868results about How to "Improve oral bioavailability" patented technology

A process for milling a solid substrate in the milling chamber of a dispersion or media mill in the presence of a two or more compositions of milling media bodies is disclosed wherein all milling media bodies contribute to the grinding of the solid substrate and wherein at least one composition of media bodies provides fragments of milling media bodies that are retained with the milled solid substrate particles in the form of a synergetic commixture produced in the milling process. More specifically, a process is disclosed for preparing a synergetic commixture comprising small particles of a solid substrate and small particulates of a first material of a desired size comprising the steps of (a) providing to the milling chamber of a media mill a contents comprising a pre-mix of a solid substrate, a fluid carrier, a plurality of milling bodies of a first material having a fracture toughness Kc1, and a plurality of milling bodies of a second material having a fracture toughness Kc2; (b) operating the media mill to grind the solid substrate and degrade at least a portion of the milling bodies of first material to produce a dispersion in the fluid carrier comprising a synergetic commixture of small particulates of the first material and small particles of the solid substrate having a desired size equal to or less than a size Sp; (c) separating the dispersion from any milling bodies and solid substrate particles having a size larger than Sp; and (d) optionally removing the fluid carrier from the dispersion to form a synergetic commixture free of fluid and comprising the particles and the small particulates, wherein KC2 is greater than KC1.

Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.

An oil-in-water nanoemulsion delivery system that includes at least one oil having a concentration of greater than or equal to 2% (w / w) of at least one polyunsaturated fatty acid, preferably of the omega-3 or omega-6 family, is disclosed. The delivery system further includes at least one emulsifier and also an aqueous phase. Preferably, one or more hydrophobic therapeutic, monitoring and / or diagnostic agents are dispersed in the oil phase. The nanoemulsions may optionally contain other conventional pharmaceutical aids such as stabilizers, preservatives, buffering agents, antioxidants, polymers, proteins and charge inducing agents. The invention also relates to a process for preparing the nanoemulsions and to their use in the oral, parenteral, opthalmic, nasal, rectal or topical delivery of hydrophobic therapeutic, monitoring or diagnostic agents.

The invention concerns excipients or combinations thereof suitable for preparing an oral formulation containing a pharmaceutical agent. More particularly, the invention is directed to stable, efficacious and bioavailable oral pharmaceutical formulations comprising paclitaxel, derivatives of paclitaxel and pharmaceutically acceptable salts thereof. The formulations of the invention increase bioavailability of paclitaxel when dissolved in the gastrointestinal system. The formulations of the invention are useful for administering paclitaxel, its derivatives, or pharmaceutically acceptable salts of such derivatives to patients in need thereof. The formulations of the invention are particularly suitable for oral administration to mammals including humans.

The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to promote absorption of the bisphosphonate at the GIT cell lining. The enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to enhance intestinal delivery of the bisphosphonate to the underlying circulation. Preferably, the enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms, and the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

A novel matrix composition for pharmaceutical use. The matrix composition has been designed so that it is especially suitable in those situation where an improved bioavailability is desired and / or in those situation where a slightly or insoluble active substance is employed. Accordingly, a controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides, and the second polymer being selected form block copolymer of ethylene oxide and propylene oxide including poly(ethylene-glycol-b-(DL-lactic acid-co-glycolic acid)-b-ethylene glycol (PEG-PLGA PEG), poly((DL-lactic acid-co-glycolic acid)-g-ethylene glycol) (PLGA-g-PEG), poloxamers and polyethylene oxide-polypropylene oxide (PEO-PPO), ii) a therapeutically, prophylactically and / or diagnostically active substance, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, wherein the active substance is released with a substantially zero order release.

The present invention provides oral dosage forms and compositions for administering antineoplastic agents, such as irinotecan, etoposide, paclitaxel, doxorubicin and vincristine, whose oral effectiveness is limited by pre-systemic and systemic deactivation in the GI tract. Gelling of the gastric retention vehicle composition, and in the case of solid forms concomitant expansion of the composition, retains the antineoplastic drug in the patient's stomach, minimizing pre-systemic and / or systemic deactivation of the drug.

An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis-HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and / or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

One aspect of the present invention relates to a method of hormone replacement in mammals, which method comprises the oral administration of an estrogenic component and a progestogenic component to a mammal in an effective amount to prevent or treat symptoms of hypoestrogenism, wherein the estrogenic component is selected from the group consisting of substances represented by the above formula in which formula 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 a progestogenic component as well as an androgenic component.

