Abstract: The present invention relates to an injectable composition of testosterone ester for the treatment of testosterone deficiency. Particularly, the present invention relates to a pharmaceutical composition comprising testosterone undecanoate, which is capable of increasing the convenience for use in injection with the low viscosity and injection force, and has improved stability.

Abstract: The present invention relates to devices and methods for treating prolapsed pelvic organ, cystitis and Atrophy in women. Particularly, the invention relates to drug loaded vaginal support devices and methods wherein the device is inserted in vagina to support as well as release the drug. Specifically the invention relates to a Vaginal Ring Pessary comprising Estrogen in Silicone rubber polymer matrix, which releases drug over a prolonged period of about 180 days. Additionally the invention relates to the method of fabrication of the device and its use in treatment of vaginal atrophy, cystitis and uterovaginal prolapse.

Abstract: Described herein are prodrugs of cysteamine and pharmaceutically acceptable salts, solvates, and esters thereof. Also described herein are pharmaceutical compositions comprising prodrugs of cysteamine, or pharmaceutically acceptable salts, solvates, and esters thereof, and methods of treatment comprising administering prodrugs of cysteamine, or pharmaceutically acceptable salts, solvates, and esters thereof.

Abstract: The present invention relates to certain cortexolone derivatives of formula (I) and the use of the same as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. The present invention also relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of the pharmaceutical compositions as antitumor medicinal products.

Abstract: [Problem] To activate an abnormal mesenchymal stem cell whose therapeutic effect is lost or reduced, or rather which has a disease-exacerbating effect so as to be in a state suitable for cell transplant therapy. [Solution] An activator for mesenchymal stem cells, mesenchymal stem cells activated by the activator, a method for producing the same, and a pharmaceutical containing the activated mesenchymal stem cells are provided.

Abstract: The present invention provides certain cortexolone derivatives of formula (I) and the same for use as antitumor active ingredients for the curative or adjuvant, or neoadjuvant or palliative treatment of precancerous lesions, dysplasias, metaplasias and tumor diseases, including malignant neoplasias and metastasis. Another aspect of the invention relates to pharmaceutical compositions comprising cortexolone derivatives of formula (I) as active ingredients and at least one physiologically acceptable excipient, and to the use of said pharmaceutical compositions as antitumor medicinal products.

Abstract: Provided are compositions, e.g., oral and personal care products, comprising (i) a zinc amino acid halide complex, and (ii) cysteine in free or in orally or cosmetically acceptable salt form, together with methods of making and using the same.

Abstract: A method for providing a K2-enriched FU-LING extract is provided. The method comprises the following steps: (a) mixing a FU-LING with a solvent to provide a first mixture; (b) alkalizing the first mixture to provide a second mixture; (c) acidifying the second mixture to provide a third mixture, (d) alkalizing the third mixture to provide a fourth mixture, wherein the fourth mixture has a pH value of more than 7; and (e) neutralizing the forth mixture, wherein the K2 is at least one of tumulosic acid, dehydrotumulosic acid, polyporenic acid C and 3-epi-dehydrotumulosic acid.

Abstract: Methods for effective remyelination in patients are disclosed comprising treating the patient with an androgen receptor ligand which exerts binding to androgen receptors and elicits androgen-receptor-induced biological responses at a dosage sufficient to induce remyelination. The androgen compound preferably comprises MENT in an androgen targeting both androgen and estrogen receptors, and the methods include combining the androgen compound with a progestin compound in order to provide both contraception in men and treatment for neurodegeneration.

Abstract: The invention provides methods to identify agents useful to prevent, inhibit or treat viral infections, e.g. filovirus infections, as well as compositions having one or more agents to prevent, inhibit or treat viral infection.

Abstract: Methods and systems for identifying and treating a patient suspected of having a tumor susceptible to growth inhibition by anti-progestins are provided. The degree of focal distribution of the progesterone receptor can be used to identify tumors susceptible to treatment with anti-progestin therapy.

Abstract: Compositions, and methods of using such compositions, useful for placement, for example injection, into the interior of human or animal eyes are provided. Such compositions include a therapeutic component, such as one or more corticosteroids, a biocompatible polymeric component, and a solvent component. The composition is in a fluid form before placement in the interior of an eye, and becomes less fluid after the composition is placed in the eye to form an extended or delayed release drug delivery element or system. The drug delivery element is formed by the dissipation of the solvent from the composition when the composition is placed in the interior of an eye. One example of a composition includes triamcinolone acetonide as a therapeutic agent. A method of treating an ophthalmic condition, or otherwise improving or enhancing vision of a patient, comprises placing the fluid composition in the interior of the eye. The method may be practiced by injecting the fluid composition into the interior of the eye.

