin 25mg

[0065] Poloxamer 188 100mg

[0066] Absolute ethanol 0.5ml

[0067] Distilled water 10ml

[0068] Prepare Sorafenib solid lipid nanoparticles: step 1, accurately weigh each component of the prescription amount, dissolve Sorafenib in a small amount of organic solvent (absolute ethanol), and then mix with glyceryl behenate Mix with soybean lecithin, heat to 85°C to melt the lipid to obtain an oil phase; step 2, add poloxamer 188 to 10ml of distilled water, and heat to the same temperature as the oil phase to form a water phase; step 3, Pour the water phase into the oil phase, shear at 11,000 rpm for 3 min, and ultrasonically break at 300 W for 3 min to obtain Sorafenib solid lipid nanoparticles.

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Abstract

The invention discloses sorafenib solid lipid nanoparticles and a preparation method thereof. The sorafenib solid lipid nanoparticles are prepared from, by weight, 0.03%-0.05% of sorafenib, 0.5%-0.98% of solid lipid, 0.25%-0.75% of fat soluble emulsifier, 0.49%-0.98% of water-soluble emulsifier and the balance distilled water. Formulated amount of the components are precisely weighed, the sorafenib is dissolved in a small amount of organic solvent and then mixed with the solid lipid and the fat soluble emulsifier, heating and melting are conducted, and an oil phase is obtained; the water-soluble emulsifier is added to the distilled water, heating is conducted to reach the temperature which is the same as that of the oil phase, and a water phase is formed; the water phase is poured into the oil phase, and after high-speed shearing and ultrasonication are conducted, the sorafenib solid lipid nanoparticles are obtained. The sorafenib solid lipid nanoparticles have the advantages of being small in particle size, high in encapsulation efficiency and good in stability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a Sorafenib solid lipid nanoparticle and a preparation method thereof. Background technique [0002] Sorafenib (sorafenib) belongs to the diaryl urea class, clinically used is the tosylate salt of Sorafenib (trade name Nexavar, Nexavar), the chemical name is 4-(4-3-[4 -Chloro-3-(trifluoromethyl)phenyl]ureidophenoxy)-N2-methylpyridine-2-carboxamide-4-toluenesulfonate, the molecular formula is C 21 h 16 CIF 3 N 4 o 3 ·C 7 h 8 o 3 S, the molecular weight is 637.03g·mol -1 . Its water solubility is poor, slightly soluble in ethanol, soluble in polyvinyl glycerol 400 (PEG400). Sorafenib can target a variety of serine / threonine kinases and receptor tyrosine kinases on tumor cells and tumor blood vessels, and simultaneously exert dual effects of anti-angiogenesis and anti-tumor cell proliferation: Sorafenib On the one hand, it can inhibit the r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/44A61K47/34A61K47/24A61K47/14A61P35/00
Inventor 谢宝刚王慧韵王海鹏刘亚兰余梦杰
Owner NANCHANG UNIV