Herein described are deuterated catecholamine derivatives of the general Formula I

##STR00001##

wherein, R.sub.1 is deuterium, R.sub.2, and R.sub.3 are independently selected from hydrogen and deuterium and wherein at least one of R.sub.2 and R.sub.3 has a deuterium enrichment in the range from 0.02 mol % to 100 mol % deuterium, and wherein the deuterium enrichment of R.sub.2 and R.sub.3 is different from each other and that the difference between the deuterium enrichment of R.sub.2 and R.sub.3 is at least 5 percentage points, R.sub.4 is hydrogen, deuterium, C.sub.1 to C.sub.6-alkyl or C.sub.5 to C.sub.6-cycloalkyl, deuterated C.sub.1 to C.sub.6-alkyl or C.sub.5 to C.sub.6-cycloalkyl, or a group that is easily hydrolytically or enzymatically cleavable under physiological conditions, as well as their physiologically acceptable salts and their stereoisomers, enantiomers or diastereomers in optically pure form. The compounds can easily be prepared by mixing deuterated and non-deuterated compounds in a predefined ratio. The compounds show anti-Parkinson effect at lower doses and show lower side effects.

A drug dosage form is provided in the form of a solid tablet which is greater than 50% by weight the local anesthetic agent. The local anesthetic agent may be selected from the group consisting of an aminoamide, an aminoester, and a combination thereof. The drug tablet may be in the form of a mini-tablet which is greater than 70 wt % drug, with the balance being excipient. For example, the anesthetic agent may include lidocaine, in a salt or base form, combined with binder and lubricant excipients. Implantable drug delivery devices including the tablets are also provided, e.g., one or more of the drug tablets may be contained in a biocompatible housing. The drug tablets may be substantially cylindrical with flat end faces, and the device may have from 10 to 100 drug tablets aligned in the housing with the flat end faces of adjacent tablets abutting one another.

The present disclosure provides programmable osmotic-controlled oral compositions providing delayed release of a therapeutically acceptable amount of a drug. In certain embodiments, the programmable osmotic-controlled compositions of the disclosure provide a lag time that is independent of the presence or absence of food, type of food, pH, gastric emptying, and volume of gastric fluid. The programmable osmotic-controlled oral compositions of the disclosure comprise a multilayer core comprising a drug for controlled release, wherein the core is coated with a semipermeable membrane comprising an orifice and, optionally, an immediate release coating, comprising a drug for immediate release, over the semipermeable membrane. The multilayered core comprises a pull layer containing the drug and a push layer. The pull layer comprises at least two layers: a placebo layer for providing a desired lag time for the drug release; and an active layer containing the drug and providing a delayed controlled release of the drug. The compositions of the disclosure can be programmed to provide a desired and precise lag time, and release drug, after the lag time, at a rhythm, e.g., that matches the human circadian rhythm of a condition's symptoms and/or of the individual being treated in the application of the therapy to optimize therapeutic outcome and minimize side effects.

The present invention relates to an oral tablet for oromucosal delivery of biologically active compounds, the tablet comprising a sugar alcohol composition comprising one or more sugar alcohol particles in an amount of at least 20% by weight of the tablet, an ion-exchange composition comprising a plurality of particles of at least one water-soluble anionic mucoadhesive polymer loaded with a cationic biologically active compound.

The present disclosure provides programmable osmotic-controlled oral compositions providing delayed release of a therapeutically acceptable amount of a drug. The programmable osmotic-controlled compositions of the disclosure provide a lag time that is independent of the presence or absence of food, type of food, pH, gastric emptying, gastric motility, and volume and viscosity of gastric fluid. The compositions of the disclosure can be programmed to provide a desired and precise lag time, and release drug, after the lag time, at a rhythm, e.g., that matches the human circadian rhythm of a condition's symptoms and/or of the individual being treated in the application of the therapy to optimize therapeutic outcome and minimize side effects.

Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.

Disclosed are a Filipendula glaberrima alcoholic extract and solvent fractions fractionated therefrom or novel compounds 1 and 2 purely isolated from a Filipendula glaberrima ethyl acetate fraction that have an excellent inhibitory effect against HMG-CoA reductase activity, an excellent antioxidant effect and a remarkably excellent effect of suppressing the formation of foam cells in macrophages. Also, disclosed is a pharmaceutical composition or health food composition for treating, preventing and ameliorating vascular diseases, hypercholesterolemia, or heart diseases caused by hypercholesterolemia, or lowering blood cholesterol levels, containing, as active ingredients, the Filipendula glaberrima alcoholic extract and the solvent fractions or the novel compounds 1 and 2.

The present invention relates to oral pharmaceutical compositions comprising eluxadoline or a prodrug or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients, and process for the preparation thereof and administration of such compositions for irritable bowel syndrome (IBS-D).

The present invention disclosed herein provides synergistic nutritional neuroprotective compositions for ameliorating neural dysfunction. Particularly, the invention relates to synergistic, efficient, nutritional composition for comprising specific combination of decarboxylated L-arginine called agmatine sulphate and nicotinamide riboside chloride, wherein agmatine sulphate and nicotinamide riboside chloride are present in the weight ratio of 1:0.05 to 1:2 along with pharmaceutically acceptable excipients. More particularly, the present invention offers synergistic effect for ameliorating neural dysfunction encompasses cerebrovascular diseases, neurodevelopmental disorders, mood disorders, mental health disorders and like thereof.

The present disclosure provides methods for safe and efficacious administration of esketamine.