Birth control technique used as and when necessary

FIELD: medicine.

SUBSTANCE: invention refers to medicine, gynaecology, birth control techniques used as and when necessary, and emergency contraception. Ulipristal acetate or its metabolite is administered orally in a female no more than 72 hours to 120 hours after a sexual encounter in a dose of 20 to 30 mg. Another dose can be administered again at least twice a month. The preparation can be administered either in the form of an immediate-release dosage form, in the form of a tablet.

EFFECT: method provides the high efficacy of emergency contraception even in low doses and late administration of the preparation - up to 120 hours after the sexual encounter as compared to a reference preparation of levonorgestrel.

7 cl

 

The present invention relates to a method of contraception that is used as needed, women, particularly women who do not have regular sexual activity.

The level of technology

Hormonal contraception considered today as the most reliable method of reversible contraception. It requires continuous reception of pills, usually daily intake, regardless of the frequency of sexual contacts. For women with infrequent sexual contact, however, drugs that depend on sexual intercourse and, thus, can be taken less often, reduced impact of effective ingredients, could be more advantageous. Being recognized for a long period of time (Canzler et al., Zbl. Gynakol, 1984, 106: 1182-1191), the need for such contraception used as needed, remains unrealized (Aitken et al., Contraception, 2008, 78:S28-S35).

In fact, women make such methods themselves of the existing (available) products. In Ghana, a study conducted in 2003, it was reported that women used the pill norethindrone sold on the market for the treatment of various gynecological problems, as a method of contraception used orally on an "as needed". More recently, anecdotal reports and the data is, collected by colleagues in the organization Family Health International, show that women in other parts of Africa and elsewhere deliberately use contraceptive pills for emergency contraception in the same way.

Despite the fact that oral methods do not provide protection against sexually transmitted infections, studies conducted several decades ago showed that different doses of levonorgestrel that is used as the regularly used postcoital contraception can protect with efficacy comparable with the overall effectiveness of condoms and other barrier methods during normal use (United Nations Development Programme/ United Nations Population Fund/ World Health Organization/ World Bank Special Programme of Research, Development and Research Training in Human Reproduction, Task Force on Post-Ovulatory Methods of Fertility Regukation. Efficacy and side effects of immediate postcoital levonorgestrel used repeatedly for contraception. Contraception 2000; 61:303-8). In addition, it was proposed to assess whether affect ovulation process a single vaginal gel injection levonorgestrel before sexual contact (- Brache et al., Contraception, 2007; 76:111-116).

Other progestational drugs were used as postcoital emergency contraception. Emergency contraception (EC) refers to duplicate the methods of emergency contraceptive assistance, to which the woman may be resorted to within the first the first few days after unprotected intercourse to prevent an unwanted pregnancy. For example, preclinical studies and early clinical trials with ulipristal-acetate, developed by HRA Pharma emergency contraception, confirmed that a single dose of component 50 mg ulipristal-acetate, is safe and effective when it is administered to a woman who is accessing emergency contraception within 72 hours after unprotected sexual contact (Creinin et al., 2006, Obstetrics & Gynecology, 108(5):1089-1097).

Summary of the invention

The invention provides a method, where the method includes the introduction as required progestogennoe funds or modulator of progesterone receptor woman within 72 hours prior to sexual contact, where the introduction can be redone at least once a week.

The invention also provides a method of contraception, including the introduction as required progestogennoe funds or modulator of progesterone receptor woman within 120 hours after intercourse, preferably at least twice a month.

In a preferred embodiment, the invention provides a method, where the method includes the introduction as required progestogennoe funds or modulator of the progesterone receptor, such as 17A-acetoxy-11b-[4-N,N-dimethylamino-phenyl]-19-n is pregna-4,9-diene-3,20-dione (ulipristal-acetate) or its metabolite, woman within 72 hours prior to sexual contact, where the introduction can be redone at least once a week.

The invention also provides a method of contraception, including the introduction as required progestogennoe funds or modulator of the progesterone receptor, such as 17A-acetoxy-11b-[4-N,N-dimethylamino-phenyl]-19-norpregna-4,9-diene-3,20-dione (ulipristal-acetate) or its metabolite, woman within 120 hours after intercourse, preferably at least twice a month.

Detailed description of the invention

The inventors have studied, could ulipristal-acetate to be used as emergency contraception, but also as regularly accept hormonal contraceptives.

