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Eriocalyxin B nanosuspension and preparation method thereof

A technology of nanosuspension and calyxin, which is applied in emulsion delivery, freeze-drying delivery, drug combination, etc., can solve safety problems and other problems, and achieve the effect of changing the distribution in the body, good stability, and small dosage

Active Publication Date: 2013-09-18
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although adopting cyclodextrin inclusion technology, surfactant solubilization (micelle), emulsion, microemulsion, liposome and solid dispersion technology etc. all can solve the solubility and dissolution rate problem of some poorly soluble drugs, but for water, All oils are not easy to dissolve eelin, these methods and technologies still have relatively large limitations, and the used solubilizers, emulsifiers, etc. often bring some safety problems

Method used

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  • Eriocalyxin B nanosuspension and preparation method thereof
  • Eriocalyxin B nanosuspension and preparation method thereof
  • Eriocalyxin B nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Airflow pulverization is carried out on the crude drug of echinocetin to obtain a fine powder with a particle diameter of less than 5 μm.

[0072] Add 200 mg of echinacein micropowder into 20 g of aqueous solution containing 0.1% (w / w) egg yolk lecithin, and process it in a shear emulsifier at 5000 rpm for 3 min to obtain a suspension.

[0073] The suspension was processed by a high-pressure homogenizer, and the homogenization conditions were 3 cycles at 300 bar, 3 cycles at 500 bar, 5 cycles at 1000 bar, and 10 cycles at 1500 bar to obtain a nanosuspension with an average particle size of 110 nm.

Embodiment 2

[0075] Airflow pulverization is carried out on the crude drug of echinocetin to obtain a fine powder with a particle diameter of less than 5 μm.

[0076] Add 200mg of echinacein micropowder to 20g aqueous solution containing 1% (w / w weight) egg yolk lecithin and 5% (w / w weight) lactose, and process it at 1000rpm for 3min in a shear emulsifier to obtain a suspension liquid.

[0077] The suspension is processed by a high-pressure homogenizer to further reduce and homogenize the particle size. The homogenization conditions are 3 times of 300bar circulation, 3 times of 500bar circulation, 5 times of 1000bar circulation, and 10 times of 1500bar circulation, and the average particle size is 110nm. nanosuspension. The nano-suspension was freeze-dried for 48 hours to obtain a dried product of the nano-suspension.

[0078] Adding 20 g of water for injection can reconstitute and form a nanosuspension with an average particle size of 110 nm.

Embodiment 3

[0080] 20 g of water, 50 mg of Poloxamer 188, 30 mg of Tween 80, 500 mg of echinacein and 20 g of stainless steel beads with a diameter of 0.5 mm were added to the mill. Start the mill, mill at 2000rpm for 45min, and filter to obtain a suspension with an average particle size of 140nm.

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Abstract

The invention discloses eriocalyxin B nanosuspension and a preparation method thereof. The eriocalyxin B nanosuspension is characterized by comprising a therapeutic effective dose of eriocalyxin B nano-suspension anhydrous substance and water or other injectable solution; and the eriocalyxin B nanosuspension anhydrous substance comprises eriocalyxin B, surface active agent, additive and an drying supporting agent, wherein the weight ratio of the eriocalyxin B to the surface active agent is 1:0.05-1:5. In the invention, the problem of the solubility of the eriocalyxin B is solved, the prepared agent can be free of organic solvent, and the dose of the surface active agent is small; moreover the nanosuspension can also change the distribution of the medicament in vivo and reduce toxic and side effect; and the prepared nanosuspension anhydrous substance has favorable stability.

Description

technical field [0001] The invention relates to a calyxin preparation. technical background [0002] Folks have used the Lamiaceae Amygdala plant as an antineoplastic drug. Academician Sun Handong of Kunming Institute of Botany, Chinese Academy of Sciences, on the basis of more than 20 years of chemical research work, extracted and isolated the effective anti-tumor monomer eriocalyx from the calyx calyx and the endemic species in Yunnan. The results of in vivo and in vitro anti-tumor activity tests conducted by Shanghai Institute of Pharmaceutical Industry, Academy of Military Medical Sciences, and Shanghai Institute of Materia Medica, Chinese Academy of Sciences show that calyxin has a broad-spectrum anti-tumor effect, and has a broad-spectrum anti-tumor effect on ovarian cancer, breast cancer, cervical cancer, Intestinal cancer, lung cancer, gastric cancer, liver cancer, prostate cancer and leukemia cell lines all have significant proliferation inhibitory effects; mouse i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K9/14A61K9/19A61K31/35A61P35/00
Inventor 侯惠民孙汉董朱兆云王健陈芳普建新夏怡然
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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