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Adefovir dipivoil dispersion tablet and preparing method

A technology for adefovir dipivoxil and dispersible tablets, which is applied to the field of dispersible tablets containing adefovir dipivoxil and its preparation, and achieves the effects of being beneficial to continuation and automation, fast in vivo absorption, and high bioavailability

Inactive Publication Date: 2005-01-12
JIANGZHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmaceutical excipients are mixed in a specific ratio and directly compressed to make a dispersible tablet preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Adefovir dipivoxil 8.3% (by weight)

[0026] Pregelatinized starch 16.7% (weight)

[0027] Microcrystalline Cellulose 33.3% (by weight)

[0028] Lactose 16.6% (by weight)

[0029] Sodium carboxymethyl starch 21.7% (weight)

[0030] Sodium Lauryl Sulfate 1.7% by weight

[0031] Magnesium Stearate 1.7% by weight

[0032] Take the prescribed amount of adefovir dipivoxil, pass through a 100-mesh sieve, and separately take the prescribed amount of lactose, microcrystalline cellulose, pregelatinized starch, carboxymethyl starch sodium, magnesium stearate, and sodium lauryl sulfate. 60 mesh sieve, mix evenly, take the auxiliary material equal to that of adefovir dipivoxil, pass through a 60 mesh sieve and mix evenly with the method of increasing in equal amount, measure the content, directly compress the powder into tablets, and make adefovir dipivoxil dispersible tablets 1000 pieces.

Embodiment 2

[0034] Adefovir dipivoxil 4.2% (by weight)

[0035] Pregelatinized starch 19.2% (weight)

[0036] Microcrystalline Cellulose 43.3% (by weight)

[0037] Lactose 16.6% (by weight)

[0038] Sodium Starch Carboxymethyl 13.3% (by weight)

[0039] Sodium Lauryl Sulfate 1.7% by weight

[0040] Appropriate amount of aspartame

[0041] Magnesium Stearate 1.7% by weight

[0042] Take the prescribed amount of adefovir dipivoxil, pass through a 100-mesh sieve, and separately take the prescribed amount of lactose, microcrystalline cellulose, pregelatinized starch, carboxymethyl starch sodium, magnesium stearate, sodium lauryl sulfate, Aspartame passes through a 60-mesh sieve, mixes evenly, takes the auxiliary material equal to that of adefovir dipivoxil, passes through a 60-mesh sieve and mixes evenly with the method of increasing the same amount, measures the content, and directly compresses the powder into tablets to obtain Ade...

Embodiment 3

[0044] Adefovir dipivoxil 8.7% (by weight)

[0045]Pregelatinized starch 14.4% by weight

[0046] Microcrystalline Cellulose 39.2% (by weight)

[0047] Lactose 21.2% (by weight)

[0048] Sodium Starch Carboxymethyl 13.9% (by weight)

[0049] Sodium Lauryl Sulfate 1.7% by weight

[0050] Sunset Yellow Appropriate amount

[0051] Magnesium stearate 0.9% by weight

[0052] Take the prescribed amount of adefovir dipivoxil, pass through a 100-mesh sieve, and separately take the prescribed amount of lactose, microcrystalline cellulose, pregelatinized starch, carboxymethyl starch sodium, magnesium stearate, sodium lauryl sulfate, Pass the sunset yellow through a 60-mesh sieve, mix evenly, take the auxiliary material equal to that of adefovir dipivoxil, pass through a 60-mesh sieve and mix evenly with the method of increasing the same amount, measure the content, and directly compress the powder into tablets to obtain adefovir dipi...

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PUM

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Abstract

A dispersing tablet of adefovirdipivoxil ester is prepared from adefovirdipivoxil ester, pregelatinized starch, microcrystalline fibres, lactose, carboxymethyl starch sodium, sodium laurylsulfate, and magnesium stearate through respective sieving, proportionally mixing and die pressing.

Description

technical field [0001] The invention relates to an adefovir dipivoxil preparation, especially a dispersible tablet containing adefovir dipivoxil and a preparation method thereof. Background technique [0002] Adefovir dipivoxil (AD for short) chemical name: 9-[2-[bis(pivaloyloxymethoxy)phosphonomethoxy]ethyl]adenine, is a kind of insoluble It is a solidified substance with various crystal forms and amorphous forms in water. Adefovir dipivoxil can be used to treat human or animal retrovirus infection (HIV, SIV, FIV), DNA virus infection (human cytomegalovirus or herpes virus, such as HSV1 or HSV2), hepatitis B virus or other hepatitis Viruses, etc., have a strong inhibitory effect on HBV strains resistant to lamivudine and famciclovir, and are a new type of antiviral drug. Starrett et al., J Med. Chem., 1994, 37: 1857-1864; Starrett et al., Antiviral Res., 1992, 19: 267-273; Benzaria et al., J. Med. Chem., 1996, 39: 4958-4965; Zhang Yong et al., J...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/675A61P31/12
Inventor 卢建中喻萍余银芳
Owner JIANGZHONG PHARMA
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