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Pharmaceutical composition and method for treating hypogonadism

Inactive Publication Date: 2005-05-26
LABORATORIES BESINS INTERNATIONAL SAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0047] The foregoing problems are solved and a technical advance is achieved with the present invention. The present invention generally comprises a testosterone gel. Daily transdermal application of the gel in hypogonadal men results in a unique pharmacokinetic steady-state profile for testosterone. Long-term treatment further results in increased bone mineral density) enhanced libido, enhanced erectile frequency and satisfaction, increased positive mood, increased muscle strength, and improved body composition without significant skin irritation. The present invention is also directed to a unique method of administering the testosterone gel employing a packet having a polyethylene liner compatible with the components of the gel.

Problems solved by technology

However, as discussed above, the clinical and survey data shows that all of these patches suffer from significant drawbacks, such as buritus, burn-like blisters, and erythema.
Thus, the transdermal patch still remains an inadequate testosterone replacement therapy alternative for most men.
However, the pharmacokinetics of a DHT-gel is markedly different from that of a testosterone gel.
Thus, DHT gels are not effective at increasing testosterone levels in hypogonadal men.

Method used

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  • Pharmaceutical composition and method for treating hypogonadism
  • Pharmaceutical composition and method for treating hypogonadism
  • Pharmaceutical composition and method for treating hypogonadism

Examples

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example 1

Treatment of Hypogonadism in Male Subjects

[0116] One embodiment of the present invention involves the transdermal application of AndroGel® as a method of treating male hypogonadism. As demonstrated below, application of the gel results in a unique pharmacokinetic profile for testosterone, as well as concomitant modulation of several other sex hormones. Application of the testosterone gel to hypogonadal male subjects also results in: (1) increased bone mineral density, (2) enhanced libido, (3) enhanced erectile capability and satisfaction, (4) increased positive mood, (5) increased muscle strength, and (6) better body composition, such increased total body lean mass and decreased total body fat mass. Moreover, the gel is not associated with significant skin irritation.

[0117] Methods

[0118] In this example, hypogonadal men were recruited and studied in 16 centers in the United States. The patients were between 19 and 68 years and had single morning serum testosterone levels at scree...

example 2

Gel Delivery Dosage Forms and Devices

[0254] The present invention is also directed to a method for dispensing and packaging the gel. In one embodiment, the invention comprises a hand-held pump capable of delivering about 2.5 g of testosterone gel with each actuation. In another embodiment, the gel is packaged in foil packets comprising a polyethylene liner. Each packet holds about 2.5 g of testosterone gel. The patient simply tears the packet along a perforated edge to remove the gel. However, because isopropyl myristate binds to the polyethylene liner, additional isopropyl myristate is added to the gel in order to obtain a pharmaceutically effective gel when using this delivery embodiment. Specifically, when dispensing the gel via the foil packet, about 41% more isopropyl myristate is used in the gel composition (i.e., about 0.705 g instead of about 0.5 g in Table 5), to compensate for this phenomenon.

[0255] The composition can also be dispensed from a rigid multi-dose container ...

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Abstract

A pharmaceutical composition useful for treating hypogonadism is disclosed. The composition comprises an androgenic or anabolic steroid, a C1-C4 alcohol, a penetration enhancer such as isopropyl myristate, and water. Also disclosed is a method for treating hypogonadism utilizing the composition.

Description

FIELD OF TH INVENTION [0001] The present invention is directed to a pharmaceutical composition comprising testosterone in a gel formulation, and to methods of using the same. BACKGROUND OF THE INVENTION [0002] A. Testosterone Metabolism in Men [0003] Testosterone is the major circulating androgen in men. More than 95% of the 6-7 mg of testosterone produced per day is secreted by the approximately 500 million Leydig cells in the testes. Two hormones produced by the pituitary gland, luteinizing hormone (“LH”) and follicle stimulating hormone (“FSH”), are required for the development and maintenance of testicular function. [0004] The most important hormone for the regulation of Leydig cell number and function is LH. In eugonadal men, LH secretion from the pituitary is inhibited through a negative-feedback pathway by increased concentrations of testosterone through the inhibition of the release of gonadotropin-releasing hormone (“GRH”) by the hypothalamus. FSH promotes spermatogenesis a...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/565A61K47/10A61K47/12A61K47/14A61P5/26
CPCA61K9/0014A61K9/06A61K47/10A61K47/12A61K47/14A61K31/565A61K31/568A61K31/557A61K31/52A61K31/485A61K31/475A61K31/415A61K2300/00A61K31/5685A61P15/08A61P5/00A61P5/26A61K47/32
Inventor DUDLEY, ROBERT E.DROUIN, DOMINIQUE
Owner LABORATORIES BESINS INTERNATIONAL SAS
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