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Formulations of fosaprepitant and aprepitant

A water-based preparation and solid preparation technology, which is applied in the field of fosaprepitant and aprepitant preparations, can solve the problems of treatment refusal and delay

Active Publication Date: 2019-05-21
ZHUHAI BEIHAI BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The syndrome has a significant impact on patients' functional status and quality of life, and patients may delay scheduled chemotherapy due to CINV and sometimes even refuse potentially curative treatments

Method used

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  • Formulations of fosaprepitant and aprepitant
  • Formulations of fosaprepitant and aprepitant
  • Formulations of fosaprepitant and aprepitant

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0536] Example 1: Composition comprising Fosaprepitant and Human Serum Albumin (HSA).

[0537] The prepared fosaprepitant dimeglumine and HSA have a weight ratio of about 1:40.

[0538] In a vial, Fosaprepitant dimeglumine (10 mg) was dissolved in water (2 ml) to give a clear solution. A solution of HSA (400 mg, 2 ml) (20% human serum albumin solution for infusion (product name: AlbuRx) from CSLBehring) was added to a vial of fosaprepitant dimeglumine aqueous solution at 0°C . After the addition was complete, a clear solution was obtained. The resulting clear aqueous solution was lyophilized overnight to give a white solid.

[0539] A 100 mg lyophilized solid sample was reconstituted by adding 2 mL of water to obtain a clear aqueous solution.

example 2

[0540] Example 2: Composition comprising fosaprepitant and human serum albumin (HSA).

[0541] The prepared fosaprepitant dimeglumine and HSA have a weight ratio of about 1:20.

[0542] In a vial, Fosaprepitant dimeglumine (10 mg) was dissolved in water (1 ml) to give a clear solution. A solution of HSA (200 mg, 1 ml) (20% human serum albumin solution for infusion (product name: AlbuRx) from CSLBehring) was added to a vial of fosaprepitant dimeglumine aqueous solution at 0°C . After the addition was complete, a clear solution was obtained. The resulting clear aqueous solution was lyophilized overnight to give a white solid.

[0543] A 100 mg lyophilized solid sample was reconstituted by adding 2 mL of water to obtain a clear aqueous solution.

example 3

[0544] Example 3: Compositions comprising fosaprepitant and human serum albumin (HSA).

[0545] The prepared fosaprepitant dimeglumine and HSA have a weight ratio of about 1:4.

[0546] In a vial, Fosaprepitant dimeglumine (25 mg) was dissolved in water (1.5 ml) to give a clear solution. A solution of HSA (100 mg, 0.5 ml) (20% human serum albumin solution for infusion (product name: AlbuRx) from CSLBehring) was added to a vial of fosaprepitant dimeglumine aqueous solution at 0°C middle. After the addition was complete, a clear solution was obtained. The resulting clear aqueous solution was lyophilized overnight to give a white solid.

[0547] A 100 mg lyophilized solid sample was reconstituted by adding 2 mL of water to obtain a clear aqueous solution.

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Abstract

This document relates to a composition comprising fosaprepitant, or a pharmaceutically acceptable salt thereof, and human serum albumin, wherein the fosaprepitant, or a pharmaceutically acceptable salt thereof, and the human serum albumin in the composition have a ratio by weight from about 1:0.1 to about 1:500. This document also relates to a composition comprising aprepitant and human serum albumin, wherein the aprepitant and the human serum albumin in the composition have a ratio by weight from about 1:80 to about 1:1000. This document also relates to a composition comprising fosaprepitant,or a pharmaceutically acceptable salt thereof, aprepitant and human serum albumin.

Description

[0001] priority statement [0002] This application claims the benefit of U.S. Provisional Application No. 62 / 370,453, filed August 3, 2016, and U.S. Provisional Application No. 62 / 412,085, filed October 24, 2016. The entire contents of the aforementioned applications are hereby incorporated by reference. technical field [0003] This document relates to compositions and formulations for the treatment and prevention of chemotherapy-induced nausea and vomiting, more particularly to compositions comprising fosaprepitant or a pharmaceutically acceptable salt thereof, compositions comprising aprepitant , and a composition comprising fosaprepitant or a pharmaceutically acceptable salt thereof and aprepitant. Background technique [0004] Nausea and vomiting are common complications of cancer chemotherapy. Patients consistently report that chemotherapy-induced nausea and vomiting (CINV) is the aspect of treatment they find most unpleasant and distressing. The syndrome has a sig...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61K31/5377A61K38/38A61K47/42
CPCA61K31/5377A61K45/06A61K47/42A61K9/08A61P1/08A61K2300/00A61K31/675A61K9/0019A61K9/19A61K38/385Y02A50/30
Inventor 孙群
Owner ZHUHAI BEIHAI BIOTECH CO LTD
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