Emulsion comprising an nk-1 receptor antagonist

A receptor antagonist, NK-1 technology, applied in the field of preparing stable NK-1 receptor antagonist emulsion and pharmaceutical preparations

Inactive Publication Date: 2018-11-23
HERON THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drugs may degrade; for example, lipophilic drugs will partition into the oil phase, which will confer some degree of protection, but hydrolytic degradation may still occur at the oil-water interface

Method used

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  • Emulsion comprising an nk-1 receptor antagonist
  • Emulsion comprising an nk-1 receptor antagonist
  • Emulsion comprising an nk-1 receptor antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] Example 1: Preparation of Aprepitant Emulsion for Intravenous Injection

[0141] To prepare the aprepitant emulsion, the oil phase was first prepared by mixing 750 mg of aprepitant and 15.0 g of lecithin (LIPOID E80) with 12.0 ml of ethanol. The mixture was dissolved by heating and stirring at 60° C. and 200 rpm for 15 minutes. To the resulting solution was added 10.0 g of soybean oil. Heat at 60°C and stir at 200 rpm for a further 15 minutes. The aqueous phase was prepared by dissolving 5.60 g of sucrose and 0.500 g of sodium oleate in 70.0 ml of water for injection. The mixture was stirred at 300 rpm for 30 minutes at room temperature. The water phase was then added to the oil phase, followed by high-speed homogenization at 20,000 rpm (Ultra- IKA T25) for 1 minute to produce a coarse emulsion. The coarse emulsion was then passed through an ice-cooled high-pressure microfluidizer at a pressure of 18,000 psi ( M-1 10L, F12Y interaction chamber) 8 times. The re...

Embodiment 2

[0145] Example 2: Preparation of Aprepitant Emulsion for Intravenous Injection

[0146] To prepare the aprepitant emulsion, the oil phase was first prepared by mixing 450 mg of aprepitant and 9.00 g of lecithin (LIPOID E80) with 4.0 ml of ethanol. The mixture was dissolved by heating and stirring at 60° C. and 200 rpm for 15 minutes. To the resulting solution was added 6.00 g of soybean oil. Heat at 60°C and stir at 200 rpm for a further 15 minutes. The aqueous phase was prepared by dissolving 3.36 g of sucrose and 0.300 g of sodium oleate in 42.0 ml of water for injection. The mixture was stirred at 300 rpm for 30 minutes at room temperature. The water phase was then added to the oil phase, followed by high-speed homogenization at 20,000 rpm (Ultra- IKA T25) for 1 minute to produce a coarse emulsion. The coarse emulsion was then passed through an ice-cooled high-pressure microfluidizer at a pressure of 18,000 psi ( M-110L, F12Y interaction chamber) 8 times. The resu...

Embodiment 3

[0149] Example 3: Preparation of Aprepitant Emulsion for Intravenous Injection

[0150] To prepare the aprepitant emulsion, the oil phase was first prepared by mixing 450 mg of aprepitant and 9.00 g of lecithin (LIPOID E80) with 6.0 ml of ethanol. The mixture was dissolved by heating and stirring at 60° C. and 200 rpm for 15 minutes. To the resulting solution was added 6.00 g of soybean oil. Heat at 60°C and stir at 200 rpm for a further 15 minutes. The aqueous phase was prepared by dissolving 15.62 g of sucrose and 0.300 g of sodium oleate in 42.0 ml of water for injection. The mixture was stirred at 300 rpm for 30 minutes at room temperature. The water phase was then added to the oil phase, followed by high-speed homogenization at 20,000 rpm (Ultra- IKA T25) for 1 minute to produce a coarse emulsion. The coarse emulsion was then passed through an ice-cooled high-pressure microfluidizer at a pressure of 18,000 psi ( M-110L, F12Y interaction chamber) 8 times. The resu...

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Abstract

Disclosed herein are novel pharmaceutical formulations of a neurokinin-1 (NK-1) receptor antagonist suitable for parenteral administration including intravenous administration. Also included are formulations including both the NK-1 receptor antagonist and dexamethasone sodium phosphate. The pharmaceutical formulations are stable oil-in-water emulsions for non-oral treatment of emesis and are particularly useful for treatment of subjects undergoing highly emetogenic cancer chemotherapy.

Description

technical field [0001] The present invention relates to emulsion formulations and systems for intravenous or parenteral administration of NK-1 receptor antagonists for the treatment of emesis. The emulsion formulations are stable for long periods of time. The present invention also describes methods for preparing stable NK-1 receptor antagonist emulsions and pharmaceutical formulations. Background technique [0002] Vomiting is a key problem experienced during anticancer cytotoxic therapy. Up to 80% of patients will experience chemotherapy-induced nausea and vomiting (CINV) without preventive treatment (Vieira dos Santos et al., 2012, J Natl Cancer Inst, 104: 1280-1292). Navari et al. (1999, N Engl J Med, 340: 190-195) showed that neurokinin-1 (NK-1 ) receptor antagonists ameliorated CINV when used in combination with cisplatin-based chemotherapy. NK-1 receptor antagonists block the binding of substance P to the receptor, thereby preventing or limiting the induction of th...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/24A61K9/107A61K31/454A61K31/496A61K31/5377
CPCA61K9/0019A61K9/1075A61K31/4035A61K31/439A61K31/454A61K31/496A61K31/5377A61K47/24A61P1/08A61P43/00A61K31/438
Inventor T·B·奥托博尼H·韩
Owner HERON THERAPEUTICS
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