Tool and method for hormonal contraception and/or for the treatment of acne

 

(57) Abstract:

The invention relates to the field of medicine. Means for hormonal contraception and/or for the treatment of acne of two made in spatial terms separately in the same packaging unit, intended for reception by time sequentially hormonal components that, depending on the circumstances, consist of a certain number placed in a packaging unit in spatial terms separately and extracted separately doses of hormones, and the first hormonal component as hormonal biologically active substances essentially contains only the calling violation follicle estrogen drug, the second hormonal component contains in combination estrogen drug and at least sufficient to suppress ovulation dosage gestagennye drug. The total number of doses of hormones is equal to the total number of days desired cycle, and the first hormonal component covers 5-14, and the second hormonal component covers 23-14 daily doses and the number of doses of the first hormonal component is less than the number of daily doses of the second hormonelike, that daily dose of the second hormonal component characterized by a first reception, and daily doses of the first hormonal component are welcome then. Also we propose a method for using this tool. The tool provides greater security of contraception. 2 C. and 14 C.p. f-crystals.

The invention relates to a tool for hormonal contraception and/or for the treatment of acne from two spatially separated in the packaging unit, designed for consistent on-time introduction of hormonal components, which respectively consist of a certain number placed in a packaging unit in spatial terms separately and extracted separately doses of hormones, and the first hormonal component as hormonal biologically active substances contains essentially exclusively calling violation follicle estrogen drug; the second hormonal component, in contrast, contains in combination astrogeny the drug and at least sufficient for (delay) suppression of ovulation dosage gestagennye drug; and the total number of doses of hormones is equal to the total number of days desired zinah doses, and the number of doses of the first hormonal component is less than the number of doses of the second hormonal component.

From the Federal Republic of Germany patent 4104385 known vast ovulation means and method for hormonal contraception of the above kind, in which case it is preferable to hormonal contraception within the desired cycle by days consistently introduced first daily dose of the first hormonal component and then injected daily dose of the second hormonal component, then with the exception of the interruption again should the first doses of the first hormonal component of the nearest subsequent cycle.

The vast ovulation tool related type, which in normal case is still used types of drugs suppressing (inhibiting) ovulation interval, during which do not receive, from six or seven days replace the continuous intake of estrogenic component, i.e., daily doses of the first hormonal component, is quite suitable. However, it turns out that when the first hormonal component use in low dosage against Sania tool for the first time, however, disturbed maturation of follicles, but ovulation does not reliably prevented. This lower contraceptive security in the first round compared with the following rounds based on the fact that the new maturation of follicles begins in the latter part of the luteal phase preceding the ovulatory cycle, when fall endogenous endogenous estradiol and progesterone.

The first application of overwhelming (check) ovulation drug usual kind, in which there is an interval without receiving means, and the pill usually begin approximately on the fifth day after the onset of menstruation, contraceptive security could improve due to the fact that the first application of a reception beginning from the first day of menstruation (Martindale, 1993, S. 1177). By using a combination of estrogen with progestogen in this early time reliably prevent ovulation normal delay ovulation drugs, and have to put up with the fact that the first round is reduced, i.e., therefore, the result is a cycle until the beginning of the nearest menstruation approximately 24 days. On the same basis in the case of conventional drugs so what, s the drug at a low dose to reduce the interval without receiving means or in the first round completely abandon him (s.a.a. o.).

As in a normal ovulatory cycle, therefore, the maturation of follicles begins in the last third of the luteal phase (before menstruation), in the case of the vast ovulation funds related type cannot be reliably ensure reliable contraception during the first intake even in the case of doses at a particularly low dosage of the first hormonal component, if you start with a reception of the first hormonal component on the first day of menstruation, because then the first round is extended until the next menstruation approximately up to 30 days.

From the Federal Republic of Germany patent 4308406 (not published) you already know the vast ovulation means in the form of a combined preparation for contraception, which is intended as estrogenic hormonal component, and also contains a progestogen hormone component, in which daily doses contain biogenic estrogen and synthetic estrogen. The invention relates not to this kind of preparations.

The basis of the invention is to improve the suppressing (inhibiting) ovulation drugs, and how the related type in the sense that when the first reception even when primativa security.

According to the invention this task in increasing the overwhelming ovulation funds related type can be resolved by such location of doses in the packaging unit (the unit) to the daily dose of the second hormonal component was characterized for the first dose and daily dose of the first hormonal component was characterized as for next steps, and daily dose of the second hormonal component does not contain a combination of biogenic estrogen and synthetic estrogen.

It may be provided that the total number of daily doses are numbered consecutively according to the days of admission for all the desired cycle, since the distribution of the first daily dose of the second hormonal component to the first day of admission.

