Fulvestrant-containing medicine preparation

A technology for fulvestrant and pharmaceutical preparations, applied in the field of pharmaceutical preparations, can solve the problems of increasing muscle stimulation at the injection site, the irritation of benzyl benzoate, slow adsorption and the like

Inactive Publication Date: 2014-12-24
HANGZHOU JIUYUAN GENE ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] But there are still some deficiencies in the FASLODEX prescription. Its pharmaceutical adjuvant benzyl benzoate is irritating and will increase the muscle stimulation to the injection site; The plug cap slowly absorbs

Method used

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  • Fulvestrant-containing medicine preparation
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  • Fulvestrant-containing medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1 Dissolution of fulvestrant in different solvents

[0041] Fulvestrant was dissolved in different solvents respectively, and the dissolution conditions are shown in Table 1:

[0042] Table 1 Dissolution of fulvestrant in different solvents (25°C)

[0043]

[0044]

[0045] From the above test, it can be known that the solubility of fulvestrant in castor oil is better than that in other oil bases, which is beneficial to the sustained release of the drug; fulvestrant has good solubility in NMP and ethanol, which are respectively 864mg / ml and >200mg / ml.

Embodiment 2

[0046] Example 2 Determination of sink conditions (37°C, determination of in vitro release method)

[0047] The solubilizing effect of different solubilizers on the drug in PBS7.4 was measured, so as to obtain the solubilizing agent that could meet the solubilizing effect of the sink condition.

[0048] Known from above-mentioned test: in vitro release condition is the PBS (pH7.4) damping fluid 500mL that contains 0.25% SDS, 37 ℃, 50rpm constant temperature water-bath shaker, 0.5mL (containing medicament 25mg) prescription, direct release method (sink condition: 5 times).

[0049] Table 2 Solubilization effect of solubilizer on FVT

[0050] Solubilizers

Embodiment 3

[0051] Example 3 Investigating the in vitro release of different formulations of fulvestrant

[0052] Prepare the prescription solution according to Table 3, and then filter the prepared solution with a 0.22 μm filter.

[0053] Table 3 Composition of different formulations of fulvestrant

[0054]

[0055] The above-mentioned several groups of preparation prescriptions were carried out in vitro release test according to the following conditions: in 500ml containing 0.25% sodium lauryl sulfate, pH7.4 PB buffer solution, add 0.5ml sample, under the condition of 37 ℃, at a constant temperature of 100rpm Keep warm with reciprocating vibration in a water bath shaker. Regular sampling and testing. The test results are as follows:

[0056] Table 4 In vitro release test results of different formulations of fulvestrant

[0057]

[0058] As can be seen from the above tests, prescription 1 and prescription 7 have very similar release profiles in vitro ( figure 1 ). Fulvestrant...

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Abstract

The invention relates to a medicine preparation suitable for intramuscular injection. The medicine preparation contains fulvestrant, a pharmaceutically acceptable oleate excipient, pharmaceutically acceptable azone and a pharmaceutically acceptable alcohol. The medicine preparation overcomes the shortages of products available in the market in terms of irritation and safety, achieves an enough high active ingredient concentration, can be given to a patient with a low injection volume, and achieves an effective release rate in treatment effect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically the invention relates to a fulvestrant pharmaceutical preparation suitable for injection administration. Background technique [0002] According to statistics, breast cancer has become the cancer with the highest morbidity and mortality among women. At present, there are about 3 million breast cancer patients in the world every year, and the mortality rate is as high as more than 50%. In recent decades, the incidence of breast cancer in my country has been increasing year by year. The patients are mainly women between the ages of 40 and 60, around menopause, and showing a younger trend. [0003] Endocrine therapy for breast cancer has a history of hundreds of years. As early as the end of the nineteenth century, it was reported that bilateral oophorectomy could be used to treat premenopausal advanced breast cancer, which opened a precedent for endocrine therapy f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/565A61P35/00
Inventor 刘晓妮马南佳姜俊王沿江周胜军戎亚雯尚小广陈历翁文锃
Owner HANGZHOU JIUYUAN GENE ENG
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