30 results about "Norethisterone" patented technology

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

A multiphasic method of contraception comprising the steps of sequentially administering to a female of child bearing age a Phase I composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 15 mcg of ethinyl estradiol for about 7 to about 14 days; a Phase II composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 10 to about 25 mcg of ethinyl estradiol for about 14 to about 22 days; a Phase III composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 15 to about 35 mcg of ethinyl estradiol for about 20 to about 31 days; and an optional Phase IV composition containing (i) an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol, or (ii) a placebo or a non-steroidal component, or (iii) a combination of (i) and (ii), for about 2 to about 8 days. The ethinyl estradiol equivalent amount of estrogen in each of the successive Phases II and III is at least 5 mcg greater than the ethinyl estradiol equivalent amount of estrogen in the immediately-preceding phase.

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

A multiphasic method of contraception comprising the steps of sequentially administering to a female of child bearing age a Phase I composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 15 mcg of ethinyl estradiol for about 7 to about 14 days; a Phase II composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 10 to about 25 mcg of ethinyl estradiol for about 14 to about 22 days; a Phase III composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 15 to about 35 mcg of ethinyl estradiol for about 20 to about 31 days; and an optional Phase IV composition containing (i) an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol, or (ii) a placebo or a non-steroidal component, or (iii) a combination of (i) and (ii), for about 2 to about 8 days. The ethinyl estradiol equivalent amount of estrogen in each of the successive Phases II and III is at least 5 mcg greater than the ethinyl estradiol equivalent amount of estrogen in the immediately-preceding phase.

A method of contraception that provides for sequentially administering to a female of child bearing age: (a) a first composition containing a progestin in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol for about 22 to about 26 days; (b) a second composition containing an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol for about 2 to about 3 days and an optional third composition that is a placebo provided that (i) if estrogen administration is continuous then the first composition is administered for 25 to 26 days, the second composition is administered for 2 to 3 days and no third composition is administered and (ii) if estrogen administration is not continuous then the first composition is administered for 22 to 24 days, the second composition is administered for 2 to 3 days and the third composition is administered for 1 to 4 days. The total cycle length is 28 days, with the first composition administered on day 1 of the menstrual cycle, defined as the first day of menstrual bleeding, or on the first Sunday after the first day of the menstrual cycle.

A formulation for male contraception comprising a progestin possessing both estrogenic and androgenic properties is remarkably effective for spermatogenesis suppression in males. The progestin Norethisterone (NET), particularly its derivatives Norethisterone acetate and Norethisterone enanthate in sufficient doses induce oligozoospermia or azoospermia in males. Formulations further comprising an androgen, such as a testosterone derivative such as a testosterone ester, particularly testosterone undecanoate, are especially effective male contraceptive formulations.

The invention relates to the field of pharmaceutical synthesis, in particular to a method for synthesizing 6-methyl-17alpha- hydroxyl-19-nor-pregnene-4,6-diene-3,20-diketone. The method comprises the steps of reacting norethisterone with ethylorthoformate to obtain 3-ethoxy-17alpha-acetenyl-19-demethyl-pregnene-3,5-diene-17beta-alcohol (2); causing the compound (2) to undergo Vilsmeier reaction to obtain 3-ethoxy-6-formoxyl-17alpha-acetenyl-19- demethyl-pregnene-3,5-diene-17beta-alcohol (3); reacting the compound (3) with NaBH4 and obtaining 6-methine-17alpha-acetenyl-17beta-hydroxyl-19-demethyl-pregnene-4-en-3-ketone (4) through acidification and dehydration; causing the compound (4) to undergo double bond shift under the effect of Pd-C / cyclohexene to obtain a product 6-methyl-17alpha-acetenyl-17beta-hydroxyl-19-demethyl-pregnene-4,6-diene-3-ketone (5); and reacting the compound (5) with benzene sulfenyl chloride to obtain 6-methyl-19-demethyl-21-phenylsulfinyl-pregnene-4,6,17(20)20-tetraene-3-ketone.

