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O/W type entecavir microemulsion oral liquid and preparation method of microemulsion oral liquid

A technology of microemulsion oral liquid and entecavir, which is applied in the field of O/W type entecavir microemulsion oral liquid and its preparation field, can solve the problems of low bioavailability of entecavir, poor water solubility, etc. good effect

Inactive Publication Date: 2021-06-04
GUANGZHOU DAGUANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of entecavir, the solubility is only about 2.4 mg / mL, resulting in low bioavailability of entecavir

Method used

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  • O/W type entecavir microemulsion oral liquid and preparation method of microemulsion oral liquid
  • O/W type entecavir microemulsion oral liquid and preparation method of microemulsion oral liquid
  • O/W type entecavir microemulsion oral liquid and preparation method of microemulsion oral liquid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of O / W type entecavir microemulsion oral liquid, by 100mL, its component composition is as follows:

[0028]

[0029]

[0030] The emulsifier is glyceryl caprate, and the emulsifier is beeswax.

[0031] The preparation method of this O / W type entecavir microemulsion oral liquid is as follows:

[0032] (1) Add entecavir into soybean oil and stir to dissolve;

[0033] (2) Add emulsifier, co-emulsifier and butyl p-hydroxybenzoate to the solution of step (1), stir evenly, then add 20% to 30% of the prescribed amount of water, stir at 10000r / min for 5min to form colostrum;

[0034] (3) Pour the colostrum in step (2) into a homogenizer, add sucralose, lemon essence and the remaining water, and disperse homogeneously at 20000r / min for 10min to form a stable O / W emulsion. Seal and sterilize to obtain O / W type entecavir microemulsion oral liquid.

Embodiment 2

[0036] A kind of O / W type entecavir microemulsion oral liquid, by 100mL, its component composition is as follows:

[0037]

[0038] The emulsifier is glyceryl caprate, and the emulsifier is beeswax.

[0039] The preparation method of this O / W type entecavir microemulsion oral liquid is as follows:

[0040] (1) Add entecavir to corn oil and stir to dissolve;

[0041] (2) Add emulsifier, co-emulsifier and butyl p-hydroxybenzoate to the solution of step (1), stir evenly, then add 20% to 30% of the prescribed amount of water, stir at 20000r / min for 3min to form colostrum;

[0042] (3) Pour the colostrum in step (2) into a homogenizer, add acesulfame-K, stevia, sweet orange essence and the rest of water, and disperse homogeneously at 10000r / min for 15min to form a stable O / W type emulsion, potting, and sterilizing to obtain O / W type entecavir microemulsion oral liquid.

Embodiment 3

[0044] A kind of O / W type entecavir microemulsion oral liquid, its difference with embodiment 1 is only that the addition of emulsifier and co-emulsion is different, in the present embodiment, the addition of emulsifier caprylic capric acid glyceride is 1.5g, The addition amount of auxiliary emulsifier beeswax is 1.5g.

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Abstract

The invention discloses an O / W type entecavir microemulsion oral liquid. The micro emulsion oral liquid is prepared from the following components by 100 mL: 0.0025-0.005 g of entecavir, 10-25 g of oil phase solvent, 1-3 g of emulsifier, 0.5-2 g of co-emulsifier, 0.05-0.2 g of preservative, 0.1-0.3 g of flavoring agent, 0.01-0.1 g of aromatic and the balance of water; and the emulsifier is caprylic capric triglyceride, and the co-emulsifier is beeswax. The O / W type microemulsion oral liquid is stable in property, good in uniformity, not prone to demulsification, layering, flocculation and other problems, good in taste and high in patient medication compliance, and the oral bioavailability of entecavir is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an O / W type entecavir microemulsion oral liquid and a preparation method thereof. Background technique [0002] The chemical name of Entecavir is 2-amino-9-[(1S,3S,4S)-4-hydroxy-3-hydroxymethyl-2-methylenepentyl]-1,9-hydrogen-6-H-purine- 6-keto-hydrate, molecular formula C 12 h 15 N 5 o 3 ·H 2 O. Entecavir is a new generation of oral guanosine nucleoside analogs used for the treatment of hepatitis B virus infection. It is mainly used for the treatment of chronic hepatitis B in adults with active virus replication and continuous increase in serum transaminases, or active liver histology. Hepatitis is currently the nucleoside analogue with the fastest and strongest virus reduction and the lowest mutation rate. It is considered to have a good clinical application prospect in the treatment of chronic hepatitis B. [0003] Oral liquid preparation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/522A61K47/14A61K47/44A61P31/20
CPCA61K31/522A61K9/0095A61K9/1075A61K47/44A61K47/14A61P31/20
Inventor 陈伟翰黄伟静韦日轮
Owner GUANGZHOU DAGUANG PHARMA
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