For this purpose, a healthy female volunteers with normal menstrual cycle received 3 months of continuous daily administration ulipristal-acetate (2,5, 5, or 10 mg) or placebo. Assessment of ovarian hormones, follicular development, endometrial histology and characteristics of menstrual bleeding was performed during the third month of treatment. One patient was treated by 10 mg ulipristal-areata/day) missed 2 days of taking the drug in its third cycle of treatment (days 1 and 2) and still had no sign of luteal activity is STI or ovulation. This prompted the inventors to consider what ulipristal-acetate could be used as a method of contraception, which could be taken as needed, not every day like any hormonal contraceptive pill.

On this basis, the invention provides a method of contraception, as appropriate, where the method includes the introduction progestogennoe funds or modulator of the progesterone receptor, such as 17A-acetoxy-11b-[4-N,N-dimethylamino-phenyl]-19-norpregna-4,9-diene-3,20-dione (ulipristal-acetate) or its metabolite, woman within 72 hours prior to sexual contact and/or within 120 hours after intercourse.

The invention additionally provides a method of contraception, where the method involves continuous introduction progestogennoe funds or modulator of the progesterone receptor, such as ulipristal-acetate and its metabolite, woman. In particular, progestogen tool or modulator of the progesterone receptor, such as ulipristal-acetate and its metabolite, may be entered less than once a day, during the menstrual cycle. Preferably, it is administered at least once per week during the menstrual cycle.

More generally, the inventors propose to use progestogen funds or modulators of progesterone receptors is for contraception, as appropriate.

Progestogen funds

Progestogen funds, also known as progestins, can represent any connection with progestogenic activity.

Progestogen means can be selected from progesterone and its derivatives such as, for example, esters of 17-hydroxy progesterone esters of 19-nor-17-hydroxy-progesterone, 17α-ethynyltestosterone and its derivatives, 17α-ethinyl-19-nor-testosterone and its derivatives, norethindrone, norethindrone-acetate, ethynodiol-diacetate, dydrogesterone, medroxy-progesterone-acetate, norethynodrel, allylestrenol, lynestrenol, quingestanol-acetate, medrogestone, norgestrienone, cimetidime, ethisterone, cyproterone-acetate, levonorgestrel, DL-norgestrela, D-17α-acetoxy-13β-ethyl-17α-ethinyl-gon-4-EN-3-one-oxime, gestodene, desogestrel, norgestimate, nestorone and drospirenone.

In the preferred embodiment, it should be understood that progestogen tool does not combine with any other hormonal contraceptive, such as with estrogen. In this case, contraception often referred to as contraceptive-only-progestin".

Modulators of progesterone receptor

Modulators of progesterone receptor for use in the present invention can be selected, for example from ulipristal-acetate, mifepristone or means of CDB-4124 or its active metabolites.

Preferred progesterone receptor modulator is ulipristal-acetate.

Ulipristal-acetate, first known as CDB-2914 is a 17α-acetoxy-11β-[4-N,N-dimethylamino-phenyl]-19-norpregna-4,9-diene-3,20-dione represented by the formula I

It is a well-known steroid, more specifically 19-norprogesterone, which has antiprogestogens and antiglucocorticoid activity. This connection and the means for producing it are described in patents: U. S. Patent Nos. 4954490, 5073548 and 5929262 and in international patent applications: WO 2004/065405 and WO 2004/078709. The properties of this connection is additionally described in the publications: Blithe et al., 2003, Steroids, 68:1013-1017, and Gainer and Ulmann, 2003, Steroids, 68:1005-1011.

Metabolites CDB-2914 include compounds described in the publication Attardi et al., Journal of Steroid Biochemistry & Molecular Biology, 2004, 88: 277-288, for example, monodimensional CDB-2914 (CDB-3877); demetilirovanny CDB-2914 (CDB-3963); alpha-hydroxy CDB-2914 (CDB-3236); derived CDB-2914 with an aromatic A-ring (CDB-4183).

monodimensional CDB-2914

demetilirovanny CDB-2914

17α-hydroxy CDB-2914

derived CDB-2914 aromatic And what olicom

As needed

The subject or patient can be any woman. The invention provides contraception, applied as needed" basis, which means that a woman can take progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, at any time in the case where it is required, that is when the sexual contact is expected or has recently occurred. Preferably, the female does not apply any other hormonal contraceptive drug. In another preferred embodiment, the subject does not use any protection (condom, intrauterine device, spermicide, etc.).

A woman may want to apply progestogen tool or modulator of the progesterone receptor, for example ulipristal-acetate and its metabolite, as regularly used contraception in the case when sexual activity becomes more regular. Preferably the introduction then perform again, at least once a week, preferably once a week or four times during the menstrual cycle, or twice during the menstrual cycle, or three times during the menstrual cycle. The term "do again" means that one unit on the licensing progestogennoe funds or modulator of the progesterone receptor, for example, ulipristal-acetate or its metabolite is administered twice or more during mestruale cycle.

