Abstract: The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

Abstract: The present invention provides compositions, methods, and kits for improving health in a woman having elevated SHBG levels, or who is receiving oral estrogen supplementation, by non-orally administering an effective amount of an androgenic steroid. Further, the present invention provides compositions, methods, and kits for coadministering an effective amount of an orally administered estrogen and an effective amount of a non-orally administered androgenic steroid for women in need of estrogen supplementation.

Abstract: Methods and compositions for male or female contraception are provided. The compositions include an effective amount of netrin-1 to reduce or inhibit sperm concentration in semen of males or to inhibit or reduce fusion of male gametes with female gametes in a female subject Still another embodiment provides a method for diagnosing male infertility by determining the amount of netrin-1 in a sample of epididymal fluid or semen from a male subject, comparing the amount of netting-1 in the sample to levels of netrin-1 in samples of epididymal fluid or semen from fertile males, wherein levels of netrin-1 in the sample from the male subject that are higher or lower than levels of netrin-1 in samples from fertile males are indicative of male infertility in the male subject.

Abstract: The present invention provides ascending-dose extended cycle regimens in which a female is administered an estrogen and a progestin for a period of greater than 30 or 31 consecutive days, optionally followed by a hormone-free period or by a period of administration of estrogen. The disclosed regimens can be administered to a female to provide contraceptive and non-contraceptive benefits.

Abstract: The present invention provides ascending-dose extended cycle regimens in which a female is administered an estrogen and a progestin for a period of greater than 30 or 31 consecutive days, optionally followed by a hormone-free period or by a period of administration of estrogen. The disclosed regimens can be administered to a female to provide contraceptive and non-contraceptive benefits.

Abstract: A method of therapeutic management of infertility by programming of controlled ovarian stimulation and assisted reproductive procedures is disclosed containing the steps of a) suppression of premature ovulation with an LHRH-antagonist in controlled ovarian stimulation and assisted reproductive techniques with multiple follicle and oocyte development; b) programming the start of controlled ovarian stimulation by the administration to a patient of progestogen only-preparations or, alternatively, combined oral contraceptive preparations; c) exogenous stimulation of the ovarian follicle growth; d) ovulation induction with HCG, native LHRH, LHRH-agonists or recombinant LH; and e) application of assisted reproduction techniques, especially of IVF, ICSI, GIFT, ZIFT or by intrauterine insemination by sperm injection, wherein onset of the patient's menstrual cycle and of controlled ovarian stimulation are programmed in order to perform oocyte pickup and fertilization procedures during Mondays to Fridays.

Abstract: The present invention relates to a flexible extended use regimen for a hormonal contraceptive useful to manage bleeding problems associated with fixed extended use of hormonal contraceptives and to a pharmaceutical package containing the respective hormonal contraceptive.

Abstract: A multiphasic estrogenic/progestogenic contraceptive regimen that provides for the reduction or elimination of estrogen in the initial phase is disclosed. Also described is a contraceptive kit that may be used to practice the method of the invention.

Abstract: The invention concerns a concentrated hormone pharmaceutical composition having from about 0.6 to about 80% of at least one hormone; from about 20 to about 90.4% of at least one solvent, and optionally a pharmaceutically acceptable carrier. The concentrated hormone pharmaceutical composition according to this invention provides a concentrated pharmaceutical composition that is easy to use and saves time and money to the pharmacies dealing with BHRT pharmaceutical products.

Abstract: The present invention provides extended cycle contraceptive regimens in which a female is administered a combined dosage form of estrogen and progestin. The disclosed extended cycle contraceptive regimens can be administered to a female as a method of providing non-contraceptive benefits.

Abstract: A method of contraception in mammalian females, which method comprises the oral administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1) in which R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a pharmaceutical kit comprising oral dosage units that contain the aforementioned estrogenic component and/or a progestogenic component.

Abstract: Methods of reducing the risk of transmission of a sexually transmitted pathogen by contacting the pathogen or cells susceptible to infection by the pathogen with a ?-cyclodextrin are provided. Methods for reducing the risk of transmission of a sexually transmitted pathogen to or from a subject by contacting the pathogen or cells susceptible to the pathogen in the subject with a pharmaceutical composition containing a ?-cyclodextrin also are provided. Accordingly, pharmaceutical compositions, which include 1) a ?-cyclodextrin, which is in an amount that blocks passage of the pathogen through lipid rafts in the membrane of a cell susceptible to the pathogen, and 2) a contraceptive, an agent for treating a sexually transmitted disease, a lubricant, or a combination thereof, are provided, as are composition formulated from a solid substrate that contains an amount of ?-cyclodextrin useful for reducing the risk of transmission of a sexually transmitted pathogen.

