Long-acting injection gel containing entecavir

An entecavir and gel technology, applied in the field of long-acting injection gel, can solve the problems of only 16% bioavailability, low oral drug penetration rate, and inability to stop the drug casually, so as to reduce the probability of virus rebound and solve gastrointestinal problems. The effect of reducing side effects and improving medication compliance

Pending Publication Date: 2021-07-09
SHANDONG GUYUCHUN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 2. During use, the drug cannot be stopped casually before there is no indication to stop the drug, otherwise the virus rebound is prone to occur
[0005] 3. Entecavir belongs to the third class of drugs in the Biopharmaceutics Classification System (BCS), its oral drug penetration rate is low, and its bioavailability in experimental animal monkeys is only 16%
[0006] Chronic hepatitis B is a disease that requires long-term medication maintenance treatment, but it has been reported that during the course of oral antiviral drugs, 63% of patients will stop taking drugs, and 57% of them will aggravate the disease

Method used

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  • Long-acting injection gel containing entecavir
  • Long-acting injection gel containing entecavir
  • Long-acting injection gel containing entecavir

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Take two parts of 150mg PLGA solids with uniform size, the specification is monomer ratio LA:GA=50:50, Mw is 40KDa, add 350mg of N-methylpyrrolidone or 350mg of ethyl acetate respectively, place in a beaker, Stir and dissolve at room temperature at 500 rpm for 60 min. Observe the dissolution phenomenon, and drop the formed liquid into the water to observe the phenomenon.

[0028] It can be seen that NMP can dissolve the added PLGA in about 30 minutes to form a clear solution with a certain viscosity, but ethyl acetate forms a suspension in 60 minutes. Drop the two liquids formed into water respectively. It can be seen that both of them will gel into small balls, but there are flocs in the PLGA dissolved in ethyl acetate. It shows that NMP is more suitable for forming gel with PLGA.

Embodiment 2

[0030] Take three parts of 150mg PLGA solid with uniform size, the specification is monomer ratio LA:GA=50:50, Mw is 40KDa, add 600mg, 400mg and 225mg of N-methylpyrrolidone respectively, put in a beaker, Stir and dissolve at 500 rpm for 60 minutes to make 20%, 27%, and 40% PLGA solutions, observe the dissolution phenomenon, and drop the formed liquid into water to observe the phenomenon.

[0031] It can be seen that NMP can dissolve the added 27% PLGA within about 30 minutes, 20% needs 15 minutes to dissolve, and 40% needs about 60 minutes to dissolve, forming a clear gel solution with a certain viscosity. The viscosity of the gel solution was the largest for the 40% PLGA solution, followed by the 27% one. The contact time with hydrogel is 6 seconds, 3 seconds and 1 second respectively. The effect of coagulation is that 20% has a certain viscosity and softness, and 40% has the strongest character and the least softness.

Embodiment 3

[0033] Take three parts of 150mg PLGA solid with uniform size, the specification is monomer ratio LA:GA=50:50, Mw is 20KDa, 30KDa, 50KDa respectively, add 350mg of N-methylpyrrolidone respectively, put it in a beaker, at room temperature Stir and dissolve at 500rpm for 60min to make a PLGA solution, observe the dissolution phenomenon, and drop the formed liquid into water to observe the phenomenon.

[0034] It can be seen that the dissolution time is 20min, 25min, and 50min respectively; in the case of gel, PLGA with 50KDa has the highest viscosity, and PLGA with 20KDa has the lowest viscosity; it coagulates quickly when it meets water. As the molecular weight of PLGA increases, the coagulation time becomes shorter.

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Abstract

The invention discloses long-acting injection gel containing entecavir, which is composed of entecavir and PLGA (poly (lactic-co-glycolic acid)) gel, and the weight ratio of the entecavir to the PLGA gel is 1: (5-50), Wherein the PLGA gel is prepared from PLGA and an organic solvent; the organic solvent is selected from N-methyl pyrrolidone and the like. The entecavir and the PLGA gel are respectively stored, and are mechanically and uniformly mixed before being used for injection. Gel is prepared by using the biocompatibility and degradation characteristic of PLGA, entecavir is uniformly dispersed in the PLGA gel, after the entecavir gel is injected into a body, a solvent is rapidly diffused, the gel is solidified, a small medicine warehouse can be formed at an injection part, a part of medicine is diffused and released along with the solvent and enters the body to play a therapeutic role, and then along with the continuous degradation of the PLGA, the carried medicine is continuously released into a human body, so that the effect of slow release of the medicine is achieved, and the long-term treatment effect is achieved.

Description

technical field [0001] The invention relates to a long-acting injection gel containing entecavir. Background technique [0002] Entecavir is the first choice drug for the treatment of chronic hepatitis B recommended in the 2015 edition of "Guidelines for the Prevention and Treatment of Chronic Hepatitis B". The dosage forms currently on the market are oral liquid and tablets. The recommended dosage of the tablets is once a day, 0.5mg or 1mg each time. When taking Entecavir oral liquid and tablets, you need to pay attention to the following two points: [0003] 1. Eating will reduce the peak drug concentration (Cmax) by 63%, bioavailability (AUC0-t) by 22%, and delay the peak time (Tmax) of the drug by 1.5h, so it should be taken on an empty stomach (at least an interval before and after meals) 2 hours); [0004] 2. During use, the drug should not be stopped casually before there is no indication to stop the drug, otherwise the virus rebound will easily occur. [0005] 3. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/34A61K31/522A61P1/16A61P31/20
CPCA61K9/06A61K9/0019A61K47/34A61K31/522A61P1/16A61P31/20
Inventor 李建牛自芬孙君娟朱震财付瑞平
Owner SHANDONG GUYUCHUN BIOTECHNOLOGY CO LTD
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