The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to promote absorption of the bisphosphonate at the GIT cell lining. The enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.

Pharmaceutical compositions suitable for oral administration comprising paclitaxel, a solvent, a surfactant, a substituted cellulosic polymer, and optionally but preferably a P-glycoprotein inhibitor. The composition may further comprise a diglyceride or mixture of diglyceride and monoglyceride. The composition generates a supersaturated paclitaxel microemulsion upon contact with water resulting in improved oral bioavailability of paclitaxel.

Described herein are methods and compositions for treating an ER-related disease condition characterized by a mutation in the ESR1 gene by administering an estrogen receptor modulator. Also described herein are methods of treating hormone resistant-estrogen receptor (ER) positive breast cancers characterized by a mutation in the ESR1 gene by administering an estrogen receptor modulator.

A dosage form is disclosed comprising a drug formulation that self-emulsifies in said dosage form.

The present invention provides aryl nitrones, compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia / reperfusion-related and chemokine mediated conditions.

Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.

N-[1S,2S]-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-trifluoromethyl]pyridine-2-yl}oxy}propanamide (Compound I) has surprisingly improved solubility and bioavailability in a lipophilic vehicle comprising a pharmaceutically acceptable digestible oil, a surfactant, or a cosolvent, or a mixture of any two or more thereof. In one embodiment of the present invention are self-emulsifying or self-microemulsifying composition comprising 1) Compound I; 2) a surfactant having an HLB of 1 to 8; and 3) a surfactant having an HLB of over 8 to 20; and optionally, 4) a digestible oil and / or cosolvent and / or antioxidant or preservative.

There is provided a compound of formula I,wherein Y1, Y2, Y3, Y4, Z1, Z2, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, for use in the treatment of spinal cord injury.

This invention relates to an oral formulation containing an effective amount of the compound of the following formula I:d-alpha-tocopheryl polyethylene glycol 1000 succinate (“TPGS”); and 2-(2-ethoxyethoxy)ethanol (“Transcutol”). R1 through R4 and n are defined herein. Also disclosed is a method of treating cancer by administering this formula to a subject orally.

The invention belongs to the medicinal preparation field, relates to a cell-penetrating peptide modified nanoparticle, and concretely relates to a nanoparticle delivery system for oral polypeptide and protein medicines, and its preparation method. The medicine delivery system is composed of the nanoparticle, cell-penetrating peptides modified on the surface of the nanoparticle, and the polypeptide protein medicines sealed by the nanoparticle, wherein the average particle size range of the medicine delivery system is 10-500nm. The cell-penetrating peptide modified nanoparticle and glucosaminoglycan having electronegative cell surfaces undergo electric property attraction and then undergo endocytosis, so the cell-penetrating peptide modified nanoparticle and the glucosaminoglycan are integrally taken into cells; and the cell-penetrating peptide modified nanoparticle has an alimentary canal mucous membrane penetrating capability after the cell-penetrating peptide modified nanoparticle is orally taken, and can deliver the polypeptide protein medicines carried by the cell-penetrating peptide modified nanoparticle to the whole body for blood circulation, so the oral biological utilization degree of the medicines are improved. The cell-penetrating peptide modified nanoparticle has the advantages of improvement of the stability of polypeptide and protein medicines in the alimentary canal, reduction of the application amount of cell-penetrating peptides, and reduction of possible toxic side effects caused by the cell-penetrating peptides.

The instant application relates to morphinan derivatives of formula I with enhanced oral bioavailability for the treatment of diseases associated with opioid receptor activity or blockade including alcohol and opiate addiction.

A composition and method of using the composition for treating a patient in need thereof, the composition comprising an oral formulation for enhanced bioavailability of therapeutic agents such as the taxane chemotherapeutic agents. The composition comprises the therapeutic agent and an absorption enhancing agent either co-administered with the agent or administered separately, the therapeutic agent in a polymer matrix resulting in a microbead and including an edible oil resulting in an emulsion. The absorption enhancing agent is a cyclosporin in one embodiment. The absorption enhancing agent is a P glycoprotein inhibitor in another embodiment.

Novel 2′-C-methyl nucleoside 5′-monophosphate and 4′-C-methyl nucleoside 5′-monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described.

This invention relates to imidazopyrimidine substituted piperidine derivatives and their use as pharmaceuticals.