Abstract: The invention relates to ?15-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.

Abstract: Methods of reducing the risk of transmission of a sexually transmitted pathogen by contacting the pathogen or cells susceptible to infection by the pathogen with a ?-cyclodextrin are provided. Methods for reducing the risk of transmission of a sexually transmitted pathogen to or from a subject by contacting the pathogen or cells susceptible to the pathogen in the subject with a pharmaceutical composition containing a ?-cyclodextrin also are provided. Accordingly, pharmaceutical compositions, which include 1) a ?-cyclodextrin, which is in an amount that blocks passage of the pathogen through lipid rafts in the membrane of a cell susceptible to the pathogen, and 2) a contraceptive, an agent for treating a sexually transmitted disease, a lubricant, or a combination thereof, are provided, as are composition formulated from a solid substrate that contains an amount of ?-cyclodextrin useful for reducing the risk of transmission of a sexually transmitted pathogen.

Abstract: The invention provides an antimicrobial and antiviral polymeric material, having microscopic particles of ionic copper encapsulated therein and protruding from surfaces thereof.

Abstract: This invention relates to cholesterol-sequestering agents and methods of using cholesterol-sequestering agents to prevent infection. The compositions of the invention can be used to reduce or prevent maternal to fetal transmission of a microorganism and/or to reduce or eliminate a microorganism present in a blood sample or a blood product.

Abstract: The present invention provides for the use of oil of clove which causes instant immobilization of human spermatozoa both in presence of seminal fluid as well as in presence of female reproductive tract fluids, including uterine components and cervical mucus and also be useful for treating and/or preventing the common vaginal infections.

Abstract: The present invention relates to two novel, testis-specific proteins (C19 and C23) that arc lysozyme paralogues. The proteins are believed to play a role in capacitation of sperm and the fertilization of the ovum. Therefore these compounds make ideal targets for the design of contraceptive agents. The C19 and C23 proteins can also be modified to establish lysozyme activity and the modified proteins can then be used in all applications that currently exist for lysozymes.

Abstract: The present invention relates to an improvement in a method of contraception, in treatment of benign gynecological disorders, and in hormone replacement. The improved method includes administering intranasally an estrogenic compound and an androgenic compound, and in some embodiments an optional progestin compound, in a once-daily bolus formulation comprised of the two or three steroids complexed with a cyclodextrin. An intranasal delivery system for administration of the formulation is also described.

Abstract: The present invention relates to methods for preventing the development of epithelial ovarian cancer by administering progestin products, either alone or in combination with other agents such as estrogen products.

Abstract: An improvement in a method of treating benign gynecological disorders is described. In the method, treatment of a benign gynecological disorder with a composition comprised of a gonadotropin releasing hormone (GnRH) compound and an estrogenic compound, and optionally, an androgenic compound, is extended to premenopausal women who are not receiving an exogenously supplied progestin on a regular or periodic basis. Treatment in accord with the invention does not increase significantly the risk of endometrial hyperplasia. The method is also suitable for contraception.

Abstract: The present invention relates to the field of chemistry and more particularly to that of therapeutic chemistry. The invention relates more particularly to novel contraceptive compositions formed from a progestative agent and an oestrogen. The invention relates specifically to novel pharmaceutical contraceptive compositions, characterized in that they contain, as active ingredients, a nomegestrol ester and oestradiol, in combination or admixture with an inert, non-toxic, pharmaceutically-acceptable vehicle or diluent which is suitable for oral administration.

Abstract: The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.

Abstract: A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ?O and ?N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.

Abstract: The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formula R—SO2—O— at their C3 position wherein R is a R1R2N group wherein R1 and R2 are independent of each other and represent a hydrogen atom, a C1-C5 alkyl radical or, together with the N atom, a polymethylene imino radical containing 4 to 6 C atoms, or a morpholino radical. The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.

