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 betwe

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

Example Embodiment

[0073] Example 1

[0074] This example 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, place them in an autoclave, set the preparation pressure at 25MPa, temperature at 50°C, and time for 12h. After the temperature in the kettle reaches the set value, Access to 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 sieving to obtain the entecavir solid dispersion of this example, which is recorded as S1.

Example Embodiment

[0082] Example 2-5

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

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

Example Embodiment

[0085] Example 6-11

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

[0087] Under the conditions of a pressure of 25MPa, a temperature of 50°C, and a reaction time of 12h, the entecavir solid dispersions of Examples 2-5 were prepared using similar steps as in Example 1. The difference lies in the hydrophilicity in each example. The dosage ratio of the sexual carrier and the entecavir and the hydrophilic carrier is shown in Table 1 below, and the obtained solid dispersion of entecavir is denoted as S6-S11.

[0088] Table 1

[0089] sample Carrier Drug carrier ratio sample Carrier Drug carrier ratio S6 Mannitol 1:5S9 PEG1：10 S7 Mannitol 1:10S10 PEG: Mannitol (4:1) 1：5 S8 PEG 1:5S11 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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