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Fulvestrant or fulvestrant derivative sustained release preparation and preparation method thereof

A technology of fulvestrant and sustained-release preparations, applied in the field of pharmaceutical preparations, can solve problems such as case reports of no adverse reactions of azone

Inactive Publication Date: 2012-07-25
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, azone has no adverse reaction case reports in clinical use

Method used

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  • Fulvestrant or fulvestrant derivative sustained release preparation and preparation method thereof
  • Fulvestrant or fulvestrant derivative sustained release preparation and preparation method thereof
  • Fulvestrant or fulvestrant derivative sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0120] The solubility test of experimental example 1 fulvestrant

[0121] Experimental Instruments and Medicines

[0122] Vortex instrument, ultrasonic cleaning machine, magnetic stirrer, high performance liquid chromatography, manual pipettes of different specifications and matching nozzles, nozzle boxes, 7ml vials, matching bottle stoppers, aluminum caps.

[0123] Fulvestrant raw material, provided by the Second Pharmaceutical Factory of Xi’an Libang Pharmaceutical Co., Ltd., batch number: 080701; 1,3-butanediol, Sinopharm Chemical Reagent Co., Ltd., batch number: F20090805, imported sub-package; glycerol, Shantou City Ziguang Guhan Amino Acid Co., Ltd., batch number 060306; corn oil, North China Pharmaceutical Kangxin Co., Ltd., batch number: 081002; sunflower oil, Shanghai Jiage Food Co., Ltd., batch number: 20091113; soybean oil for injection, Xi'an Libang Pharmaceutical Co., Ltd. Provided by the First Pharmaceutical Factory; olive oil, injection grade, in bulk; rapeseed...

experiment example 2

[0129] Experimental Example 2 Miscibility test of different solvents in vitro

[0130] Divide the above-mentioned different solvents into oily solvents and non-oil-soluble solvents, accurately measure 0.5ml of each of the different solutions, mix each other, vortex for 5 minutes, and stand still for 10 minutes, observe and record the mutual miscibility of different solvents, the next day Observe and verify again, the results are as follows:

[0131] Table 2 Miscibility statistics between two different solvents

[0132]

[0133] Remarks: Take 0.5ml of each of the two solvents, mix with each other, observe the miscibility at rest, the experimental temperature is room temperature, the mixed oil is a mixture of soybean oil and castor oil, N-methylpyrrolidone is also called N-methyl-2 - pyrrolidone.

[0134] The experimental results show that oil-soluble azone and N-methyl-2-pyrrolidone can choose different oil solutions as dispersants, and dimethyl sulfoxide can only choose cas...

experiment example 3

[0135] Experimental Example 3 Miscibility test of different excipients in vitro

[0136] With reference to Experimental Example 1 and 2 experimental results, oil-soluble azone, dimethyl sulfoxide, N-methyl-2-pyrrolidone are respectively used as cosolvents, benzyl benzoate, ethyl oleate, glyceryl triacetate, Soybean oil and castor oil were used as dispersants, and benzyl alcohol and chlorobutanol were used as analgesics. The miscibility tests of different excipients were carried out, and the results are shown in Table 3.

[0137] Table 3 Miscibility and dissolution statistics among cosolvents, dispersants, and analgesics

[0138]

[0139] Remarks: Take 0.5ml of different solvents, miscible, observe the miscibility at rest, the ratio of mixed oil is 1:1, the experimental temperature is room temperature, W is benzyl alcohol, U is chlorobutanol.

[0140] The experimental results show that oil-soluble azone and N-methyl-2-pyrrolidone can choose ethyl oleate, benzyl benzoate, gl...

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Abstract

The invention relates to a long-acting fulvestrant or fulvestrant derivative sustained release preparation and preparation method of the long-acting fulvestrant or fulvestrant derivative sustained release preparation. The formula of the preparation provided by the invention comprises (1) 10mg / ml to 500mg / ml fulvestrant or fulvestrant derivative served as the active compound based on the content of preparation, (2) 3% to 80% of ketone compound or dimethyl sulfoxide served as the cosolvent based on the total weight of the preparation, (3) dispersing agent using vegetable oil or synthetic grease (ester), (4) analgesic, and (5) optional antioxidant.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to fulvestrant or its derivative sustained-release preparations and a preparation method thereof, in particular to the formulation and preparation of a class of breast cancer treatment drug fulvestrant or its derivative sustained-release preparations method. Background technique [0002] According to statistics, nearly 1 million breast cancer patients are diagnosed every year in the world, accounting for 20% of new malignant tumors in women, and its incidence rate accounts for 7-10% of various malignant tumors in the whole body. It is a disease that seriously affects women's body and mind. One of the most common malignant tumors that threatens health and even life. In recent decades, the incidence of breast cancer in my country has been increasing year by year, and the patients are mainly women between the ages of 40 and 60, before and after menopause, and they are getting ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/565A61K47/20A61K47/22A61K47/44A61P35/00
CPCA61K47/08A61K47/14A61K47/44A61K47/20A61K9/08A61K47/22A61K31/565A61P35/00
Inventor 卢伍党余惟平陈涛蔡睿
Owner XIAN LIBANG PHARMA
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