Aldfuwei ester injection having liver target and its preparation method

A technology of adefovir dipivoxil and dipivoxil injection, which is applied in the field of medicine and can solve the problem of lack of liver targeting

Inactive Publication Date: 2011-08-31
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no liver-targeted adefovir dipivoxil injection in the patents that have been applied for (for example, the patent publication number is 03114984.7 (adfovir and adefovir dipivaloyloxymethyl ester parenteral administration preparation) Prepared solution injections do not have liver targeting

Method used

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  • Aldfuwei ester injection having liver target and its preparation method
  • Aldfuwei ester injection having liver target and its preparation method
  • Aldfuwei ester injection having liver target and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1 Adefovir dipivoxil liposome

[0015] Component Weight (g)

[0016] Adefovir dipivoxil 1

[0017] Soy Lecithin 5

[0018] Proper amount of ethanol

[0019] citrate buffer to 500

[0020] Preparation Process:

[0021] Weigh the prescribed amount of adefovir dipivoxil and soybean lecithin, dissolve with an appropriate amount of ethanol, add citric acid buffer (0.1mol / L, pH4.0), stir and hydrate at 40°C, pass through a homogenizer (or Microjet) (the first step is to adjust the homogenization pressure to 520-600kg / cm 2 , the second step and then adjusted to 100 ~ 140kg / cm 2. Microfluidizer, the first step is to adjust the homogenization pressure to 4000-8000psi, and the second step is to adjust to 10000-16000psi) to obtain adefovir dipivoxil liposomes, the particle size of which is 20nm~300nm. The obtained liposome liquid can be added with 2% (W / V) trehalose for freeze-drying to obtain freeze-dried liposome. After reconstitution, its particle size is 10...

Embodiment 2

[0022] Embodiment 2 Adefovir dipivoxil liposome

[0023] Component Weight (g)

[0024] Adefovir dipivoxil 1

[0025] Soy Lecithin 20

[0026] Proper amount of ethanol

[0027] Alpha-tocopherol 0.1

[0028] Phosphate buffer to 1000

[0029] Preparation Process:

[0030] Weigh the prescribed amount of adefovir dipivoxil, soybean lecithin, and α-tocopherol, dissolve them with an appropriate amount of ethanol, add phosphate buffer (0.01mol / L, pH5.0), stir and hydrate at 40°C, and pass Homogenizer (or micro jet), the first step is to adjust the homogenization pressure to 520kg / cm 2 , the second step and then adjusted to 100kg / cm 2 (or microfluidizer, the first step is to adjust the homogenization pressure to 4000psi, and the second step is to adjust to 10000psi) to obtain adefovir dipivoxil liposomes, the particle size of which is 55nm~580nm. Gained liposome liquid can add the mannitol of 6% (W / V) and the glucose of 1% (W / V) and carry out freeze-drying, obtain freeze-dried ...

Embodiment 3

[0031] Embodiment 3 adefovir dipivoxil liposome

[0032] Component Weight (g)

[0033] Adefovir dipivoxil 1

[0034] Yolk Lecithin 30

[0035] Cholesterol 1

[0036] Alpha Lipoic Acid 0.5

[0037] Proper amount of ethanol

[0038] Acetate buffer up to 1000

[0039] Preparation Process:

[0040] Weigh the prescribed amount of adefovir dipivoxil, egg yolk lecithin, cholesterol, α-lipoic acid, after dissolving with appropriate amount of ethanol, adopt the ethanol injection method to add in the phosphate buffer (0.03mol / L, pH6.0), 50 Stir and hydrate at ℃, pass through a homogenizer (or micro jet), and adjust the homogenization pressure to 600kg / cm in the first step 2 , the second step and then adjusted to 100kg / cm 2 (or microfluidizer, the first step is to adjust the homogenization pressure to 5000psi, and the second step is to adjust to 10000psi) to obtain adefovir dipivoxil liposomes, the particle size is 58nm~510nm, and the encapsulation efficiency is greater than 80%....

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Abstract

A liver-targetted injection of adefevirdipivoxil ester is proportionally prepared from adefevirdipivoxil ester, phsophatide and cholesterol. It can be also prepared to be emulsion from adefevirdipivoxil ester, oil phase, emulsifier and emulsifying aid. Its preparing process is also disclosed.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a liver-targeted adefovir dipivoxil injection and a preparation method thereof. Background technique: [0002] The structural formula of Adefovir dipivoxil is as follows: [0003] [0004] Adefovir dipivoxil is the prodrug of adefovir, which is a purine derivative. It can be taken orally and hydrolyzed into adefovir after oral administration. It has antiviral effect without phosphorylation. This product can inhibit the activity of HBV DNA polymerase, penetrate into the DNA of hepatitis B virus, inhibit the replication of the virus, and has a strong inhibitory effect on HBV strains resistant to lamivudine and famciclovir. Clinically, it can be used for the treatment of hepatitis and AIDS. [0005] The CA accession number of adefovir dipivoxil is [142340-994]. The earliest compound patent of adefovir is Czechoslovak patent CS263951, the priority date is 1985.04.25, and the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61K9/19A61P1/16
Inventor 邓意辉吴红兵王绍宁
Owner SHENYANG PHARMA UNIVERSITY
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