Freeze-dried powder injection of tropisetron hydrochloride composition serving as vomit-stopping drug and preparation method of freeze-dried powder injection

A technology for tropisetron hydrochloride and freeze-dried powder injection, which is applied in the field of medicine, can solve the problems such as unsatisfactory hygroscopicity of impurity content crystal form, difficulty in preparation preparation, influence on stability, etc., and achieves low content of insoluble particles and good fluidity , good stability

Inactive Publication Date: 2015-10-14
QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the prior art, there have been many studies on the crystal form of tropisetron hydrochloride, but the impurity content, stability and hygroscopicity of the crystal form are still not ideal, which affects its own stability and also brings problems to the preparation of the preparation. here comes the difficulty

Method used

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  • Freeze-dried powder injection of tropisetron hydrochloride composition serving as vomit-stopping drug and preparation method of freeze-dried powder injection
  • Freeze-dried powder injection of tropisetron hydrochloride composition serving as vomit-stopping drug and preparation method of freeze-dried powder injection
  • Freeze-dried powder injection of tropisetron hydrochloride composition serving as vomit-stopping drug and preparation method of freeze-dried powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of Tropisetron Hydrochloride Crystals

[0028] (1) Grind the crude product of tropisetron hydrochloride, pass it through a 60-mesh sieve, then add it into deionized water whose volume is 6 times the weight of tropisetron hydrochloride, and stir at 130 rpm for 10 minutes;

[0029] (2) Add ethanol whose volume is 4 times the weight of tropisetron hydrochloride under stirring at 90 rpm, and raise the temperature to 30°C at the same time;

[0030] (3) After the solution is added, let it stand for 3 hours, and add dropwise a mixed solution of ether and chloroform whose volume is 8 times the weight of tropisetron hydrochloride at 0°C under the condition of stirring at 150 rpm. The volume ratio of methane is 2: 3, and the uniform dropwise addition is completed within 2h;

[0031] (4) After the dropwise addition was completed, the temperature was lowered to -5°C, and stirring was continued at a stirring rate of 110 rpm for 2 h, and the crystals were pr...

Embodiment 2

[0033] Example 2: Preparation of tropisetron hydrochloride freeze-dried powder injection:

[0034] Prescription: in parts by weight, 3 parts of tropisetron hydrochloride crystalline compound prepared in Example 1, and 15 parts of trehalose.

[0035] Take the tropisetron hydrochloride compound of the present invention, stir and dissolve it with water for injection, add the prescribed amount of trehalose, adjust the pH value to 6.0-8.0, then stir until the pH remains constant, add water for injection until the volume of the solution is tropane hydrochloride 100 times the weight of setron, then coarsely filter with activated carbon, pass through 1.0μm, 0.45μm, 0.22μm microporous membranes in turn to sterilize and filter, filter into a sterile room, measure pH and content after passing, fill, press half Stopper, put it into a freeze-drying box that has been cooled to -40°C, freeze-dry at low temperature, press the stopper out of the box, and roll the cap.

[0036] Described fre...

Embodiment 3

[0040] Example 3: Preparation of tropisetron hydrochloride freeze-dried powder injection:

[0041] Prescription: in parts by weight, 3 parts of tropisetron hydrochloride crystalline compound prepared in Example 1, and 18 parts of trehalose.

[0042] Take the tropisetron hydrochloride compound of the present invention, stir and dissolve it with water for injection, add the prescribed amount of trehalose, adjust the pH value to 6.0-8.0, then stir until the pH remains constant, add water for injection until the volume of the solution is tropane hydrochloride 100 times the weight of setron, then coarsely filter with activated carbon, pass through 1.0μm, 0.45μm, 0.22μm microporous membranes in turn to sterilize and filter, filter into a sterile room, measure pH and content after passing, fill, press half Stopper, put it into a freeze-drying box that has been cooled to -40°C, freeze-dry at low temperature, press the stopper out of the box, and roll the cap.

[0043] Described fre...

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Abstract

The invention relates to a freeze-dried powder injection of a tropisetron hydrochloride composition serving as a vomit-stopping drug and a preparation method of the freeze-dried powder injection, belonging to the technical field of medicines. The composition comprises tropisetron hydrochloride and an excipient, wherein the excipient is trehalose, and the tropisetron hydrochloride is a compound in a novel crystal form; an x-ray powder diffraction diagram obtained through Cu-K alpha ray measurement is as shown in the figure 1; the tropisetron hydrochloride is different from the tropisetron hydrochloride reported by the prior art. Experiments prove that the compound in the novel crystal form is high in purity, good in flowability and stability, low in impurity content, low in moisture absorption possibility as well as safe and reliable in clinical application; and the freeze-dried powder injection prepared from the compound in the novel crystal form is good in stability after being matched with a solvent, extremely low in insoluble particle content and very suitable for clinical application.

Description

Technical field [0001] The present invention is a pharmaceutical technology field involving a kind of antivirus hydrochloride composition of the Joan composition. Background technique [0002] Tyl Hydrochloride is a selective peripheral neuron and a central nervous system 5 -hydroxylidin receptor antagonist. It can choose to block the vomiting reflex center.The 5 -hydroxylidal receptor of the club in the final region of the central nervous nerve can prevent and treat nausea and vomiting caused by chemotherapy, and does not cause adverse reactions in the outerotoma. [0003] In existing technologies, there are many studies for the crystal type of tot alkyl hydrochloride, but the impurities, stability, and crystalline humidity are still unsatisfactory.It's difficult. [0004] After a large number of experimental studies of the present invention, a hydrochloric acidocarcin compound that is different from existing technology has been made.Low is convenient for preparation of preparat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/46C07D451/12A61P1/08
Inventor 王贵宾
Owner QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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