Drug formulations having long and medium chain triglycerides

A technology of long-chain triglycerides and medium-chain triglycerides, which is applied in the field of emulsified preparations of ansamycin, and can solve the problem of no combination of medium-chain triglycerides and ansamycin

Inactive Publication Date: 2010-06-30
CONFORMAL THERAPEUTICS CORP (US)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, to the applicant's knowledge so far, they have not been used in combination with medium chain triglycerides and ansamycins

Method used

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  • Drug formulations having long and medium chain triglycerides
  • Drug formulations having long and medium chain triglycerides
  • Drug formulations having long and medium chain triglycerides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1: Preparation of 17-AAG; Alternative 1

[0084] To 45.0 g (80.4 mmol) of geldanamycin dissolved in 1.45 L of dry THF in a 2 L dry flask was added dropwise 36.0 mL (470 mmol) of allylamine dissolved in 50 mL of dry THF over 30 minutes . The reaction mixture was stirred at room temperature under nitrogen for 4 hours until TLC analysis indicated that the reaction was complete [GDM: bright yellow: Rf = 0.40; (5% MeOH-95% CHCl 3 ); 17-AAG: purple: Rf = 0.42 (5% MeOH-95% CHCl 3 )]. The solvent was removed by rotary evaporation, and the crude product was heated at 25 °C in 420 mL H 2 A slurry was formed in O:EtOH (90:10), then filtered, and dried at 45 °C for 8 hours to give 40.9 g (66.4 mmol) of 17-AAG as purple crystals (82.6% yield, purity monitored by HPLC at 254 nm >98%). The melting point measured by differential scanning colorimetry (DSC) is 206-212°C. 1 The results obtained by H NMR and HPLC were consistent with the desired product.

Embodiment 2

[0085] Embodiment 2: Preparation of low melting point type 17-AAG

[0086] An alternative method of purification is to dissolve the crude 17-AAG from Example 1 in 800 mL of 2-propanol (isopropanol) at 80 °C and then cool to room temperature. Filtration followed by drying at 45° C. for 8 hours afforded 44.6 g (72.36 mmol) of 17-AAG as purple crystals (90% yield, >99% purity by HPLC at 254 nm). The melting point measured by differential scanning colorimetry (DSC) is 147-175°C. 1 The results obtained by H NMR and HPLC were consistent with the desired product.

Embodiment 3

[0087] Example 3: Preparation of low melting point type 17-AAG, alternative 1

[0088] An alternative purification method is to dissolve the product 17-AAG of Example 2 in 400 mL of H 2O:EtOH (90:10) was slurried at 25°C, filtered, and dried at 45°C for 8 hours to afford 42.4 g (68.6 mmol) of purple crystals of 17-AAG (95% yield by HPLC at 254 nm Monitored for purity >99%). The melting point is 147-175°C. 1 The results obtained by H NMR and HPLC were consistent with the desired product.

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Abstract

Drug formulations having emulsifying agents and both medium and long chain triglycerides are described. In preferred embodiments, the long chain triglycerides negate or lessen deleterious central nervous system effects that are caused by medium chain triglycerides.

Description

[0001] This application is a divisional application of an invention patent application with an application date of October 4, 2003 and an invention title of "pharmaceutical preparation containing long-chain and medium-chain triglycerides". [0002] related application [0003] This application claims priority to the following and is hereby incorporated by reference in its entirety: U.S. Provisional Patent Application 60 / 2003, filed July 29, 2003, entitled "Ansamycin Formulations and Methods of Making and Using the Same" 491,050; U.S. Provisional Patent Application No. 60 / 478,430, filed June 12, 2003, entitled "Phospholipid-Based Formulations and Methods of Making and Using the Same," Ulm et al., filed March 13, 2003, and entitled " HSP90 Inhibitor Formulations and Data," U.S. Provisional Patent Application No. 60 / 454,812; and PCT Application PCT / US03 / , filed April 4, 2003 by Ulm et al., entitled "Novel Ansamycin Formulations and Methods of Making and Using the Same" 10533, whi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/395A61K47/14A61K31/23A61P31/00A61P25/20A61K9/00A61K9/107A61K9/19A61K31/00A61K31/33
CPCA61K9/0019A61K47/14A61K31/00A61K31/395A61K9/19A61K9/1075A61K9/107A61K31/33A61P25/20A61P29/00A61P31/00A61P31/10A61P31/12A61P35/00A61P35/02A61P43/00
Inventor 埃德加·H·厄尔马罗伯特·曼斯菲尔德马库斯·贝姆
Owner CONFORMAL THERAPEUTICS CORP (US)
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