Abstract: Topical drug delivery systems for ophthalmic use including mixed nanomicellar formulations of water-insoluble drugs and methods of treating diseases affecting the posterior ocular segments are disclosed. In an embodiment, an aqueous ophthalmic solution includes nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein a corticosteroid at a concentration from about 0.01% w/v to about 1.00% w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the nanomicelles comprise vitamin E TPGS at a concentration ranging from about 3.0% w/v to about 5.0% w/v stabilized with octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v.

Abstract: The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

Abstract: The present invention relates to compositions and methods useful for the treatment of ear disorders, administered to a treated ear in the form of a foam or a mousse. Administering a medicament in such forms will increase the residence time of the medicament in the ear canal, provide relatively uniform distribution of the composition, and can increase the penetration of the active pharmaceutical ingredient in the affected area, may release active substances slowly, enhance treatment effectiveness, increase compliance and is more convenient to use than currently available ear medications. The administration in the form of a foam or a mousse may preferably be provided as a metered dose, of a volume suitable to fill the ear canal.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

Abstract: Various prodrug compounds having the general structure: Active agent-(acid)-(linker)-SO2NR1R2 are described herein. Compounds having this general structure were shown to be more orally active than the unmodified parent molecule.

Abstract: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx??(I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position ? or ?; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

Abstract: Disclosed is a process for the preparation of drug/carrier inclusion composites which involves co-grinding the mixture of drug and carrier powders in a fluid-jet mill, in particular one using air or nitrogen as the fluid, which is suitably modified to allow mechanical fusion of the powders.

Abstract: Aerosol solution formulation for use in an aerosol inhaler which includes at least one active ingredient selected from 20-ketosteroids and quinolinone derivatives, a propellant containing a hydrofluoroalkane, a cosolvent, and a specific amount of a sequestering agent that stabilizes the formulation. By way of example, the stabilizing agent may be phosphoric acid or sulphuric acid.

Abstract: Phytoecdysones to avoid weight gain in obese mammals previously having undergone a hypocaloric weight-loss diet. The phytoecdysones are added to a food composition. The phytoecdysones can be from plants, such as quinoa.

Abstract: The present disclosure is drawn to oral pharmaceutical compositions and dosage forms containing select testosterone esters and related methods. In one embodiment of the present invention, an oral pharmaceutical composition for administration to subjects in need of testosterone is provided. The composition comprises a testosterone ester and a pharmaceutically acceptable carrier. The testosterone ester can have the structure wherein R is —C13H25O or —C14H27O. One or both of the esters can be present in the pharmaceutical composition. The composition is formulated such that upon single dose administration to a group of human subject, the composition provides a mean serum testosterone Cavg t12-t24 that is within about 35% to about 70% of the mean serum testosterone Cavg t0-t24.

Abstract: A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

Abstract: A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.

Abstract: The present invention is directed to steroid hormone delivery systems and methods of preparing the same. In particular, the steroid hormone delivery systems provided include a primary construct having one or more hydrophobic steroid hormone esters in the form of a liposome, a lipid particle, a micelle, an emulsion or a niosome which is then formulated into a secondary construct for administration. Exemplary secondary constructs include a film for sublingual or buccal administration.

Abstract: Corticosteroid microparticle formulations are provided for use for treating pain, including pain caused by inflammatory diseases such as osteoarthritis or rheumatoid arthritis, and for slowing, arresting or reversing structural damage to tissues caused by an inflammatory disease, for example damage to articular and/or peri-articular tissues caused by osteoarthritis or rheumatoid arthritis. Corticosteroid microparticle formulations are administered locally as a sustained release dosage form (with or without an immediate release component) that results in efficacy accompanied by clinically insignificant or no measurable effect on endogenous cortisol production.

Abstract: The present invention relates to the use of an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating a disease associated with antinuclear antibodies, wherein the inhibitor of CDK2 and/or CDK7 and/or CDK9 or pharmaceutically acceptable salt thereof is administered in an amount sufficient to down-regulate the levels of antinuclear antibodies. A further aspect of the invention relates to a combination comprising an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, and methylprednisolone, and its use in the treatment of diseases associated with antinuclear antibodies, such as SLE.

Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.

Abstract: An anhydrous multiphase gel system consisting of an outer lipid matrix and an inner phase gelled by means of a polymer is described, which can be obtained by a) Melting the lipid phase with the formation of a liquid lipid phase, b) Mixing and homogenizing polymers or polymer blends capable of swelling with the formation of a polymer phase to be dispersed, c) Combining the polymer phase with the liquid lipid phase and homogenizing the phases, and d) Cold stirring the phase mixture until a solid gel-like mixed structure of the entire system is formed. The anhydrous multiphase gel system is particularly suitable for taking up difficulty soluble active substances in high concentration and for providing topical and transdermal applications. The described system is called an EDRS, “Entrapped Drug Reservoir System”.

Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.

Abstract: The present invention relates to a composition, particularly a pharmaceutical composition comprising a testosterone derivative having a log P of at least 5 and a vehicle, wherein the vehicle comprises a fat component in an amount sufficient to achieve lymphatic absorption in a mammal, wherein the fat component comprises a mono- or triglyceride of long chain fatty acids

Abstract: The disclosure relates to methods of using brassinosteroid compounds, including those defined by formula I or a derivative thereof, for inducing an anabolically favorable state for growth, repair, and maintenance of skeletal muscle and skin.

Abstract: Described are drug delivery systems incorporating electrospun fibers that comprise and deliver physicochemically diverse drug compounds. Such fibers provide significant advantages in drug agent release, such as adaptability for solid dosage delivery to mucosal tissues. This is in addition to allowing for controlled drug release. Systems and methods for large-scale electrospinning productivity are described, including novel microarchitectures allowing for variable pharmacokinetics in drug release.

Abstract: The present invention provides an absorbable coating for an implantable device and the methods of making and using the same.

Abstract: The present invention provides compositions and methods for cytoprotection. In particular, it provides zinc chelate compositions comprising at least one zinc ion and at least one aminothiol ligand.

Abstract: Methods for effective remyelination in patients are disclosed comprising treating the patient with an androgen receptor ligand which exerts binding to androgen receptors and elicits androgen-receptor-induced biological responses at a dosage sufficient to induce remyelination. The androgen compound preferably comprises MENT in an androgen targeting both androgen and estrogen receptors, and the methods include combining the androgen compound with a progestin compound in order to provide both contraception in men and treatment for neurodegeneration.

Abstract: The present invention provides methods of preventing or delaying the development of cancer (e.g., breast cancer) in BRCA1 mutation positive patients by beginning progesterone receptor antagonist treatment at an early age (e.g., by age 35, 30, or 25). In certain embodiment, such early treatment is long-term treatment, which may substitute or delay a preventative ovariectomy, single or double mastectomy (e.g., in patients wishing to delay or avoid a mastectomy, or patients that cannot afford a mastectomy).

Abstract: A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

Abstract: The invention relates to an effervescent tablet for preparing a mouth rinsing solution, wherein the effervescent tablet exhibits a high release rate of budesonide. A high availability of the active ingredient during use as a mouth rinsing solution on the inflamed mucosa of the upper digestive tract is thereby achieved. The advantage of the formulation according to the invention lies in the bioavailability comparable to oral forms of administration, which allows the formulation to be used safely over an extended period of time.

Abstract: A minimally invasive controlled drug delivery system for delivering a particular drug or drugs to a particular location of the eye, the system including a porous film template having pores configured and dimensioned to at least partially receive at least one drug therein, and wherein the template is dimensioned to be delivered into or onto the eye.

Abstract: Polymeric micellar clusters formed from amphiphilic carbohydrate polymers and their uses in formulating drugs is disclosed, and in particular the finding that amphiphilic carbohydrate polymers are capable of self assembling to form micellar clusters in which the carbohydrate amphiphiles aggregate into hierarchically organized micellar clusters of individual aggregates. The micellar clusters may be transformed into stable nanoparticles with drugs, especially hydrophobic drugs that have poor aqueous solubility, and may improve the transfer of hydrophobic drugs across biological barriers.

Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.

Abstract: Provided is a composition containing placenta extracts as active ingredients. Placenta extracts are natural substances extracted from placentas of livestock and show effects that can replace steroids and reduce adverse effects of steroids, so that placenta extracts have a wide range of applications including contraceptives, anti-osteoporosis drugs, anti-anemic drugs, therapeutic agents for wasting diseases of muscular atrophy, agents for treating sexual dysfunction, therapeutic agents for wounds, and adipocyte differentiation stimulating agents for improving meat quality of livestock, etc.

Abstract: This invention relates to methods and compositions which are useful in the modulation of endogenous growth hormone levels in a mammal. Also included are methods of treating a mammal which include the administration of said compositions.

Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.

Abstract: Disclosed herein are methods for modulation of gel temperature of poloxamer-containing formulations. Also described herein are sustained release pharmaceutical formulations that gel upon contact with the body and are administered by direct application of these compositions and formulations onto or via perfusion into the targeted structure(s).

Abstract: The present invention provides a method for preparing a sterile suspension of a glucocorticosteroid. The glucocorticosteroids used in the invention are preferably antiinflammatory glucocorticosteroids. By making the last stage of product preparation be the sterilization process, the potential for contamination during manufacture and heat degradation of products is greatly reduced.