Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Patent
1998-09-28
2000-06-20
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
424455, 424457, 424489, 514177, 514182, A61K 948, A61K 966, A61K 952, A61K 914, A61K 3156
Patent
active
060775319
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a medicament based on estradiol and progesterone intended for the treatment of menopausal pathology.
In effect, it is known that the estrogenic deficiency which manifests itself during the period of the menopause is sometimes difficult for the feminine organism to tolerate, due in particular to the fact that it is felt not only at the level of the central nervous system, where it is responsible for outward signs of neurovegetative order, such as hot flushes, but also at the level of the osseous cartilage.
In the past, various methods of administration of estradiol have been proposed, and in particular a method of administration by the percutaneous route. As for the medicament forming the subject matter of the present invention, it can be administered by the oral route.
It is also known that, in the case of estrogenotherapy, it is usual to administer a treatment of progesterone in order to avoid in particular the risks of hyperplasia of the endometrium.
Rather than oblige the patient to take these two medicaments separately, it will be understood that it is particularly advantageous to group them together in one and the same medicament in order to allow them to be absorbed in a single dose.
Patent FR-A-2 408 345 in particular discloses medicaments based on progesterone which can be administered by the oral route. In certain of these medicaments, the progesterone is in the micronized state in suspension in a liquid constituted by oil. It is an object of the present invention to include with this medicament an appropriate quantity of estradiol.
One difficulty arises from the fact that, in order to obtain a complete dissolution of the estradiol in certain oils, and particularly in peanut oil, the quantity of oil necessary is such that the volume of the capsule of medicament is in that case such as to render absorption thereof by the user more difficult. Of course, the volume of this capsule may be reduced, but in that case the quantity of oil contained therein is insufficient to allow a total dissolution of the estradiol, with the result that the latter risks recrystallizing, which, as is well known, reduces its active character. In fact, it is perfectly well known that the size of the particles has a direct effect on the absorption of the lipophilic molecules and therefore on their activity.
U.S. Pat. No. 4,900,734 also discloses compositions intended for the treatment of menopausal pathology, containing a progesterone in the micronized state in suspension in an oil of polyunsaturated type and estradiol solubilized in this oil.
The present invention has for an object to propose a means for dispensing the estradiol and the quantity of progesterone which must normally be associated therewith, in a single capsule of small dimensions.
The present invention thus relates to a medicament constituted by a capsule soluble in a biological medium, containing a progesterone in the micronized state in suspension in oil, characterized in that the capsule also contains estradiol enclosed in microspheres also in suspension in the oil and which are constituted by at least one polymer adapted not to dissolve in oil and to dissolve in a biological medium.
In a form of embodiment of the invention, this polymer is a cellulosic polymer, particularly of the type marketed under the Trademark "KLUCEL EFEP". This polymer may also be an acrylic polymer marketed in particular under the Trademark "EUDRAGIT E100".
Applicants have established, in particularly interesting manner, as shown in the kinetic dissolution curves shown hereinbelow, that the speed of dissolution of the estradiol contained in microspheres is at least equal to, if not greater than, what it is in the normal state, i.e. in a micronized state (in other words, a state in which the particles present dimensions of the order of 5 .mu.m). This property is particularly advantageous insofar as, up to the present time, the fact of placing an active substance in microspheres had for its effect to slow down release thereof.
Various forms of embodim
REFERENCES:
patent: 4196188 (1980-04-01), Besins
patent: 4624665 (1986-11-01), Nuwayser
patent: 4900734 (1990-02-01), Maxson et al.
patent: 5340584 (1994-08-01), Spicer et al.
Chemical Abstracts, vol. 90, No. 22, May 1979.
Laboratoires Besins Iscovesco
Page Thurman K.
Ware Todd D
LandOfFree
Estradiol and progesterone-based medicament does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Estradiol and progesterone-based medicament, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Estradiol and progesterone-based medicament will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1849996