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A topical nanoparticulate spironolactone formulation

A nanoparticle and spironolactone technology is applied in aerosol delivery, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. It can solve the problem of narrow particle size range, difficult preparation technology, and product stability. counterproductive issues

Inactive Publication Date: 2006-03-01
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 a topical formulation

[0061] Preparation of nano-particle spironolactone

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

[0063] Under magnetic stirring, combine the aqueous formulation of the stabilizer with water or injection buffer until a clear solution is obtained; wet the spironolactone with an aqueous solution of a suitable amount of surfactant to form a slurry; the resulting suspension is dispersed by high shear The instrument is used for dispersion; the suspension is magnetically stirred to eliminate bubbles; the obtained suspension is passed through a high-pressure piston gap homogenizer to obtain nano suspensions. Use Avestin C5 TM Prepare preparations 1-7, using Avestin C50 TM Preparation 8-9 was prepared. In the homogenization proces...

Embodiment 2

[0123] Example 2: The size of spironolactone particles before and after storage

[0124] figure 1 , 2 And 3 are the microscope images of the spironolactone of the present invention just after preparation, after 7 months of storage, and compared with commercially available spironolactone. The distance between each vertical grid in the figure is 0.01 mm or 10 microns.

[0125] figure 1 with 2 The particles shown in are too small to be barely visible under an optical microscope. The pellets no longer grow up after 7 months of storage. In contrast, the commercially available spironolactone "Spiroderm" ( image 3 ) There are 20 micron spironolactone crystals.

Embodiment 3

[0126] Example 3: Liquidity research

[0127] In the Franz diffusion cell, the measurement results from the "Crystalip TM The flux of the spironolactone (2%) formulation of the matrix-bound nanosuspension formulation through the artificial membrane was compared with the 2% by weight spironolactone in the aqueous cream BP (Aqueouscream BP) as a control .

[0128] Raw materials

Provider

Crystalip TM Spironolactone nano-suspensions 2% by weight

The batch number is 4014-000 / 06atc

Spironolactone

Lot number is 510 / 0

SkyePharma, Switzerland

Aqueous cream B.P.

Lot number is 28076

Hillcross, UK

Ethanol

R grade analytical pure

VWR International Ltd., UK

Sodium Dihydrogen Phosphate Dihydrate

Lot number is L298

Merckeurolab

Deionized water

Elga Ltd., UK

Acetonitrile HPLC grade

Rathburns Chemicals Ltd., UK

Regenerated cellulose membrane

NBS-Biological, UK

[0129] Metho...

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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 application of nanoparticulate spironolactone (spironolactone) in local treatment of diseases related to antiandrogens. Such conditions include: acne, hirsutism, androgenetic alopecia or rosacea. Background technique [0002] It is known that spironolactone is an aldosterone inhibitor and is often used as a potassium-sparing diuretic. Commercially available spironolactone such as aldactone can be used for the treatment of, for example, congestive heart failure. The solubility of spironolactone in water is extremely low, 2.8 mg / 100 ml. This low solubility has a negative impact on the absorption of the drug in the body, resulting in poor bioavailability, requiring a higher dose of the drug to achieve the desired blood concentration level. The low solubility of spironolactone also limits its applicability in pharmaceutical formulation. [0003] Other drug applications use the anti-androgenic function of spironolactone to tr...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/06A61K47/14A61K31/585A61K9/00A61K9/14
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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