In any case, the woman always applies progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, as needed, not on a daily basis, and preferably not more than ten consecutive days, preferably not more than nine, eight, seven, six, five, four, three or two days in a row. Preferably progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, do not enter more than four days, three or two days in a row.

Route of administration

Progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, may be introduced by any convenient means, including oral, buccal, sublingual, parenteral, transdermal, vaginal, rectal and so forth.

For a brief discussion of the methods of the present invention in relation to the delivery of the medicinal product, see publication Langer, Science 249:1527-1533 (1990), which is incorporated in this document by reference. Methods of obtaining input connections known or obvious to a person skilled in this field and are described in more detail, for example, in the book Remington''s Pharmaceutical Science, 17th Ed., Mack Publishing ompany has, Easton, Pa. (1985), which is incorporated in this document by reference and which further in this document referred to as the "Remington".

Disposable standard dosage of the compositions of the instant release are preferred.

For solid compositions can be used commonly used non-toxic solid carriers include, for example, pharmaceutical grade mannitol, lactose, starch, magnesium stearate, saccharin sodium, talc, cellulose, glucose, sucrose. For oral administration of pharmaceutically acceptable non-toxic composition is obtained by implementation of any of the commonly used excipients, such as those carriers listed above.

Oral solid dosage forms preferably are extruded tablets or capsules. Molded tablets may contain diluents to increase progestogennoe funds or progesterone receptor modulator, in order to be able to produce the pressed tablet of practicable size. Binders, which are substances that impart cohesive properties of powder substances may also be necessary. Can be used povidone, starch, gelatin, sugars such as lactose or dextrose, natural and synthetic grass is e gum. Leavening agents, as a rule, are necessary in tablets to facilitate raspadaemosti tablets. Leavening agents include starches, clays, cellulose, algina, gum and crosslinked polymers. Finally, small amounts of substances called as sliding substances and regulators flowability (glidant) include tablets to prevent adhesion of the material of the tablet to the surfaces in the process and to improve the characteristics of flowability of the powder material during manufacture. Colloidal silicon dioxide is most often used as a control flowability, and compounds such as talc, magnesium stearate or stearic acid are most commonly used as sliding materials. The method and manufacture of compressed tablets are well known to specialists in this field (see Remington).

Capsules are solid dosage forms in which preferably is either hard or soft gelatin shell as a container for the mixture progestogennoe funds or progesterone receptor modulator and inert ingredients. The method and manufacture of hard gelatin and soft elastic capsules are well known to specialists in this field (see Remington).

Buccal or sublingual form or device is and are useful.

For injecting liquid standard dosage forms prepared using the compounds and sterile environment for drugs where the water is preferred. Progestogen tool or progesterone receptor modulator, depending on the environment for a drug and concentration, can be either suspended or dissolved in the medium for drugs. In preparing solutions the compound can be dissolved in water for injection and subjected to filtration and sterilized before filling into a suitable vial or ampoule and sealing. Mainly auxiliary means, such as a local anesthetic, preservative and substances that contribute to the formation of the buffer solution may be dissolved in the medium for drugs. To enhance the stability of the composition can be frozen after being filled in a test tube, and the water can be removed under vacuum. Dry liofilizovannye powder is then sealed in the vial and set it put an extra tube with water for injection to recovery of liquid (solution, suspension) before use. Parenteral suspensions can be prepared almost the same way except that the compounds are suspended in the environment for a drug smestorage, to be dissolved and sterilization cannot be accomplished by filtration. The connection can be sterilized by exposure to ethylene oxide before suspendirovanie in a sterile environment for medicines. Mainly in the composition include a surfactant or wetting agent to facilitate homogeneous distribution progestogennoe funds or progesterone receptor modulator.

In addition, for delivery progestogennoe funds or progesterone receptor modulator can be applied suppository or pessary. The active connection can be implemented in any of the known bases for suppositories known in the field of ways. Examples of such bases include cocoa butter, polyethylene glycol (carbowax), polyethylenterephthalat and mixtures of these compounds with other compatible substances for modifying the temperature of melting or dissolution rate. These suppositories can weigh from about 1 to 2.5 grams.

Transdermal delivery system, comprising a substance that promotes infiltration, and sealed the basis of transdermal systems are used to deliver progestogennoe funds or progesterone receptor modulator. Examples of substances that promote infiltration include dimethylsulfoxide, dim tileceramic and dimethylformamide. Percutaneous gels can be pre-emptive, too. Examples of such gels are described, for example, in U. S. patent Patent 5904931.

