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A kind of flexible nano liposome gel of tamoxifen and preparation method thereof

A technology of tamoxifen and nano-lipid, which is applied in the field of pharmaceutical preparations, can solve the problems of increasing drug efficacy and less toxic and side effects, and achieve the effects of promoting percutaneous penetration, convenient operation, and low preparation cost

Active Publication Date: 2020-08-11
JINGCHU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The TAM magnetic microspheres prepared by Liu Rangru et al. can increase its drug concentration at the tumor site and increase its efficacy. The TAM microemulsion external preparation prepared by Zhang Yi et al. has a good transdermal effect, which makes the development of TAM preparations It has become the first choice for research to improve the side effects of tamoxifen and improve the drug efficacy. It is reported that TAM external preparations include ointment and cream, but there is no report of TAM transfer body gel, so it is necessary to improve the existing dosage forms , to prepare a dosage form with constant drug release rate, high bioavailability, and less toxic side effects, which requires the efforts of scientific researchers to explore

Method used

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  • A kind of flexible nano liposome gel of tamoxifen and preparation method thereof
  • A kind of flexible nano liposome gel of tamoxifen and preparation method thereof
  • A kind of flexible nano liposome gel of tamoxifen and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A flexible nanoliposome gel of tamoxifen is prepared from the raw materials of the following mass fractions:

[0038]

[0039] The phospholipid material is a composite phospholipid of hydrogenated soybean lecithin and soybean lecithin, which is denoted as SPC / HSPC (the molar ratio of SPC and HSPC is 3:1).

[0040] The preparation method of above-mentioned tamoxifen flexible nano liposome gel, its steps are:

[0041] 1) Tamoxifen, cholesterol, SPC / HSPC, and fatty acid glycerides were dissolved in chloroform to obtain solution A. Solution A was evaporated under reduced pressure at 37° C. to remove chloroform, and PBS buffer (pH=7.4) was added. Hydrate at normal temperature and pressure for 15 minutes to obtain a flexible nanoliposome suspension of tamoxifen;

[0042]2) Mix sodium carboxymethylcellulose, sodium deoxycholate and distilled water evenly to obtain solution B, then dissolve laurocapram, benzoic acid and propylene glycol in ethanol to obtain solution C, and ...

Embodiment 2

[0053] A flexible nanoliposome gel of tamoxifen is prepared from the raw materials of the following mass fractions:

[0054]

[0055]

[0056] The phospholipid material is a complex phospholipid of dipalmitoylphosphatidylcholine and soybean lecithin, which is recorded as DPPC / HSPC (the molar ratio of DPPC and HSPC is 1:3).

[0057] The preparation method of above-mentioned tamoxifen flexible nano liposome gel, its steps are:

[0058] 1) Dissolve tamoxifen, cholesterol, DPPC / HSPC, and sodium cholate in chloroform to obtain solution A, remove chloroform by rotary evaporation under reduced pressure at 37°C, add PBS buffer (pH=7.4), Hydrate at normal temperature and pressure for 15 minutes to obtain a flexible nanoliposome suspension of tamoxifen;

[0059] 2) Mix sodium carboxymethylcellulose, sodium deoxycholate and distilled water evenly to obtain solution B, then dissolve laurocapram, benzoic acid and propylene glycol in ethanol to obtain solution C, and gradually add so...

Embodiment 3

[0070] A flexible nanoliposome gel of tamoxifen is prepared from the raw materials of the following mass fractions:

[0071]

[0072]

[0073] The preparation method of above-mentioned tamoxifen flexible nano liposome gel, its steps are:

[0074] 1) Dissolve tamoxifen, cholesterol, HSPC and polysorbate in chloroform to obtain solution A. Rotate solution A under reduced pressure at 37°C to remove chloroform, add PBS buffer (pH=7.4), and Hydrate under normal pressure for 15 minutes to obtain tamoxifen flexible nanoliposome suspension;

[0075] 2) Mix sodium carboxymethylcellulose, fatty acid glyceride and distilled water evenly to obtain solution B, then dissolve laurocapram, benzoic acid and propylene glycol in ethanol to obtain solution C, and gradually add solution C to solution B , stirred at a speed of 500rpm for 15min, after mixing and swelling, adding ammonia water to adjust the pH value to about 7.0 to obtain a blank gel matrix;

[0076] 3) Mix the blank gel matr...

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Abstract

The invention discloses a tamoxifen flexible nano-liposome gel and a preparation method thereof. The gel is prepared from the following raw materials at a certain ratio: tamoxifen, cholesterol, phospholipid material, water-soluble gel substrate, transdermal penetration enhancer, surface active agent, preservative, humectants, pbs buffer solution, ammonia water, distilled water and ethyl alcohol. The preparation method comprises the following steps: 1) preparing a tamoxifen flexible nano-liposome suspension; 2) preparing a blank gel substrate; and 3) uniformly mixing the tamoxifen flexible nano-liposome suspension with the blank gel substrate, thereby acquiring the tamoxifen flexible nano-liposome gel. The gel has higher drug-carrying capacity and encapsulating effect to tamoxifen and has higher stability and transdermal permeability. The preparation method is simple, the operation is convenient and the preparation cost is low.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a tamoxifen flexible nano liposome gel and a preparation method thereof. Background technique [0002] Tamoxifen (TAM) is a selective estrogen receptor modulator (SERM), which can interfere with certain activities of estrogen, simulate the effects of other estrogens, and up-regulate the production of transforming growth factor-β, which Reduction is associated with the development of malignancies and also has a specific inhibitory effect on protein kinase C. These effects all have an inhibitory effect on tumor cells that rely on estrogen to continue to grow. Clinically, it is mostly used for the treatment of breast cancer with progressive development of estrogen (ER+) and progesterone receptor (PR+) before menopause. [0003] Nearly 100 countries in the world use TAM to treat advanced recurrent breast cancer and ovarian cancer, mainly for the treatment and pr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K31/138A61K47/38A61P5/32A61P35/00A61K9/127
CPCA61K9/0014A61K9/06A61K9/127A61K31/138A61K47/38
Inventor 彭佩陈军杨希雄沈艳顾薇
Owner JINGCHU UNIV OF TECH