Palonosetron composition for injection

A technology of palonosetron and composition, applied in the field of freeze-dried composition for injection containing palonosetron and melatonin, capable of solving low absolute bioavailability, short maintenance time in vivo, and first-pass effect Strong and other problems, to shorten the course of treatment, reduce the first-pass effect, improve the effect of treatment

Inactive Publication Date: 2013-10-09
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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  • Palonosetron composition for injection
  • Palonosetron composition for injection
  • Palonosetron composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0020] 1. Prescription

[0021]

[0022] 2. Preparation process

[0023] a) Add 2.5 g of palonosetron hydrochloride (calculated as palonosetron) and 15 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 Palonosetron, 0.25mg per bottle;

[0026] d) F...

Embodiment 2

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

[0028] 1. Prescription

[0029]

[0030] 2. Preparation process

[0031] a) Add 2.5g of palonosetron hydrochloride (calculated as palonosetron) and 15g 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 Palonosetron, 0.25mg per bottle;

[0034] d) Fill ...

Embodiment 3

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

[0036] 1. Prescription

[0037]

[0038] 2. Preparation process

[0039] a) Add 2.5g of palonosetron hydrochloride (calculated as palonosetron) and 15g 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 Palonosetron, 0.25mg per bottle;

[0042]d) Fill...

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Abstract

The invention provides a palonosetron composition for injection and relates to the technical field of medicaments and medicament manufacturing. The main medicaments of the composition are palonosetron and melatonin, wherein the melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The palonosetron composition for injection provided by the invention can be used for improving the treatment effect of the palonosetron, avoiding instability, quick distribution and elimination and the like of MT ((Metal Thionein) caused by oral absorption, reducing the first-pass effect of the MT and reducing the dosage of the palonosetron; The medicament administration design combining the quick release with the slow release satisfies physiological secretion characteristics of the MT, can be used for solving the problem that the half-life period of the MT is short, increasing the biological utilization rate of the palonosetron composition, and achieving the synergism of the palonosetron for treating CINV (Chemotherapy Induced Nausea And Vomiting). The quick release part and the slow release part are combined, so that not only can the CINV be treated, but also the treatment effect of the palonosetron on the CINV can be improved, and therefore, the treatment course is shortened, the dosage of the palonosetron is reduced, the side effect of the palonosetron is lowered, and the body immunity can be improved. A certain concentration of melatonin is kept in the blood of the human body, so that the stress response of the organisms can be effectively lowered for facilitating the treatment of the CINV.

Description

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

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/473A61K9/19A61K47/40A61P1/08A61P37/04A61K31/4045
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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