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High concentration formulation

a formulation and concentration technology, applied in the field of high concentration formulations, can solve the problems of greater and unwanted systemic exposure to actives and/or their metabolites

Inactive Publication Date: 2019-09-19
CASSIOPEA SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about a new pharmaceutical formulation that can be applied topically to treat alopecia. The formulation contains a therapeutic agent called cortexolone-17α-propionate, which is present in a concentration of greater than 2% by weight. This formulation is advantageous because it delivers the therapeutic agent directly to the skin and scalp, while minimizing systemic exposure to the drug. This results in optimal treatment for alopecia, with minimal side-effects. The formulation is stable and can be stored at room temperature for at least two years. Additionally, the patent describes a method of treating alopecia by applying the formulation twice a day for at least six months, which can lead to significant hair growth and a reduced risk of adverse side-effects.

Problems solved by technology

Although certain formulations of cortexolone-17α-propionate have been disclosed in the art, these formulations were limited to a concentration of less than 2% by weight due to inherent solubility limitations of the active and concerns that the administration of higher concentrations could lead to greater and unwanted systemic exposure to the active and / or its metabolites—particularly after repeated administration.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Evaluation of Cortexolone-17α-propionate Solubility

[0222]5 g of cortexolone-17α-propionate was added to 100 ml of each of the solvents or solvent mixtures shown in Table 1, below, in an effort to produce a 5% w / v solution of cortexolone-17α-propionate. In the examples in Table 1, ethanol refers to ethanol 96°.

TABLE 1Cortexolone-17α-propionate Solubility atSolvent (v:v)Room TemperatureWaterInsolubleEthanolHighly solubleTRANSCUTOL ®Very solublePropylene glycolSparingly solubleIsopropyl myristateInsolubleIsopropyl palmitate,InsolubleCaprylocaproyl polyoxy1-8 glyceridesSparingly solubleNF (LABRASOL ®)TRANSCUTOL ® / water (1:1)InsolubleTRANSCUTOL ® / water / ethanolSoluble(1:1:1)Ethanol / propylene glycol (1:1)SolubleEthanol / propylene glycol / Very solubleTRANSCUTOL ® (1:1:1)Water / propylene glycol / InsolubleTRANSCUTOL ® (1:1:1)Water / propylene glycol / SolubleTRANSCUTOL ® (1:1:2)

[0223]As can be seen from the data in Table 1, water is an unsuitable solvent for cortexolone-17α-propionate when used alone...

example 2

Evaluation of pH on Cortexolone-17α-propionate Stability

[0224]In a suitable container, under stirring, 50 g of cortexolone-17α-propionate was dissolved in a mixture of TRANSCUTOL® (461 g) and ethanol 96° (200 g). After complete dissolution of the cortexolone-17α-propionate, water (283 g) was added slowly. Finally, polysorbate 80 (5 g) and Alpha tocopherols (Vitamin E) (1 g) were added to the formulation. The natural pH of this formulation was measured using a standard pH electrode to be about 5.1.

[0225]The formulation was then split into three equal batches, each weighing about 300 g. Citric acid was added to the first batch to lower the pH to about 4. Sodium citrate was added the second batch to increase the pH to about 6. The third batch, having a natural pH of about 5.1, was used as a control. The three batches were then subjected to a short term stability study at 30° C., with the results shown in Table 2.

TABLE 2Cortexolone-21-propionate Contents*After 1After 2After 3monthmonths...

example 3

Antioxidant Evaluation

[0227]To a formulation containing 5 weight percent cortexolone-17α-propionate in a mixture of TRANSCUTOL®, propylene glycol, and ethanol (96°) in ratio of about 1:1:1 by weight, and further containing polysorbate 80 at 0.1 weight percent, the following antioxidants were added: Alpha tocopherols (Vitamin E) 0.3 weight percent; butylated hydroxyanisole (BHA) 0.01 weight percent, or ascorbyl palmitate 0.5 weight percent. The three formulations were then studied under short term stability conditions. The results are shown in Table 3.

TABLE 3Total Impurities Contents (Impurity percent = (sum of the % (w / w) of each impurity) / % (w / w) of cortexolone 17-alpha propionate * 100)After 1After 2After 3 monthmonthsmonthsAntioxidantTime 0(30° C.)(30° C.)(30° C.)Alpha0.62%1.33%1.56%1.78%tocopherols(Vitamin E)BHA1.37%2.86%2.57%NAAscorbyl0.05%0.22%0.29%0.37%palmitate

[0228]Ascorbyl palmitate provided the least amount of total degradation products.

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Abstract

The present disclosure provides high concentration formulations of cortexolone-17α-propionate suitable for treating alopecia.

Description

BACKGROUND[0001]Alopecia is a group of disorders with multiple and varying etiologies that results in hair loss from the body. The most common form of alopecia is androgenetic alopecia (“AGA”). AGA is also commonly called alopecia androgenetica, male pattern baldness, or male-pattern or female-pattern hair loss. It has been reported that AGA affects roughly 50% of men over 40. This form of alopecia may eventually affect up to 80% of white men by the age of 70 and about half of all women. Hair loss is often a cause of great concern to a patient for cosmetic and psychological reasons, but it can also be an important sign of systemic disease.[0002]AGA is a hereditary hair follicle disease that is also androgen-dependent. Dihydrotestosterone, in particular, plays a major role in the development and progression of AGA. Hair loss with AGA is progressive such that patients with disease experience a reduction in the normal 4:1 terminal-to-vellus hair ratio over a period of time. During this...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/573A61P1/00A61K47/26A61P17/14A61K9/00A61K9/08A61K9/06A61K47/10A61K47/22
CPCA61K31/573A61K47/10A61K9/0014A61P17/14A61K47/22A61K47/26A61P1/00A61K9/06A61K9/08A61K9/10A61K9/1075A61K9/0019A61K47/14A61P5/28C07J5/00
Inventor LONGO, LUIGI MARIA
Owner CASSIOPEA SPA
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