2-methoxyestradiol nanosuspension frozen powder and preparation method thereof

A technology of methoxyestradiol and nanosuspension, applied in the field of medicine, can solve the problems of difficult to achieve high drug loading and targeting effect, low oral bioavailability, poor water solubility, etc., and achieve good long-term stability , Conducive to long-term storage and transportation, the effect of high drug content

Inactive Publication Date: 2009-12-30
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In view of the above situation, in order to overcome the defects of the prior art, the main purpose of the present invention is to provide a kind of 2-methoxyestradiol nanosuspension which can be directly used for intravenous injection and is easy to prepare, good in stability and remarkable in effect. The freeze-dried powder and its preparation method effectively solve the problems of poor water solubility, short half-life, low oral bioavailability, and difficulty in achieving high drug loading and targeting effects in common injections in 2-methoxyestradiol. The technical solution to solve is: 2-methoxyestradiol nano-suspension freeze-dried powder of the present invention is calculated by weight ratio: 1 part of 2-methoxyestradiol, 1 to 50 parts of surfactant , lyoprotectant composed of 3 to 30 parts

Method used

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  • 2-methoxyestradiol nanosuspension frozen powder and preparation method thereof
  • 2-methoxyestradiol nanosuspension frozen powder and preparation method thereof
  • 2-methoxyestradiol nanosuspension frozen powder and preparation method thereof

Examples

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Embodiment 1

[0030] Weigh 600mg of poloxamer 188, add it to 20ml of phosphate buffered saline (PBS buffer), heat at a slight temperature (30-40°C) to dissolve it completely, add micronized 2-methoxyestradiol under magnetic stirring Diol raw material 150mg, 10000rpm internal homogenizer pre-emulsification for 5min to obtain the primary suspension; the primary suspension was subjected to high-pressure emulsification, the conditions were 9k psi cycle 3 times, 12k psi cycle 3 times, 18k psi Cycle 20 times to obtain a milky white nanosuspension, dissolve 1000mg trehalose in the nanosuspension, sterilize with Co-60, sub-package in vials, pre-freeze at -80°C for 10 hours, and then freeze-dry for 12 hours to obtain freeze-dried powder. The lyophilized powder was reconstituted with water for injection, the average particle size was 320nm, and the Zeta potential was -25.68mV.

[0031] The in vitro release results of the product of this example are shown in Table 1, and the results show that the pre...

Embodiment 2

[0033] Weigh 600mg of Poloxamer 188 and 300mg of Tween80, add it into 20ml of phosphate buffered saline (PBS buffer), heat at a slight temperature (30-40°C) to dissolve it completely, add micronized 2-formazol under magnetic stirring Oxyestradiol bulk drug 150mg, 10000rpm in-cut homogenizer pre-emulsification for 5min to obtain the primary suspension; the primary suspension was subjected to high-pressure emulsification, the conditions were 9k psi cycle 3 times, 12k psi cycle 3 times , 18k psi cycled 20 times to obtain a milky white nanosuspension. Dissolve 1000mg of mannitol in the nanosuspension, sterilize it with Co-60, divide it into vials, pre-freeze at -20°C for 10 hours, then freeze-dry it for 12 hours and take it out , to obtain freeze-dried powder. The lyophilized powder was reconstituted with water for injection, the average particle size was 290nm, and the zeta potential was -33.8mV.

[0034] The in vitro release results of the product of this example are shown in T...

Embodiment 3

[0036]Weigh 300mg of poloxamer 407 and add it to 20ml of phosphate buffered saline (PBS buffer), heat at a slight temperature (30-40°C) to dissolve completely, weigh 200mg of 2-methoxyestradiol raw material, soybean egg Add 900 mg of phospholipids into 8 ml of dichloromethane, heat slightly to dissolve completely, add the oil phase dropwise to the water phase under magnetic stirring, pre-emulsify with a 10,000 rpm internal cutting homogenizer for 5 min, and pour it into the rotary film evaporator. In the round bottom flask, keep the temperature of the water bath at 40 ° C, start the vacuum pump, vacuum rotary evaporation for 4 hours, form the primary suspension, and carry out high-pressure emulsification of the primary suspension under the conditions of 9k psi cycle 3 times, 12k psi cycle 3 times, 18k psi cycled 20 times to obtain a milky white nanosuspension. Dissolve 300mg trehalose and 700mg mannitol in the nanosuspension, sterilize it with Co-60, use vials for aliquot packa...

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Abstract

The invention relates to a 2-methoxyestradiol nanosuspension frozen powder and a preparation method thereof, which effectively solves the problems of poor solubility, short half-life period, low oral bioavailability, difficulty for common injection to achieve high drug loading and targeting effect existing in 2-methoxyestradiol. The 2-methoxyestradiol nanosuspension frozen powder prepared by the invention comprises the following components by weight ratio: 1 part of 2-methoxyestradiol, 1-50 parts of surface active agent and 3-30 parts of cryoprotector. The preparation of the 2-methoxyestradiol nanosuspension frozen powder can be realized by the following method: 1. preparing primary nanosuspension by using a precipitation method or a dispersion method; 2. preparing nanosuspension by using the method of reducing the particle diameter including a high pressure homogenizer method and an ultrasound comminution method; 3. preparing the frozen powder; and 4. re-dissolving the frozen powder by water for injection when in use. The frozen powder for intravenous injection prepared by the invention has fine stability and is favor of transporting and storing drugs.

Description

1. Technical field [0001] The invention relates to the field of medicine, in particular to a 2-methoxyestradiol nano-suspension freeze-dried powder and a preparation method thereof. 2. Background technology [0002] 2-Methoxyestradiol (1,3,5-triene-2,3,17β-trihydroxy-2-methyl ether sterol) is a steroid hormone compound, which belongs to a new type of hormone anti-tumor drug, and is a natural Physiological metabolites of steroids in the body, studies have shown that they have significant antitumor activity. Its anti-tumor mechanism may be the induction of tumor and endothelial cell apoptosis (Lin H.L. et al. Cancer.92 (2001): 500-509), and is also related to the inhibition of neovascularization and tumor cell growth (Barchiesi F. et al. Circ.Res .99 (2006): 266-274), studies have shown that it has a significant inhibitory effect on a variety of tumors (myeloma, liver cancer, lung cancer, breast cancer, cervical cancer, etc.). It has been reported in the literature that the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/10A61K31/565A61K47/34A61K47/38A61K47/36A61K47/28A61K47/26A61K47/20A61P35/00A61K47/10
Inventor 杜斌张振中赵娅王舒雨赵芝兰
Owner ZHENGZHOU UNIV
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