Methods and compositions using gonadotropin hormone releasing hormone

A gonadotropin and hormone-releasing technology, which is applied in drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problems of decreased bone formation markers and increased bone resorption markers, etc.

Inactive Publication Date: 2006-05-31
DEBIOPHARM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Finally, another study showed that specific inhibition of aromatase activity also resulted in a marked increase in markers of bone resorption and a decrease in markers of bone formation

Method used

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  • Methods and compositions using gonadotropin hormone releasing hormone
  • Methods and compositions using gonadotropin hormone releasing hormone
  • Methods and compositions using gonadotropin hormone releasing hormone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Preparation of a composition releasing triptorelin and estradiol over a period of at least one month

[0038] 1. Triptorelin preparation

[0039] This formulation was obtained as described in Example 1 of US Patent No. 5,134,122.

[0040] 2. Estradiol formulation embedded in PLGA microspheres

[0041] The aqueous phase (solution A) was prepared by mixing 160 g of PVA (polyvinyl alcohol) and 7840 g of MilliQ water at 40° C. under magnetic stirring. Next prepared by dissolving 4.9 g of 50:50 poly(D,L-lactide-co-glycolide) polymer (intrinsic viscosity (iv) = 0.42 dl / g) in 50 g of ethyl acetate under magnetic stirring Organic Phase (Solution B). 100 mg estradiol was dissolved in 800 μl DMSO (dimethyl sulfoxide) (solution C).

[0042] Mix solution B and solution C together and pump the resulting solution into the homogenizer at a rate of 5 ml / min. Solution A was pumped in parallel into the homogenizer at a rate of 750 ml / min. The rotational speed of th...

Embodiment 4

[0044] The serum release of estradiol in rats after a single intramuscular injection of the obtained formulation is reported in Example 4.

Embodiment 2

[0045] Example 2: Preparation of a composition releasing triptorelin and estradiol over a period of at least one month

[0046] 1. Triptoline preparation

[0047] This formulation was obtained as described in Example 1 of US Patent No. 5,134,122.

[0048] 2. Estradiol formulation embedded in PLGA microspheres

[0049] The aqueous phase (solution A) was prepared by mixing 80 g of PVA (polyvinyl alcohol) and 3920 g of MilliQ water at 40° C. under magnetic stirring. Next prepared by dissolving 4.5 g of 65:35 poly(D,L-lactide-co-glycolide) polymer (intrinsic viscosity (iv) = 0.62 dl / g) in 25 g of ethyl acetate under magnetic stirring Organic Phase (Solution B). 92 mg estradiol was dissolved in 800 μl DMSO (dimethyl sulfoxide) (solution C).

[0050] Mix solution B and solution C together and pump the resulting solution into the homogenizer at a rate of 5 ml / min. Solution A was pumped in parallel into the homogenizer at a rate of 630 ml / min. The rotational speed of the r...

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Abstract

The present invention relates to compositions comprising two sustained-release formulations, the first capable of releasing the gonadotropin-releasing hormone component and the second capable of releasing the estrogenic component. Compositions of the present invention can be used for improved androgen ablation therapy of prostate cancer to minimize loss of bone mineral density and frequency and severity of hot flashes by maintaining low adequate estrogen levels during treatment .

Description

Background technique [0001] Agonists and antagonists of gonadotropin-releasing hormone (GnRH) are used to treat benign gynecological conditions including premenstrual syndrome and androgen-dependent prostate cancer. GnRH is also known as luteinizing hormone-releasing hormone. GnRH is secreted in pulses by the hypothalamus in the pituitary portal system. Because hormones have half-lives on the order of minutes, the pituitary gland is exposed to pulsations of hormones. This exposure results in the secretion of gonadotropins, namely luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In men, LH acts on the Leydig cells of the testis to stimulate the secretion of testosterone. FSH is responsible for sperm production. Testosterone appears to have a feedback-inhibiting effect on the secretion of GnRH, reducing the sensitivity of the pituitary gland to the hormone. In women, FSH acts on the ovaries to stimulate the secretion of estrogen. The main role of LH in wome...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/00A61K9/16A61K9/50A61K31/565A61P13/08A61P35/00
CPCA61K9/0019A61K9/0024A61K9/1647A61K9/19A61K9/5084A61K31/56A61K31/565A61K38/09A61K38/24A61P13/08A61P3/12A61P35/00A61P5/02A61P5/30A61K2300/00A61K9/0021A61K9/0014
Inventor H·珀切特F·海姆加特纳C·科迪B·杜克雷
Owner DEBIOPHARM SA
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