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A kind of long-acting injection microsphere containing entecavir and preparation method thereof
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A technology of entecavir and microspheres, which is applied in the field of long-acting injection microspheres and its preparation, can solve the problems of aggravation of the disease, viral rebound, and inability to stop the drug casually.
Active Publication Date: 2021-04-20
YANTAI UNIV
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[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] Chronic hepatitis B is a disease that requires long-term maintenance treatment, but it has been reported that 63% of patients will stop taking antiviral drugs on their own, and 57% of them will aggravate the disease
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Embodiment 1
[0023] The present invention adopts S / W / O (water-in-oil-in-oil) process to prepare entecavir microspheres, and the specific preparation method is:
[0024] Weigh 4g of PLGA and dissolve it in 20mL of dichloromethane, add 0.4-0.8g of entecavir after jet crushing to it to obtain entecavir-PLGA suspension, ultrasonically disperse the suspension at high speed, specifically 6500-10000 / min ultrasonic Disperse for 3 to 5 minutes;
[0025] Quickly drop the entecavir-PLGA dispersion solution into 1% polyvinyl alcohol (PVA) aqueous solution, stir and emulsify at 1000r / min for 3-5min, quickly transfer to 0.1%PVA, magnetically stir for 4-6h to remove dichloromethane, 1000-1200 The washed balls were collected through a mesh sieve and freeze-dried to obtain the finished entecavir microspheres.
[0026] It is important for the application to add Entecavir to the PLGA solution after entecavir jet milling, jet milling can reduce the particle size of entecavir, specifically making the particle...
Embodiment 2- Embodiment 6
[0032] Embodiment 2-embodiment 6, its preparation method is the same as embodiment 1. The only difference lies in the type and viscosity of PLGA, see Table 1 for details.
[0033] The model and the viscosity of the PLGA of table 1 embodiment 1-6
[0034]
[0035] Note: In the PLGA model, 5050, 6535, and 8515 indicate that the lactic acid / glycolic acid (LA / GA) in the polymer material is 50:50, 65:35, and 85:15, respectively. A indicates that the polymer is terminated with a carboxyl group, and E indicates that Polymers are terminated with ester groups.
[0036] Determination of drug loading and encapsulation efficiency:
[0038] Accurately weigh 10 mg of entecavir microspheres prepared in Example 1, add an appropriate amount of dichloromethane to d...
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Abstract
The invention relates to a long-acting injection microsphere containing entecavir and a preparation method thereof. The preparation method of the long-acting injection microspheres containing entecavir, the steps include: adding the entecavir pulverized by a jet mill into the PLGA solution to obtain the entecavir-PLGA suspension, which is ultrasonically dispersed at high speed, and quickly Drop into polyvinyl alcohol solution, 800-1500r / min shear and stir emulsification for 3-5min, transfer to polyvinyl alcohol, magnetically stir for 4-6h, sieve to collect the precipitate and freeze-dry to obtain microspheres. The entecavir-PLGA slow-release microspheres in the prior art only have a slow-release time of 20 days in vitro, while the microspheres prepared by the present invention have a drug release in vitro of up to 60 days, and a drug release in vivo of up to 6 weeks, and remains effective for 42 days. It is expected to develop into a long-acting injection injected every 42 days.
Description
technical field [0001] The invention relates to a long-acting injection microsphere containing entecavir and a preparation method thereof. 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 0.5 mg once a day. When taking Entecavir Oral Liquid and Tablets, you need to pay attention to the following 2 points: [0003] 1. Eating will reduce the peak drug concentration (Cmax) by 63%, and the bioavailability (AUC 0-t ) decreased by 22%, and the drug peak time (Tmax) was delayed by 1.5h, so it should be taken on an empty stomach (at least 2 hours before or after meals); [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 ...
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