The invention relates to an impurity analysis method of a steroid compound, and especially relates to an impurity detection analysis method of norethisterone derivatives and intermediates thereof. The method comprises the following steps: (1) a chromatographic column with octadecylsilane chemically bonded silica as a filler is selected; a mobile phase gradient elution is carried out, and the mobile phase contains water, methanol and acetonitrile; the detection wavelength is 230-254nm; and (2) a proper amount of the test sample norethisterone derivatives or intermediates thereof are selected, methanol is precisely weighed for dissolving and diluting the test sample to form a sample solution of a certain concentration, the solution is uniformly shaken, and a high performance liquid chromatography analysis is carried out at a proper flow velocity and a proper column temperature, in order to record a chromatogram. The method can be used for rapidly and accurately realizing impurity analysis of norethisterone derivatives, and is especially suitable for the impurity analysis of norethisterone enanthate, and simultaneously can be used for impurity analysis of norethisterone derivative intermediates, and can be used for effectively tracing impurities generated in the synthesis process.

The invention discloses an application of an ER and Ki-67 expression ratio in endometrial tissues in fertility function retention treatment prognosis of endometrial cancer (EC) and atypical endometrial hyperplasia (AH). According to the invention, 53 EC patients and 68 AH patients orally take MPA or MA, then gonadotropin is combined to release a hormone agonist and / or a levoynorethindrone intrauterine sustained release system, the patients are divided into a recurrence group and a non-recurrence group according to whether recurrence occurs after complete remission, then ER, PR, P16, P53, PTEN, Ki-67 and the like are subjected to immunohistochemical analysis, and statistical analysis is carried out. Results show that the expression rate of the Ki-67 is of great significance in predicting recurrence after the EC and AH retention fertility function treatment, and the optimal critical value (3.55) of ER / Ki-67 can predict recurrence after the EC and AH retention fertility function treatment better than that of a single immunohistochemical marker. The method has an important application value.

The present invention discloses a method of detecting norethisterone and a special enzyme linked immunosorbent kit thereof. The enzyme linked immunosorbent kit which is used for detecting the norethisterone comprises norethisterone haptens and specific antibodies of the norethisterone; and the specific antibodies are polyclonal antibodies or monoclonal antibodies of the norethisterone. The kit adopts the high specificity monoclonal antibodies of the norethisterone, which guarantees the reliability of detection results, and the experimental results show that the kit has the characteristics of high specificity, high sensitivity, high precision, high accuracy and the like; and the main reagents of the kit all adopt the form of working liquid, the operation is convenient, and the cost is low.

The invention relates to a method for removing norgestrel, norethisterone enanthate and norethindrone in waste water of a pharmaceutical factory. 1-vinyl-1-methyl-2,4-2(c-1-ene-2-base)cyclohexane, tetradecanoic acid-1-methyl ethyl ester, hydroxysuccinic acid, sodium pentahydyoxycaproate, argininyl-fructoyl-glucose, 5-allylguaiacol, 1 hydrogen-tetrazolium-1-acetic acid, (2R, 3R)-3,5,7-trihydroxy-2-(3,4,5-3 hydroxy phenyl) benzodihydropyran-4-ketone, alpha-naphthol-8-sulfonic acid, nitrilotrimethylene triphosphonic acid, 3-[10,10-dimethyl-9(10H)-anthracene subunits]-N, N-dimethyl propyl amine hydrochloride, beta-caryophyllene, alchlor, arginine and microcrystalline cellulose are sequentially added into the waste water in three steps. According to the method, the complexing ability with target materials is high, and the removing rate can reach 99.9 percent.

A hard shell capsule includes a body and a cap cooperatively defining a hollow core hard shell capsule. Each of the body and the cap has a composition that includes a polymer forming a hard polymer structure of the body and of the cap and comprises a drug. The body further comprises a therapeutically effective amount of drug A loaded throughout the composition; the cap further comprises a composition comprising a therapeutically effective amount of drug B loaded throughout the composition. The body and cap compositions together containing a therapeutically effective amount of the drugs A and B; said drugs being oral contraceptive agents. The core of the capsule is filled with therapeutically effective amount of a second drug(s), a dietary supplement, minerals, a complexing agent and other excipients. With the help of FIG. 2, the invention can be very well understood easily. Drugs A and B are selected from the group of oral contraceptives, but are not limited to, Cyproterone acetate, Estradiol, Oestradiol, Norethindrone acetate, Ethinyl Estradiol, Levonorgestrel, Dienogest, Drospirenone, Desogestrel, Ethynodiol, Diacetate, Mestranol, Nomegestrol acetate, Norgestrel, Norgestimate, Dienogest, Norelgestromin, Norethisterone, Gestodene, Oestradiol valerate, and Ethynodiol diacetate.

