Abstract: Applicants describe the synthesis of fluorotamoxifen and iodotamoxifen analogs with the halogen atom positioned on the aliphatic chain of the tamoxifen molecule. The halogenated-tamoxifen derivatives possess superior binding affinities to estrogen receptors of pig uteri compared with tamoxifen. The fluorinated tamoxifens have potential use in imaging estrogen receptors by PET whereas the iodinated tamoxifens have potential use in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing fluorotamoxifen and iodotamoxifen derivatives with high specific activity are also disclosed. Fluorotamoxifen and iodotamoxifen derivatives may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors.

Abstract: An excipient for a pharmaceutical compound which melts at body temperature but will not spontaneously deform at higher temperatures encountered in shipment and storage comprises:______________________________________ Low MW Polyethylene glycol 75-90% (M.P. about 37.degree. C.) Medium to high MW polyethylene glycol 0-4% Long chain saturated carboxylic acid 0-4% Polyethylene oxide 0-4% (MW 100,000-5,000,000) Colloidal silica 10-20%. ______________________________________The excipient is particularly advantageous for the preparation of dosage forms for buccal administration of pharmaceutical compounds.

Abstract: This invention is directed to a delivery system and a method useful for the treatment of benign ovarian secretory disorders 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 steriod to counteract the possibility of side effects which may develop during prolonged therapy 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.

Abstract: This invention describes the use of a hydroxyoctadecadienic acid, its acid oxidized to keto form or the ester derivatives of the acids, where the ester derivatives are low esters with 1 to 4 carbon atoms for the preparation of a pharmaceutical for treatment of breast carcinomas or benign prostatic hyperplasia. In particular, those compounds are suitable in which the double bonds and the hydroxy group or the oxo group are present on the carbon atoms at positions 9 to 13.

Abstract: Novel (E)-1-[4'-(2-alkylaminoethoxy)phenyl]-1- (3'-hydroxyphenyl)-2-phenylbut-1-enes of the general formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different, provided that, when R.sup.1 and R.sup.2 are the same, each of them is a methyl or ethyl radical, and when R.sup.1 and R.sup.2 are different, one of them is hydrogen and the other is a methyl or ethyl radical, and the therapeutically compatible salts thereof, have a marked anti-estrogenic effect and are suitable for treating hormone-dependent mammary tumors.The compounds can be prepared by dehydrating carbinols of the general formula ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different, provided that, when R.sup.1 and R.sup.2 are the same, each of them is a methyl or ethyl radical, and when R.sup.1 and R.sup.2 are different, one of them is a benzyl radical and the other is a methyl or ethyl radical; and wherein R.sup.

Abstract: The new pharmaceutical composition and processes are provided for treating and preventing diabetes.The pharmaceutical composition is composed of three ingredients: Oleanolic acid, Saponins of Litchi and Kuguasu.The pharmaceutical composition is nontoxic.

Abstract: Disclosed is a method for treating menopausal symptoms and treating and preventing osteoporosis, wherein a true antiestrogen is administered and estrogen is not. This treatment is effective for female osteoporosis and can also be used to treat male osteoporosis. Examples of true antiestrogens are clomiphene, and its isomers, citrates and derivatives, as well as several other compounds which appear in the specification.

Abstract: The method of regulating fertility in swine which comprises administering to a pregnant sow near term an amount of epostane sufficient to induce parturition of live piglets on the following day is disclosed.

Abstract: A transdermal delivery system for the administering of ethinyl estradiol and levonorgestrel, in combination, utilizing a polymer matrix having the drug formulation along with a permeation enhancer dispersed throughout.

Abstract: A device for the controlled release and delivery of a pharmacologically active agent, comprising a vinyl gel layer and a pharmacologically active agent uniformly dispersed in the layer in a pharmacologically effective amount, the vinyl layer comprising an emulsion polymerized polyvinyl chloride resin, a primary plasticizer for the polyvinyl chloride resin, and an organic, nonvolatile gel forming additive in an amount sufficient to form a gel.

Abstract: A solution containing luprostial and 1,2-propanediol, characterized in that it contains luprostial in the form of its sodium salt in a solvent mixture comprising 50-90 percent by weight of 1,2-propanediol and 10-50 percent by weight of water, and has a pH between about 6 and 8.

Abstract: Azido-, 4-nitro and 2,4-dinitrophenylhydrazones as well as 4,4'-dihydroxybenzophenone-hydrazone and other hydrazones are disclosed which have antiestrogenic activity useful in treating estrogen-requiring tumor cells. The described hydrazones bind to estrogen receptors in the cytoplasm of tumor cells. The azido-, 4-nitro- and 2,4-dinitro-phenyl branches of the molecules appear to bind to the receptors and prevent translocation of estrogenic information into the nucleus, thereby blocking the synthesis of necessary macromolecules such as proteins. Absence of geometric isomerization from antiestrogenic to estrogenic forms of the drug minimizes estrogenic side-effects.

Abstract: A synthetic hormone complex comprising means for binding to the surface of a cell and means for altering second messenger mobilization by the cell. One form of the synthetic hormone complex functions as an antagonist with specific binding affinity for a cell receptor, said hormone in combination with a calcium ion channel inhibitor. Another synthetic hormone complex functioning as an Agonist comprising two or more molecules of a hormone having specific binding affinity for a cell receptor wherein a spacer binding the hormones is 10 to 300 angstroms in length. A method of regulating hormones or other regulatory factors comprising contacting a synthetic hormone complex with a cell surface or internal receptor thereby altering the incorporation of second messenger molecules thereby regulating the physiological function of the cell.