The disclosure provides an effervescent composition adapted for oral use, the composition including an effervescent material; one or more fillers in a total amount of at least about 30% by weight, the one or more fillers including at least one sugar alcohol; at least one active ingredient; and optionally, a lipid in an amount of at least about 20% by weight. Melting effervescent compositions are also provided, which include the lipid.

The present disclosure concerns effervescent compositions and methods of making and using the same. In some embodiments, the disclosed effervescent compositions are formed from an input blend comprising an acid and a base by granulating the input blend in a twin-screw processor. The granules formed from the input blend can be formed by an in situ granulating agent, which can be a portion of the acid that melts during granulation. In some embodiments, the effervescent compositions can be made using a twin-screw processor comprising an intake zone for receiving an input blend comprising an acid and a base; a granulation initiation zone for melting only a portion of the acid to serve as an in situ granulating agent; a granulation completion zone for granulating the input blend; and an outlet for discharging the granules.

The disclosure relates to an effervescent therapeutic composition for delivering multiple compounds to a patient in a single administration. In some embodiments, the effervescent therapeutic composition includes an alkaline effervescing compound, one or more compressible binders, a pharmaceutically acceptable salt of metformin, a pharmaceutically acceptable cobalamin, and an acid compound or an acid salt. In other embodiments, the effervescent therapeutic composition may include a folate or folic acid and metformin. In yet other embodiments, the effervescent therapeutic composition may include a folate or folic acid, cobalamin, and metformin.

Separable microneedle arrays and microneedle patches are provided that may achieve sustained release of drug. The microneedle arrays may include one or more features that facilitate separation of the microneedles, such as a bubble structure. The microneedle arrays may include an effervescent material.

The present disclosure is directed to floating gastroretentive dosage forms with prolonged gastric residence time. The disclosure also provides rapidly expanding sustained release or combined immediate release and sustained release formulations comprising drugs that require targeted release in the proximal gastrointestinal tract for maximum therapeutic benefit. The rapidly expanding floating gastroretentive dosage forms comprise a permeable elastic membrane providing desired characteristics for drug release and mechanical strength to maintain tablet integrity.

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.

The present invention includes a method for the treatment of age-related macular degeneration, glaucoma, or diabetic retinopathy in a human that comprises administering to the human a therapeutically effective amount of N-acetylcysteine amide (NACA) or (2R,2R′)-3,3′-disulfanediyl bis(2-acetamidopropanamide) (diNACA) sufficient to treat or reduce the symptoms of the age-related macular degeneration, glaucoma, or diabetic retinopathy.

A capsule device with thermally-stable specific gravity control is disclosed. The capsule device comprises a capsule unit adapted to be swallowable by a human subject and an inflatable balloon comprising a thermally-stable effervescent formulation inside the inflatable balloon, where the thermally-stable effervescent formulation has a particular particle size between a first mesh size and a second mesh size, and the inflatable balloon is attached to the capsule unit. After the capsule unit with the inflatable balloon attached is swallowed, the inflatable balloon starts to inflate so as to lower specific gravity of a combination of the capsule unit and the inflatable balloon when the inflatable balloon is exposed to body fluid and the body fluid gets in touch with the thermally-stable effervescent formulation inside the inflatable balloon.

Provided herein is an amorphous compound represented by Formula (I): ##STR00001##
and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.

The present invention relates to effervescent compositions of Metformin and optionally other anti-diabetic agents and processes for preparation thereof. More particularly provides an effervescent composition comprising Metformin, an acid and a base such that the composition is free of affirmatively added binders and granulating solvents. The effervescent composition of the present invention has retained carbon dioxide content of at least 90% of the input blend.