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Composition and preparation process of a kind of estriol nanometer oral preparation

A technology of estriol and nanocrystalline suspension, which is applied in the field of medicine, can solve the problems of low oral bioavailability, high side effects of estrogen, and clinical application limitations, etc., achieve good prevention and treatment effects, improve curative effect, and be convenient to carry and the effect of taking

Active Publication Date: 2021-03-02
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the inconvenient use of injections, the "523" tablet has added cyclopentyloxy at the 3-position of the steroid core and α-ethynyl at the 17-position in order to increase solubility and bioavailability. Although the bioavailability has been improved, However, it shows side effects of high estrogen activity. With the increase of dosage and administration times, it can cause temporary breast swelling and induration; women can cause menstrual disorders; men can cause testicular atrophy and spermatogenic cell inhibition, etc. , so its clinical application is limited
However, estriol has a weak effect as a sex hormone. The disadvantage is that its solubility is very low, so its oral bioavailability is very low. In addition to the therapeutic effect, it greatly reduces the occurrence of adverse reactions compared with other hormone drugs

Method used

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  • Composition and preparation process of a kind of estriol nanometer oral preparation
  • Composition and preparation process of a kind of estriol nanometer oral preparation
  • Composition and preparation process of a kind of estriol nanometer oral preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1 prepares estriol nanocrystal suspension with different stabilizers

[0051] prescription:

[0052]

[0053] method:

[0054] Dissolve 1.0 g of sodium lauryl sulfate and 5.0 g of stabilizer (poloxamer 188, poloxamer 407, HPMC E3, PVP K30 for the four groups respectively) in 100 ml of purified water, and add the 10.0 g of estriol bulk drug that has been air-pulverized to 2 μm is mixed uniformly, and then sheared by a high-speed shear disperser at 10,000 r / min for 5 minutes to fully suspend. Utilize the planetary high-energy ball mill (P-7, Mercedes-Benz, Germany) to grind the suspension for a suitable time, and use the American PSS particle size tester to measure the drug particle distribution results as follows:

[0055] Table 1 Investigation of the influence of different stabilizers on grinding

[0056]

[0057] The results showed that grinding with four stabilizers could effectively reduce the particle size of estriol raw material. However, Polox...

Embodiment 2

[0058] Example 2 Preparation of estriol nanocrystal suspension with different charge protecting agents

[0059] prescription:

[0060]

[0061] method:

[0062] Dissolve 1.0g of charge protection agent (three groups of sodium lauryl sulfate, sodium docusate, sodium lauryl sulfate: sodium docusate = 1:1) and 5.0 g of poloxamer 188 in sequence In 100ml of purified water, add 10.0g of estriol raw material that has been air-pulverized to 2μm under stirring state to make it evenly mixed, and then shear it through a high-speed shear dispersing homogenizer at 10000r / min for 5min to fully suspend. Utilize the planetary high-energy ball mill (P-7, Mercedes-Benz, Germany) to grind the suspension for a suitable time, and use the American PSS particle size tester to measure the drug particle distribution results as follows:

[0063] Table 2 Investigation of the Effects of Different Charge Protectants on Grinding

[0064]

[0065] The results showed that grinding with sodium laury...

Embodiment 3

[0066] Example 3 Preparation of estriol nanocrystal suspension with different concentrations of raw materials

[0067] prescription:

[0068]

[0069] method:

[0070] Dissolve 1.0 g of sodium lauryl sulfate and 5.0 g of poloxamer in 100 ml of purified water in sequence, and add 0.1 g, 0.5 g, 1 g, 3 g, and 5 g of estriol raw materials that have been jet-milled to 2 μm in advance under stirring , 8g, 10g, 12g, 15g, 20g to make it evenly mixed, and then through a high-speed shear dispersing homogenizer 10000r / min shear 5min to fully suspend. Utilize the planetary high-energy ball mill (P-7, Mercedes-Benz, Germany) to grind the suspension for a suitable time, and use the American PSS particle size tester to measure the drug particle distribution results as follows:

[0071] Table 3 API Concentration Investigation

[0072]

[0073]

[0074] The results show that after grinding, the particle size and the concentration of the raw material drug form a U-shaped distributio...

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Abstract

The invention describes a method for preparing oral preparations of estriol, wherein, estriol exists in a nano-crystal state with a particle size between 20nm and 1000nm, and the preparation method is wet grinding or a high-pressure homogenization process, and the nano-crystal state The estriol is mixed with the corresponding auxiliary materials. The preparation dosage forms include oral tablets, capsules, granules, freeze-dried oral disintegration, suspension oral liquid, etc. The oral preparation of estriol is easy to carry and take, and has high bioavailability. Clinically, it can be used to prevent and / or treat possible damage caused by radiation to the body.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a preparation process of estriol nano crystal suspension and oral preparation thereof. Background technique [0002] The application of nuclear energy and nuclear technology has achieved great economic and social benefits. However, nuclear waste and nuclear power plant leakage accidents, industrial flaw detectors and industrial radioactive source machine failures, iatrogenic radiation injuries, nuclear weapons, nuclear dirty bombs, etc. have made The occurrence of nuclear radiation accidents shows an increasing trend, and the number of patients with acute radiation sickness is gradually increasing. The characteristics of nuclear radiation accidents are that the body is exposed to large doses of radiation in a short period of time, causing extensive body damage, complex clinical manifestations, and obvious stages of disease development. The clinical course can be divided into initia...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/565A61P17/16A61P39/00B02C17/08
CPCA61K9/0053A61K9/10A61K31/565A61P17/16A61P39/00B02C17/08
Inventor 卢伍党卫东陈涛
Owner XIAN LIBANG PHARMA TECH
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