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
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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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