A61K9/1617

DRY POWDER COMPOSITIONS OF TREPROSTINIL PRODRUGS AND METHODS OF USE THEREOF
20220409537 · 2022-12-29 · ·

The present disclosure provides a dry powder composition of treprostinil prodrugs and a method of treating pulmonary hypertension (e.g., pulmonary arterial hypertension), portopulmonary hypertension, or pulmonary fibrosis in a patient in need thereof. The dry powder composition includes (a) from about 0.1 wt % to about 3 wt % of a compound of Formula (I):

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or an enantiomer, diastereomer, or a pharmaceutically acceptable salt thereof, (b) from about 0.01 wt % to about 3 wt % of DSPE-PEG2000, (c) from about 10 wt % to about 50 wt % of leucine, and the balance being (d) a sugar selected from the group consisting of trehalose and mannitol. The entirety of (a), (b), (c), and (d) is 100 wt %, and R.sup.1 is tetradecyl, pentadecyl, hexadecyl, heptadecyl, or octadecyl. The method includes administering an effective amount of the dry powder composition to the lungs of the patient by inhalation via a dry powder inhaler. In certain compositions and methods provided herein, R.sup.1 is hexadecyl, e.g., linear hexadecyl.

Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
11795168 · 2023-10-24 · ·

The present disclosure is directed to solid and salt forms of inhibitors of the CBP/p300 family of bromodomains made up of salts and crystalline forms of Formula (I). The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains (e.g., certain forms of cancer), and methods of synthesis of these compounds.

Functionalized microbubble embodiments for ultrasound-mediated treatment and methods of making and using the same

Disclosed herein are embodiments of a functionalized microbubble designed for treating and/or preventing vascular obstructions, including microvascular obstructions. The functionalized microbubble embodiments comprise a microbubble that can be activated upon exposure to ultrasound and further that has a lipid-based shell that is attached to an exteriorly-attached therapeutically active agent, such as a thrombolytic agent. Also disclosed herein are embodiments of a method for making and using the functionalized microbubble embodiments.

PRODUCTION OF ENCAPSULATED NANOPARTICLES AT COMMERCIAL SCALE

The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.

SOLID PREPARATION, METHOD FOR PRODUCING SOLID PREPARATION, AND METHOD FOR GENERATING HYDROGEN

One solid preparation of the present invention mainly includes silicon fine particles, and has a capability of generating hydrogen. In addition, one specific example of the solid preparation mainly includes silicon fine particles having a crystallite diameter principally of 1 nm or more and 100 nm or less, and exhibits a capability of generating hydrogen in an amount of 3 ml/g or more when brought into contact with a water-containing liquid having a pH value of 7 or more. In this solid preparation, hydrogen is generated when the silicon fine particles are brought into contact with a water-containing liquid having a pH value of 7 or more. Therefore, taking advantage of the characteristics of the solid preparation, generation of hydrogen is promoted in, for example, a gastrointestinal tract where the pH value is 7 or more due to secretion of pancreatic fluid after passage through the stomach after oral ingestion.

INTRANASAL DELIVERY OF OLANZAPINE BY PRECISION OLFACTORY DEVICE

Methods are provided for acute treatment of agitation, including agitation in patients with schizophrenia or bipolar disorder, comprising administering to a subject with agitation an effective dose of a dry pharmaceutical composition comprising olanzapine, wherein the dose is administered by an intranasal delivery device that provides, following intranasal administration, (a) a mean peak plasma olanzapine concentration (C.sub.max) of at least 30 ng/mL, with (b) a mean time to C.sub.max (T.sub.max) of olanzapine of less than 0.5 hours. Dry pharmaceutical compositions and devices suitable for intranasal delivery of olanzapine are provided.

SELF-ASSEMBLED GELS FOR CONTROLLED DELIVERY OF BIOLOGICS AND METHODS OF MAKING THEREOF

Gels are formed based on generally recognized as safe (GRAS) low molecular weight amphiphilic molecules in a self-assembly process. Therapeutic or prophylactic agents, such as biological macromolecules, are loaded without exposure to temperatures and/or organic solvents which can degrade or destroy the biologic agents and/or their activity. The resulting self-assembled gel composition contains microstructures having pores and aqueous domains at their interior, rendering them permeable to hydrophilic and hydrophobic molecules. This permeability allows sequestration of the biological macromolecules. Once sequestered, the electrostatic, hydrophobic-hydrophobic etc. interactions between the biological macromolecules and the amphiphilic gelators keep the labile payload encapsulated with high stability until the microstructures are degraded.

Formulations and methods for contemporaneous stabilization of active proteins during spray drying and storage

A method of treatment of plasma with a physiologically compatible spray dry stable acidic substance (SDSAS) prior to or contemporaneously with spray drying of the plasma that results in greater recovery and greater long-term stabilization of the dried plasma proteins as compared to spray dried plasma that has not be subject to the formulation method of the present invention, as well as compositions related to plasma dried by the methods of the present invention.

Cationic lipids and transfection methods

The present invention relates in part to novel cationic lipids and their use, e.g., in delivering nucleic acids to cells.

MULTIPARTICULATE DOSAGE FORMS COMPRISING DEUTETRABENAZINE

Provided herein are controlled release multiparticulate dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile.