Abstract: This invention relates to the use of butylurea as a contraceptive agent. Butylurea may be used either alone or with a pharmaceutically acceptable carrier, and may be used in conjunction with conventional contraceptive means to abrogate sperm motility.

Abstract: Monoclonal antibody NUH2 produced by a hybridoma having ATCC deposit no. HB 9762. An isolated antigen capable of specifically binding to anti-human sperm antibodies including NUH2 and comprising at least an epitope having a sialyl I structure, and any analogues derived from said antigen. Methods of using the monoclonal antibody and antigen for contraception and treating infertility in human females.

Abstract: Contraceptive devices which are effective for extended periods of time are described, in the form of means for releasing an effective amount of a gonadotropin hormone releasing hormone composition and means for releasing an effective amount of an estrogenic hormone over a first period of time, and means for releasing an effective amount of a progestogen for a second period of time, the second period of time being substantially shorter than and running simultaneously with a portion of the first period of time. The gonadotropin hormone releasing hormone composition is selected from gonadotropin hormone releasing hormone, gonadotropin hormone releasing hormone analogues, gonadotropin hormone releasing hormone agonists, gonadotropin hormone releasing hormone antagonists and mixtures thereof. Contraceptive methods employing the devices are also described.

Abstract: Continuous administration of compositions containing a fixed quantity of synthetic estrogen in combination with a synthetic progestogenic agent are useful to relieve menopausal symptoms, to prevent osteoporosis and for other hormone-replacement treatments. Also described is an improved manufacturing process for such compositions especially for low tablet dosage forms.

Abstract: A vaginal progesterone suppository is provided in the form of a tablet which delivers biologically effective amounts of progesterone for at least about 48 hours, and blood amounts above basal levels for 72 hours. The tablet is formulated to preferably have a hardness on its edge of 8-13 kg, and disintegrates from its surface to form a milky suspension in 6-8 hours after it is inserted in the vaginal vault. The tablet contains, by weight, about 13-20% progesterone, 65-85% lactose, 2-10% corn starch paste binder, 3-10% corn starch disintegrant, and 0.1-0.9% magnesium stearate as a lubricant. The ratio by weight of progesterone to lactose is preferably 1:6, and the ratio of starch paste binder to starch disintegrant is preferably 1:1. This dosage form is an effective treatment for many progesterone deficiency conditions, and provides enhanced bioavailability.

Abstract: This invention concerns compounds having the structure: ##STR1## wherein each of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.2', R.sup.3', R.sup.4', and R.sup.5', is independently hydrogen (--H), or a hydroxyl (--OH), methoxy (--OMe), methyl (--Me), carboxaldehyde (--CHO) or phenylformazen (Ph--N.dbd.CH--) group.This invention also provides a novel process of synthesizing the compounds of the subject invention, including intermediate compounds useful in the process.The present invention also provides pharmaceutical compositions comprising a pharmaceutically effective amount of a compound according to the subject invention and a pharmaceutically acceptable carrier. Finally, the invention provides spermicidal methods and methods of killing or of retarding the proliferation of, cancer cells.

Abstract: This invention is concerned with a contraceptive formulation and a method of contraception which employs a combination of estrogen and progestin and wherein a short period of relatively dominant estrogenic activity alternates with a short period of relatively dominant progestagenic activity. The invention also concerns a hormonal replacement formulation and method for use in menopausal or castrate women which employs a similar combination of estrogen and progestin.

Abstract: Pharmaceutical compositions comprising a combination of a polymeric biguanide and a spermicidal surfactant, useful for contraceptive purposes, for their spermicidal or sperm-immobilizing effect, and contraceptive methods and devices using them.The polymeric biguanide is preferably a compound as described in U.K. Patent Specification No. 702,268 or a bisbiguanide as described in U.K. Patent Specification No. 705,838 or 1,095,902, but especially chlorhexidine. The spermicidal surfactant may be derived from ethylene oxide, preferably a condensate of nonylphenol and ethylene oxide, and especially with 9 to 11 molecular proportions thereof.To avoid short-lived activity, the compositions are preferably made substantially free from anions (notably halide ions and especially chloride ions) which cause deactivation, apparently by reducing the solubility of the active ingredients.

Abstract: Contraceptive methods and delivery systems involving few undesirable side effects during administration are based on novel triphasic estrogen/progestogen combinations, wherein the amount of estrogen is increased stepwise over the three phases.

