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Toremifene citrate nano suspension, toremifene citrate tablet for treating ebola and preparation methods thereof

A technology of toremifene citrate and nanosuspension, which is applied in the field of medicine, can solve the problems of low oral bioavailability, large dose of anti-Ebola treatment, and low solubility of toremifene citrate. Achieve the effect of improving oral bioavailability, improving solubility and dissolution rate, and increasing adhesion

Inactive Publication Date: 2017-06-13
中国人民解放军第三O二医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, about 40% of the drugs obtained through high-throughput screening are insoluble in water, which makes the bioavailability of oral administration low, or it is difficult to make injections, etc., thus limiting the wide clinical application of drugs
Toremifene citrate has low solubility and low oral bioavailability, and it can be known from relevant literature that the therapeutic dose of anti-Ebola is relatively large

Method used

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  • Toremifene citrate nano suspension, toremifene citrate tablet for treating ebola and preparation methods thereof
  • Toremifene citrate nano suspension, toremifene citrate tablet for treating ebola and preparation methods thereof
  • Toremifene citrate nano suspension, toremifene citrate tablet for treating ebola and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: A preparation of toremifene citrate nanosuspension for the treatment of Ebola:

[0051]Weigh the raw materials containing the following weights in every 1000g toremifene citrate nanosuspension:

[0052]

[0053] Preparation method: Disperse toremifene citrate, PVP K30 and SDS in water, stir well and mix well, cut with high-speed shearing machine at 12000rmp for 3min, then use high-pressure homogenization method at 100Mpa, cycle 15 homogenization cycles .

Embodiment 2

[0054] Example 2: A preparation of toremifene citrate nanosuspension for the treatment of Ebola:

[0055] Weigh the raw materials containing the following weights in every 1000g toremifene citrate nanosuspension:

[0056]

[0057] Preparation method: disperse PVP K30 and SDS in redistilled water as a dispersion medium, mix well to form suspension A, disperse toremifene citrate in suspension A, mix well to form suspension B, Then suspensoid B was cut with a high-speed shearing machine at 12000rmp for 5 minutes to obtain suspension C, and then high-pressure homogenization method was used at 100Mpa to circulate 15 homogenization cycles to obtain toremifene citrate suspension agent.

Embodiment 3

[0058] Example 3: A preparation of toremifene citrate nanosuspension for the treatment of Ebola:

[0059] Weigh the raw materials containing the following weights in every 1000g toremifene citrate nanosuspension:

[0060]

[0061] Preparation method: Disperse toremifene citrate, PVP K30 and SDS in water, stir well and mix well, cut with high-speed shearing machine at 12000rmp for 3min, then use high-pressure homogenization method at 100Mpa, cycle 15 homogenization cycles .

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Abstract

The invention discloses a toremifene citrate nano suspension, a toremifene citrate tablet for treating ebola and preparation methods thereof, and belongs to the technical field of medicines. The toremifene citrate nano suspension is prepared from the following raw materials in parts by weight: 1 part of toremifene citrate, 0.1 to 2 parts of stabilizer and 10 to 500 parts of redistilled water. The toremifene citrate tablet is prepared from an effective component and a pharmaceutically acceptable carrier, wherein the effective component is the toremifene citrate nano suspension. The medicine toremifene citrate tablet provided by the invention has the following advantages that the solubility and the dissolution rate of the toremifene citrate are ameliorated by utilizing a nano suspending technique, the adhesiveness of the toremifene citrate to a gastrointestinal mucous membrane is increased, the first pass effect is avoided, the oral bioavailability is improved, and further, the drug loading capacity is high, and the like; meanwhile, a fluidized bed drying technique is adopted; the process is simple; the industrial mass production is suitable.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a toremifene citrate nanosuspension for treating Ebola, toremifene citrate tablets and a preparation method thereof. Background technique [0002] Toremifene Citrate, first listed in Finland in 1988, the chemical name is 2[4-(4-chloro-1,2-diphenyl-1-butenyl)phenoxy-N , N-dimethylethylamine citrate, molecular formula C32H36ClNO8, molecular weight 598.08, structural formula: [0003] [0004] Toremifene citrate is a non-steroidal triphenylethylene derivative, toremifene citrate binds to estrogen receptors and can produce estrogen-like or anti-estrogenic effects, or both , can be used as an oral selective estrogen receptor modulator for the treatment of advanced (metastatic) breast cancer. In the recent research process, it was found that toremifene has a good inhibitory effect on Ebola virus, and its currently known anti-Ebola virus mechanism is that toremifene ca...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/20A61K31/138A61P31/14
Inventor 董源黄昂韩晋张木子荷
Owner 中国人民解放军第三O二医院
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