1536 results about "Lipophilicity" patented technology

The invention provides a drug-oligomer conjugate having the following general formula:wherein D is a therapeutic drug moiety; H and H' are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the -H', -L and -H-L substituents; the H-L bond(s) are hydrolyzable and the D-L' bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p is 0 and m and n are each at least 1. The therapeutic drug moiety is preferably a therapeutic protein or peptide, preferably insulin or a functional equivalent thereof.

Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

Compositions are provided comprising a lipophilic active compound, e.g., a human or veterinary drug or a nutraceutical, interwoven with a polymeric matrix formed by two or more polymers, wherein one of the polymers is an amphiphilic polymer and the other polymer is either an amphiphilic polymer with a different hydrophobic-hydrophilic balance or a hydrophilic polymer, and the active lipophilic compound has modified physicochemical properties. The composition forms colloidal nanodispersion upon contact with aqueous media.

An apparatus and system for delivering a lipophilic agent associated with a medical device including: a medical device, a first lipophilic agent capable of penetrating a body lumen, wherein the transfer coefficients of the first lipophilic agent is by an amount that is statistically significant of at least approximately 5,000, wherein the first lipophilic agent is associated with the medical device, wherein the first lipophilic agent / medical device is placed adjacent to said body lumen, and wherein a therapeutically effective amount of the first lipophilic agent is delivered to a desired area within a subject. Furthermore, the invention relates to a method for improving patency in a subject involving placement of a medical device in a body lumen for treating and / or preventing adjacent diseases or maintaining patency of the body lumen.

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

The present invention relates to a process for preparing silica microcapsules and more particularly, to a process for preparing silica microcapsules comprising the steps of dissolving tetraethyl orthosilicate (TEOS) into an aqueous solution containing a hydrolysis catalyst to control a degree of hydrolysis and contribute hydrophilicity or lipophilicity, adding a core material and an appropriate amount of aminopropyltrialkoxysilane(APS) as a gelling agent into the solution, and emulsifying and dispersing the resulting solution to a solution having a polarity opposite to that of the core material to microcapsulate by coating the core material with silica shell via a sol-gel reaction. The process for preparing microcapsules of the present invention reduces environmental pollution compared to conventional processes using an alkali gelling agent such as an ammonia solution, and are suitable for both organic or inorganic core materials having hydrophilic or lipophilic property.

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. In a preferred embodiment, a drug is modified to increase its lipophilicity. In some embodiments the modified drug is homogeneously dispersed within spherical microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and / or organic solvent insoluble. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.

The present invention provides a controlled release device for sustained or pulsatile delivery of pharmaceutically active substances for a predetermined period of time. This invention further provides such device in which sustained or pulsatile delivery is obtained by the unique blend and intimate mixture of pharmaceutically active substances with a microbial polysaccharide and uncrosslinked linear polymer and optionally a crosslinked polymer and / or lipophillic polymer and / or saturated polyglycolyzed glyceride. The invention also provides a process for the manufacture of such devices and pharmaceutical compositions containing the same.

Compositions and methods are for disclosed for treating a skin condition that results from reactive oxygen species production in skin of a subject, including applying a topical formulation that contains a lipophilic cation-mitochondrially targeted antioxidant compound and that delivers a therapeutically effective amount of the antioxidant compound to skin fibroblasts and keratinocytes.

There may be provided compositions of lipophilic pharmaceutical agents with improved solubility and stability. For example, there may be provided a non-aqueous composition that comprises a lipophilic pharmaceutical agent, and an amphiphilic polymeric solvent such as PEG400 but essentially free of organic solvents and non-solubilized particles. The composition may be further diluted with a desired aqueous diluent such as an infusion fluid for parenteral administration to a subject such as a human. The compositions may be useful for the treatment for diseases or conditions that are sensitive to lipophilic agents, such as infectious diseases, malignant or autoimmune diseases.

A method of forming electrospun fiber mats from a plurality of different biodegradable polymeric fibers is provided, in which a plurality of up to six different biodegradable polymer solutions are electrospun together by a method comprising the steps of providing a plurality of up to six different biodegradable polymer solutions each containing at least one biologically or pharmaceutically active material and each in communication with a needle for electrospinning a biodegradable polymer fiber from the solution, and pumping each solution through its respective needle into an electric field under conditions effective to produce uncontrolled charged jet streams of the polymer solutions directed at a grounded rotating mandrel, thereby forming fiber threads of the biologically or pharmaceutically active compounds and polymers in the solutions that are deposited on the mandrel to form an electrospun non-woven fiber mat, wherein the needles are positioned for co-deposition of the fiber threads from the polymer solution streams together on the mandrel to form a fiber mat.

