Claims (15)
1. Kontracepcijski komplet koji sadrži jednu ili više ambalažnih jedinica gdje svaka ambalažna jedinica sadrži 21 do 28 dnevnih aktivnih jedinica doziranja i gdje
(a) količina drospirenona u svakoj dnevnoj jedinici aktivne doze iznosi najmanje 2 mg, bez estrogena i
(b) svaka dnevno aktivna dozna jedinica sastoji se od kontracepcijskog pripravka pogodnog za oralnu primjenu, koji sadrži drospirenon, pri čemu drospirenon ima veličinu čestica d50 od 10 µm do 60 µm, tako da:
(i) više od 50% drospirenona koji je u početku prisutan u navedenoj dnevnoj jedinici za doziranje rastopi se u roku od 30 minuta i
(ii) najmanje 50% spomenutog drospirenona je otopljeno u vremenskom rasponu od 3 sata do 4 sata,
kada se dnevna aktivna jedinica doziranja podvrgava in vitro ispitivanju otapanja, prema USP XXIII Paddle metodi, u postocima drospirenona odnosi se na količinu drospirenona koja je u početku prisutna u navedenoj jedinici dnevnog aktivnog doziranja. 1. A contraceptive kit containing one or more packaging units where each packaging unit contains 21 to 28 daily active dosage units and where
(a) the amount of drospirenone in each daily unit of the active dose is at least 2 mg, without estrogen and
(b) each daily active dosage unit consists of a contraceptive preparation suitable for oral administration, containing drospirenone, wherein drospirenone has a particle size d50 of 10 µm to 60 µm, so that:
(i) more than 50% of the drospirenone initially present in said daily dosage unit dissolves within 30 minutes and
(ii) at least 50% of said drospirenone is dissolved in a time span of 3 hours to 4 hours,
when the daily active dosage unit is subjected to an in vitro dissolution test, according to the USP XXIII Paddle method, the percentage of drospirenone refers to the amount of drospirenone that is initially present in the stated daily active dosage unit.
2. Komplet za kontracepciju prema zahtjevu 1, naznačen time, da drospirenon ima raspodjelu veličine čestica koja je naznačena time što:
(i) veličina čestica d90 manja od 100 µm;
(ii) d50 veličine čestica u rasponu od 10 µm do 60 µm; i
(iii) veličina čestica d10 veća od 3 µm.2. The contraceptive kit according to claim 1, characterized in that the drospirenone has a particle size distribution characterized in that:
(i) particle size d90 less than 100 µm;
(ii) d50 particle size ranging from 10 µm to 60 µm; and
(iii) particle size d10 greater than 3 µm.
3. Komplet za kontracepciju prema bilo kojem od zahtjeva 1 ili 2, naznačen time, da je drospirenon jedini kontracepcijski sastojak.3. A contraceptive kit according to any one of claims 1 or 2, characterized in that drospirenone is the only contraceptive ingredient.
4. Komplet za kontracepciju prema bilo kojem od zahtjeva 1 do 3, naznačen time, da se količina drospirenona u svakoj dnevnoj jedinici doze kreće u rasponu od oko 2.0 mg do oko 6.0 mg, poželjno od oko 3.0 mg do otprilike 4.5 mg, poželjnije oko 4 mg.4. The contraceptive kit according to any one of claims 1 to 3, characterized in that the amount of drospirenone in each daily dosage unit ranges from about 2.0 mg to about 6.0 mg, preferably from about 3.0 mg to about 4.5 mg, more preferably about 4 mg.
5. Komplet za kontracepciju prema bilo kojem od zahtjeva 1 do 4, naznačen time da jedna ili više ambalažnih jedinica nadalje sadrži 1 do 7 dnevnih jedinica doziranja farmaceutski prihvatljivog placeba.5. The contraceptive kit according to any one of claims 1 to 4, characterized in that one or more packaging units further contain 1 to 7 daily dosage units of a pharmaceutically acceptable placebo.
6. Komplet za kontracepciju prema bilo kojem od zahtjeva 1 do 5, naznačen time što svaka ambalažna jedinica sadrži 24 jedinice aktivne doze dnevno.6. A contraceptive kit according to any one of claims 1 to 5, characterized in that each packaging unit contains 24 units of active dose per day.
7. Komplet za kontracepciju prema zahtjevu 6, naznačen time, da nadalje obuhvaća 4 dnevne jedinice doze placeba.7. The contraceptive kit according to claim 6, characterized in that it further comprises 4 daily units of the placebo dose.
8. Kontracepcijski komplet prema bilo kojem od zahtjeva 1 do 7, naznačen time, da navedeni kontracepcijski pripravak sadrži:
- drospirenon u količini koja iznosi 1% do 10% težine,
- barem jedno vezivo koje ima 50 do 65 % težine,
- barem jedno punilo koje čini 25% do 35% težine,
- najmanje jednog glidanta koji ima 0.2% do 6% težine, i
- barem jedno mazivo koje ima težinu od 0.2 do 0.6 % težine koji su povezani s ukupnom masom navedenog kontracepcijskog pripravka.8. Contraceptive kit according to any one of claims 1 to 7, characterized in that said contraceptive preparation contains:
- drospirenone in an amount of 1% to 10% by weight,
- at least one binder that is 50 to 65% by weight,
- at least one filler that makes up 25% to 35% of the weight,
- at least one glider that has 0.2% to 6% of the weight, and
- at least one lubricant that has a weight of 0.2 to 0.6% of the weight associated with the total mass of the said contraceptive preparation.
