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Formulations and compositions of docetaxel

A technology of docetaxel and composition, applied in the field of preparations and compositions containing docetaxel and human serum albumin, can solve problems such as limitations

Pending Publication Date: 2020-11-13
ZHUHAI BEIHAI BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These properties limit the administration of docetaxel

Method used

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  • Formulations and compositions of docetaxel
  • Formulations and compositions of docetaxel
  • Formulations and compositions of docetaxel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0241] Example 1: Compositions comprising docetaxel, human serum albumin (HSA) and amino acids

[0242] To 7 different round bottom flasks were added (A) 4.5ml water; (B) 10mg arginine (Arg) dissolved in 4.5ml water; (C) 10mg aspartic acid (Arg) dissolved in 4.5ml water ( Asp); (D) 10 mg cysteine ​​(Cys) dissolved in 4.5 ml water; (E) 10 mg glutamate (Glu) dissolved in 4.5 ml water; (F) 10 mg lysine dissolved in 4.5 ml water Acid (Lys); and (G) 10 mg of Proline (Pro) dissolved in 4.5 ml of water, each of which contained 2.5 ml of 20% human albumin solution (500 mg HSA) for infusion in each round bottom flask. (Note: All amino acids used in the Examples section (all examples) are L-amino acids). After placing the flasks in an ice bath, a mixed solvent (2.5 ml of tert-butanol and 0.5 ml of ethanol) in which docetaxel (5 mg) was dissolved was added dropwise to each of the 7 flasks under stirring, respectively. After the addition was complete, a clear solution was obtained. The...

Embodiment 2

[0248] Example 2: Compositions Comprising Docetaxel, Human Serum Albumin (HSA) and Amino Acids

[0249] To 7 different round bottom flasks were added (A) 4.5ml water; (B) 10mg alanine (Ala) dissolved in 4.5ml water; (C) 10mg asparagine (Asn) dissolved in 4.5ml water ), (D) 10mg cysteine ​​hydrochloride (Cys.HCl) dissolved in 4.5ml water; (E) 10mg glycine (Gly) dissolved in 4.5ml water; (F) 10mg dissolved in 4.5ml water Histidine (His) and (G) 10 mg serine (Ser) dissolved in 4.5 ml of water, each round bottom flask containing 2.5 ml of 20% human albumin solution (500 mg HSA) for infusion. After placing the flasks in an ice bath, a mixed solvent (2.5 ml of tert-butanol and 0.5 ml of ethanol) in which docetaxel (5 mg) was dissolved was added dropwise to each of the 7 flasks under stirring, respectively. After the addition was complete, a clear solution was obtained. The resulting clear aqueous solution was lyophilized overnight to yield a white solid.

[0250] Take 35 mg of ly...

Embodiment 3

[0255] Example 3: Compositions comprising docetaxel, human serum albumin (HSA), amino acids and sugar alcohols

[0256]To 4 different round bottom flasks were added (A) 10 mg aspartic acid (Asp) and 1 mg cysteine ​​hydrochloride (Cys.HCl) dissolved in 4.5 ml water; (B) dissolved in 4.5 ml 10mg aspartic acid (Asp), 1mg cysteine ​​hydrochloride (Cys.HCl) and 25mg mannitol in water; (C) 10mg aspartic acid (Asp), 1mg Cys Cystine hydrochloride (Cys.HCl) and 50 mg mannitol; and (D) 10 mg aspartic acid (Asp), 1 mg cysteine ​​hydrochloride (Cys.HCl) and 100 mg of mannitol, each of which contained 2.5 ml of 20% human albumin solution for infusion (500 mg HSA) in each round bottom flask. After the flask was placed in an ice-water bath at about 10°C, under stirring, a mixed solvent (2.5 ml of tert-butanol and 0.5 ml of ethanol) in which docetaxel (5 mg) was dissolved was added dropwise to each of the four flasks. ). After the addition was complete, a clear solution was obtained. The ...

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Abstract

The document relates to a composition comprising Docetaxel, human serum albumin, and one or more amino acids selected from aspartic acid, glutamic acid, and cysteine, wherein the human serum albumin and the Docetaxel in the composition have a ratio by weight of no less than 60:1. The document also relates to a composition comprising Docetaxel, human serum albumin, one or more amino acids selectedfrom aspartic acid, glutamic acid, and cysteine, and a sugar alcohol or a sugar, wherein the human serum albumin and the Docetaxel in the composition have a ratio by weight of no less than 60:1.

Description

technical field [0001] The present invention relates to preparations and compositions for the treatment of proliferative diseases, in particular to preparations and compositions comprising docetaxel and human serum albumin, more specifically to formulations and compositions comprising docetaxel and human serum albumin with improved stability formulations and compositions. Background technique [0002] Many drugs used parenterally are insoluble in water and therefore need to be formulated with irritating, allergic or toxic solubilizers, surfactants, solvents and / or emulsifiers when administered to a patient. See eg Briggs et al., Anesthesis 37, 1099 (1982) and Waugh et al., Am. J. Hosp. Pharmacists, 48, 1520 (1991). Furthermore, many of these drugs, especially those administered intravenously, can cause adverse side effects such as vein irritation, phlebitis, burning and pain upon injection, venous thrombosis, extravasation, and other administration-related side effects. Ad...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K38/17A61K38/38
CPCA61K31/337A61K47/183A61K47/26A61K47/42A61K9/08A61P35/00A61K38/385A61K31/198A61K9/0019A61K9/19A61K47/10A61K2300/00
Inventor 群·孙
Owner ZHUHAI BEIHAI BIOTECH CO LTD
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