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Percutaneous drug administration cream ,ointment of letrozole and preparation method thereof

A technology of letrozole and cream, applied in the field of transdermal cream

Inactive Publication Date: 2008-05-07
INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are only oral preparations of this drug at home and abroad, and its disadvantages are: the first-pass effect of the liver cannot be avoided in clinical application; the incidence of adverse reactions that may be related to this drug is 33%, and the main manifestations are nausea, headache, and bone pain

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Prescription Name of main and auxiliary materials Dosage g / 100g

[0015] Letrozole 0.50

[0016] Carbomer 0.75

[0017] Azone 3.0

[0018] TW 1.9

[0019] Ethanol 20

[0020] Propylene glycol 20

[0021] Purified water up to 100

[0022] 0.75g carbomer is adjusted to pH 6.5~7.5 with 10% NaOH solution, stirs to make swelling evenly; Add 0.50g letrozole raw material medicine 0.50g that crosses 200 mesh sieves into 20g ethanol and 20g propylene glycol, stir to dissolve, and The main drug solution and the carbomer solution were uniformly mixed, 3.0 g of azone, 1.9 g of Tuwen 80 were added, and purified water was added to a total amount of 100 g, and the mixture was ground until it was emulsified evenly to form a 0.5% letrozole cream.

[0023] The above-mentioned gained emulsifiable paste is carried out in vitro transdermal release test, and the results are as follows:

[0024] Release medium Time Cumulative rele...

Embodiment 2

[0032] Prescription Name of main and auxiliary materials Dosage g / 100g

[0033] Letrozole 1.0

[0034] Carbomer 0.75

[0035] Azone 3.0

[0036] TW 1.9

[0037] Ethanol 20

[0038] Propylene glycol 20

[0039] Purified water up to 100

[0040] Adjust 0.75g of carbomer with 10% NaOH solution to pH 6.5-7.5, stir to make the swelling uniform; add 1.0g of letrozole raw material drug passed through a 200 mesh sieve to 20g of ethanol and 20g of propylene glycol, stir to make the suspension uniform , mix the main drug suspension and carbomer solution evenly, add 3.0g of azone, 1.9g of soil temperature 80, and add purified water to a total of 100g, grind until emulsification is uniform, and form 1.0% letrozole milk ointment.

[0041] The above-mentioned gained emulsifiable paste is carried out in vitro transdermal release test, and the results are as follows:

[0042] Release medium Time Cumulative release amount μg

[0...

Embodiment 3

[0050] Prescription Name of main and auxiliary materials Dosage g / 100g

[0051] Letrozole 1.0

[0052] Ethanol 20

[0053] Propylene glycol 20

[0054] water 20

[0055] Azone 3.0

[0056] Sodium Lauryl Sulfate 0.8

[0057] Octadecanol 12

[0058] Lanolin 23.2

[0059]Take 1.0g of the letrozole bulk drug passed through a 200 mesh sieve, add 20g of ethanol, 20g of propylene glycol and 20g of purified water, stir to make the suspension uniform, and form a water phase; take 23.2g of lanolin and 12g of stearyl alcohol, heat to melt, add Azone 3.0g, stir to make it miscible, and cool down to 65°C to form an oil phase; add 0.8g of sodium lauryl sulfate to the water phase, stir to dissolve and add the oil phase under stirring when heated to 65°C, continue Stir until the emulsification is uniform, and the temperature drops to room temperature to form a 1% oil-in-water ointment.

[0060] The above-mentioned gained ...

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PUM

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Abstract

The invention relates to the cream and the ointment of Letrozole tablet percutaneous administration and the preparation method of the cream and the ointment thereof, and relates to the cream and the ointment of the percutaneous administration and the preparation method of the cream and the ointment thereof. The invention solves the problems that the prior Letrozole tablet oral preparation cannot avoid the first pass effect of liver and the bad reaction is numerous. The cream and the ointment of the percutaneous administration are characterized in that the cream and the ointment of the percutaneous administration comprise raw materials and penetrating agent with the following percentages: 0.01 to 20 percent of Letrozole tablet and 0.1 to 20 percent of percutaneous penetrating agent. The invention has the method that through vitro and a skin penetration test, the Letrozole tablet only with oral preparation is filtered out a formula with good non-steady state / steady state distribution by a skin release curve, and then the cream and the ointment of the percutaneous administration are prepared, so as to lead principal medicine to avoid the liver first pass effect of oral administration to directly reach mammary gland target tissue, and to lead the concentration of target tissue internal medicine to be improved. Compared with the prior preparation at home and at abroad, the invention technically has the advantages that the prepared external preparation can reduce the side effect of Letrozole tablet and improve the curative effect of the Letrozole tablet, thereby the invention has good promotion and application value.

Description

technical field [0001] The invention relates to a percutaneous administration cream and ointment of the chemical drug letrozole and a preparation method thereof. Background technique [0002] Letrozole, English name Letrozole, chemical name 1-[bis(4-cyanophenyl)methyl]-1,2,4-triazole, molecular weight 285.31, melting point 182°-184°C, artificial Synthetic Benzyltriazole Derivatives. Letrozole reduces the level of estrogen by inhibiting aromatase, thereby eliminating the stimulating effect of estrogen on tumor growth. The in vivo activity of letrozole is 150-250 times stronger than that of the first-generation aromatase inhibitor, aminoglutethimide, and has a higher therapeutic index. At present, the drug only has oral preparations at home and abroad, and its disadvantages are: the first-pass effect of the liver cannot be avoided in clinical application; the incidence of adverse reactions that may be related to the drug is 33%, with nausea, headache, and bone pain as the ma...

Claims

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Application Information

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IPC IPC(8): A61K31/4196A61K9/06A61P35/00
Inventor 齐瑗晶卢霞周玲刘拥军刘爱芹于胜海
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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