20 results about "Drospirenone" patented technology

The present invention relates to a composition comprising an estetrol component and drospirenone for use in treating unscheduled bleeding and spotting in an adolescent female subject. The invention also encompasses associated uses and methods of contraception as well as improving health-related quality of life and alleviating menstrual symptoms in adolescent subjects.

The present invention relates to a combined oral contraceptive having a beneficial effect on blood pressure, to the associated compositions, dosage units, and packaging units thereof. Particularly, the present invention concerns the use of a composition comprising from about 1 mg to about 40 mg of estetrol and from about 0.5 mg to about 10 mg of drospirenone and which, during use, has a favorable effect on blood pressure.

This invention relates to methods for treating endometriosis and providing effective contraception. Specifically, it relates to drospirenone in methods for treating endometriosis, endometriosis-associated pelvic pain (EAPP), and / or dysmenorrhea, the method comprising administering drospirenone in a biphasic regimen. The invention also relates to the use of drospirenone administered in such a biphasic regimen as a contraceptive and for inducing amenorrhea, and to pharmaceutical compositions and devices comprising drospirenone administered in such a biphasic regimen.

This invention discloses the application of ethinylestradiol and drospirenone in the preparation of drugs for treating post-traumatic stress disorder (PTSD). Ethinylestradiol, as an estrogen receptor agonist, regulates the hypothalamic-pituitary-gonadal axis and is used to treat female hypogonadism, menopausal syndrome, and advanced breast cancer, often in combination with progestins as oral contraceptives. The use of drospirenone and ethinylestradiol tablets (II) after induced abortion can shorten vaginal bleeding time, promote endometrial repair, and reduce the incidence of postoperative complications and repeat miscarriages. This invention has found that ethinylestradiol and drospirenone can reverse the abnormal decrease in hormones and neurosteroids caused by PTSD after spontaneous abortion, particularly the abnormal decrease in serotonin and tetrahydroprogesterone.

The present invention pertains to the field of oral pharmaceutical compositions and their use for providing contraception. More specifically, the present invention relates to oral chewable tablets of drospirenone, their use for providing contraception to an individual and a kit comprising daily dosage units of such oral chewable tablets.

The present invention relates to a pharmaceutical composition comprising estetrol and drospirenone for use in relieving pain associated with endometriosis in a patient. The pharmaceutical compositions described in the present invention are particularly effective in relieving pain associated with endometriosis in patients having high levels, frequencies and / or intensities of pain, e.g., measured by visual analog scale (VAS) scoring, and / or with other complications such as adenomyosis or hysteromyoma. Uses related to the above and corresponding methods of treatment are also described.

Use of drospirenone in an amount of at least 3 mg contained in a daily active dosage unit as the sole contraceptive ingredient as a contraceptive for obese female patients.

The present invention relates to drospirenone for use in a method for treating endometriosis, endometriosis associated pelvic pain (EAPP) and / or dysmenorrhea, comprising administering drospirenone in a biphasic regimen. The present invention furthermore relates to the use of drospirenone administered in such a biphasic regimen as a contraceptive and for inducing amenorrhea, as well as to a pharmaceutical composition and a kit comprising drospirenone administered in such a biphasic regimen.

Described are methods of providing contraception in a woman having a BMI ≥30.0 kg / m2, comprising: selecting a woman determined to have a BMI ≥30.0 kg / m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg. Also described are methods of contraception that achieves a Pearl Index of <5 in women having a BMI ≥30.0 kg / m2, comprising: selecting a woman determined to have a BMI ≥30.0 kg / m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg, wherein the method comprises daily administration of the estetrol component and drospirenone on 24 consecutive days followed by a hormone-free period of 4 consecutive day.

The invention discloses a preparation method of liposome / cellulose hydrogel carrying a large amount of water-soluble drospirenone, and belongs to the field of drospirenone solubilization and slow release application. The method comprises the following steps: 1, preparing drospirenone liposome by adopting an ethanol injection method: weighing soybean lecithin, drospirenone and cholesterol, adding an absolute ethanol solution, dissolving in a water bath at 30 DEG C to form an oil phase, injecting the oil phase into PBS (Phosphate Buffer Solution), and stirring in a water bath; 2, hydroxyethyl cellulose is dissolved in distilled water, a NaOH solution and C3H5ClO are added, sealing and stirring are conducted, and standing and crosslinking are conducted; and washing the sample to remove excessive alkali and cross-linking agent. And freeze-drying to obtain dry hydrogel, putting the dry hydrogel into the liposome supernatant, and completely absorbing to obtain the drospirenone liposome hydrogel. The problem of poor water solubility of drospirenone is solved by adopting a liposome solubilization method, and the problem of poor stability of high-drug-loading drospirenone / liposome is solved through hydrogel immobilization. After the preparation process is optimized, the maximum encapsulation efficiency of the drospirenone liposome reaches 80-85%, and the drug delivery system can realize long-acting release.

