Pharmaceutical composition of adefovir dipivoxil and its preparation method

Abstract

The invention relates to a method for preparing the adefovir dipivoxil polyester drug compound, with high stability and safety. The invention uses adefovir dipivoxil polyester, some pre-gelatinized amidon, and other findings, to be pressed into tablets directly. And the inventive compound comprises adefovir dipivoxil polyester at 1-20mass%, some pre-gelatinized amidon at 20-35mass%, and microcrystal cellulose at 60-79mass%.

Description

technical field [0001] The invention belongs to the technical field of medicine, and mainly relates to a pharmaceutical composition of adefovir dipivoxil, and also provides a preparation method of the composition. Background technique [0002] Adefovir dipivoxil is a newly synthesized adenosine analog in recent years. Chemical name: 9-{2-[di-(pivaloyloxymethoxy)phosphorylmethoxy]ethyl}adenine Holy A et al in Collect Czech Chem Commun, 1987, 52:2801 and CollectCzech Chem Commun, 1989, 54: 2190 reported the preparation method of adefovir dipivoxil. In the patents CN1347695 and WO2000035460, some crystal form patents and preparation method patents of adefovir dipivoxil are disclosed. At the same time, it is disclosed that adefovir dipivoxil can be prepared into pharmaceutical preparations with pregelatinized starch lactose, etc. CN1562046A also discloses the Defovir dipivoxil can be prepared into dispersible tablets with pregelatinized starch, microcrystalline cellulose, lact...

AI Technical Summary

Problems solved by technology

[0003] Existing adefovir dipivoxil tablets or capsules are mainly made into common oral preparations by wet granulation. In this granulation method, liquids such as water are added to make adefovir dipivoxil and auxiliary materials moist and soft. Then drying, tableting or direct filling, the prepared product will inevitably contain more moisture, the product placement stability of the drug is not good, and the preparation process is complicated, labor, and energy consumption are large; it is not conducive to the production and clinical practice of the product. application

[0004] Although there are processes in the prior art that use direct dry powder compression, the product uses adefovir dipivoxil as the main drug, pregelatinized starch, microcrystalline cellulose, lactose and other auxiliary materials, although it solves the shortcomings of wet compression, But the stability of the product prepared by this method is still not good, which affects the validity period of the product

At the same time, the fluidity of the product powder prepared by the existing technology is not good, which affects the product quality, is not conducive to large-scale industrial production, and wastes resources

The fluidity of powder is an important property of powder. The fluidity of powder is very important to the quality control of pharmaceutical preparations. High-speed tablet presses require materials to have higher fluidity. The requirement is very high, and it is an important factor affecting the accuracy of filling (Edited by Bi Dianzhou. Pharmacy. Beijing: People's Health Publishing House, 2002.76). Therefore, the poor fluidity of the powder prepared by the prior art affects the quality of the product, which is not conducive to the product. mass production