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Stable and ready-to-use oil-in-water propofol microemulsion

A technology of microemulsion and propofol, which is applied in the direction of emulsion delivery, medical preparations of non-active ingredients, liquid delivery, etc., can solve the problems of side effects, the importance of not clearly increasing the concentration of propofol, etc., and achieve effective hypnosis and Lower risk of anesthesia, side effects and potential adverse effects, safer and more reliable short-term or long-term effects

Inactive Publication Date: 2009-10-07
CRISTALIA PROD QUI FARM LTDA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the authors did not clarify the importance of increasing propofol concentrations
In contrast, it is well known that high concentrations of propofol may cause side effects, notably, for example, heart failure, metabolic acidosis, and rhabdomyolysis [De Cosmo, G et al. "Sedationin PACU: The Role of Propofol" Current Drug Targets. 2005.6(7): 741]

Method used

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  • Stable and ready-to-use oil-in-water propofol microemulsion
  • Stable and ready-to-use oil-in-water propofol microemulsion
  • Stable and ready-to-use oil-in-water propofol microemulsion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of embodiment 1.1% and 0.5% propofol-containing microemulsions.

[0051] A complete formulation of the present invention can be described as Microemulsion 1 and Microemulsion 2 formulations, the ratios of which are preferred propofol and excipients are described in Table 1 as follows:

[0052] Table 1: Propofol microemulsions.

[0053]

[0054] According to the present invention, microemulsion 1 and microemulsion 2 are prepared as follows:

[0055] 70% of the total water for injection was added to a stainless steel reactor with a stirring system. In addition, macrogol 15 hydroxystearate (SOLUTOL HS 15) was added into a stainless steel container, and heated to 50°C with constant stirring to obtain a completely melted product. Next, 6% of the total water for injection and propofol were added to the melted surfactant with constant stirring.

[0056] The contents of the stainless steel vessel were added to a reactor filled with 70% total water for injectio...

Embodiment 2

[0060] Example 2. The stability of propofol microemulsion of the present invention.

[0061] Freshly prepared microemulsions 1 and 2 according to Example 1 were tested to evaluate their properties. Evaluation of the particle size is the most important issue of the present invention, since the stability of this parameter is a drawback of the propofol microemulsions described in the prior art.

[0062] Particle size was monitored during a 12 month stability test (see Table 2) under normal temperature conditions and a 180 day accelerated stability test at 40°C (Table 3).

[0063] The results shown in Tables 2 and 3 show that there was not any significant change in particle size during the monitoring time. Even earlier samples exhibit particle sizes significantly smaller than the maximum 50nm maximum established by the present invention as the preferred limit.

[0064] Table 2. Effect of storage time on the particle size of propofol microemulsions according to the usual conditio...

Embodiment 3

[0068] Example 3. Comparative analysis of the stability of the propofol microemulsion of the prior art and the microemulsion of the present invention.

[0069] The formulations are described in the referenced patent US 6,743,436 (Examples 1, 5 and 6), which were chosen for comparison to illustrate the improvement of physicochemical properties achieved by the pharmaceutical composition of the present invention, as the closest existing comparison to this new composition. have technology.

[0070] When the composition was again prepared as taught by the referenced patent, it was observed that the general turbidity of the composition did not comply with the parameters of a microemulsion, and the analysis showed a particle size well above the limit of 100 nm (see Table 4).

[0071] Table 4. Determination of particle size in accelerated stability test (40°C ± 2°C).

[0072]

[0073] * Poloxamer is a surfactant, combined with Solutol HS15 as a co-surfactant;

[0074] ** Poloxame...

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Abstract

The present invention describes a new propofol-containing anesthetic pharmaceutical composition for parenteral administration, in the form of an oil-in-water microemulsion in which the oily phase is constituted by propofol in the form of particles with size comprised between 1 and 100 nm using a single surfactant selected from the group consisting of polyethylene glycol stearates with general formula C17H35COO.(OCH2CH2)nH or C17H35COO.(OCH2CH2)n.COOC17H35. The anesthetic pharmaceutical composition of the present invention is more potent for induction of hypnosis and anesthesia, has a ready-to-use presentation and highly stable particle size, presenting improved physicochemical properties, and preventing the potential risks of undesirable effects encountered in the state-of-the-art propofol formulations.

Description

field of invention [0001] The present invention describes an injectable ready-to-use anesthetic composition for parenteral administration, which is an oil-in-water microemulsion containing propofol as the active drug, and its dispersed hydrophobic particles are smaller in size and more Stabilized so that it is a microemulsion with a transparent appearance. Background technique [0002] Active Drug Propofol, the active drug of the present invention, has the assigned chemical name of 2,6-bis-(1-methylethyl)-phenol. Its preparation has been described, for example, in patents US 2,831,898 and US 4,447,657, and its anesthetic and sedative / hypnotic activity in mammals was first described in patent US 4,056,635. [0003] An injectable anesthetic fat emulsion containing propofol at a concentration of 1% to 2% (w / v) is currently marketed under the brand name In Brazil, there is also the brand name of of this medicine. [0004] Propofol has short-term effects sufficient to induc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/03A61K31/05A61K9/10A61K9/107A61K47/14A61P23/00
CPCA61K31/05A61K9/1075A61K31/03A61P23/00A61P23/02A61P25/20
Inventor O·帕切科R·莫雷拉M·里西
Owner CRISTALIA PROD QUI FARM LTDA
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