Aldoforwe ester self-emulsifying capsule preparation and its making method

Abstract

The invention is concerned with a kind of Adefovir Dipivoxil self-emulsification capsule preparation and its produce method. Adefovir Dipivoxil is anti-hepatitis B virus agent with instability and the biology utilization ratio of existing preparation is low with complicated process and big harmless of dust. Mix the middle solution with Adefovir Dipivoxil in the amount of prescription and oil, dispose the middle solvent by extrusion method after rotating-film evaporating technique, add emulsifying agent, heat in water with constant temperature or ultrasonographic to get even and transparent liquid and produce into soft capsule or hard capsule. The production has nice stability, high biology utilization ratio and easy for using.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to an anti-hepatitis B virus drug adefovir dipivoxil self-emulsifying capsule preparation and a preparation method thereof. Background technique [0002] Adefovir dipivoxil (adefovir dipivoxil) is an antiviral drug developed by Gilead Sciences of the United States, and has a good curative effect on the treatment of hepatitis B. Adefovir dipivoxil is a nucleic acid analog, which inhibits the replication and proliferation of the virus by inhibiting the activity of hepatitis B DNA polymerase, and has resistance to lamivudine (Heptin) virus mutation strain and another mutant strain of hepatitis B virus called "precore mutant" that infects about 50% of hepatitis B patients in the Asia-Pacific region has a fairly good inhibitory effect. [0003] Adefovir dipivoxil is a water-insoluble solid with amorphous and polymorphic forms, so the existing preparations ha...

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Problems solved by technology

[0003] Adefovir dipivoxil is a water-insoluble solid with amorphous and polymorphic forms, so the existing preparations have the following two problems: the first is to make adefovir dipivoxil with the amorphous Common tablet, drop pill, solid capsule and other dosage forms are easy to degrade due to the poor stability of active ingredients when stored under natural conditions, resulting in a decline in drug efficacy, and the loss of amorphous adefovir dipivoxil obtained by conventional spray drying reaches 80% %above

In addition, its crystalline solid preparation will inevitably undergo crystal transformation during storage, thereby affecting the absorption of the drug; second, whether it is an amorphous or a crystalline substance, its poor water solubility will lead to oral biomedicine. Poor utilization, high dosage

Chinese patent (publication number 1429555A) discloses the soft capsule dosage form of adefovir dipivoxil, although this dosage form has improved the stability of adefovir dipivoxil to a certain extent, bioavailability is still low; Another Chinese patent ( Publication number CN1546046A) discloses a kind of adefovir dipivoxil dispersible tablet, and this preparation improves its bioavailability to a certain extent, but does not solve the stability problem of adefovir dipivoxil, and the technology is more complicated, is not suitable for technology Production

In addition, the dust generated during the actual production operation of adefovir dipivoxil solid preparations can easily cause lesions in workers' respiratory tracts, skin and other parts.

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