The present invention provides novel dietary supplement compositions based on the use of a particular oil phase which comprises of Coenzyme Q10 and optionally other lipophilic dietary ingredients of low water solubility and a liquid mixture which comprises one or more emulsifiers, a fatty acid monoester formed between an short chain alcohol of C1 to C4 chain length and a saturated, or mono-unsaturated, or di-unsaturated (both conjugated and non-conjugated) fatty acid of C6 to C24 chain length, or medium chain mono- / di-esters, or the mixture of above. The composition is in a form of self-emulsifiable in the aqueous medium, for example, a simulated gastric fluid, which should provide a high oral bioavailability for the lipophilic dietary ingredients.

The present invention relates to the formulations of ester derivatives of capsaicin and ester derivatives of myristoleic acid. These derivatives are capable of reverting to the active parent compound following enzymatic or chemical hydrolysis. These derivatives have a higher lipophilicity, lipid solubility and less irritation to the skin than the parent compound, and hence are better able to be incorporated into certain pharmaceutical formulations, including cream and ointment pharmaceutical formulations. The pharmaceutical compositions of the present invention contain a compound of following formula (Ia):R—CO-CAP   (Ia)wherein CAP refers to collectively the capsaicins represented in FIG. 1 and a compound of formula (Ib):MCO-O—R   (Ib)wherein MCO refers to myristoleic acid.In formulae Ia and Ib, R is selected from alkyl groups of up to about 18 carbon atoms and aryl groups of up to about 18 carbon atoms and alkylene group of up to about 18 carbon atoms and an arylene group of up to about 18 carbon atoms. The alkyl, aryl and alkylene groups may be substituted or un-substituted, branched or straight chains. In addition, R may contain heteroatoms and may be straight chained or branched.The pharmaceutical compositions containing compounds of formulae Ia and Ib are useful for pain management in mammals in vivo and have been contemplated to be used in the treatment of various pains in humans.

Gel-forming macromers including at least four polymeric blocks, at least two of which are hydrophobic and at least one of which is hydrophilic, and including a crosslinkable group are provided. The macromers can be covalently crosslinked to form a gel on a tissue surface in vivo. The gels formed from the macromers have a combination of properties including thermosensitivity and lipophilicity, and are useful in a variety of medical applications including drug delivery and tissue coating.

Methods for improving solubility and bioavailability of lipophilic compounds are described. Particularly, described are stabilized superstaturated solid solutions, particularly in power form, of lipophilic drugs, such as steroidal molecules.

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

Pharmaceutical compositions and methods of use of a composition containing a double-stranded RNA (dsRNA), cationic lipids, non-cationic lipids, and lipophilic delivery-enhancing compounds.

Gel-forming macromers including at least four polymeric blocks, at least two of which are hydrophobic and at least one of which is hydrophilic, and including a crosslinkable group are provided. The macromers can be covalently crosslinked to form a gel on a tissue surface in vivo. The gels formed from the macromers have a combination of properties including thermosensitivity and lipophilicity, and are useful in a variety of medical applications including drug delivery and tissue coating.

Improved performance in the phase separation of aqueous brines from hydrocarbons within an electrostatic desalter operation is obtained by the addition to the crude oil emulsions entering the desalter of an effective asphaltene dispersing amount of an alkyl phenol-formaldehyde liquid resin polymer, optionally in the presence of a lipophilic / hydrophilic vinylic polymer. The preferred resin is a nonyl phenol-formaldehyde resin having a molecular weight of from 1,000-20,000, and the preferred vinylic polymer is a copolymer of lauryl (meth)acrylate and hydroxyethyl (meth)acrylate. Best results from the electrostatic desalter are obtained when also using a demulsifier chemical treatment along with the asphaltene dispersing treatments. Desalter efficiency is increased and desalter brine effluent quality is greatly increased.

A magnetic coated carrier suitable for constituting a two-component type developer for use in electrophotography is composed of magnetic coated carrier particles comprising magnetic coated carrier particles comprising magnetic carrier core particles each comprising a binder resin and metal oxide particles, and a coating layer surface-coating each carrier core particle. The metal oxide particles have been subjected to a surface lipophilicity-imparting treatment. The magnetic carrier core particles have a resistivity of at least 1x1010 ohm.cm, and the magnetic coated carrier has a resistivity of at least 1x1012 ohm.cm. The magnetic coated carrier has a particle size distribution such that (i) it has a number-average particle size Dn of 5-100 mu m, (ii) it satisfies a relationship of Dn / sigma > / =3.5, wherein sigma denotes a standard deviation of number-basis particle size distribution of the carrier, and (iii) it contains at most 25% by number of particles having particle sizes of at most Dnx+E,fra 2 / 3+EE .

