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Tropisetron composition for injection

A technology of tropisetron and composition, which is applied in the field of freeze-dried compositions for injection containing tropisetron and melatonin, can solve the problem of low absolute bioavailability, short maintenance time in vivo, strong first-pass effect, etc. problems, to shorten the course of treatment, reduce the first-pass effect, and improve the effect of treatment

Inactive Publication Date: 2013-10-23
HAINAN WEI KANG PHARMA QIANSHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although MT has a variety of physiological functions and pharmacological effects, it has unstable oral absorption kinetics, rapid distribution and clearance, and t 1 / 2 Short (30-50min), large individual differences, strong first-pass effect, low absolute bioavailability (1%-37%), and short maintenance time in vivo (1-3h)

Method used

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  • Tropisetron composition for injection
  • Tropisetron composition for injection
  • Tropisetron composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1, preparation of tropisetron composition freeze-dried powder for injection, in 1000 pieces

[0020] 1. Prescription

[0021]

[0022] 2. Preparation process

[0023] a) Add 5 g of tropisetron hydrochloride (calculated as tropisetron) and 30 g of mannitol into 1500 ml of water for injection and stir to dissolve, then add 1 g of melatonin and stir evenly;

[0024] b) Add 3g of melatonin and 14.66g of moderately substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 6 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0025] c) Add NaOH solution to adjust the pH value after mixing the above-mentioned group a and b solutions, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, filter the liquid medicine through 0.45 μm and 0.22 μm microporous membranes, and detect the content of intermediates, According to tropisetron, 5 mg per bottle;

[0026] d) Fill acco...

Embodiment 2

[0027] Embodiment 2, preparation of tropisetron composition freeze-dried powder for injection, in 1000 pieces

[0028] 1. Prescription

[0029]

[0030] 2. Preparation process

[0031] a) Add 5 g of tropisetron hydrochloride (calculated as tropisetron) and 30 g of mannitol into 1500 ml of water for injection and stir to dissolve, then add 2 g of melatonin and stir evenly;

[0032] b) Add 6g of melatonin and 29.32g of moderately substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 8 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0033] c) Add NaOH solution to adjust the pH value after mixing the above-mentioned group a and b solutions, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, filter the liquid medicine through 0.45 μm and 0.22 μm microporous membranes, and detect the content of intermediates, According to tropisetron, 5 mg per bottle;

[0034] d) Fill acco...

Embodiment 3

[0035] Embodiment 3, preparation of tropisetron composition freeze-dried powder for injection, in 1000 pieces

[0036] 1. Prescription

[0037]

[0038] 2. Preparation process

[0039] a) Add 5 g of tropisetron hydrochloride (calculated as tropisetron) and 30 g of mannitol into 1500 ml of water for injection and stir to dissolve, then add 0.6 g of melatonin and stir evenly;

[0040] b) Add 1.8g of melatonin and 8.8g of moderately substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 5 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0041] c) Add NaOH solution to adjust the pH value after mixing the above-mentioned group a and b solutions, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, filter the liquid medicine through 0.45 μm and 0.22 μm microporous membranes, and detect the content of intermediates, According to tropisetron, 5 mg per bottle;

[0042] d) Fill ac...

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Abstract

The invention provides a tropisetron composition for injection and relates to the technical fields of medicines and medicine preparation. The tropisetron composition is characterized in that the main medicines are tropisetron and melatonin, wherein the melatonin comprises a quick release part and a slow release part included by cyclodextrin. According to the tropisetron composition provided by the invention, the treating effect of the tropisetron is improved; problems of instability and rapidness in distribution and clearing caused when MT (melatonin) is orally absorbed are avoided, and a first-pass effect of the MT is reduced; the use level of the tropisetron is lowered; a medicine administration design in which a quick release manner and a slow release manner are combined is accordant with physiological secretion characteristics of the MT, the problem of the MT that the half-life period is short is solved, and the biological availability of a product is improved; the treatment of the tropisetron to CINV (Chemotherapy Induced Nausea and Vomiting) is enhanced, after the tropisetron and the melatonin are combined, not only the CINV can be treated, the treatment effect of the tropisetron to the CINV can be improved, the treatment course can be shortened, but also the use level of the tropisetron is lowered, the side effect of the tropisetron is reduced, and the immune capability of a human body can be improved; by maintaining the melatonin with a certain concentration in the blood of the human body, a stress reaction of the body can be effectively reduced, and the treatment of the CINV is benefited.

Description

Technical field: [0001] The invention relates to the technical field of medicine and medicine manufacture, in particular to a tropisetron composition for injection, and more specifically, to a freeze-dried composition for injection containing tropisetron and melatonin. Background technique: [0002] Because platinum, doxorubicin and other anti-tumor drugs will cause severe vomiting during the use, acute and severe nausea and vomiting may lead to dehydration, electrolyte imbalance, and malnutrition in patients, and severe cases may be caused by damage to the digestive tract mucosa. Bleeding, infection, and even death will make patients fear chemotherapy and significantly reduce their compliance. As a result, chemotherapy will be reduced or discontinued, which will seriously affect the therapeutic effect. Therefore, antiemetic drugs are important adjuvant drugs for antitumor therapy, especially The use of drugs for the treatment of moderate and severe vomiting is also mainly c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/46A61K9/19A61K47/40A61P1/08A61K31/4045
Inventor 汪六一汪金灿郝结兵李彪吴函峰
Owner HAINAN WEI KANG PHARMA QIANSHAN
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