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Compound enteric-coated tablets of entecavir phospholipid complex and diammonium glycyrrhizinate

A technology of diammonium glycyrrhizinate and phosphatidylcholine, which is applied in the field of medicine, can solve the problems of lower drug efficacy, low bioavailability, and damage to the injection site, and achieve improved safety and effectiveness, improved bioavailability, and improved The effect of curative effect

Active Publication Date: 2016-05-18
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Most of the diammonium glycyrrhizinate preparations on the market are injections and ordinary capsule preparations. The injections require the assistance of professional medical staff to complete, and the patients' compliance with medication is poor, and the injection site will also suffer from varying degrees of damage, causing long-term drug use. to great physical and mental pain
Oral administration can increase the compliance of patients. However, since diammonium glycyrrhizinate is unstable and easy to degrade in an acidic environment, after ordinary capsules are taken, diammonium glycyrrhizinate is easily destroyed by gastric acid in the stomach, thereby reducing Drug efficacy, and there are problems such as short retention time of the drug in the body after taking the drug, uneven absorption and distribution, low bioavailability, and insignificant drug efficacy

Method used

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  • Compound enteric-coated tablets of entecavir phospholipid complex and diammonium glycyrrhizinate
  • Compound enteric-coated tablets of entecavir phospholipid complex and diammonium glycyrrhizinate
  • Compound enteric-coated tablets of entecavir phospholipid complex and diammonium glycyrrhizinate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: the preparation of entecavir phospholipid complex

[0033] Dissolve entecavir and lecithin (the ratio of the two is 1:5~80, w / w) in a mixed solvent of isopropanol and ethanol (the volume ratio of the two solvents is 1:1), and the drug concentration of entecavir is 0.2~2.0mg / mL, magnetically stirred at 120r / min in a constant temperature water bath at 55°C for 30 minutes, recovered the solvent under reduced pressure, and dried in vacuum to obtain the phospholipid complex.

Embodiment 2

[0034] Embodiment 2: the preparation of enteric coating liquid

[0035] prescription:

[0036] components

Component weight (g)

Udage L100-55

16.0

polyethylene glycol 4000

2.0

NaOH

0.2

Talc powder

6.8

purified water

75.0

total

100.0

[0037] Preparation:

[0038] Weigh the prescribed amount of polyethylene glycol 4000 and NaOH, dissolve them in the prescribed amount of purified water, add talcum powder and Eudragit L100-55 to it under stirring to make a suspension, stir well and pass through 80 mesh Sieve to obtain an aqueous coating solution containing 16% of the enteric coating material Eudragit L100-55.

Embodiment 3～5

[0039] Embodiments 3-5: Preparation of Entecavir Phospholipid Complex and Diammonium Glycyrrhizinate Compound Enteric-Coated Tablets (made into 1000 tablets)

[0040] prescription:

[0041]

[0042] Preparation:

[0043] 1. Preparation of Entecavir Phospholipid Complex

[0044] The entecavir phospholipid complex was prepared according to the method in Example 1, and it was ground through an 80-mesh sieve for subsequent use.

[0045] 2. Tablet core preparation

[0046] 1) Diammonium Glycyrrhizinate, Sodium Lauryl Sulfate, and micropowder silica gel of prescription quantity are taken by weighing and pulverized through 80 mesh sieves respectively, then in a V-type mixer, add entecavir phospholipid complex and mix homogeneously by equal addition method, Intermediate 1 was obtained;

[0047]2) Pregelatinized starch, mannitol, hypromellose, and cross-linked carmellose sodium were weighed and pulverized through an 80-mesh sieve, and then mixed uniformly in a tank mixer to obta...

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PUM

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Abstract

The invention provides compound enteric-coated tablets of entecavir phospholipid complex and diammonium glycyrrhizinate and also relates to a preparation method of the compound enteric-coated tablets and an application in treatment of hepatitis B. The compound enteric-coated tablets provided by the invention have a slow release effect and can improve the bioavailability, safety and effectiveness of the medicines; and moreover, the entecavir phospholipid complex and diammonium glycyrrhizinate together realize anti-virus and liver protection effects to improve the curative effect on hepatitis B.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a compound enteric-coated tablet of entecavir phospholipid complex and diammonium glycyrrhizinate, a preparation method and application thereof. Background technique [0002] Entecavir is a guanosine nucleoside analogue, which has inhibitory effect on hepatitis B virus (HBV) polymerase, and is a highly effective anti-hepatitis B virus drug; it is phosphorylated into an active triphosphate in the body, and the triphosphate is in the cell The half-life is 15 hours. Entecavir has high anti-hepatitis B virus activity. Its oral tablet once a day, with a dose of 0.5mg, can effectively kill the virus and block the virus replication process. It is currently the first-line drug for the treatment of HBV. [0003] The chemical name of Entecavir is: 2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl]-6H- Purin-6-one, the structural formula is: [0004] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/522A61K31/704A61K9/32A61P1/16A61P31/20A61K47/54
CPCA61K9/2813A61K9/2846A61K9/2853A61K31/522A61K31/704A61K2300/00
Inventor 王善春王广基张喜全顾红梅刘雷王祥建董平束蓓艳
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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