Abstract: Compositions and methods for providing long lasting contraceptive protection comprising a mixture of a contraceptive effective amount of spermicidal agent, a polymeric gum, a dispersing agent, and a water miscible polyethylene glycol polymer suppository base; and mammalian contraceptive methods utilizing the compositions of the invention in suppository form to provide up to 12 hours of contraceptive protection after initial insertion of the suppository.

Abstract: Contraceptive methods and delivery systems involving few undesirable side effects during administration are based on novel triphasic estrogen/progestogen combinations, wherein the amount of estrogen is increased stepwise over the three phases.

Abstract: A contraceptive method for living animals (including human beings) can utilize a polyurethane or polyvinylacetate (PVA) disc as an inert carrier for contraceptive preparations, the disc being implanted before intercourse to engage the external os of the cervical canal. Preferred contraceptive preparations include (1) the copper (II) salt of ethylenediamine-tetraacetic acid (EDTACu) and L-L-ascorbic acid; (2) the sialic acid-removing enzyme neuraminidase; and (3) an asialoglycoprotein, such as asialofetuin. Of these preparations, which can be used separately or in any combination, the first two act on the cervical mucus to change it from the open cellular structure found at midcycle of the menstrual period to the closed cellular structure and thus form an impenetrable barrier for spermatozoa. The second and third preparations remove sialic acid from spermatozoa, the presence of which is necessary for successful fertilization.

Abstract: A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.

Abstract: The inventive composition comprises an active ingredient, for example a quaternary ammonium compound, which active ingredient is capable of inhibiting or destroying a unicellular living organism, such as spermatazoa, bacteria or virus. The active ingredient is combined in a synergistic amount with an activating ingredient capable of inhibiting or destroying the enzymes associated with the unicellular organism. The activating ingredient may be capable of releasing fluoride ions, for example, an inorganic fluoride compound. The composition according to the invention is useful, for example, as a spermicide, or as an antibiotic, or as an anti-STD preparation for local or topical application.

Abstract: The in-vivo or in-vitro administration of platelet activating factor (PAF) or analogue enhances the viability of fertilized embryos and improves rates of implantation in the uterus. Conversely, reduction of PAF concentration by in-vivo administration of PAF-antagonists such as Iloprost or PAF antibodies, has a contraceptive effect; particularly when used in conjunction with a post-coital contraceptive such as estrogen or a prostaglandin.

Abstract: An estrogen sulfotransferase inhibitor composition comprises a compound of the formula ##STR1## wherein R.sub.1 is F, Br, NO.sub.2, or H; R.sub.2 is F, Br, NO.sub.2, NH.sub.2, or H; R is H or alkyl of 1-4 carbon atoms; R.sub.3 is O or H.sub.2 ; and R.sub.4 is H.sub.2, O, or .alpha.-H, .beta.-OH; R.sub.5 is H.sub.2, .alpha.-H and .beta.-OH or B-H and .alpha.-OH in admixture with a pharmaceutically acceptable carrier with the proviso that R.sub.1, R.sub.2 and R.sub.3 cannot all be hydrogen and one of R.sub.1 and R.sub.2 is F.

Abstract: A contraceptive composition for application to the vagina of a female mammal comprising a contraceptive amount of a contraceptive combination, the combination containing a spermicidal or sperm-immobilizing polyethoxyethanol and a beta-adrenergic blocker (as herein before defined).The polyethoxyethanol may be, for example, an octoxynol or, which is preferred, a nonoxynol, especially nonoxynol-9. The beta-adrenergic blocker is preferably a spermicidal or sperm-immobilizing beta-adrenergic blocker, propranolol (in particular the d-isomer) being especially preferred.The composition may also contain a spermicidal or sperm-immobilizing preservative.

Abstract: A protein having a molecular weight of from about 10,000 to 18,000 daltons, isoelectric points of from about pH 4.0 to 6.5 and having the reversible biological effect of inhibiting aromatase activity in a biological system, and antibodies to the protein, modulate follicular development and spermatogenesis and provide for diagnostic tests of gonadal functions.

Abstract: This invention is directed to a delivery system and a method useful for preventing pregnancy in female mammals by administering an LHRH composition. The method comprises administering during the entire follicular phase of the menstrual cycle, beginning at the time of menses, an LHRH composition and sufficient levels of an estrogenic steroid to counteract the possibility of side effects which may develop during prolonged therepy with LHRH. Following the follicular phase, at the beginning of the luteal phase, and for the entire course of the luteal phase, the LHRH/estrogenic steroid combination administered during the follicular phase, in combination with a physiological amount of progestational steroid, is administered.The delivery system comprises means for administering the LHRH composition, estrogenic steroid and progestational steroid.