This work describes a new class of short polypeptides that can self-assemble to form regular nanotubes with an average diameters of about 50 nm. These peptides (7 to 8 amino acids) have a structure very similar to those observed in surfactant molecules with a defined hydrophilic head group constituting of charged amino acids and a lipophilic tail made out of hydrophobic amino acids such as alanine, valine or leucine. Cryo-TEM micrographs show numerous three-fold junctions connecting the self-assembling nanostructures and thus leading to the formation of a rather dense network of entangled nanotubes. Additionally, the observation of clear openings at the end of the supramolecular structures confirms the presence of tubular organization.

The present invention relates to the formulations of ester derivatives of capsaicin and ester derivatives of myristoleic acid. These derivatives are capable of reverting to the active parent compound following enzymatic or chemical hydrolysis. These derivatives have a higher lipophilicity, lipid solubility and less irritation to the skin than the parent compound, and hence are better able to be incorporated into certain pharmaceutical formulations, including cream and ointment pharmaceutical formulations. The pharmaceutical compositions of the present invention contain a compound of following formula (Ia):R—CO—CAP  (Ia)wherein CAP refers to collectively the capsaicins represented in FIG. 1 and a compound of formula (Ib):MCO—O—R  (Ib)wherein MCO refers to myristoleic acid.In formulae Ia and Ib, R is selected from alkyl groups of up to about 18 carbon atoms and aryl groups of up to about 18 carbon atoms and alkylene group of up to about 18 carbon atoms and an arylene group of up to about 18 carbon atoms. The alkyl, aryl and alkylene groups may be substituted or un-substituted, branched or straight chains. In addition, R may contain heteroatoms and may be straight chained or branched.The pharmaceutical compositions containing compounds of formulae Ia and Ib are useful for pain management in mammals in vivo and have been contemplated to be used in the treatment of various pains in humans.

The invention relates to a fatty alcohol polyoxypropylene polyoxyethylene ether carboxylate, a preparation thereof and an application thereof. The structural general formula of the fatty alcohol polyoxypropylene polyoxyethylene ether carboxylate is RO(PO)n(EO)mCH2COOX, wherein R is an aliphatic alkyl group or an alkylphenyl group; (PO)n is polyoxypropylene; n is between 6 and 12; (EO)m is polyoxyethylene; m is between 1 and 4; X is an alkali metal, the fatty alcohol and the polyoxypropylene at the left terminal of the structural general formula are lipophilic groups; and polyoxyethylene and the carboxyl group at the right terminal of the structural general formula are hydrophilic groups. Polyoxypropylene is added to increase the lipophilicity of fatty alcohol carboxylate surfactants to adapt to the application of tertiary oil recovery, and a small amount of polyoxyethylene is added to adjust the hydrophilicity and simultaneously carboxylate fatty alcohol polyoxypropylene esters on condition that the current fatty alcohol raw material is unchanged.

The invention provides a preparation method of an oil-water separation material, which comprises the following steps: soaking a sponge material in a graphene oxide solution, taking out the obtained sponge material and centrifuging the sponge material, so that a graphene oxide coated sponge material is obtained; and carrying out a reduction reaction on the graphene oxide coated sponge material under the action of a reducing agent so as to obtain the oil-water separation material. The oil-water separation material prepared by using the method provided by the invention is a reduced graphene oxide coated sponge material, is coated with a graphene layer uniformly and tightly and has good rebound resilience and mechanical stability, and the reduced graphene oxide layer provides good hydrophobicity and lipophilicity, therefore, the preparation method disclosed by the invention can be applied to oil-water separation technologies.

The invention relates to the clay surface modification, in particular to modified clay with silane coupling agent grafted surface, preparation method and application thereof. The grafting modification of the silane coupling agent with a grafting amount of 0.2-5*10<-3> mol / gram clay is performed in solvent by using reactive hydroxyl group on a clay sheet layer. The inventive modified clay, in which the silane coupling agent is grafted on the clay sheet layer via the covalent bond, has strong thermostability and realizes clay functionalization while improving the clay surface lipophilicity. As the inventive clay has high thermostability and enhanced interaction with polymer, it can be used for the preparation of polymer / clay nanometer composite material to improve the clay dispersibility in the polymeric matrix for stripping and dispersing, thereby improving the performance of the composite material.

This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and / or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.

This invention provides a soluble inclusion complex formed of a water-insoluble lipophilic compound and an amphiphilic polymer and which demonstrated improved solubility and stability. The lipophilic compound within the inclusion complex may consist of pharmaceutical compounds, food additives, cosmetics, agricultural products and veterinary products. The invention also provides novel methods for preparing the inclusion complex, as well as a novel chemical reactor for forming the inclusion complex.