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Arsenic trioxide solid lipid nano granule and formulation

A technology of solid lipid nanometer and arsenic trioxide, which is applied in the directions of liposome delivery, liquid delivery, medical preparations of inactive ingredients, etc., can solve problems such as poor solubility and stability, improve compliance, solve stability problems, The effect of reducing medication costs and risks

Inactive Publication Date: 2012-03-07
HANGZHOU MINSHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention solves the stability problem caused by the poor solubility of the drug at low temperature through the formulation of arsenic trioxide solid lipid nanoparticles, its preparation and preparation method

Method used

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  • Arsenic trioxide solid lipid nano granule and formulation
  • Arsenic trioxide solid lipid nano granule and formulation
  • Arsenic trioxide solid lipid nano granule and formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The prescription consists of:

[0051]

[0052] Preparation method: Heating glyceryl tristearate and lecithin in a water bath at 40-100°C until melting, adding arsenic trioxide pulverized by ball milling, and dispersing evenly; rapidly cooling the drug-containing melt with dry ice or liquid nitrogen, passing through ball milling or milk Bowl milling grinds solid drug-containing lipids into particles; dissolves Poloxamer 188 and EDTA-2Na in distilled water to make a water phase, and then disperses the solid lipid particles into a low-temperature water phase to form primary Suspension: Finally, the primary suspension is subjected to high-pressure homogenization at room temperature or below room temperature to obtain a suspension that can be used to prepare the final product.

[0053] Check: the encapsulation rate of nanoparticles is 93.4%, the average particle size of nanoparticles is 190nm, see the attached figure 1 , Zeta potential -29mV, see attached figure 2 . ...

Embodiment 2

[0055] The prescription consists of:

[0056] Preparation method: heat glyceryl tristearate, glyceryl distearate, and lecithin in a water bath at 40-100°C until melting, add arsenic trioxide pulverized by ball milling, and disperse evenly; mix evenly as the oil phase; Mu 188 and EDTA-2Na are fully dispersed in water, heated to the same temperature as the oil phase as the water phase; add the oil phase to the water phase under high-speed stirring, and continue to stir for a certain period of time to form colostrum; high-pressure homogenization for 2 to 10 times; Cool to room temperature to obtain a suspension that can be used to prepare the final product.

[0057] Inspection: the encapsulation efficiency of the nanoparticles is 91.5%, the average particle size of the nanoparticles is 200nm, and the Zeta potential is -29mV.

Embodiment 3

[0059] The prescription consists of:

[0060] Preparation method: heat stearic acid, glyceryl palmitate, and lecithin in a water bath at 40-100°C to melt, add arsenic trioxide pulverized by ball milling, and mix uniformly as an oil phase; poloxamer 188, Tween-80, Dissolve glycerin and EDTA-2Na in water, heat to the same temperature as the oil phase as the water phase; add the oil phase to the water phase under stirring, and stir gently to form a transparent nanoemulsion, and then disperse the hot nanoemulsion in In cold water (2-3°C), a suspension that can be used to prepare the final product is obtained. Inspection: the encapsulation efficiency of the nanoparticles is 90.8%, the average particle size of the nanoparticles is 162nm, and the Zeta potential is -31mV.

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Abstract

The invention discloses a solid lipid nanoparticle of arsenic trioxide which is more stable and more suitable for clinical application, and a preparation thereof and a preparation method thereof. The solid lipid nanoparticle contains arsenic trioxide, phospholipid, an emulsifier, a co-emulsifier, solid lipid material and an antioxidant by the ratio of 0.1-10%: 1-30%: 1-20%: 0-5%: 2-20%: 0.001-0.5% (by weight / volume). The solid lipid nanoparticles of arsenic trioxide can be applied to the preparation of the anti-tumor solid or liquid pharmaceutical preparations, and can be further made into solid preparations or liquid preparations which are more suitable for clinical application, especially for oral preparations. With regard to the preparation method of the solid lipid nanoparticle of arsenic trioxide, the cold homogenization technique, the high pressure homogenization technique, the fusion ultrasonic method and the microemulsion technique and the like can be used for preparing suspension; or the suspension is further added with the freeze-dried support, frozen and dried, thus obtaining a freeze dried solid lipid nanoparticle product of arsenic trioxide.

Description

technical field [0001] The invention relates to an antitumor drug arsenic trioxide, in particular to a solid lipid nanoparticle of arsenic trioxide, its preparation and a preparation method. Background technique [0002] Arsenic trioxide (As 2 o 3 ) commonly known as arsenic, is a poisonous substance, but also blindly ancient Chinese medicine. Since it was experimentally used to treat acute promyelocytic leukemia (APL) in the 1970s, it has been gradually accepted and widely used clinically. At present, both SFDA and FDA have approved its production and sales as an anti-tumor drug for the treatment of APL. The research on the treatment of solid tumors by arsenic trioxide is also being further deepened. Existing research results have shown that arsenic trioxide can inhibit the growth and induce apoptosis of some solid tumor cells such as gastric cancer, colon cancer, and lung cancer. In September 2004, SFDA approved the addition of arsenic trioxide injection as a new indic...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K33/36A61K9/10A61K47/24A61P35/00
Inventor 李青坡何佳奇阮建山杜斯文
Owner HANGZHOU MINSHENG PHARM CO LTD
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