Entecavir injection

Abstract

The invention relates to an Entecavir injection comprising a small-capacity injection, a large-capacity sterilized injection and a freeze-dry sterile powder injection. The Entecavir injection is characterized by being prepared from 0.1-2.5mg of single-dosage active Entecavir and an additive which comprises a solvent for injection, 0-10% of pH regulator, 0-10% of antioxidant, 0-60% of solubilizer, 0-20% of isotonic regulator, 0.1-20% of filler and 0.1-20% of filling scaffold agent, and the percentage is the percent of the total quality of the injection in the liquid volume. The Entecavir comprises the injection and the sterile powder injection and has favorable inhibited effect on hepatitis B and good stability.

Description

technical field [0001] The invention relates to an injection of entecavir and a preparation method thereof, specifically, a sterilized solution, emulsion or suspension for injection into the body made of active form of entecavir, as well as a preparation before use Sterile powder or concentrated solution for solution or suspension. Background technique [0002] Entecavir is a guanosine analogue with the chemical name 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl 】-1,9-dihydro-6H-purin-6-one, the molecular structure is as follows: [0003] [0004] Molecular formula C 12 h 15 N 5 o 3 , molecular weight 277.3, usually contains a crystal water, its monohydrate formula C 12 h 15 N 5 o 3 .H 2 O, molecular weight 295.3. [0005] US Patent No. 5,206,244 discloses entecavir and its use in the treatment of hepatitis B. International publications WO98 / 09964 and WO2004, 052310 respectively disclose two improved entecavir synthesis methods. US pa...

AI Technical Summary

Problems solved by technology

At present, the pharmaceutical preparations of entecavir marketed at home and abroad are all oral dosage forms, such as tablets and oral liquids. Eating will cause delays in the absorption of entecavir, which will lead to malabsorption and decreased bioavailability. Therefore, such oral dosage forms should be taken on an empty stomach, at least Take it two hours before or after meals to achieve better drug absorption

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