Aprepitant composition for injection

A technology of aprepitant and composition, applied in the field of freeze-dried composition for injection containing aprepitant and melatonin, which can solve the problem of low absolute bioavailability, short maintenance time in vivo, strong first-pass effect, etc. problem, to achieve the effect of facilitating treatment, reducing the first-pass effect, and improving the treatment effect

Inactive Publication Date: 2013-09-25
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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  • Aprepitant composition for injection
  • Aprepitant composition for injection
  • Aprepitant composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0020] 1. Prescription

[0021]

[0022] 2. Preparation process

[0023] a) Add 80g of aprepitant and 500g 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 aprepitant, 80mg per bottle;

[0026] d) Fill according to the test requirements, put it into a f...

Embodiment 2

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

[0028] 1. Prescription

[0029]

[0030] 2. Preparation process

[0031] a) Add 80g of aprepitant and 400g of mannitol to 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 aprepitant, 80mg per bottle;

[0034] d) Fill according to the test requirements, put it into a fre...

Embodiment 3

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

[0036] 1. Prescription

[0037]

[0038] 2. Preparation process

[0039] a) Add 80g of aprepitant and 500g 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 aprepitant, 80mg per bottle;

[0042] d) Fill according to the test requirements, put it into a...

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Abstract

The invention provides an aprepitant composition for injection, and relates to the technical field of medicaments and preparation of the medicaments. The composition comprises main drugs of aprepitant and melatonin, wherein the melatonin comprises a quick release part and a slow-released part cladded by cyclodextrin. By adopting the aprepitant composition for injection provided by the invention, the treatment effect of the aprepitant is improved; the instability, distribution, fast removal and the like caused by oral absorption of MT (melatonin) are avoided; the first-pass effect of the MT is reduced; the dosage of the aprepitant is reduced; the administration design of combining quick release with slow release accords with the physiological secretion characteristics of the MT; the short half-life period of the MT is solved; the product bioavailability is improved; the composition has synergism on treatment of CINV (chemotherapy induced nausea and vomiting) by the aprepitant; not only can the CINV be treated after combining the MT with the aprepitant, but also the treatment effect of the aprepitant on the CINV is improved; the treatment course is shortened; the dosage of the aprepitant is also reduced; the side effect of the aprepitant is reduced; the human immunity can be improved; certain concentration of melatonin is maintained in blood of a human body, so that the stress reaction of the organism can be effectively reduced; treatment of the CINV is facilitated.

Description

Technical field: [0001] The invention relates to the technical field of medicine and medicine manufacture, in particular to an injection aprepitant composition, and more specifically, to an injection freeze-dried composition containing aprepitant 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 concentra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/4045A61K9/19A61P1/08
CPCA61K9/0019A61K9/19A61K31/4045A61K31/5377A61K47/40A61P1/08A61K2300/00
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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