9. Komplet za kontracepciju prema bilo kojem od zahtjeva 1 do 8, naznačen time, da navedeni kontracepcijski pripravak sadrži drospirenon, najmanje jedno vezivo, najmanje jedno punilo, najmanje jedno sredstvo za klizanje i najmanje jedno mazivo, pri čemu:
(i) najmanje jedno vezivo je mikrokristalna celuloza,
(ii) najmanje jedno punilo je bezvodna laktoza,
(iii) najmanje jedno sredstvo za klizanje je silicijev dioksid i
(iv) najmanje jedno mazivo je magnezijev stearat.9. A contraceptive kit according to any one of claims 1 to 8, characterized in that said contraceptive preparation contains drospirenone, at least one binder, at least one filler, at least one lubricant and at least one lubricant, wherein:
(i) at least one binder is microcrystalline cellulose,
(ii) at least one filler is anhydrous lactose,
(iii) at least one slip agent is silicon dioxide and
(iv) at least one lubricant is magnesium stearate.
10. Farmaceutski pripravak pogodan za oralnu primjenu, naznačen time da sadrži drospirenon, naznačen time, da:
(a) dnevna aktivna dozna jedinica navedenog pripravka sadrži količinu drospirenona od najmanje 2 mg, bez estrogena i
(b) navedena jedinica aktivne doze sadrži drospirenon, a drospirenon ima veličinu čestica d50 u rasponu od 10 µm do 60 µm, tako da:
(i) više od 50% drospirenona koji je u početku prisutan u navedenoj dnevnoj jedinici za doziranje rastopi se u roku od 30 minuta, i
(ii) najmanje 50% spomenutog drospirenona je otopljeno u vremenskom rasponu od 3 sata do 4 sata,
kada se dnevna aktivna jedinica doziranja podvrgava in vitro ispitivanju otapanja, prema USP XXIII Paddle metodi, u postocima drospirenona se odnosi na količinu drospirenona koja je prvobitno prisutna u navedenoj jedinici dnevnog aktivnog doziranja,
za upotrebu kao kontraceptiva za pacijenticu kojoj je potrebna.10. Pharmaceutical preparation suitable for oral administration, characterized in that it contains drospirenone, characterized in that:
(a) the daily active dosage unit of the said preparation contains an amount of drospirenone of at least 2 mg, without estrogen and
(b) the specified active dose unit contains drospirenone, and drospirenone has a particle size d50 in the range of 10 µm to 60 µm, so that:
(i) more than 50% of the drospirenone initially present in said daily dosage unit dissolves within 30 minutes, and
(ii) at least 50% of said drospirenone is dissolved in a time span of 3 hours to 4 hours,
when the daily active dosage unit is subjected to an in vitro dissolution test, according to the USP XXIII Paddle method, the percentage of drospirenone refers to the amount of drospirenone originally present in the specified daily active dosage unit,
for use as a contraceptive for a patient in need.
11. Farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 10, naznačen time što je navedeni pripravak definiran u bilo kojem od zahtjeva 1 do 4, 8 ili 9.11. Pharmaceutical preparation for use in accordance with claim 10, characterized in that said preparation is defined in any of claims 1 to 4, 8 or 9.
12. Farmaceutski pripravak za uporabu u skladu s bilo kojim od patentnih zahtjeva 10 ili 11, naznačen time što se jedinice dnevne doze pripravka primjenjuju navedenom pacijentu tijekom perioda od 21 do 28 uzastopnih dana.12. A pharmaceutical preparation for use in accordance with any of claims 10 or 11, characterized in that the daily dose units of the preparation are administered to said patient during a period of 21 to 28 consecutive days.
13. Farmaceutski pripravak za uporabu prema bilo kojem od zahtjeva 10 do 12, naznačen time, da se jedinice za dnevno doziranje smjese primjenjuju u dvije faze:
prva faza u kojoj se aktivne jedinice za dnevno doziranje daju pacijentu tijekom perioda od 21 do 27 uzastopnih dana, nakon čega slijedi
druga faza u kojoj se kontracepcijsko sredstvo ne daje ženskom pacijentu tijekom razdoblja od 1 do 7 uzastopnih dana.13. Pharmaceutical preparation for use according to any one of claims 10 to 12, characterized in that the daily dosage units of the mixture are applied in two phases:
the first phase in which the active daily dosage units are administered to the patient over a period of 21 to 27 consecutive days, followed by
the second phase in which the contraceptive is not administered to the female patient for a period of 1 to 7 consecutive days.
14. Farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 13, naznačen time, da se tijekom navedene druge faze svakodnevno primjenjuju placebo dozne jedinice.14. Pharmaceutical preparation for use in accordance with claim 13, characterized in that placebo dosage units are administered daily during the second phase.
15. Farmaceutski pripravak za uporabu prema bilo kojem od zahtjeva 13 ili 14, naznačen time, da prva faza traje 24 uzastopna dana, a druga faza traje 4 uzastopna dana.15. Pharmaceutical preparation for use according to any one of claims 13 or 14, characterized in that the first phase lasts for 24 consecutive days and the second phase lasts for 4 consecutive days.