Anaesthetic formulation

A technology of anesthetics and anesthetics, applied in anesthetics, drug combinations, pharmaceutical formulations, etc., can solve problems such as increased injection pain, inhibition, and complexity of syringe delivery equipment

Active Publication Date: 2012-11-28
DRAWBRIDGE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Attempts to reformulate into a water-based formulation have resulted in increased injection pain
Propofol can also cause cardiovascular and respiratory depression and has a low therapeutic index5, ie, only 5 times the normal anesthetic dose may cause death
Also, this anesthetic is incompatible with plastic storage containers and plastic syringes, complicating syringe delivery devices that are frequently used in standard use for intravenous anesthesia and sedation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0108] Anesthesia of alfaxalone in 30% w / v (7) sulfobutyl ether β-cyclodextrin

[0109] Alfa Salon is formulated as 6ml of clear colorless liquid which contains:

[0110] Alfa Salon 60mg (10mg / ml);

[0111] (7) 1800 mg of sulfobutyl ether β-cyclodextrin;

[0112] Saline (0.9% w / v) 6ml.

[0113] This is the molar compounding ratio of alfasalone and (7) sulfobutyl ether β-cyclodextrin 1:4.6. Male Wistar rats (weight [wt] 270-315 g) with an indwelling catheter in the jugular vein were placed in a Perspex holder and given injections, the accompanying observations are shown in Table 1 upon release from the holder.

[0114] Table 1

[0115] Effects of Alfaxalon Preparation on Wistar Rats

[0116]

[0117] KEY

[0118]

[0119] Rats given 25 and 100 mg / kg body weight recovered over 60 minutes; they did not die or suffer any adverse effects at these doses. In these experiments it was seen that intravenous administration of alfaxalone at 10 mg / ml dissolved in (7) sulfobuty...

example 2

[0121] Pharmacokinetics in Rats

[0122] Two groups of 10 rats implanted with internal jugular vein intravenous catheter and carotid arterial catheter received intravenous injection of 10 mg / kg body weight of Alfasalone (7) sulfobutyl ether β-cyclodextrin preparation via jugular vein (n=10 rats) or a mixture of alfaxalone and alfadolone in Cremophor EL (polyoxyethylene castor oil) at 1.1 ml / kg (n=10 rats). Blood drawn from the carotid artery or tail at various time intervals after this injection was analyzed for alfaxalon blood levels. These blood levels were fitted to a three-compartment pharmacokinetic model and means±sem of key parameters were calculated for both steroidal anesthetic formulations.

[0123] It is expected that there will be no significant differences between the calculated PK parameters for (7) sulfobutyl ether β-cyclodextrin formulation and Althesin (registered trademark) formulation. This would suggest that the new formulation is expected to work in a si...

example 3

[0128] Anesthetic effect of alfaxalone in (7) sulfobutyl ether β-cyclodextrin compared with alfaxalone and propofol as Althesin (registered trademark)

[0129] Male Wistar rats (wt 150-220 g) were implanted with an indwelling intravenous catheter in the internal jugular vein under halothane anesthesia. After 24 hours, each rat received intravenous injections in the following dose ranges: Propofol (10 mg / ml in 10% w / v Intralipid emulsion; Diprivan [registered trademark]); Althesin [registered trademark] ( Alfaxalone in 20% w / v CremophorEL 9 mg / ml plus alfadrolone acetate 3 mg / ml); or Phaxan CD (Alfaxalone 10 mg / ml in a 1:2 molar complex with Captisol (registered trademark)-(7)sulfobutyl ether β-cyclodextrin). The following were assessed at regular intervals after the intravenous infusion:

[0130] 1. Righting Reflex: Score: 1 Normal; 2 Slow; 3 Some Attempt; 4 None - This is a measure of the onset and duration of loss of consciousness;

[0131] 2. Tail pinch reaction: scored ...

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Abstract

The present invention relates generally to the field of drug delivery systems for neuroactive steroid anaesthetic agents. More particularly, anaesthetic and sedative formulations are provided in the form of host / guest preparations comprising one or more neuroactive steroid anaesthetics and a cyclodextrin. Particular cyclodextrins contemplated include sulfoalkyl ether cyclodextrins and modified forms thereof.

Description

[0001] submit data [0002] This application is comparable to U.S. Provisional Patent Application No. 61 / 297,249, filed January 21, 2010, entitled "Anaesthetic Preparations" and U.S. Provisional Patent Application No. 61, filed September 22, 2010, entitled "Anaesthetic Preparations" / 385,318 are related and claim priority from them, the entire contents of which are hereby incorporated by reference. technical field [0003] The present invention relates generally to the field of drug delivery systems for neuroactive steroidal anesthetics. More specifically, anesthetic and sedative compositions are provided in the form of host / guest formulations comprising one or more neuroactive steroidal anesthetics and cyclodextrins or modified forms thereof. Background technique [0004] Bibliographic details of the references provided in this subject specification are listed at the end of this specification. [0005] Reference to any prior art is not, and should not be taken as, an ackn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K47/40A61K31/57A61P23/00
CPCA61K47/40B82Y5/00A61K31/57A61K47/48969A61K31/56A61K47/6951A61K31/573A61P23/00A61P25/20
Inventor 朱丽叶·玛格丽特·古德柴尔德科林·斯坦利·古德柴尔德本杰明·詹姆斯·博伊德
Owner DRAWBRIDGE PHARMA
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