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Preparation method and application of tropisetron citrate crystal form II

A technology of tropisetron citrate and tropisetron, which is applied in the fields of medicine and biology, can solve the problem of undisclosed crystal form and preparation method of tropisetron citrate, no mention of spectral characteristics of crystal form, and no crystal form. Problems such as stereotyping, to achieve the effect of high yield, low cost and good safety

Active Publication Date: 2015-06-10
回音必集团抚州制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In Chinese patent 200910114940, it is disclosed that the applicant of the present invention is Huiyinbi Group Fuzhou Pharmaceutical Co., Ltd. A synthesis process of tropisetron citrate, but the crystal form is amorphous, and the existing literature does not disclose the crystal form and preparation method of tropisetron citrate, and does not mention the relevant crystal form. spectral characteristics

Method used

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  • Preparation method and application of tropisetron citrate crystal form II
  • Preparation method and application of tropisetron citrate crystal form II
  • Preparation method and application of tropisetron citrate crystal form II

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Example 1 Preparation of Tropisetron Citrate Form II

[0031] Take 1.0g of tropisetron citrate raw material, add 20~50ml of 20% acetone water, and the temperature of the water bath is not higher than 60 oC Stir to dissolve, cool and keep for 10 oC The following crystallization, the crystallization time is not less than 2 hours, after the crystallization ends, suction filtration is separated, obtains tropisetron citrate solid, at 60 o C~80 oC , bake for 0.5~1 hour first, then bake at 90 oC ~105 oC Let it dry for 1-2 hours. The obtained tropisetron citrate crystal form II X-diffraction spectrum, infrared spectrogram and differential scanning calorimetry diagram and attached figure 1 , attached figure 2 , attached image 3 unanimous.

Embodiment 2

[0032] Example 2 Tablet of tropisetron citrate crystal form II and its preparation

[0033] Prescription: Tropisetron citrate crystal form II 8.38g, lactose 70g, microcrystalline cellulose 40g, hypromellose 10g, sodium starch glycolate 6g, magnesium stearate 9g, polyethylene glycol 6000 6 g, appropriate amount of 5% povidone aqueous solution.

[0034]Preparation method: pass the above raw materials through an 80 mesh sieve and weigh them according to the above amounts, then mix the prescribed amount of tropisetron citrate, lactose, hypromellose, polyethylene glycol 6000 and 20g of microcrystalline cellulose Uniformly, use 5% povidone aqueous solution to make soft materials, cross 20 mesh sieves to granulate, then dry, granulate, then mix evenly with 20g microcrystalline cellulose, sodium carboxymethyl starch and magnesium stearate in prescription quantities, Compress it into 1000 tablets to obtain tropisetron citrate crystal form II tablets, each containing 8.38 mg of tropi...

Embodiment 3

[0035] Example 3 Capsules Containing Tropisetron Citrate Form II and Its Preparation

[0036] Prescription: Tropisetron citrate crystal form II 8.38g, lactose 50g, microcrystalline cellulose 60g, sodium carboxymethyl starch 30g, magnesium stearate 1g.

[0037] Preparation method: above-mentioned lactose, microcrystalline cellulose, and sodium carboxymethyl starch were pulverized respectively through a 100 mesh sieve, and o C dried for more than 10 hours, cooled to room temperature, mixed evenly with tropisetron citrate, dry granulated, added magnesium stearate, mixed evenly, filled into 1000 empty capsules, and acquired tropisetron citrate For the capsules of agar crystal form II, each capsule contains 8.38 mg of tropisetron citrate crystal form II, calculated as 5 mg of tropisetron citrate.

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Abstract

The invention discloses a preparation method and an application of a tropisetron citrate crystal form II. The tropisetron citrate crystal form II is obtained through selecting from different crystal solvents and temperatures. The tropisetron citrate crystal form is simple in preparation technology, and has good stability; a sample prepared with the method can effectively reduce residual quantity of introduced solvents, such as methylbenzene, trichloromethane and pyridine in a synthesis process; product purity is better; and industrial production is facilitated.

Description

Technical field [0001] The present invention is a medical and biological field. It involves a new type of antivaritic oxic acid total citrus citrus citrus citrus citron crystal Ⅱ preparation method and its application in drug development. Background technique [0002] Tropisetron Hydrochloride (foreign product name: Navoban), developed by Switzerland, is an efficient, selective 5-HT3 receptor antagonist.Patients in preventing and treating tumor patients with nausea and vomiting caused by chemotherapy, radiotherapy or postoperative.The oral absorption of this drug is rapid and complete, with good tolerance, and adverse reactions of no taper. It can be used as the preferred drug for patients with cancer and chemotherapy patients.With the end of the protection period, domestic imitation research began, Echo Bing Group Fuzhou Pharmaceutical Co., Ltd. The independent research and development has obtained the patented patent of citrate alkamine, and the raw materials and preparations a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D451/12C07C59/265C07C51/43A61K31/46A61P1/08
Inventor 王大冲王建张恒袁继刚
Owner 回音必集团抚州制药有限公司