Formulation
A formulation having excellent gastric protection properties comprises an active pharmaceutical ingredient and a waxy compound, dispersed in a pharmaceutically acceptable oily carrier. The formulation presents a palatable and stable oral dosage form which is particularly suitable for acid-sensitive active pharmaceutical ingredients, and which is also suitable for active pharmaceutical ingredients which are liable to cause stomach irritation.
1. A liquid formulation for oral administration comprising an active pharmaceutical ingredient, a waxy compound, and a pharmaceutically acceptable oily carrier, characterised in that the active pharmaceutical ingredient is an acid-sensitive active pharmaceutical ingredient, and that in said formulation, particles comprising both said active pharmaceutical ingredient and said waxy compound are dispersed in said pharmaceutically acceptable oily carrier.
2. A liquid formulation as claimed in claim 1 , wherein the active pharmaceutical ingredient is a proton pump inhibiting compound.
3. A liquid formulation as claimed in claim 2 , wherein the active pharmaceutical ingredient is selected from omeprazole, lansoprazole, dexlansoprazole, esomeprazole, pantoprazole, rabeprazole and ilaprazole.
4. A liquid formulation as claimed in claim 3 , wherein the active pharmaceutical ingredient is omeprazole.
5. A liquid formulation as claimed in claim 1 , wherein the concentration of the active pharmaceutical ingredient is from 1 mg/ml to 10 mg/ml of the formulation.
6. A liquid formulation as claimed in claim 1 provided as a 5 ml unit dose containing from 5 to 50 mg of the active pharmaceutical ingredient.
7. A liquid formulation as claimed in claim 1 , wherein the waxy compound has a melting point range of from 40° C. to 80° C.
8. A liquid formulation as claimed in claim 1 , wherein the waxy compound has an HLB value of less than 5.
9. A liquid formulation as claimed in claim 1 , wherein the waxy compound is selected from a higher alkane; a lipid; a plant or animal wax; petrolatum wax; a long-chain aliphatic ester; a fatty acid that is solid at ambient temperature; an ester of dicarboxylic acid; and a polyethylene glycol that is solid at ambient temperature.
10. A liquid formulation as claimed in claim 9 , wherein the waxy compound is a long-chain mono- or di-glyceride or a mixture of such compounds.
11. A liquid formulation as claimed in claim 10 , wherein the waxy compound is a long-chain mono- or diglyceride containing fatty acid residues of length greater than 20 carbon atoms.
12. A liquid formulation as claimed in claim 9 , wherein the waxy compound is glyceryl behenate.
13. A liquid formulation as claimed in claim 12 , wherein the glyceryl behenate is a mixture of glyceryl monobehenate and glyceryl dibehenate.
14. A liquid formulation as claimed in claim 1 , wherein the pharmaceutically acceptable oily carrier comprises a triglyceride-based oil.
15. A liquid formulation as claimed in claim 14 , wherein the triglyceride-based oil is a vegetable oil or an analogous synthetic or semi-synthetic material, a mixture of such materials.
16. A liquid formulation as claimed in claim 15 , where in the vegetable oil is selected from castor oil, coconut oil, corn oil, ground nut oil, olive oil, palm oil, rapeseed oil, soybean oil, arachis oil, and sunflower oil.
17. A liquid formulation as claimed in claim 14 , wherein the triglyceride-based oil comprises purified or fractionated triglycerides selected from medium chain triglycerides containing fatty acid residues of 6-12 carbon atoms in length and long chain triglycerides containing acid residues of more than 12 carbon atoms in length.
18. A liquid formulation as claimed in claim 17 , wherein the triglyceride-based oil comprises predominantly medium-chain triglycerides.
19. A liquid formulation as claimed in claim 18 , wherein the medium-chain triglycerides are capric/caprylic triglycerides.
20. A liquid formulation as claimed in claim 1 , wherein the pharmaceutically acceptable oily carrier consists essentially of a triglyceride-based oil.
21. A liquid formulation as claimed in claim 20 , wherein the pharmaceutically acceptable oily carrier also comprises a waxy compound, wherein a major proportion of said carrier comprises the triglyceride-based oil and a minor proportion of said carrier comprises the waxy compound.
22. A liquid formulation as claimed in claim 21 , wherein the waxy compound is selected from a higher alkane; a lipid; a plant or animal wax; petrolatum wax; a long-chain aliphatic ester; a fatty acid that is solid at ambient temperature; an ester of dicarboxylic acid; and a polyethylene glycol that is solid at ambient temperature.
23. A liquid formulation for oral administration comprising an active pharmaceutical ingredient (API), a waxy compound, and a pharmaceutically acceptable oily carrier, characterised in that the API is a substance which may induce an adverse event upon a patient's stomach, and particles comprising said active pharmaceutical ingredient and said waxy compound are dispersed in said pharmaceutically acceptable oily carrier.
24. A method of treating a patient having or susceptible to a condition that may be ameliorated or prevented by an active pharmaceutical ingredient that is sensitive to the acidity of the patient's stomach, which method involves oral administration to the patient of a formulation according to claim 1 .
25. A method of treating a patient having or susceptible to a condition that may be ameliorated or prevented by an active pharmaceutical ingredient that may induce an adverse event upon a patient's stomach, which method involves oral administration to the patient of a formulation according to claim 1 .