Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing
Reexamination Certificate
2001-03-19
2003-10-14
Hartley, Michael G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
C424S045000, C424S489000, C424S434000, C424S501000, C514S573000, C514S284000, C128S200140
Reexamination Certificate
active
06632419
ABSTRACT:
FIELD OF THE INVENTION
This invention relates generally to a method of treating humans with a decreased libido. More specifically, the invention relates to acute, bolus non-invasive administration of testosterone to enhance libido over a discrete period of time.
BACKGROUND OF THE INVENTION
The presence of a normal amount of libido, defined as the urge to engage in sexual activity, is an important component of an individual's well-being. In both men and women the primary naturally occurring hormone responsible for libido is testosterone. In males, the baseline testosterone level is a relatively constant throughout life, decreasing slowly in old age. In contrast, women elaborate testosterone only as part of the process of ovulation. Each maturing follicle produces testosterone at the mid-point of the menstrual cycle, consistent with observations that female libido peaks with ovulation. As a woman ages, the number of maturing follicles per month decreases, and there is a decreasing total amount of testosterone produced. A common complaint of post menopausal women is decreased libido. This decrease in libido is characterized by a lack of interest in sexual intercourse, the lack of ability to achieve orgasm, or decrease in intensity of orgasm. It is important to note that this decrease in libido is often associated with a profound sense of loss of a once normal and active interest in sexual activity. Low levels of testosterone in, e.g., hypogonadal men are associated with lack of libido and absence of erections. They respond to therapy with exogenous testosterone (Cunningham et al.,
J Clin Endocrinol Metab,
(March 1990) 70:792-7; Behre et al.,
J Clin Endocrinol Metab,
(November 1992) 75:1204-10; and women also respond to testosterone therapy, see Tuiten et al.,
Arch. Gen. Phychiatry,
(February 2000) 57:149-153.
Clinicians frequently confronted with the problem of managing female patients presenting with decreased libido have limited tools to address the problem. Testosterone is available as an oral preparation and can be given, for instance, in combination with estrogen to restore testosterone levels. However, the replacement of the once pulsatile endogenous delivery of testosterone with the sustained blood level of the hormone produces unwanted side effects. Women taking testosterone for a few weeks typically begin to complain of the emergence of secondary sexual characteristics such as unwanted body hair, oily hair, and, with prolonged a use, deepening voice. For this reason, oral testosterone replacement therapy is not a practical solution for most patients with decreased libido.
Other forms of testosterone replacement therapy for women are being explored. A transdermal patch capable of delivering a steady rate of testosterone is being tested for use in women. As with oral testosterone replacement therapy, the study state blood levels of testosterone produced via transdermal delivery are likely to be associated with the same side effect profile issues.
It is recognized that testosterone in females decreases with age (Human Biology, May 1980, volume of 52, No. 2, pages 181-0191.). It is also known that sexual motivation in post menopausal women is associated with the levels of exogenously introduced testosterone (Psychosomatic Medicine volume 47, No. 4, 1985). Further, providing intravenous testosterone to women as part of clinical studies is known (American Journal of Obstetrics and Gynecology, December 1986 pages 1288 to 1292).
A transdermal patch for men is sold by Alza Corporation under the name of Testoderm®. An injectable for intramuscular injectable is sold by Bristol-Meyers Squibb Company under the name Delatestryl®, and by Star under the name Virilon® IM. While these dosage forms may increase steady state levels of testosterone in men, they do not result in the physiologically correct pulsatile release that occurs in men with normal testosterone production. A bolus delivery of testosterone that provides an approximation to the pulsatile delivery yielding short brief peaks that can provide the physiological stimulus for increase of sexual desire and improved erectile function.
SUMMARY OF THE INVENTION
A method of increasing the libido of a woman over a discrete period of time (e.g. 30-240 minutes) by the administration of testosterone is disclosed. The method of the invention does not maintain therapeutic levels of testosterone over long periods e.g. days, weeks or months. Because the method of the invention only maintains therapeutic levels over a short period the adverse side effects of long term testosterone treatment are avoided.
The testosterone formulation may be comprised of a reduced version of testosterone having been reduced by 5&agr;-reductase to 5&ggr;-dihydroxytestosterone which is delivered in a bolus dose. The testosterone formulation may be administered in a variety of different ways, e.g. may be aerosolized preferably producing particles which have a size in a range of from about 1 to 3 microns which can be inhaled into areas of the lung where they can readily enter the blood stream.
An aerosol containing testosterone or its reduced version 5-&ggr;-dihydrotestorone is inhaled into the lungs of a patient. Once inhaled, particles of the drug deposits on lung tissue and from there enter the patient's circulatory system and thereby increase the patient's serum testosterone level. The percentage increase in the patient's testosterone level will vary depending on the needs of the patient. However, the patient's normal baseline serum testosterone level is preferably increased 25% or more and more preferably 100% or more. By preferably providing the testosterone in a reduced form i.e. 5&agr;-dihydroxytestosterone because the delivery is by inhalation the patient's serum level of an active form of the hormone is quickly raised to a desired level e.g. in thirty minutes or less, more preferably fifteen minutes or less. When the patient's blood serum level of the active form of the hormone is raised to a desired level the patient's libido is increased. The increased level gradually subsides (as the hormone is metabolized and cleared) thereby avoiding the adverse side effects generated by maintaining enhanced hormone levels over long periods.
An aspect of the invention is a method of increasing the libido of an adult human female patient by the administration of a bolus dose of testosterone which quickly increases the level of testosterone in the patient for a relatively brief time.
Another aspect of the invention is a method of treatment whereby testosterone or derivative thereof is aerosolized, inhaled and provided to the circulatory system of the patient at levels sufficient to increase libido (over a short period of time) and propensity for orgasm.
Another aspect of the invention is to combine bolus delivery of testosterone with additional treatment such as a topical cream applied to the vaginal area to increase blood flow to that area.
An advantage of the invention is that the testosterone levels are raised within minutes of administration (preferably 30 minutes or less) and return to normal levels within hours—preferably in less than four hours.
Another advantage is that the administered testosterone is quickly metabolized allowing the patient's testosterone levels to return to normal thereby avoiding the adverse effects of long term administration.
A feature of the invention is that aerosolized particles of testosterone having a diameter of about 0.5 to 8 microns (preferably 1-3 microns) are created and inhaled deeply into the lungs thereby enhancing the speed and efficiency of administration.
It is an object of this invention to describe the utility of delivering testosterone or dihydrotestosterone by inhalation as a means of treating women with decreased libido and/or decreased propensity to have orgasms.
It is another object of this invention to describe liquid formulations (which includes suspensions) of testosterone and derivatives thereof such as 5&agr;-dihydrotestosterone appropriate for pulmonary deliv
Cole Robert
Rubsamen Reid M.
Aradigm Corporation
Bozicevic Field & Francis LLP
Haghighatian Mina
Hartley Michael G.
LaSalle Carol
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