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Pharmaceutical preparation for injection administration and preparation method thereof

A pharmaceutical preparation and drug delivery technology, applied in the field of pharmaceutical preparations and preparations for the treatment of advanced breast cancer in women, can solve the problems of decreased gastrointestinal absorption function, low bioavailability, difficulty of anastrozole, etc., and achieve the goal of overcoming gastrointestinal problems. Intestinal stimulation, volume and weight reduction, transport and storage suitable effects

Inactive Publication Date: 2009-11-04
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the common anastrozole preparations in the market are tablets, which are inconvenient for patients to take, have low bioavailability, and are highly irritating to the gastrointestinal tract, especially for severe cancer patients who have difficulty taking medicine and long-term use of anti-inflammatory drugs. For patients with decreased gastrointestinal absorption function caused by tumor drugs, the compliance of anastrozole tablets decreases, which greatly limits the clinical application of anastrozole
For this reason, some researchers made anastrozole into dispersible tablets to solve the problems of nausea, vomiting, diarrhea and other adverse reactions caused by long-term application of anastrozole, but its bioavailability is still very limited (CN1634042A)
In addition, because anastrozole is poorly soluble in water, it is generally considered unsuitable for injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: freeze-dried powder injection

[0023] prescription:

[0024] Anastrozole 1g

[0025] Mannitol 100g

[0026] Hydrochloric acid (0.1mol / l) appropriate amount

[0027] Add water for injection to 2000ml

[0028]

[0029] 1000 pieces

[0030] Preparation process: take the prescribed amount of anastrozole and freeze-dried support agent, add water for injection, adjust the pH to 5.5 with a pH regulator, and stir to dissolve. Add 0.1% activated carbon for needles, stir at room temperature for 15 minutes, filter water for injection to 2000ml, pass through a 0.2μm microporous membrane, measure the content, and put it in 7ml vials, 3ml each. Put the canned samples into a freeze dryer, first lower the temperature to -45°C, keep it warm for 2 hours, vacuumize after heating, and heat up at about 2°C / hour, when the temperature reaches -5°C, press 5°C / hour Heat up to 25°C within 1 hour, keep warm for 2 hours, a...

Embodiment 2

[0032] Embodiment 2: freeze-dried powder injection

[0033] prescription:

[0034] Anastrozole 1g

[0035] Dextran 100g

[0036] Hydrochloric acid (0.1mol / l) 5g

[0037] Add water for injection to 2000ml

[0038]

[0039] 1000 pieces

[0040] Preparation process: with embodiment 1.

[0041] The samples were kept for 6 months under natural conditions, and the high pressure liquid phase inspection showed that the quality was stable. It passed the pyrogen test and the light inspection of clarity.

Embodiment 3

[0042] Embodiment 3: freeze-dried powder injection

[0043] prescription:

[0044] Anastrozole 1g

[0045] Hydrolyzed Gelatin 150g

[0046] Hydrochloric acid (0.1mol / l) appropriate amount

[0047] Add water for injection to 2000ml

[0048]

[0049] 1000 pieces

[0050] Preparation process: with embodiment 1.

[0051] The samples were kept for 6 months under natural conditions, and the high pressure liquid phase inspection showed that the quality was stable. It passed the pyrogen test and the light inspection of clarity.

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PUM

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Abstract

The invention relates to a pharmaceutical preparation for injection administration, comprising anastrozole and a pH regulator with a pH value of 4 to 7. The pharmaceutical preparations can be lyophilized powder for injection, an injection or an infusion. The invention also provides a preparation method of the pharmaceutical preparation, comprising the step that the pH regulator is used to adjust the pH value of an anastrozole solution to be 4 to 7. The invention has the advantages: (1) the problems that the anastrozole is insoluble in water and inapplicable to make injections in the prior art are successfully solved, the defect that anastrozole tablets irritate the intestines and the stomach is overcome, and the bioavailability of the anastrozole tablets is greatly improved so as to be more effectively used in the treatment of the late breast cancer of women; (2) the anastrozole pharmaceutical preparation for injection administration has stable properties to light, heat, oxygen, water, and the like, has no pollution, is convenient to prepare, transport and store and is suitable for mass production; (3) the lyophilized powder for injection solves the problems of winter transportation and storage in North and alpine regions, reduces the size and the weight of a product with the same dosage and greatly decreases the transportation cost of business links; and (4) the injection and the infusion can effectively prevent pollution in the dispensation process.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for injection administration and a preparation method thereof, in particular to a pharmaceutical preparation for injection administration for treating advanced breast cancer in women and a preparation method thereof. Background technique [0002] Aromatase inhibitors can inhibit the activity of aromatase, thereby reducing the level of estrogen in the human body and achieving the purpose of treating breast cancer. Anastrozole is a third-generation aromatase inhibitor, which has a very good therapeutic effect for the treatment of advanced breast cancer in postmenopausal women, and is also effective for patients who have failed tamoxifen treatment. Compared with the first-generation aromatase inhibitor aminoglutethimide and the second-generation aromatase inhibitor formestane, anastrozole has stronger effects and fewer side effects. [0003] At present, the common anastrozole preparations in the marke...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4196A61K9/19A61P35/00
Inventor 王浩史可吟靳朝东罗振福李玲
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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