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Pharmaceutical composition comprising solvent mixture and a vitamin D derivative or analogue

A composition and analog technology, which is applied in the direction of drug combination, drug delivery, medical preparations containing active ingredients, etc., can solve the problem of low ability to dissolve vitamin D analogs

Inactive Publication Date: 2012-11-07
LEO PHARMA AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] While vegetable oils and their derivatives (e.g. medium chain triglycerides based on coconut oil fractions) have previously been used as alternatives to alcoholic solvents to formulate vitamin D derivatives in topical compositions (see US 2008 / 0239681), Its ability to dissolve vitamin D analogs such as calcipotriol is rather low

Method used

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  • Pharmaceutical composition comprising solvent mixture and a vitamin D derivative or analogue
  • Pharmaceutical composition comprising solvent mixture and a vitamin D derivative or analogue
  • Pharmaceutical composition comprising solvent mixture and a vitamin D derivative or analogue

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Experimental program
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Embodiment approach

[0031] The vitamin D derivative or analog contained in the composition of the present invention may be selected from calcipotriol, calcitriol, tacalcitol, maxacalcitol, paricalcitol and alpha-calcitol . A preferred vitamin D analog that has proven effective in the treatment of psoriasis is calcipotriol. Calcipotriol may be in anhydrous or monohydrate form, preferably monohydrate, prior to dissolution in the solvent mixture.

[0032] In solvent mixtures used in the compositions of the present invention, the fatty acid ester solvent component is preferably selected from glycerides, such as fatty acids (e.g. C 6-24 triglycerides of fatty acids), and C 10-18Isopropyl esters of alkanoic or alkenoic acids such as isopropyl myristate, isopropyl palmitate, isopropyl isostearate, isopropyl linoleate, isopropyl monooleate, and octyl Lauryl alcohol or propylene glycol esters, such as propylene glycol dipelargonate. While medium chain triglycerides (as defined herein) are generally pr...

Embodiment 1

[0057] Test different solvent mixtures

[0058] Calcipotriol monohydrate was tested for solubility in compositions as shown in Table 1 below.

[0059] Table 1

[0060] Ingredient mg / g

[0061]Solubility was determined by shaking 3 ml of vehicle and excess calcipotriol monohydrate in a controlled room at 25±2°C for 24 hours. Experiments were performed as double assays. After 24 hours, the suspension was treated with -LCR filter for filtration, transfer the filtrate to a clean reaction tube and dilute with isopropanol. Concentrations were determined by reverse phase HPLC with UV detection (264 nm) compared to a standard curve.

[0062] The solubility of calcipotriol monohydrate in each solution is shown in Table 2 below.

[0063] Table 2

[0064] Solution 1

[0065] The results of this experiment indicated that the solubilization capacity of solution 6 containing medium chain triglycerides, N-methylpyrrolidone and polyoxypropylene-15-stearyl ether was ...

Embodiment 3

[0067] Stability of Calcipotriol in Different Solvent Mixtures

[0068] The compositions of the three solvent mixtures containing 25% NMP and 0% or 15% polyoxypropylene-15-stearyl ether are shown in Table 3 below.

[0069] table 3

[0070]

[0071] The solvent mixture was stored at 40°C for 1 month and at 25°C and 40°C for 3 months, after which the calcipotriol content was determined by HPLC. The results are presented in Table 4 below as a percentage of the initial assay.

[0072] Table 4

[0073] storage

[0074] The results showed that the only solvent mixture that showed satisfactory stability was the one containing 15% Solvent mixture 3 of E (polyoxypropylene-15-stearyl ether).

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Abstract

A substantially anhydrous, topical pharmaceutical composition comprising a non not alcoholic three-component solvent mixture and a biologically active vitamin D derivative or analogue dissolved therein as well as a pharmaceutically acceptable carrier may be used in the treatment of dermal conditions.

Description

technical field [0001] The present invention relates to topical pharmaceutical compositions comprising biologically active vitamin D derivatives or analogs dissolved in a triple solvent mixture, and their use in the treatment of skin diseases or conditions. Background technique [0002] Psoriasis is a chronic inflammatory skin disease characterized by erythematous, dry, scaly patches resulting from hyperkeratosis. Spots are most commonly seen on the elbows, knees, and scalp, although more extensive lesions may appear on other parts of the body, particularly the lumbosacral region. The most common treatment of mild to moderate psoriasis involves topical application of a composition containing a corticosteroid as the active ingredient. While effective, corticosteroids have the disadvantage of a number of adverse effects such as skin atrophy, striae, acneiform drug eruptions, perioral dermatitis, dermatophytic and bacterial overgrowth, hypopigmentation of pigmented skin, and r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/593A61K47/10A61K47/14A61K47/22
CPCA61K47/14A61K47/10A61K9/0014A61K9/06A61K47/22A61K31/593A61P17/00A61P17/02A61P17/06A61P17/10
Inventor K·彼得松
Owner LEO PHARMA AS
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