Progestogen tool or progesterone receptor modulator can be entered by vaginal, for example in the form of a gel or vaginal device.

In another embodiment, the method of the invention includes an introduction, as necessary, vaginal device, such as a contraceptive vaginal ring that releases progestogen tool or progesterone receptor modulator, woman within 24 hours before or after sex.

Contraceptive vaginal ring typically contains a synthetic polymer, which may be a silicone elastomer or asilicone resin. In a particular embodiment, the ring contains a polymer core surrounded by outer polymeric layer containing progestogen tool or modulator of the progesterone receptor. In a particular embodiment, the ring is the same as the ring, described in international patent application WO 2006/010097.

Preferably contraceptive vaginal ring is removed within 12 hours after sex. Most preferably contraceptive vaginal ring is left in place for at least 6-12 hours.

Oral path I which is preferred. In comparison with oral routes other routes of administration may be appropriate with the use of blood levels to ensure clinical success.

Dosage

Disposable standard dosage progestogennoe funds or progesterone receptor modulator, for example ulipristal-acetate or its metabolite, may be between 10 and 40 mg, preferably 20 mg or 30 mg, Preferably disposable standard dosage progestogennoe funds or progesterone receptor modulator, for example ulipristal-acetate or its metabolite, is a dosage, which should be administered orally.

Mode dose

In the first embodiment of the invention, progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, may be entered within 72 hours prior to sexual contact, preferably within 48 hours prior to sexual contact, more preferably within 24 hours prior to sexual contact, even more preferably within 12 hours before sexual contact.

In the second embodiment of the invention, progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, may be entered within 120 hours after intercourse, predpochtitel what about within 72 hours after intercourse, more preferably within 48 hours after sex, even more preferably within 24 hours after intercourse, even more preferably within 12 hours after sex.

In a preferred embodiment, the introduction perform again, at least twice a month, preferably three times a month or once a week.

To achieve optimum efficiency two options for implementation may be combined, i.e. progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, may be entered within 72 hours prior to sexual contact, and the same woman can also take progestogen tool or progesterone receptor modulator, for example ulipristal-acetate and its metabolite, within 120 hours after intercourse.

The following example is provided only to illustrate and not to limit.

Example: Repeated ingestion ulipristal-acetate within the menstrual cycle

Several women received ulipristal-acetate (30 mg) after stated sexual contact, twice during the menstrual cycle.

Pregnancy was not recorded.

Patient 1threception2threception
Woman 1Sex: December 11, 2007, 06:00*
Welcome Ulipristal-acetate: December 13, 2007 11:25
Sex: December 14, 2007, 21:00
Welcome Ulipristal-acetate: December 14, 2007 14:37
Woman 2Sex: December 12, 2007, 05:00
Welcome Ulipristal-acetate: December 14, 2007 11:05
Sex: December 15, 2007 23:00
Welcome Ulipristal-acetate: December 18, 2007 10:45
Woman 3Sex: December 15, 2007 06:00
Welcome Ulipristal-acetate: December 17, 2007 11:40
Sex: December 15, 2007, 22:00
Welcome Ulipristal-acetate: December 18, 2007 11:15
Woman 4Sex: December 14, 2007 01:00
Welcome Ulipristal-acetate: December 17, 2007 12:20
Sex: 07 December, 2007 20:00
Welcome Ulipristal-acetate: December 12, 2007 10:58
Woman 5Sex: November 5, 2007 06:00
Welcome Ulipristal-acetate: 08 November, 2007,
15:30
Gender is th contact: November 2, 2007 08:00
Welcome Ulipristal-acetate: November 5, 2007
15:00
*time is expressed in 24-hour format

1. Method of contraception, including oral administration ulipristal-acetate or its metabolite woman through more than 72 hours and up to 120 hours after sex in an amount of from 20 to 30 mg.

2. The method according to p. 1, where the method is performed repeatedly at least twice a month.

3. The method according to p. 1, where ulipristal-acetate or its metabolite is administered in a dosage of 30 mg

4. The method according to p. 1, where ulipristal-acetate or its metabolite is administered at a dose of 20 mg.

5. The method according to p. 1, where ulipristal-acetate or its metabolite is administered in a form with immediate release.

6. The method according to p. 1, where ulipristal-acetate or its metabolite is administered in tablet form.

7. The method according to p. 1, where the method is a method of emergency contraception.



 

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5 cl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and represents a controlled-release aceclofenac preparation for oral administration once a day, exhibiting the fast analgesic and anti-inflammatory action, containing a fast-release layer containing aceclofenac, a solubiliser, a water-soluble additive, a disintegrating agent, a vehicle and a fast-acting additive, as well as a sustained-release layer containing aceclofenac, a solubiliser and a release control base consisting of mixture of hydroxypropyl methyl cellulose (HPMC) with a viscosity of 80,000 sP to 120,000 sP and carbomer taken in mass ratio 7:1 to 9:1.