Abstract: Antibody or antigen containing microparticles for the active or passive immunization of the internal female reproductive organs, comprising: microparticles of an antigen or antibody incorporated in a matrix material which is biocompatible and biologically degradable, said microparticles capable of being transported after deposition in the vagina by the natural transport mechanism of the internal female reproductive organs across the cervix into the uterus.

Abstract: The invention discloses a novel use of Mullerian Inhibiting Substances (MIS) as a contraceptive agent. MIS has been found to inhibit the maturation of oocytes in vitro. Additionally, the invention provides a means for restoring the fertility of females who are infertile due to abnormal production of MIS.

Abstract: A protein moiety having a molecular weight of from 12,000 to 15,000 inhibits aromatase levels, stimulates 3.beta.-ol dehydrogenase levels and modulates the formation of mature ova substantially independently of steroidal sex hormones. The moiety may be isolated from follicular effluent or produced by granulosa cell cultures.

Abstract: The disclosed invention provides methods and compositions ulilizing L-.alpha.-amino acids for enhancing the rate of penetration through the skin of both topical medicaments and of drugs employed for systemic administration. Fifteen L-.alpha.-amino acids were tested and found to enhance the rate of penetration of levonorgestrel through hairless mouse skin. These were Tryptophan, Glutamic Acid, Glycine, Proline, Alanine, Serine, Arginine, Aspartic Acid, Leucine, Isoleucine, Cysteine, Valine, .alpha.-Aminobutyric Acid, Norvaline and Norleucine. The effect of pH on the rate of penetration of the various amino acids was also examined and found to be unpredictable overall.

Abstract: A method of prophylactics with respect to detoxification of Staphylococcus aureus and other toxins by ascorbic acid, salts and esters, topically applied by means of carriers which are otherwise regularly employed in the area where Staphylococcus aureus or other bacteria colonize, such as a pharmacological appliance including gauze pads, an absorbant mass or pad associated with menses, douches, and contraceptive compositions.

Abstract: A method of prophylactics with respect to deodorization by ascorbic acid, salts and esters, topically applied by means of carriers which are otherwise regularly employed in the vaginal area, such as a pharmacological appliance including gauze pads, an absorbant mass or pad associated with menses, douches, and contraceptive compositions.

Abstract: A vehicle which provides rapid release of a drug and prolonged release of a drug is disclosed.

Abstract: Plant extracts are employed to provide a menses inducing composition for topical application. Common commercially available fenugreek seeds and commercially available ginger are mixed in a preferred range of ratios and combined in a dry powder form for topical application to the outside of the abdomen of the female to induce menses.

Abstract: Conditioning of the vaginal tract for sexual activity, by a method including adjusting and controlling its surface pH, with soluble means for accomplishing such conditioning. The specified conditioning favors increased duration of sexual intercourse, as is often desired, and is compatible here with such diverse goals as favoring or discouraging conception. Normally the human vagina is strongly acidic, which may render intercourse with some males unduly brief. Through this invention the vaginal pH is increased about several pH units, by applying thereto a capsule, tablet, or suppository containing an alkalizer, to be released upon dissolution, so that the surface of the vaginal tract nears and preferably reaches or somewhat exceeds a neutral pH of 7 for a desired period of time. Thereafter, the vagina is enabled to return to its normally acidic condition, or is preferably actively returned thereto by subsequent release of an acidifier from such topically applied means.

Abstract: There are provided post-coital contraceptive pharmaceutical compositions comprising a blocker of progesterone activity (antiprogesterone) at comparatively high dosage, or a combination of such blocker of progesterone activity with a blocker of estrogen and of progesterone synthesis.

Abstract: Postcoital contraception is carried out by the intravaginal administration of an aqueous solution of 2-hydroxy-propanoic acid, 3-hydroxy-3-carboxy-pentanodioic acid and acetic acid.

Abstract: A substantially anhydrous foamable composition capable of forming a substantially stable foam on contact with water is formed from a mixture of water soluble polysaccharide gum, an effervescent base and a biocompatible gelling salt. These compositions upon contact with water form extremely stable foams which are capable of acting as carriers for pharmaceutically active compositions.