The tool according to the invention can also be characterized by solid numbering daily doses.

An alternative to this, the tool according to the invention can also be characterized by variable numbering doses so that on the first day of admission prescribed by the choice of the first daily dose of the first or of the second hormonal component.

In case the funds soglasna least partially formulated for oral administration.

Further, it may be provided that at least one of the hormonal components at least partially completed form for percutaneous introduction.

Further, according to the invention offers at least a few daily doses of at least one of the hormonal components to combine in one dose extended (prolonged) steps.

It is proposed in spatial terms separately to konfektionierung in one packaging unit of the at least two pairs of first and second hormonal component.

In addition, the invention can vary at least one dose of the prolonged action (depo-dose) combining at least two pairs of hormonal components.

Finally, the tool according to the invention can also differ in that the daily dose of the second hormonal component (components) are gradually increasing estrogen.

The method according to the invention, which is carried out, in particular, the use of hormonal means according to the invention, characterized in that the first introduction means in the first day of menstruation begin with the first daily dosimetrie daily dose of the second hormonal component; then, without interval, which does not enter the vehicle, take all doses of the first hormonal component; and, finally, then, without interval, which does not enter, you should receive the first daily dose of the second hormonal component of the subsequent cycle.

However when injected hormonal means, in the case of the first injection means possible to dispense doses of the first hormonal component.

It may be provided that at least one of the hormonal component is administered orally.

Further, the invention provides that at least one of the hormonal component is administered transdermally.

Also stipulate that at least a few daily doses of at least one of the hormonal components impose a dose of the prolonged action (depo-dose).

Finally, it may be provided that the daily dose of the second hormonal component (components) are gradually increasing estrogen.

The basis of the invention laid the unexpected discovery that in the case of suppressing ovulation funds related type can achieve high contrace is therefore component estrogen/gestagen, on the first day of menstruation. Accordingly, you can also do in the case of switching from a drug with a higher dosage of the usual kind for the vast ovulation tool related type, consequently, on the immediate receiving daily doses of the second hormonal component after the last tablet of the composition of oestrogen/gestagen conventional drug, although it is not directly necessary.

Proposed according to the invention the method can be carried out with the use of conventional packaging (for example, 7 daily doses of the first hormonal component and 21 daily dose of the second hormonal component) related type due to the fact that in the first cycle of reception of refuse from seven daily doses, respectively tablets, the first hormonal component, so, therefore, immediately on the first day of menstruation begin with the first daily dose of the second hormonal component. Following this offer admission in the usual way.

On the other hand, however, you can also do so as to apply a packing unit, which contains the second hormonal component for reception days 1-21, if desired obakemono unit, beginning with the second hormonal component, etc.

A further alternative is that the used packaging unit in which you can install a digital designation of days of admission for enjoying, so the first day of admission falls on the first daily dose of the first hormonal component, or on the first daily dose of the second hormonal component, and if necessary, you can apply full (runde) packing form, which is used, for example, in the case of sales of the drug "Trisequens".

The first hormonal component and the second hormonal component in the case of the vast ovulation means according to the invention, however, can be formulated accordingly to patent Germany 4104385, which in this respect to make a reference for further clarification.

Regarding envisaged in the invention, if necessary, if not also preferably, the means for percutaneous introduction of at least one of the hormonal components, it should be noted that from a Brit. Med. J. 297 (1988), 900-901 already know that you can cause suppression (delay) ovulation due to percutaneous injection daily 200 mcg of estradiol using patches that the level of estradiol, without the introduction of progestogen. To avoid endometrial hyperplasia at the same time in each cycle is additionally within 7-10 days to introduce a progestogen, which, however, due to the short duration of use does not make any significant contribution to contraception. The method described in the case of young women are less reliable, and in contrast to the invention does not use a hormonal component, in which gestagenna the drug is at least sufficient to suppress ovulation dosage.

The following describes the embodiments of the invention.

Example 1

For suppressing ovulation processing apply the next product that contains 21 daily dose, respectively, with 2 mg estradiol and 1 mg of norethisterone and 7 daily doses of 2 mg estradiol. The first daily dose of 2 mg estradiol and 1 mg of norethisterone take on the first day of menstruation as the first introduction, then enter the next 20 daily doses containing 2 mg estradiol and 1 mg of norethisterone and after that enter 7 daily doses of 2 mg estradiol with direct joining of the first of the 21st daily dose, respectively, with 2 mg estradiol and 1 mg of norethisterone very near the fir side effects at a very good contraceptive security.

Example 2

Apply the vast ovulation tool that contains 18 daily doses, each with 20 mcg ethinylestradiol and 150 mcg levonorgestrel and 10 daily doses, each 20 mcg ethinyl estradiol. Introduction corresponds to example 1. Observations also correspond to those of example 1.