The present invention refers to a process for the industrial-scale preparation of 17β-hydroxy-6β,7β; 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone, known by the common name of Drospirenone, in the form of a fine powder without the use of mechanical grinding or micronization techniques, but rather exploiting a double change of crystalline form, from Crystalline Form I to Crystalline Form II and from Crystalline Form II to Crystalline Form I. The invention also refers to the new Crystalline Form II of Drospirenone obtained in the process.

The present invention relates to a combined oral contraceptive having a beneficial effect on blood pressure, to the associated compositions, dosage units, and packaging units thereof. Particularly, the present invention concerns the use of a composition comprising from about 1 mg to about 40 mg of estetrol and from about 0.5 mg to about 10 mg of drospirenone and which, during use, has a favorable effect on blood pressure.

The present application relates to the field of pharmaceutical analysis method, specifically relates to a kind of detection method of related substance in drospirenone ethinylestradiol tablet (II).The method can simultaneously determine drospirenone ethinylestradiol tablet (II) drospirenone, ethinylestradiol and 13 kinds of related substances, method specificity is strong, sensitivity is high, suitable for drospirenone ethinylestradiol tablet (II) Process research, intermediate process control, finished product quality detection and stability research.

The invention provides application of blood nourishing oral liquid combined with drospirenone ethinylestradiol in clinical symptoms and endometrial receptivity after an induced abortion operation, and belongs to the technical field of biological medicine. According to the application of the blood nourishing oral liquid and the drospirenone ethinylestradiol in preparation of the medicine for improving the clinical symptoms after the induced abortion operation, the result of the embodiment shows that compared with a drospirenone ethinylestradiol single administration group, the combined administration group has the advantages that the vaginal bleeding duration is shorter, the vaginal bleeding amount is smaller, the abdominal pain degree is lower, and the clinical symptoms after the induced abortion operation can be improved. The dominant follicle size, the endometrial thickness, the endometrial volume, the type A endometrial rate, the type III endometrial and the ratio of the endometrial-muscular layer binding band are all higher than those of a control group, and the aneurysm hemodynamic indexes are all lower than those of a single administration group. Therefore, the blood-nourishing oral liquid combined with drospirenone ethinylestradiol can effectively improve postoperative clinical symptoms of patients, promote follicle development and improve endometrial receptivity.

Described are methods of providing contraception in a woman having a BMI≥30.0 kg / m2, comprising: selecting a woman determined to have a BMI≥30.0 kg / m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg. Also described are methods of contraception that achieves a Pearl Index of <5 in women having a BMI≥30.0 kg / m2, comprising: selecting a woman determined to have a BMI≥30.0 kg / m2, and then orally administering to the selected woman a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg, wherein the method comprises daily administration of the estetrol component and drospirenone on 24 consecutive days followed by a hormone-free period of 4 consecutive days.

Described are methods of providing contraception with increased likelihood of scheduled bleeding in a woman having a BMI<30.0 kg / m2 and methods of providing contraception with reduced likelihood of scheduled bleeding in a woman having a BMI≥30.0 kg / m2. The methods comprise orally administering a therapeutically effective amount of an estetrol component at a daily dose of from 14 mg to 16 mg, based on the estetrol moiety, and drospirenone at a daily dose of from 2.5 mg to 3.5 mg. Also provided are compositions comprising an estetrol component and drospirenone for use in such methods.

The present invention relates to drospirenone for use in a method for treating endometriosis, endometriosis associated pelvic pain (EAPP) and / or dysmenorrhea, comprising administering drospirenone in a biphasic regimen. The present invention furthermore relates to the use of drospirenone administered in such a biphasic regimen as a contraceptive and for inducing amenorrhea, as well as to a pharmaceutical composition and a kit comprising drospirenone administered in such a biphasic regimen.

The invention relates to the technical field of synthesis, and discloses a synthesis method of a drospirenone EP impurity E. The method comprises the following steps: adding a compound I, vinylboronic acid pinacol ester, stannic chloride and chiral diol into a first organic solvent, reacting for a first time at a first temperature, extracting, drying, and carrying out column chromatography separation to obtain a compound II; dissolving the compound II in a second organic solvent, adding acetic anhydride, a palladium catalyst and a catalyst ligand, replacing and introducing carbon dioxide, stirring and reacting for a second time at a second temperature, and performing extraction, drying and column chromatography separation to obtain a compound III; and dissolving the compound III in a third organic solvent, adding a condensing agent, carrying out a stirring reaction at a third temperature for a fourth period of time, and carrying out extraction, drying and column chromatography separation to obtain the compound 17R-Drospirenone. In the embodiment of the invention, the synthesis route of the drospirenone EP impurity E is short, the yield is high, and the synthesis cost of the drospirenone EP impurity E is effectively reduced.

The present invention refers to a process for the industrial-scale preparation of 17β-hydroxy- 6β,7β;15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid y-lactone, known by the common name of

The present invention relates to drospirenone for use in a method for treating endometriosis, endometriosis associated pelvic pain (EAPP) and / or dysmenorrhea, comprising administering drospirenone in a biphasic regimen. The present invention furthermore relates to the use of drospirenone administered in such a biphasic regimen as a contraceptive and for inducing amenorrhea, as well as to a pharmaceutical composition and a kit comprising drospirenone administered in such a biphasic regimen.