Abstract: Methods of reducing the risk of transmission of a sexually transmitted pathogen by contacting the pathogen or cells susceptible to infection by the pathogen with a &bgr;-cyclodextrin are provided. Methods for reducing the risk of transmission of a sexually transmitted pathogen to or from a subject by contacting the pathogen or cells susceptible to the pathogen in the subject with a pharmaceutical composition containing a &bgr;-cyclodextrin also are provided. Accordingly, pharmaceutical compositions, which include 1) a &bgr;-cyclodextrin, which is in an amount that blocks passage of the pathogen through lipid rafts in the membrane of a cell susceptible to the pathogen, and 2) a contraceptive, an agent for treating a sexually transmitted disease, a lubricant, or a combination thereof, are provided, as are composition formulated from a solid substrate that contains an amount of &bgr;-cyclodextrin useful for reducing the risk of transmission of a sexually transmitted pathogen.

Abstract: Disclosed is an immunocontraceptive vaccine composition comprising a teleost homolog of zona pellucida (TH-ZP), together with a pharmaceutically acceptable diluent or carrier, for reducing or preventing fertilization in a fish, and a method for its use. Also disclosed is immunocontraceptive vaccine composition comprising an antigen from an inner perivitelline layer (IPVL), together with a pharmaceutically acceptable diluent or carrier, for reducing or preventing fertilization in a bird, and a method for its use.

Abstract: Contraceptive activity as well as anti-microbial, particularly anti-viral protection is provided by contraceptive compositions containing a thiourea compound of the invention exhibiting spermicidal or sperm-immobilizing activity. Preferred compounds of the invention are cyclohexenyl-substituted thiourea compounds.

Abstract: The present invention relates to methods of providing male contraception using a specified androgen without the need of a separate sterilizing agent. The invention also describes methods for non-contraceptive androgen replacement and devices useful for carrying out both processes.

Abstract: The invention is directed to a novel class of 17&bgr;-acyl-17&agr;-propynyl steroids which exhibit potent antiprogestational activity.

Abstract: Amphipathic lytic peptides are ideally suited to use in a ligand/cytotoxin combination to induce sterility or long-term contraception in mammals. The peptides act directly on cell membranes, and need not be internalized. Administering a combination of gonadotropin-releasing hormone (GnRH) (or a GnRH agonist) and a membrane-active lytic peptide produces long-term contraception or sterilization in mammals in vivo. The compounds are relatively small, and are not antigenic. Lysis of gonadotropes has been observed to be very rapid (on the order of ten minutes.) The two components—the ligand and the lytic peptide—may optionally be administered as a fusion peptide, or they may be administered separately, with the ligand administered slightly before the lytic peptide, to activate cells with receptors for the ligand, and thereby make those cells susceptible to lysis by the lytic peptide.

Abstract: Non-absorbent substrates for use in inhibiting the production of exoproteins from Gram positive bacteria, such as harmful proteins produced by Staphylococcus species, are provided. The substrates are particularly useful for inhibiting the production of TSST-1, alpha-toxin and/or enterotoxins A, B and C from S. aureus bacteria. The substrates include an alkyl polyglycoside incorporated in or on at least a portion of the substrate. The alkyl polyglycoside typically has an HLB of about 10 to 15 and/or an average number of carbon atoms in the alkyl chain of about 8 to about 12.

Abstract: The present invention relates to a chewable, palatable oral contraceptive tablet, comprising an oral contraceptive agent, a chewable carrier suitable for human consumption, and not comprising a ferrocene compound, as well as use of these tablets in a method of human female oral contraception, and in a method of enhancing compliance with a human female oral contraceptive regimen.

Abstract: Acylcarnitine analogues having alkyl side chains of 10 to 30 carbon atoms display excellent spermicidal and anti-HIV activity, a well as being potent inhibitors of the growth of Candida albicans.

Abstract: Sterol derivative compounds, structurally related to natural compounds which can be extracted from bull testes and from human follicular fluid, useful for regulating meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.

Abstract: The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formula R—SO2—O— at their C3 position wherein R is a R1R2N group wherein R1 and R2 are independent of each other and represent a hydrogen atom, a C1-C5 alkyl radical or, together with the N atom, a polymethylene imino radical containing 4 to 6 C atoms, or a morpholino radical. The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.

Abstract: The invention relates to (androst-5-en-17beta-yl)alkylsulfoxides and sulfones having general formula (I), wherein R1, R2, R3, X and Y are defined in the specification. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.