The invention discloses a preparation method of tibolone, and belongs to the technical field of preparation and processing of steroid hormone drugs. According to the method, 6,7-didehydronorethindroneis used as an initial raw material, and tibolone is prepared through Grignard reaction, dietherification reaction and hydrolysis reaction. The 7-methyl introduction step is included in the Grignard reaction step in the synthesis route, so that special protection on 17-site hydroxyl is avoided, and the ratio of the 7-alpha methyl intermediate to the 7-beta methyl isomer obtained through the reaction is larger than 20:1; therefore, the single 7-alpha methyl intermediate can be obtained through simple treatment without chromatographic separation, the purification process is simple, and the purity of the final product reaches 99.0% or above, and the yield is higher than 60%; the raw materials are cheap and easily available, the reaction steps are few, the reaction conditions are mild and safe, and the control operation is easy; in addition, reagents used in the reaction are low in environmental pollution, and good economic and social benefits are achieved.

The invention relates to a compound estradiol valerate tablet and its preparation process, wherein the active constituents of the tablet include oestradiol valerate and norethisterone, and at least include a crumbling agent, a soluble deflocculating agent with binding property, a binding agent and a lubricating agent. The tablet has rather good bioavailability in vivo and increased dissolving degree externally.

The present application discloses, among other things, asymmetric synthesis a diastereomeric compound of formula (I) (e.g., α-anordrin) or salt thereof. Also provided are methods and compositions for treatment of estrogen deficiency as well as preventing or reducing an estrogen deficiency symptom using a diastereomeric compound of formula (I) (e.g., α-anordrin) or salt thereof alone or in combination with at least one additional agent. Further provided are methods and compositions for reducing a side effect of an additional agent in the context of combination therapy with a diastereomeric compound of formula (I) (e.g., α-anordrin) or salt thereof.

The invention discloses a norethisterone acetate-containing compound estradiol transdermal sustained release preparation and a preparation method thereof. The preparation comprises a backing layer, a protective film and a frame layer between the backing layer and the protective film, wherein the frame layer comprises an upper frame layer, a lower frame layer and a controlled release film between the upper frame layer and the lower frame layer; and the backing layer covers the surface of the lower frame layer. The upper and lower frame layers are respectively wrapped by estradiol and norethisterone acetate in a certain ratio, an intermediate frame layer is wrapped by a special transdermal patch of the controlled release film, estrogen estradiol effects in relieving or eliminating climacteric syndromes and preventing osteoporosis are fully played, and the preparation also has the characteristics of small stimulus to human bodies, small side effects, quality stability and long effective time.

The invention relates to a rapid-to-disintegrate hormone vaginal soft capsule shell. The hormone vaginal soft capsule shell consists of a compound capsule shell capable of rapidly disintegrating in asmall amount of weakly acidic vaginal fluid and a functional content; the capsule shell consists of 6%-12% of carrageenan, 10%-40% of modified starch, 10%-25% of plasticizer, 3%-5% of disintegrating agent, 0%-0.2% of preservative and water; and the functional content can be hormone drugs including progesterone, estriol, norethindrone, megestrol and the like. The invention further discloses a method for preparing the soft capsule shell by using the composition and a soft capsule prepared from the soft capsule shell. The vagina soft capsule shell provided by the invention has the advantages of rapid disintegration, excellent aging resistance, stable components and the like.

The present invention discloses a method of detecting norethisterone and a special enzyme linked immunosorbent kit thereof. The enzyme linked immunosorbent kit which is used for detecting the norethisterone comprises norethisterone haptens and specific antibodies of the norethisterone; and the specific antibodies are polyclonal antibodies or monoclonal antibodies of the norethisterone. The kit adopts the high specificity monoclonal antibodies of the norethisterone, which guarantees the reliability of detection results, and the experimental results show that the kit has the characteristics of high specificity, high sensitivity, high precision, high accuracy and the like; and the main reagents of the kit all adopt the form of working liquid, the operation is convenient, and the cost is low.

The invention discloses an analysis method for various active ingredients in oral contraceptive pill placebo tablets. Firstly, put the placebo tablet to be tested into a measuring bottle, then add water to make it disintegrate, and then add an organic solvent (acetonitrile) for ultrasonic extraction. Then use acetonitrile to set the volume to scale, filter and get the filtrate as the test sample analysis; adopt liquid chromatography to analyze the test sample, start the chromatographic acquisition computer system to collect data; get norethindrone acetate, desogestrel and ethinyl estradiol contrast For the product, prepare the reference solution with a mixed solution of acetonitrile and water, and carry out liquid chromatography analysis simultaneously to check whether the placebo tablet contains multiple active ingredients. The invention has the advantages of strong specificity, rapid analysis, strong anti-interference and high sensitivity, and solves the problem that multiple active ingredients in oral contraceptive placebo tablets need to be repeatedly measured.

