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Preparation method of dolutegravir micro powder

A technology of dolutegravir and micropowder, applied in the field of dolutegravir micropowder preparation, can solve the problems of poor solubility, affecting bioavailability, etc., and achieve the effect of lowering temperature and excellent ultrafine effect.

Pending Publication Date: 2022-03-22
JIANGSU YUXIANG CHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although dolutegravir has excellent performance, its solubility in water is too poor, thus affecting its bioavailability

Method used

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  • Preparation method of dolutegravir micro powder
  • Preparation method of dolutegravir micro powder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) In the reaction kettle, add solvent ethanol, dissolve the original powder of dolutegravir in ethanol, and prepare the ethanol solution of dolutegravir, wherein the concentration of dolutegravir is 50mg / ml.

[0027] (2) In another reaction kettle, an aqueous solution of sodium tripolyphosphate was prepared with pure water at a concentration of 1%.

[0028] (3) Turn on the strong stirring of the above-mentioned saline solution, control the temperature at -10°C, and pass the ethanol solution of Dolutegravir through a high-pressure delivery pump through a jet mixer based on the Venturi effect set on the reaction kettle Spray into the saline solution and the reactor's jet mixer is immersed in the liquid phase of the reactor. Continue vigorous stirring for 60 min. Obtain dolutegravir suspension. Wherein the volume ratio of the saline solution and the ethanol solution of dolutegravir is 5:1, figure 1 It is a schematic diagram of a jet mixer based on the Venturi effect i...

Embodiment 2

[0031] (1) In the reaction kettle, add solvent ethanol, dissolve the original powder of dolutegravir in ethanol, and prepare the ethanol solution of dolutegravir, wherein the concentration of dolutegravir is 100mg / ml.

[0032] (2) In another reaction kettle, an aqueous solution of disodium edetate was prepared with pure water at a concentration of 5%.

[0033] (3) Turn on the strong stirring of the above-mentioned saline solution, control the temperature at 10°C, and spray the ethanol solution of dolutegravir through a high-pressure delivery pump through a jet mixer based on the Venturi effect installed on the reaction kettle. into the brine-containing solution, and the jet mixer of the reactor is immersed in the liquid phase of the reactor. Continue vigorous stirring for 30 min. Obtain dolutegravir suspension. Wherein the volume ratio of the saline solution and the ethanol solution of dolutegravir is 50:1, figure 1 It is a schematic diagram of a jet mixer based on the Vent...

Embodiment 3

[0036] (1) In the reaction kettle, add solvent ethanol, dissolve the original powder of dolutegravir in ethanol, and prepare the ethanol solution of dolutegravir, wherein the concentration of dolutegravir is 75mg / ml.

[0037] (2) In another reaction kettle, an aqueous solution of trisodium ethylenediamine disuccinate was prepared with pure water at a concentration of 3%.

[0038] (3) Turn on the strong stirring of the above-mentioned saline solution, control the temperature at 0°C, and spray the ethanol solution of dolutegravir through a high-pressure delivery pump through a jet mixer based on the Venturi effect installed on the reaction kettle. into the brine-containing solution, and the jet mixer of the reactor is immersed in the liquid phase of the reactor. Continue vigorous stirring for 45 min. Obtain dolutegravir suspension. Wherein the volume ratio of the saline solution and the ethanol solution of dolutegravir is 25:1, figure 1 It is a schematic diagram of a jet mixe...

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Abstract

The invention discloses a dolutegravir micro powder preparation method, which comprises: adding a solvent ethanol in a reaction kettle, dissolving dolutegravir raw powder in ethanol to prepare a dolutegravir ethanol solution with a concentration of 50-100 mg/ml, adopting purified water to prepare a salt-containing aqueous solution with a salt concentration of 1-5% in another reaction kettle, the salt-containing aqueous solution, especially the aqueous solution of sodium tripolyphosphate, disodium ethylene diamine tetraacetate or trisodium ethylene diamine disuccinate, is adopted, and the ultra-micro effect is particularly excellent. On one hand, the addition of the substances can greatly reduce the temperature for separating out crystals, and on the other hand, the aqueous solution has low surface tension and excellent dispersion stability effect, is particularly beneficial to separating out superfine nanocrystals from an easily soluble solvent, namely ethanol, and is not easy to coalesce.

Description

technical field [0001] The invention belongs to the technical field of organic chemistry, and in particular relates to a method for preparing dolutegravir micropowder. Background technique [0002] Dolutegravir (Dolutegravir, Tivicay) is a new anti-AIDS drug jointly developed by the British pharmaceutical giant GlaxoSmithKline (GSK) and Japan's Shionogi Pharmaceutical Company (Shionogi). In July 2012, GlaxoSmithKline Pharmaceuticals and Shionogi Pharmaceuticals announced the results of the Phase III clinical trial of the new AIDS drug Dolutegravir. After 48 weeks of treatment with dolutegravir and two other old AIDS drugs, 88% of the patients in the body recovered. The virus was successfully suppressed, and after taking the three-in-one oral drug Atripla (Efofovirenz / emtricitabine / tenofovir fumaric acid tablets) from Gilead Sciences, 81% of the patients The virus was suppressed, and GlaxoSmithKline's drug dolutegravir was slightly better. In the comparative trial, 10% of p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/02A61K47/18A61K31/5365A61P31/18C07D498/14
CPCA61K9/143A61K9/145A61K31/5365A61P31/18C07D498/14
Inventor 张治国李思远王金程红伟程云涛徐官根
Owner JIANGSU YUXIANG CHEM
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