Composition for the management of nausea and vomiting
View Patent ↗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, PO 3 − 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).
1. A 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;
(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.
2. The dosage form of claim 1 , wherein the riboflavin compound is riboflavin.
3. The dosage form of claim 1 , wherein the riboflavin compound is riboflavin-5-phosphate.
4. The dosage form of claim 1 , wherein the riboflavin compound is flavin adenine dinucleotide
5. The dosage form of claim 1 , wherein said Doxylamine or pharmaceutically acceptable salt thereof is Doxylamine succinate.
6. The dosage form of claim 1 , wherein said Pyridoxine or pharmaceutically acceptable salt thereof is Pyridoxine hydrochloride.
7. The dosage form of claim 1 , wherein said dosage form is in the form of a tablet, a pill, or a capsule.
8. The dosage form of claim 7 , wherein said dosage form is in the form of a tablet.
9. The dosage form of claim 1 , wherein:
(a) the Doxylamine or pharmaceutically acceptable salt thereof is Doxylamine succinate;
(b) the Pyridoxine or pharmaceutically acceptable salt thereof is Pyridoxine hydrochloride; and
(c) the riboflavin compound is riboflavin.
10. The dosage form of claim 1 , wherein said dosage form comprises:
(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;
(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.
11. The dosage form of claim 10 , wherein:
(a) the Doxylamine or pharmaceutically acceptable salt thereof is Doxylamine succinate;
(b) the Pyridoxine or pharmaceutically acceptable salt thereof is Pyridoxine hydrochloride; and
(c) the riboflavin compound is riboflavin.
12. The dosage form of claim 1 , wherein said dosage form comprises:
(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.
13. The dosage form of claim 12 , wherein:
(a) the Doxylamine or pharmaceutically acceptable salt thereof is Doxylamine succinate;
(b) the Pyridoxine or pharmaceutically acceptable salt thereof is Pyridoxine hydrochloride; and
(c) the riboflavin compound is riboflavin.
14. The dosage form of claim 1 , wherein a coating surrounds said delayed release coating.
15. The dosage form of claim 9 , wherein a coating surrounds said delayed release coating.