Abstract: The present invention relates to hydroxynorketamine for the use in the treatment of depression. In particular, the present invention concerns hydroxynorketamine for use in the treatment of depression, wherein hydroxynorketamine is administered in form of at least one prodrug, and wherein the at least one prodrug is orally administered in a modified-release dosage form.

Abstract: The present invention relates to hydroxynorketamine for the use in the treatment of depression. In particular, the present invention concerns hydroxynorketamine for use in the treatment of depression, wherein hydroxynorketamine is administered in form of at least one prodrug, and wherein the at least one prodrug is orally administered in a modified-release dosage form. The prodrug is selected from (S)-Ketamine, (R)-Ketamine, (R,S)-Ketamine, (S)-Norketamine, (R)-Norketamine, (R,S)-Norketamine, (S)-Hydroxyketamine, (R)-Hydroxyketamine, (R,S)-Hydroxyketamine.

Abstract: The present invention relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day.

Abstract: A method for treating depression in patients with depression and bipolar disorder who have not responded to antidepressants and to avoid dose dumping upon ingestion of alcohol. The present invention also relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day.

Abstract: The present invention relates to a solid oral pharmaceutical dosage form with a novel and well defined order of specific coatings allowing for the very defined and controlled release of at least one pharmaceutical active ingredient (API) and a broad range of potential uses. Particularly, the dosage form according to the invention comprises an immediate release active core, a first delayed-release layer comprising an enteric coating, a second sustained release layer comprising a retard polymer, and a third immediate release layer comprising an active pharmaceutical ingredient. The solid oral pharmaceutical dosage form as such is characterized in having a bi-modal release profile of the at least one API with a much less variable second delayed release than known prior art pharmaceutical compositions, allowing for the application of different APIs or combinations thereof in for a variety of indications.

Abstract: The present invention relates to hydroxynorketamine for the use in the treatment of depression. In particular, the present invention concerns hydroxynorketamine for use in the treatment of depression, wherein hydroxynorketamine is administered in form of at least one prodrug, and wherein the at least one prodrug is orally administered in a modified-release dosage form. The prodrug is selected from (S)-Ketamine, (R)-Ketamine, (R,S)-Ketamine, (S)-Norketamine, (R)-Norketamine, (R,S)-Norketamine, (S)-Hydroxyketamine, (R)-Hydroxyketamine, (R,S)-Hydroxyketamine.

Abstract: A method for treating depression in patients with depression and bipolar disorder who have not responded to antidepressants and to avoid dose dumping upon ingestion of alcohol. The present invention also relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day.

Abstract: The present invention relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day.

Abstract: The invention relates to a method of treatment using a solid oral pharmaceutical dosage form comprising an opioid receptor antagonist for use in the treatment of opioid induced constipation comprising the opioid antagonist equivalent to 24 mg of naloxone hydrochloride as twice daily formulation or equivalent to 48 mg of naloxone hydrochloride as once daily formulation, characterized in that the opioid antagonist has a rapid first pass metabolism with a plasma half-life of 2 hours or less in humans within the first 3 hours of oral administration of a solution, wherein the steady state pharmacokinetics result in a constant level of naloxone in the bloodstream, wherein the pharmacokinetics are independent of whether the dosage is administered once or twice daily, wherein the oral dosage form releases the opioid antagonist in a prolonged manner, wherein the in vitro release rate of the opioid antagonist measured using the paddle stirrer method according to Ph. Eur. at 75 rpm in 1000 ml 0.

Abstract: The present invention relates to a solid oral pharmaceutical composition comprising naloxone, or a pharmaceutical acceptable salt thereof, as an active substance, wherein the composition releases the active substance in a prolonged manner. In order to provide a composition that is suitable for an administration period of at least twelve-hours for the treatment of opioid-induced constipation, it is proposed that the composition should have an in vitro release rate of the active substance measured using the paddle stirrer method according to Ph. Eur. at 75 rpm in 500 ml 0.1 N hydrochloric acid at 37° C., of 0% to 75% in 2 h, of 3% to 95 % in 4 h, of 20% to 100% in 10 h, of 30% to 100% in 16 h, of 50% to 100% in 24 h, and of more than 80% in 36 h, wherein the composition has a IC50/Cmax value of at least 40. In an alternative embodiment, the composition can be a multilayer tablet.

