Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Ramosetron composition for injection

A technology of ramosetron and its composition, which is applied in the field of pharmaceuticals and pharmaceutical manufacturing, can solve the problems of low absolute bioavailability, short maintenance time in vivo, strong first-pass effect, etc., shorten the course of treatment, reduce the first-pass effect, Improve the effect of treatment

Inactive Publication Date: 2013-10-02
HAINAN WEI KANG PHARMA QIANSHAN
View PDF0 Cites 1 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Ramosetron composition for injection
  • Ramosetron composition for injection
  • Ramosetron composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0020] 1. Prescription

[0021]

[0022] 2. Preparation process

[0023] a) Add 1 g of ramosetron hydrochloride (calculated as ramosetron) and 5 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 ramosetron, 0.1mg per bottle;

[0026] d) Fill accordin...

Embodiment 2

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

[0028] 1. Prescription

[0029]

[0030] 2. Preparation process

[0031] a) Add 1 g of ramosetron hydrochloride (calculated as ramosetron) and 5 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 ramosetron, 0.1mg per bottle;

[0034] d) Fill acco...

Embodiment 3

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

[0036] 1. Prescription

[0037]

[0038] 2. Preparation process

[0039] a) Add 1 g of ramosetron hydrochloride (calculated as ramosetron) and 5 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 ramosetron, 0.1mg per bottle;

[0042] d) Fill ac...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a ramosetron composition for injection, and relates to the technical field of medicines and medicine manufacturing. Main medicines of the composition are ramosetron and melatonin. The melatonin comprises a quick release part and a slow release part contained in cyclodextrin. The ramosetron composition for injection provided by the invention has the functions of improving the treatment effect of ranitidine, avoiding instability, fast distribution and elimination and the like of MT (Melatonin) caused by oral absorption, reducing the first pass effect of MT and reducing the dosage of ramosetron. Delivery design combining quick release and slow release meets the physiological secretion characteristic of MT, solves the problem of short half life of MT and improves the bioavailability of the product. The composition has a synergistic effect on treatment of CINV (Chemotherapy Induced Nausea And Vomiting) by ramosetron, and after the melatonin is combined with ramosetron, not only is the CINV treated, is the treatment effect of the ramosetron on the CINV improved and is the course of treatment shortened, but also the use level of the ramosetron and the side effect of the ramosetron are reduced, and the immunity of human body is improved. The melatonin in a certain concentration in human blood has the capability of effectively reducing melatonin of human body to the benefit of treatment of the CINV.

Description

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/4184A61K47/48A61K9/19A61P1/08A61P37/04A61K31/4045
Inventor 汪六一汪金灿郝结兵李彪吴函峰
Owner HAINAN WEI KANG PHARMA QIANSHAN
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com