Abstract: Methods and compositions for inhibiting or preventing spermatogenesis in a male mammal. Also disclosed are compounds and formulations for use in such methods.

Abstract: The present invention comprises methods and compositions for use in inhibiting egg production by parasitic trematode worms comprising administering to an individual in need thereof an effective amount of an agent which transiently inhibits the influx of calcium through a cell membrane calcium channel. Inhibition of egg production in the worms ameliorates many of the symptoms and pathology related to infection by trematode related diseases, including Schistosomiasis. The methods can also effect disease transmission by reducing the number of eggs released into the environment available to continue the worm life cycle.

Abstract: The present invention relates to a hormonal contraceptive product having two hormonal components, an estrogen and a gestagen, and a process for the combined, continuous administration of the product of the invention.

Abstract: Certain compounds, structurally related to natural compounds which can be extracted i.a. from bull testes and from human follicular fluid, can be used for regulating the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives. These compounds have the structural formula wherein the substituents are as defined in the specification.

Abstract: 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.

Abstract: The present invention provides antiviral proteins, peptides and conjugates, as well as methods of obtaining these agents. The antiviral proteins, peptides and conjugates of the present invention can be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the infectivity, replication and cytopathic effects of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2, in the treatment or prevention of viral infection.

Abstract: Certain antibody molecules are so stable and so potent at immobilizing sperm as well as the pathogens for sexually transmitted diseases (STDs) that they make possible new prophylactic contraceptive methods: (a) for men, a skin lotion containing antibodies against sperm and against STD pathogens to be applied to the penis and external genitals during sexual activity, thereby delivering prophylactically effective doses of antibodies to virtually all areas of skin and epithelia across which most STDs, including AIDS, are usually transmitted, and, during vaginal intercourse, the penis will deliver a contraceptively reliable dose of the antibodies to the cervical region of the vagina; and (b) for women, intrauterine devices (IUDs) and intravaginal devices (IVDS) that release antibodies into the uterus or into the vagina to provide continuous protection against pregnancy and STDs for periods of months to years.

Abstract: A process for preparing a spermicidal agent from neem oil includes (a) mixing neem oil with an aliphatic hydrocarbon solvent so that a precipitate forms, and filtering the mixture to separate the filtrate solution from the precipitate; (b) contacting the filtrate solution of step (a) with a polar extractant solvent whereby a spermicidal agent is extracted from the filtrate solution into the polar extractant solvent; and (c) removing solvent from the polar extractant solvent to produce a concentrated solution containing extract a spermicidal agent.

Abstract: A chemical composition, method and product for administration into the vaginal canal. The composition, method and product are effective in preventing the spread of sexually transmitted diseases, including the spread of AIDS.

Abstract: The present invention relates to therapeutically active compounds of formula I a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.

Abstract: The invention relates to a steroid compound having the formula (I) comprising a ring E, said ring sharing carbon atoms at position 16 and 17 with the five-membered ring D and being &agr; with respect to said D-ring. In addition, the carbon atom at position 17 is substituted with an oxygen atom-comprising group through a CO bond. The invention also relates to a pharmaceutical composition comprising said steroid compound. The steroid compounds of the present invention are very suitable for use in the prevention or treatment of peri-menopausal or menopausal complaints, more preferably the prevention or treatment of osteoporosis. Furthermore, the steroid compounds of the present invention can be used for contraceptive purposes.

Abstract: Novel compositions extracted from corn products provide contraceptive and anti-neoplastic activities. Using novel extraction procedures, compositions may be isolated from corn products. For example, a Zea mays plant product is extracted in a first solvent to produce a solvent extract, the solvent extract is dried to produce an extracted solid, the extracted solid is solubilized in a second solvent, the solubilized extract is purified in a chromatographic process, and an active fraction is collected from the chromatographic process. Compositions may be applied to animal bedding or food, and are adaptable to any suitable method of administration. The contraceptive activity of these compositions is effective for both males and females.

Abstract: A buccal dosage unit is provided for administering a contraceptive composition to fertile mammalian males. The buccal dosage unit comprises a an androgenic agent and a progestin in a polymeric carrier that bioerodes and provides for delivery of the active agents throughout a predetermined drug delivery period that is preferably in the range of approximately 8 to 24 hours.