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Entecavir solid dispersion and Entecavir preparation

A technology of solid dispersion and entecavir, which is applied in the direction of pill delivery, antiviral agents, active ingredients of heterocyclic compounds, etc. It can solve the problems of easily destroying drug activity, difficult to crush and sieve, difficult to control the heating and cooling rate of melting method, etc. , to achieve the effect of improving bioavailability, improving solubility and dissolution rate

Inactive Publication Date: 2017-05-31
HUNAN QIANJIN XIELI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solvent method requires the use of a large amount of organic solvents, causing serious environmental pollution, and the residual organic solvents will cause toxic and side effects on the human body; the heating and cooling rate of the melting method is difficult to control, the reproducibility between batches is poor, the preparation conditions are severe, and the activity of the drug is easily destroyed; grinding The solid dispersion obtained by this method also has problems such as being difficult to pulverize and sieve, which also limits its further preparation into pharmaceutical preparations.

Method used

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  • Entecavir solid dispersion and Entecavir preparation
  • Entecavir solid dispersion and Entecavir preparation
  • Entecavir solid dispersion and Entecavir preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] This embodiment is used to illustrate the entecavir solid dispersion provided by the present invention.

[0075] Take 0.5g of entecavir, 2.0g of PEG-4000, and 0.5g of mannitol, mix them evenly, put them in an autoclave, set the preparation pressure to 25MPa, the temperature to 50°C, and the time to 12h. After the temperature in the kettle reaches the set value, into CO 2 Until the pressure reaches the set value, keep the temperature and pressure for the set time, collect the solid dispersion in the kettle under reduced pressure, pulverize, and sieve to obtain the entecavir solid dispersion of this embodiment, which is designated as S1.

Embodiment 2-5

[0083] The present examples 2-5 are used to illustrate the preferred process conditions for preparing entecavir solid dispersion by supercritical fluid technology provided by the present invention.

[0084] Using PEG as the hydrophilic carrier material, and the mass ratio of entecavir to PEG is 1:5, under the conditions of pressure of 25MPa and temperature of 50°C, the steps similar to those of Example 1 were used to prepare the samples of Example 2-5. Entecavir solid dispersion, the difference is that each embodiment sets the reaction time as 6h, 9h, 12h and 24h respectively, which is recorded as S2-S5.

Embodiment 6-11

[0086] The present examples 6-11 are used to illustrate the preferred process conditions for preparing entecavir solid dispersion by supercritical fluid technology provided by the present invention.

[0087] Under the conditions that the pressure is 25MPa, the temperature is 50°C, and the reaction time is 12h, the entecavir solid dispersions of Examples 2-5 are prepared by the steps similar to Example 1, except that the hydrophilic The dosage ratio of the carrier, entecavir and hydrophilic carrier is shown in the following table 1, and the obtained entecavir solid dispersion is recorded as S6-S11.

[0088] Table 1

[0089] sample carrier drug carrier ratio sample carrier drug carrier ratio S6 Mannitol 1:5 S9 PEG 1：10 S7 Mannitol 1:10 S10 PEG: Mannitol (4:1) 1：5 S8 PEG 1:5 S11 PEG: Mannitol (4:1) 1：10

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Abstract

The invention provides an Entecavir solid dispersion and an Entecavir preparation. The Entecavir solid dispersion is prepared from Entecavir and a hydrophilic carrier by a super-critical fluid method; the Entecavir preparation is prepared from the Entecavir solid dispersion and pharmaceutical auxiliary materials. The Entecavir solid dispersion and the Entecavir preparation have the advantage that by utilizing the solid dispersing technique, a medicine is dispersed into the carrier in a molecule or unfixed-shape state, so that the highly dispersed state of the medicine is guaranteed, the dissolving degree and rate of the indissolvable medicine are effectively increased, and the bioavailability of the medicine is improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceuticals, in particular to an entecavir solid dispersion and an entecavir preparation. Background technique [0002] Entecavir is a highly effective antiviral agent with good inhibitory effect on hepatitis B virus. The molecular formula is: C 12 h 15 N 5 o 3 ·H 2 O, the molecular weight is 295.3, its structural formula is: [0003] [0004] Because its content in the preparation is very low, only containing 0.5 mg or 1 mg, the amount of the main drug and the amount of the auxiliary material are greatly different during the preparation process, and it is not easy to mix, so it is easy to cause unqualified content uniformity. CN102144983 B mixes the raw material drug and the auxiliary materials in equal increments, which improves the dispersion uniformity and content uniformity of the preparation, but fails to effectively solve the dissolution rate problem of entecavir. [0005] The solubil...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/10A61K9/20A61K47/36A61K47/26A61K31/522A61P31/20
CPCA61K9/146A61K9/2018A61K9/2059A61K31/522
Inventor 徐彬滨谭喜平钟林波王洪锋
Owner HUNAN QIANJIN XIELI PHARMA CO LTD
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