Abstract: The invention relates to a method of treatment using a solid oral pharmaceutical dosage form comprising an opioid receptor antagonist for use in the treatment of opioid induced constipation comprising the opioid antagonist equivalent to 24 mg of naloxone hydrochloride as twice daily formulation or equivalent to 48 mg of naloxone hydrochloride as once daily formulation, characterized in that the opioid antagonist has a rapid first pass metabolism with a plasma half-life of 2 hours or less in humans within the first 3 hours of oral administration of a solution, wherein the steady state pharmacokinetics result in a constant level of naloxone in the bloodstream, wherein the pharmacokinetics are independent of whether the dosage is administered once or twice daily, wherein the oral dosage form releases the opioid antagonist in a prolonged manner, wherein the in vitro release rate of the opioid antagonist measured using the paddle stirrer method according to Ph. Eur. at 75 rpm in 1000 ml 0.

Abstract: The present invention relates to an oral dosage form for administration of ketamine and a method of preparing an oral dosage form for administration of ketamine, preferably once or twice a day.

Abstract: The present invention relates to a solid oral pharmaceutical composition comprising naloxone, or a pharmaceutical acceptable salt thereof, as an active substance, wherein the composition releases the active substance in a prolonged manner. In order to provide a composition that is suitable for an administration period of at least twelve-hours for the treatment of opioid-induced constipation, it is proposed that the composition should have an in vitro release rate of the active substance measured using the paddle stirrer method according to Ph. Eur. at 75 rpm in 500 ml 0.1 N hydrochloric acid at 37° C., of 0% to 75% in 2 h, of 3% to 95 % in 4 h, of 20% to 100% in 10 h, of 30% to 100% in 16 h, of 50% to 100% in 24 h, and of more than 80% in 36 h, wherein the composition has a IC50/Cmax value of at least 40. In an alternative embodiment, the composition can be a multilayer tablet.

Abstract: The present invention relates to a solid oral pharmaceutical composition comprising naloxone, or a pharmaceutically acceptable salt thereof, as an active substance, wherein the composition releases the active substance in a prolonged manner. In order to provide a composition that is suitable for an administration period of at least twelve-hours for the treatment of opioid-induced constipation, it is proposed that the composition should have an in vitro release rate of the active substance measured using the paddle stirrer method according to Ph. Eur. at 75 rpm in 500 ml 0.1 N hydrochloric acid at 37° C., of 0% to 75% in 2 h, of 3% to 95% in 4 h, of 20% to 100% in 10 h, of 30% to 100% in 16 h, of 50% to 100% in 24 h, and of more than 80% in 36 h, wherein the composition has a IC50/Cmax value of at least 40. In an alternative embodiment, the composition can be a multilayer tablet.

Abstract: The present invention relates to a pharmaceutical composition comprising an opioid receptor antagonist, or a derivative or a pharmaceutically acceptable salt thereof, as an active substance, wherein the composition releases the active substance in a prolonged manner. The composition that is suitable for an administration period of at least twelve-hours for the treatment of severe opioid-induced constipation in patients receiving a daily dosage of opioid equivalent to at least 80 mg of morphine.

Abstract: The present invention relates to a composition comprising an opioid receptor antagonist in an extended release formulation for use in treating a patient with severe constipation characterised by a defined whole gut transit time.

Abstract: The present invention relates to a pharmaceutical composition comprising a ?-receptor antagonist as an active substance, wherein the antagonist is prepared in an extended release formulation. The composition is intended for the treatment of patients with opioid-induced constipation, wherein the dosage of the ?-receptor agonist is independent of the opioid dosage. The preferred dosage of the ?-receptor antagonist of the composition is equivalent to a daily dosage of 20-70 mg naloxone.

Abstract: The present invention relates to a controlled-release oral dosage form for administration of oxycodone once a day and a method of preparing a controlled-release oral dosage form for administration of oxycodone once a day.

Abstract: The present invention relates to a solid oral pharmaceutical composition comprising naloxone, or a pharmaceutically acceptable salt thereof, as an active substance, wherein the composition releases the active substance in a prolonged manner. In order to provide a composition that is suitable for an administration period of at least twelve-hours for the treatment of opioid-induced constipation, it is proposed that the composition should have an in vitro release rate of the active substance measured using the paddle stirrer method according to Ph. Eur. at 75 rpm in 500 ml 0.1 N hydrochloric acid at 37° C., of 0% to 75% in 2 h, of 3% to 95% in 4 h, of 20% to 100% in 10 h, of 30% to 100% in 16 h, of 50% to 100% in 24 h, and of more than 80% in 36 h, wherein the composition has a IC50/Cmax value of at least 40. In an alternative embodiment, the composition can be a multilayer tablet.

Abstract: The present invention relates to a controlled-release oral dosage form for administration of oxycodone once a day and a method of preparing a controlled-release oral dosage form for administration of oxycodone once a day.