Abstract: This invention relates to the use of a bisbiguanide compound of the formula:R.sup.1 R.sup.2 N.C(:NH)N:C(NH.sub.2)N--A--N.C(NH.sub.2):N.C(:NH)NR.sup.3 R.sup.4 Iwherein either:(i) R.sup.1 and R.sup.3, which may be the same or different, are each a phenyl radical which is substituted by alkyl, alkoxy, nitro or halogen, R.sup.2 and R.sup.4 are both hydrogen, and A is a 3-9C polymethylene diradical, wherein the polymethylene chain may be interrupted by oxygen atoms and/or by aromatic nuclei; or(ii) the bivalent bridge A is:(a) alkylene of from 2 to 12 carbon atoms having the valence bonds attached to different carbon atoms,(b) --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n -- wherein m an n each represent an integer from 2 to 6 and X is O or S,(c) ##STR1## (d) ##STR2## wherein Z and Z.sup.1 are each alkylene of from 1 to 3 carbon atoms, (e) ##STR3## wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --, (f) ##STR4## R.sup.1 and R.sup.

Abstract: This invention relates to the use of polymeric biguanides as topical contraceptive agents, which operate both by rendering vaginal mucus impenetrable to sperm, or by a direct spermicidal action.

Abstract: A pressurized contraception composition in an aerosol container and adapted to form a spray upon release of pressure therefrom which composition is a liquid inside the container and forms a gel on contact with living tissue and process employing same, whereby the composition comprises water, propellant, a polyoxyethylene-polyoxybutylene copolymer, and a sperm function inhibitor.

Abstract: A pressurized contraception composition in an aerosol container and adapted to form a spray upon release of pressure therefrom which composition is a liquid inside the container and forms a gel on contact with living tissue and process employing same, whereby the composition comprises water, propellant, a polyoxyethylene-polyoxypropylene copolymer, and preferably a sperm function inhibitor.

Abstract: The use of phenothiazine 5-oxide drugs as vaginal contraceptives is disclosed. The invention may be implemented by incorporating an effective amount of a phenothiazine 5-oxide drug in a known method such as jelly, foam, or suppository introduction means for use prior to intercourse.

Abstract: The use of phenothiazine 5-oxide drugs by injecting or introducing such drugs directly into the uterus is disclosed as a means of preventing pregnancy after intercourse has occurred. Various means of introducing such drugs are disclosed, such as by mixing such drugs with jelly carriers, foam carriers, or paraffin oil.

Abstract: The invention relates to contraceptive vaginal tablets as well as to a process for preparing them. The tablets of the invention have the following composition:0.2 to 3 parts by weight of boric acid,10 to 20 parts by weight of tartaric acid,1 to 2 parts by weight of vitamin K.sub.3 -sodium bisulfite adduct,0.8 to 1.2 parts by weight of polyvinyl pyrrolidone,2 to 5 parts by weight of magnesium stearate,8 to 12 parts by weight of carboxymethyl cellulose,8 to 12 parts by weight of lactose and50 to 65 parts by weight of microcrystalline cellulose.The vaginal tablets contain preferably 5 to 10 mg of vitamin K.sub.3 -sodium bisulfite adduct and have a total weight of 500 mg.The tablets of the invention are prepared preferably in such way that the boric acid, the tartaric acid and the vitamin K.sub.

Abstract: 3,5-diphenyl-1H-1,2,4-triazoles with contragestational activity of the following formula ##STR1## wherein R may be located on one or the other of the two adjacent nitrogen atoms and may represent hydrogen or a group R.sub.5 CO-- wherein R.sub.5 is an aliphatic saturated or unsaturated hydrocarbyl containing from 1 to 20 carbon atoms, R.sub.1, R.sub.2 and R.sub.3, each independently are selected from hydrogen, lower alkyl and lower alkoxy or R.sub.2 and R.sub.3 together may represent a methylenedioxy group, and R.sub.4 is an aliphatic saturated or unsaturated hydrocarbyl group of from 1 to 20 carbons, with the proviso that when R is hydrogen or an R.sub.5 CO-- group wherein R.sub.5 contains 4 or less carbon atoms, R.sub.4 must contain 5 or more carbons.These compounds have proven to be highly effective in terminating pregnancy in several animal species after a single parenteral injection.

Abstract: A method of contraception in which an estrogen and a progestogen are administered daily for 21 days, the first seven days at a low contraceptively effective daily dose, the next 7 days at a daily progestogen dose about 1.5-2 times that of the first 7 days, and the next 7 days at a daily progestogen dose of 2-2.5 times that of the first 7 days, provided that the dosage of the estrogen is maintained at a constant level for the entire 21 days.

Abstract: A contraceptive agent is provided which comprises biologically-active alpha-lactalbumin. The agent can be administered to female mammals using a variety of pharmaceutically acceptable vehicles, provided the alpha-lactalbumin retains its biological activity in the presence of the vehicle.