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Fosaprepitant dimeglumine composition for injection

A fosaprepitant dimeglumine and composition technology, applied in the field of freeze-dried compositions for injection containing fosaprepitant dimeglumine and melatonin, can solve the problem of low absolute bioavailability and maintenance in vivo Short time, large individual differences, etc., to achieve the effect of facilitating treatment, reducing the first-pass effect, and reducing dosage

Inactive Publication Date: 2013-09-18
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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  • Fosaprepitant dimeglumine composition for injection
  • Fosaprepitant dimeglumine composition for injection
  • Fosaprepitant dimeglumine composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0020] 1. Prescription

[0021]

[0022] 2. Preparation process

[0023] a) Add 115g of fosaprepitant dimeglumine (calculated as fosaprepitant) and 600g of mannitol into 1500ml of water for injection and stir to dissolve, then add 1g 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 fosaprepitant, 1...

Embodiment 2

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

[0028] 1. Prescription

[0029]

[0030] 2. Preparation process

[0031] a) Add 115g of fosaprepitant dimeglumine (calculated as fosaprepitant) and 200g of mannitol into 1500ml of water for injection and stir to dissolve, then add 2g 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 fosaprepitant, 1...

Embodiment 3

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

[0036] 1. Prescription

[0037]

[0038] 2. Preparation process

[0039] a) Add 115g of fosaprepitant dimeglumine (calculated as fosaprepitant) and 300g of mannitol into 1500ml of water for injection and stir to dissolve, then add 0.6g 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 fosaprepitant,...

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Abstract

The invention provides a fosaprepitant dimeglumine composition for injection, and relates to the technical field of medicine manufacturing. The main medicine of the composition comprises fosaprepitant dimeglumine and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-included slow release part. According to the fosaprepitant dimeglumine composition for injection provided by the invention, the therapeutic effect of fosaprepitant dimeglumine is improved, instability caused by oral administration of MT (Melatonin) is avoided and MT is quick to distribute and eliminate and the like, and the first pass effect of MT is reduced. The dosage of fosaprepitant dimeglumine is reduced. The design of dosage combining quick release and slow release is in accordance with secretion characteristic of MT, so that the problem of half-life period of MT is solved and the bioavailability of the product is improved. The composition has the synergistic effect to treat CINV (Chemotherapy Induced Nausea And Vomiting) by fosaprepitant dimeglumine, and fosaprepitant dimeglumine and melatonin are combined to not only treat CINV so as to improve the therapeutic effect of fosaprepitant dimeglumine to CINV and shorten the course of treatment, but also reduce the use level of fosaprepitant dimeglumine, reduce the side effect of fosaprepitant dimeglumine and improve the immunity of a human body. The stress response of organism can be effectively reduced by maintaining melatonin in a certain concentration in blood of a human body to the benefit of treatment of CINV.

Description

Technical field: [0001] The present invention relates to the technical field of medicine and medicine manufacture, in particular to a fosaprepitant dimeglumine composition for injection, more specifically, to an injection containing fosaprepitant dimeglumine and melatonin The composition is lyophilized. 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 ...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61K9/19A61P1/08A61K31/4045
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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