Composition for the management of nausea and vomiting

摘要

A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I);
wherein R is H, PO3- or
;
The system exhibits an improved pharmacokinetic profile relative to the current Diclectin®/Diclegis® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP).

主权项

1. A method for alleviating the symptoms of nausea and vomiting in a human subject, said method comprising administering to a human subject in need thereof pharmaceutical dosage form comprising the following (I) or (II):
(I)
(A) a core consisting of:
(a) about 10 mg of Doxylamine or a pharmaceutically acceptable salt thereof;(b) about 10 mg of Pyridoxine or a pharmaceutically acceptable salt thereof; and(c) about 40 mg of a riboflavin compound selected from riboflavin, riboflavin-5-phosphate and flavin adenine dinucleotide, or a pharmaceutically acceptable salt thereof; and(d) one or more pharmaceutically acceptable excipients;(B) a delayed release coating surrounding said core;(C) an immediate release component surrounding said delayed release coating and consisting of:
(a) about 10 mg of Doxylamine or a pharmaceutically acceptable salt thereof;(b) about 10 mg of Pyridoxine or a pharmaceutically acceptable salt thereof; and(c) one or more pharmaceutically acceptable excipients and/or coatings; or (II)
(A) a core consisting of the following ingredients:
(a) about 10 mg of Doxylamine or a pharmaceutically acceptable salt thereof;(b) about 10 mg of Pyridoxine or a pharmaceutically acceptable salt thereof; and(c) one or more pharmaceutically acceptable excipients;(B) a delayed release coating surrounding said core;(C) an immediate release component surrounding said delayed release coating and consisting of:
(a) about 10 mg of Doxylamine or a pharmaceutically acceptable salt thereof;(b) about 10 mg of Pyridoxine or a pharmaceutically acceptable salt thereof;(c) about 40 mg of a riboflavin compound selected from riboflavin, riboflavin-5-phosphate and flavin adenine dinucleotide, or a pharmaceutically acceptable salt thereof; and(d) one or more pharmaceutically acceptable excipients and/or coatings.