EFFECT: invention provides a sequential and uniform dissolution rate and a controlled release of the active agent.

7 cl, 12 tbl, 11 dwg, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a prolonged-release pharmaceutical composition containing entacapone, consisting of an immediate-release layer and a prolonged-release layer.

EFFECT: composition provides the prolonged release of the therapeutic agent, its uniform blood plasma concentration and lower rate of composition intake.

11 cl, 11 ex, 23 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, chemical-pharmaceutical industry and concerns agents possessing the nootropic and neuromodulatory activity. A tabletted pharmaceutical composition possessingthe nootropic and neuromodulatory activity, characterised by the fact that as an active substance, it contains N-cabamoylmethyl-4-phenyl-2-pyrrolidone; the additives are lactose monohydrate, microcrystalline cellulose, sodium croscarmellose, colloidal silicon dioxide (aerosil) and calcium stearate. The tablets of the composition are prepared by direct compression.

EFFECT: produced preparation has a lower variability of the pharmacological action.

3 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for treating gastroduodenal ulcer in the form of tablets, capsules or gel, containing therapeutic agents and a consistency base applicable for each dosage, wherein the therapeutic agents are as follows: recombinant interferon specified in a group: recombinant interferon alpha, recombinant interferon beta, recombinant interferon gamma; antiseptics; amino acids specified in a group: arginine, histidine, lysine, cysteine, methionine, glutamic acid; and antioxidants specified in a group: beta-carotene, vitamin C, vitamin E.

EFFECT: invention has the integrated body effect promoting faster healing of the mucosal defect accompanying the aggravated gastroduodenal ulcer and preventing recurrences, including by the eradication effect.

6 cl, 5 ex

Enterosorbent // 2538669

FIELD: chemistry.

SUBSTANCE: invention represents enterosorbent in form of pill, which contains colloidal silicon dioxide, microcrystal cellulose, dextrose, sodium croscarmellose, pharmaceutical talc and magnesium stearate, and components in enterosorbent are in specified ratio in wt %.

EFFECT: increase of sorption capacity and considerable reduction of production process due to reduction of granulate drying operation.

2 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a tabletted multiunit dosage form containing an active substance specified in a compound of N+K+ATPhase inhibitor, one its individual enantiomer and its alkaline salt, wherein individually enteric-coated units of a nuclear material containing the active substance optionally mixed with alkaline compounds, is mixed with tablet excipients and tabletted. The enteric coating is at least 10 mcm thick and has such mechanical properties that tabletting the individual units mixed with the excipients in the multiunit tabletted dosage form does not reduce the acid stability of the enteric coated units by more than 10%. The invention also refers to a method for preparing the multiunit dosage form, according to which the material units containing the active substance are mixed whenever necessary with the alkaline compounds; then these can be coated with separate layers; the enteric coating is applied, mixed with the excipients and tabletted.

EFFECT: what is declared is a method for inhibiting gastric acid secretion or treating gastrointestinal diseases in mammals and humans by administering a therapeutically effective dose of the multiunit tabletted dosage form.

17 cl, 2 tbl, 19 ex

FIELD: medicine.

SUBSTANCE: invention represents a method for preparing a drug substance of polyprenylphosphates and beta-sitosterol consisting in pre-mixing polyprenylphosphates and sorbitol in a mortar, a size of which fits the total volume of the mixed substances. Between a wall and/or a bottom of the mortar and the introduced polyprenylphosphates, there is a layer of sorbitol; the blended mixture of the polyprenylphosphates in sorbitol is homogenised. Sorbitol, a dry mixture of polyprenylphosphates in sorbitol in a ratio of 1:8 and beta-sitosterol are added into a homogeniser, and pulsed homogenisation is performed for 10 minutes. The homogenisation is performed at a rotation rate of 500-700 rpm for 4 minutes, 1000-1200 rpm for 2 minutes and then 500-600 rpm for 4 minutes; the rotation rate variation requires a pause of 20 minutes. Each pause of the process is followed by the intensive agitation of a mixture cup; the prepared powder is sieved at a mesh size of 20 mcm; if a sieving weight makes less than 0.1% of the weight of the loaded ingredients; the homogenisation process is terminated.

EFFECT: preparing the drug substance with the maximum effective concentration of the active substances uniformly weight-distributed and higher bioavailability.

3 cl, 2 ex, 1 tbl, 7 dwg

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