The invention discloses a stable pharmaceutical composition containing ethinylestradiol and norethindrone acetate. Vitamin E is added, so that the stability of ethinylestradiol is improved; and by using a specific amount of vitamin E, the production of related substances of ethinylestradiol and norethindrone acetate is controlled at the same time, and the overall stability of the compound preparation is improved.

The invention discloses a preparation method of norethindrone acetate, and belongs to the technical field of preparation and processing of medicines. According to the method, 19-nor-4-rostenedione isused as an initial raw material, and the norethindrone acetate is prepared through four steps of protection, ethynylation, hydrolysis and esterification. According to the preparation method of norethindrone acetate, the defects of a traditional process are overcome, reaction conditions are mild, and formation of impurities is reduced; the method is high in overall conversion rate, simple and convenient to operate, suitable for industrial production and wide in market prospect.

The invention discloses a western medicine composition for treating tetanus and a preparation method thereof. The western medicine composition consists of the following raw materials in parts by weight: 3-7 parts of norethisterone tablets, 0.5-2 parts of ox horn, 8-15 parts of hydroxyethyl cellulose powder, 2-5 parts of cocoon shells, 2-5 parts of cut tobacco, 10-50 parts of normal saline, and 0.01-0.1 part of vitamin C. The western medicine composition achieves a synergistic effect by virtue of raw material compounding, has the effects of clearing away heat and toxic materials, diminishing inflammation and swelling, and drawing out toxin, and can inhibit and kill activity of haemophellolus influenza; complications are not discovered in a treatment process, and obvious toxic or side effects do not appear; the curative effect is short, the effect is achieved quickly, the preparation method is simple, the production cost is low, the economic pressure of a patient is reduced, pains are avoided in the treatment process, and the taste is good; and clinical tests prove that the western medicine composition is safe and effective for treating tetanus.

The invention discloses a western medicine combination for treatment of tetanus and a preparation method thereof. The western medicine combination is composed of, by weight, 3-7 parts of norethisterone tablets, 0.5-2 parts of ox horns, 8-15 parts of leflunomide powder, 2-5 parts of cocoon shells, 2-5 parts of tobacco shreds, 10-50 parts of normal saline and 0.01-0.1 part of vitamin C. Through the synergistic effect of raw material compounding, the western medicine combination has the effects of clearing away heat and toxic materials, diminishing inflammation and swelling and drawing out poison, and can restrain and kill the viability of clostridium tetani; in the therapeutic process, no complication is founded, and no obvious toxic and side effect occurs; the course of treatment is short, quick effect is achieved, the preparation method is simple, the production cost is low, the economic pressure of patients is lowered, the patients have no pains in the treatment process, and the taste is good; and clinical tests prove that the western medicine combination is safe and effective and can be used for treatment of tetanus.

The present invention relates to a method for analyzing impurities of steroidal compounds, in particular to a method for detecting and analyzing impurities of norethindrone derivatives and their intermediates, comprising: (1) choosing octadecylsilane bonded silica gel as filler The chromatographic column; the gradient elution of the mobile phase, the composition of the mobile phase is water, methanol and acetonitrile; the detection wavelength is 230 ~ 254nm; (2) take the test sample norethindrone derivative or its intermediate amount, accurately weigh the methanol Dissolve and dilute to a certain concentration of the sample solution, shake it up, inject the sample, perform high-performance liquid chromatography analysis at an appropriate flow rate and column temperature, and record the chromatogram. The invention can quickly and accurately realize the impurity analysis of norethindrone derivatives, especially for the impurity analysis of norethindrone enanthate, and can be used for the impurity analysis of norethindrone derivative intermediates, and can effectively track the impurities produced in the synthesis process. Impurities.

A stable pharmaceutical composition comprising ethinyl estradiol and norethindrone acetate, the stability of ethinyl estradiol is improved by adding vitamin E; and by using specific amount of vitamin E, the stability of ethinyl estradiol and norethindrone acetate is controlled The production of related substances improves the overall stability of the compound preparation.