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A topical nanoparticulate spironolactone formulation

A technology of nano-particles and spironolactone, which is applied in the direction of aerosol delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the adverse effects of product stability, tiny particles and nanoparticles Aggregation and flocculation, narrow particle size range, etc.

Inactive Publication Date: 2007-04-18
JAGOTEC AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is not a simple matter to prepare such small particles, and further difficulties have arisen in both aspects of related preparation techniques and how to obtain qualified products
For example, there are difficulties in obtaining a continuous, narrow particle size range, especially in batch production
Moreover, it is necessary to obtain stable products such as nano-suspensions, but microparticles and nanoparticles have a tendency to aggregate and flocculate, which is counterproductive to product stability

Method used

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  • A topical nanoparticulate spironolactone formulation
  • A topical nanoparticulate spironolactone formulation
  • A topical nanoparticulate spironolactone formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1: Preparation of Nanoparticulate Spironolactone as Topical Formulation

[0061] Preparation of Nanoparticle Spironolactone

[0062] Table 1 shows a typical preparation method of nanoparticulate spironolactone incorporated into the crystal structure according to the present invention. Nanoparticle spironolactone can be prepared as follows:

[0063] Combine the aqueous formulation of the stabilizer with water or injection buffer under magnetic stirring until a clear solution is obtained; wet the spironolactone with the appropriate amount of aqueous surfactant to form a slurry; disperse the resulting suspension with high shear Disperse the suspension with magnetic force to eliminate foam; the obtained suspension passes through a high-pressure piston gap homogenizer to obtain a nano-suspension. Use Avestin C5 TM Formulations 1-7 were prepared using Avestin C50 TM Formulations 8-9 were prepared. During homogenization, drug particles are broken up by cavitation ...

Embodiment 2

[0122] Example 2: Size of spironolactone particles before and after storage

[0123] Figures 1, 2 and 3 are micrographs of spironolactone of the present invention when it is just prepared, after being stored for 7 months, and compared with commercially available spironolactone. The distance between each vertical grid in the figure is 0.01 mm or 10 microns.

[0124] The particles shown in Figures 1 and 2 are so small that they are barely visible under an optical microscope. The particles did not grow any longer after storage for 7 months. In contrast, the commercially available spirosterolactone "Spiroderm" (Figure 3) presents spironolactone crystals as large as 20 microns.

Embodiment 3

[0125] Example 3: Flux Study

[0126] raw material

provider

Crystalip TM Spironolactone nanosuspension 2% by weight

Lot number is 4014-000 / 06atc

Spironolactone

The batch number is 510 / 0

Skye Pharma, Switzerland

Aqueous Cream B.P.

The batch number is 28076

Hillcross, UK

ethanol

R grade analytically pure

VWR International Ltd., UK

Sodium dihydrogen phosphate dihydrate

The batch number is L298

Merckeurolab

Deionized water

Elga Ltd., UK

Acetonitrile HPLC grade

Rathburns Chemicals Ltd., UK

regenerated cellulose film

NBS-Biological, UK

[0127] Methods of Flow Research

[0128] Crystalip TMThe formulation was provided by SkyePharma AG, and the commercially available spironolactone control was no longer used in the experiment, so a standard cream base control was prepared as follows. Briefly, 100 mg of spironolactone powder was accurately weighed an...

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Abstract

The invention relates to a topical nanoparticulate spironolactone formulation comprising nanoparticles having a mean diameter, measured by photon correlation spectroscopy, in the range of from about 300nm to about 900nm. The nanoparticles are incorporated into a crystalline network system comprising a dispersion of solid crystals of polar lipids, said lipids exposing their hydrophilic side outwards and their hydrophobic side inwards towards the spironolactone nanoparticles.

Description

technical field [0001] The present invention relates to the use of nanoparticle spironolactone (spironolactone) in local treatment of diseases related to antiandrogen substances. Such conditions include: acne, hirsutism, androgenetic alopecia, or rosacea. Background technique [0002] Spironolactone is known to be an aldosterone inhibitor and is often used as a potassium-sparing diuretic. Commercially available spironolactones such as spironolactone (aldactone) are useful in treatments such as congestive heart failure. The solubility of spironolactone in water is extremely low, 2.8mg / 100ml. This low solubility negatively affects drug absorption in the body, resulting in poor bioavailability, necessitating higher doses of the drug to achieve the desired blood concentration levels. The low solubility of spironolactone also limits its availability in drug formulation. [0003] Other pharmaceutical applications exploit the antiandrogenic properties of spironolactone to treat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/585A61K9/51A61K9/06A61K47/14A61K9/00A61K9/14
CPCA61K9/145A61K47/14A61K9/146A61K9/06A61K9/0014A61K31/585A61P17/10A61P17/14
Inventor G·维格诺尔特P·格勒尼耶A·尼亚米尔斯D·谢勒P·贝克P·康卡德
Owner JAGOTEC AG
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