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Medicine lipid composition

A composition and substance technology, applied in the field of active agent delivery system, amphiphilic composition and preparation, can solve the problems such as difficult to provide dispersion

Active Publication Date: 2008-02-13
CAMURUS AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is found in the literature that it is difficult to provide stable specific dispersions, and only lamellar dispersions are stable enough to be stored for more than a few days (Kamo et al. Langmuir 19, 9191-9195 (2003))

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0135] Example 1 - Non-Layered Inverse Phase Nanoparticles

[0136] 1.1 - Preparation of non-lamellar dispersions

[0137] Non-lamellar (>80 wt% amphiphile) and lamellar (amphiphile <20wt%) particle dispersion. The components were mixed at the molecular level by heating at 70°C for 5 minutes and vortexing. The molten homogeneous lipid (2.012 g) was added dropwise to 38.01 g deionized water. The resulting crude dispersion was placed on a shaking table (350 rpm) and shaken for 24 hours to obtain a cloudy homogeneous dispersion.

[0138] Particle size was measured using laser diffraction (Coulter LS230). The size distribution was found to be narrow and unimodal with an average particle size of 95 nm.

[0139] 1.2-Heat treatment

[0140] An optional heat treatment cycle was carried out on the dispersion prepared in Example 1.1.

[0141] A sample (25 mL) of the dispersion produced in Example 1.1 was autoclaved (125°C, 20 minutes) and cooled to room temperature. The particle...

Embodiment 2

[0147] Example 2 - Other Compositions

[0148] A second composition was prepared by the method of Examples 1.1 and 1.2 to evaluate the effect of adding a higher concentration of stabilizer. Solutions of SPC and GDO (40 / 60 wt / wt) (2.017 g) and P80 (0.514 g) were molecularly mixed by heating at 70°C for 5 minutes and vortexing. The molten homogeneous lipid (2.006 g) was added dropwise to 38.00 g deionized water. The resulting crude dispersion was placed on a shaking table and shaken for 24 hours to obtain a cloudy homogeneous dispersion. Thereafter the dispersion was heat treated according to Example 1.2.

[0149] The size distributions before and after heat treatment were found to be narrow and unimodal with mean particle sizes of 88 and 129 nm, respectively. As shown in Figure 2, heat treatment also narrowed the particle size distribution. Figure 3 shows cryo-TEM pictures taken from samples before and after heat treatment. The cryo-TEM results clearly demonstrate the form...

Embodiment 3

[0156] Example 3 - Other Compositions

[0157] Another composition was prepared by the method of Examples 1.1 and 1.2 to evaluate the effect of adding another type of stabilizer. SPC and GDO (40 / 60wt / wt) (2.004g) and Solutol were mixed at the molecular level by heating at 70°C for 5 minutes and vortexing  Solution of HS 15 (0.516 g). The molten homogeneous lipid (2.042 g) was added dropwise to 38.00 g deionized water. The resulting coarse dispersion was placed on a shaking table and shaken for 24 hours to obtain a cloudy dispersion containing some weakly dispersed macroscopic particles. In order to obtain a uniform dispersion, the samples were homogenized using a Microfluidizer at 5000 PSI and room temperature. The sample was passed through the homogenizer 5 times to obtain a milky homogeneous dispersion. Thereafter the dispersion was heat treated according to Example 1.2.

[0158] Figure 4 shows the size distribution obtained before and after heat treatment, showing tha...

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Abstract

The present invention relates to a particulate composition containing; a) 5 to 90% of at least one phosphatidyl choline component b) 5 to 90% of at least one diacyl glycerol component, at least one tocopherol, or mixtures thereof, and c) 1 to 40% of at least one non-ionic stabilising amphiphile, where all parts are by weight relative to the sum of the weights of a+b+c and where the composition contains particles of at least one non-lamellar phase structure or forms particles of at least one non-lamellar phase structure when contacted with an aqueous fluid. The invention additionally relates to pharmaceutical formulations containing such compositions, methods for their formation and methods of treatment comprising their administration.

Description

technical field [0001] The present invention relates to the protection, solubilization, stabilization and delivery of active agents in pharmaceutical and neutraceutical compositions. In particular, the invention relates to amphiphilic compositions and formulations, and active agent delivery systems based on these. Background technique [0002] Formulations based on amphiphilic substances show considerable potential in the delivery of many substances, especially in vivo delivery to the human or animal body. Since amphiphiles have polar and nonpolar groups that aggregate to form polar and nonpolar regions, they can effectively dissolve polar and nonpolar compounds. Furthermore, many structures formed by amphiphilic substances / structuring agents in polar and / or nonpolar solvents have considerable polar / nonpolar boundary regions where The boundary region can absorb and stabilize other amphiphiles. [0003] The formation of non-lamellar regions is a well known phenomenon in am...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
Inventor 马库斯·约翰松弗雷德里克·蒂贝里
Owner CAMURUS AB
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