Example 3

For suppressing ovulation processing all four weeks (each with 1 day) perform intramuscular injection of 50 mg of astrogeological. Additionally, from the 6th to the 28th day (23 daily dose) daily administered 2 mg cyproterone, oral. With good contraceptive security tool shows no side effects.

Example 4

For suppressing ovulation processing daily injected with 100 g of estradiol - using the patch, which replaces two times per week, i.e., day 1, day 4, day 8, day 11, and so on, accordingly, every 3.5 days. Additionally, between the 8-th and 28-th day daily (21 daily dose) administered at 150 micrograms of desogestrel. It also does not see any noteworthy side effects, with good contraceptive security.

Disclosed in the above description and in the claims the hallmarks of izaberete is its various forms.

1. Means for hormonal contraception and/or for the treatment of acne from two spatially separated in one packaging unit designed for sequential injection time of hormonal components, each of which consists of a number placed in a packaging unit in spatial terms separately and extracted separately doses of hormones, and the first hormonal component as hormonal biologically active substance contains, essentially, only the calling violation follicle estrogen drug, the second hormonal component contains in combination estrogen drug and at least sufficient to suppress ovulation dosage gestagennye drug the total number of doses of hormones is equal to the total number of days desired cycle, and the first hormonal component comprises 5 to 14, and the second hormonal component covers 23 - 14 daily doses and the number of doses of the first hormonal component is less than the number of doses of the second hormonal component, characterized in that it has this kind of location daily doses in the packaging unit that daily doses storeapart characterized by, how to receive later, and the daily dose of the second hormonal component contain either biogenic or synthetic estrogen.

2. Means under item 1, characterized in that the total number of daily doses consecutively numbered by days of admission for all the desired cycle, since the distribution of the first daily dose of the second hormonal component to the first day of admission.

3. Means under item 2, characterized in that it has solid numbers of doses.

4. Means under item 2, characterized in that it has variable numbers of doses so that on the first day of admission prescribed by the choice of the first daily dose of the first or of the second hormonal component.

5. A tool according to any one of paragraphs.1 to 4, characterized in that at least one of the hormonal components, at least partially intended for oral administration.

6. A tool according to any one of paragraphs.1 to 5, characterized in that at least one of the hormonal components, at least partially designed for percutaneous introduction.

7. A tool according to any one of paragraphs.1 - 6, characterized in that at least a few daily doses of at least one hormone is 7, characterized in that at least two pairs of first and second hormonal component feature in spatial terms separately in one packaging unit.

9. Means under item 7 or 8, characterized in that at least one dose of combining at least two pairs of hormonal components, is the dose of long-acting (depot-dose).

10. A tool according to any one of paragraphs.1 to 9, characterized in that the daily dose of the second hormonal component (components) are gradually increasing estrogen.

11. Method for hormonal contraception and/or for the treatment of acne by introducing hormonal means of two spatially separated in a single packaging unit, intended for the introduction of time-sequentially hormonal components, each of which consists of a number placed in a packaging unit in spatial terms separately and extracted separately doses of hormones, and the first hormonal component as hormonal biologically active substances contains essentially exclusively calling violation follicle estrogen drug, vocational to suppress ovulation dosage gestagennye drug the total number of doses of hormones is equal to the total number of days desired cycle, the first hormonal component comprises 5 to 14, and the second hormonal component covers 23 - 14 daily doses and the number of doses of the first hormonal component is less than the number of doses of the second hormonal component, characterized in that the injected hormonal agent according to any one of paragraphs.1 - 10, with the first introduction means in the first day of menstruation begin with the first daily dose of the second hormonal component, after that without an interval, during which not enter the vehicle, take it all following daily doses of the second hormonal component, then no interval during which not enter the tool, take the first daily dose of the first hormonal component, and finally, then, without interval, during which not enter, you should receive the first daily dose of the second hormonal component of the subsequent cycle.

12. The method according to p. 11 when using hormonal drugs, in which daily doses of the first hormonal component are characterized as to receive first, and daily dose of the second hormonal component are characterized, gormonalnogo component.

13. The method according to p. 11 or 12, characterized in that at least one of the hormonal component is administered orally.

14. The method according to any of paragraphs.11 to 13, characterized in that at least one of the hormonal component is administered transdermally.

15. The method according to any of paragraphs.11 to 14, characterized in that at least a few daily doses of at least one of the hormonal components impose a dose of the prolonged action (depo-dose).

16. The method according to any of paragraphs.11 to 15, wherein the daily dose of the second hormonal component (components) are gradually increasing estrogen.

 

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