TH51654A - Omeprazole pharmaceutical formulation - Google Patents

Abstract

DC60 (27/03/55) An enteric-coated pharmaceutical formulation for oral administration containing an active ingredient selected from the omeprazole group, alkaline salts of omeprazole, (-)-enanchiomer of omeprazole, and alkaline salts of (-)-enanchiomer of omeprazole, the formulation incorporates a core material of the active ingredient and may include an alkaline-reactive compound. The active ingredient is contained within a pharmaceutically acceptable mixture of components, such as binders, and the core material is a separating layer and an enteric coating. Low-viscosity hydroxypropyl methylcellulose (HPMC) with a specific clouding point is used in the manufacture of the pharmaceutical formulation. Furthermore, the application describes the process for its preparation and the use of the patented formulation. Oral enteric-coated pharmaceutical formulations contain an active ingredient selected from the omeprazole group, alkaline salts of omeprazole, (-)-enanchiomers of omeprazole, and alkaline salts of (-)-enanchiomers of omeprazole. The formulation incorporates a core material of the active ingredient and may include an alkaline-reactive compound. The active ingredient is contained within a pharmaceutically acceptable mixture of components such as binders, and the core material forms a separating layer and an enteric coating. Low-viscosity hydroxypropyl methylcellulose (HPMC) with a specific clouding point is used in the manufacture of pharmaceutical formulations. Furthermore, the processes for its preparation and the use of the patented formulations are described.

Claims (20)

1. An enteric coated formulation for oral administration, comprising (a) a core material incorporating an active ingredient selected from the group containing omeprazole, alkaline salts of omeprazole (-), enaziomer of omeprazole, and alkaline salts of (-) enaziomer, and possibly a binder in the active ingredient mixture; (b) a separation layer; and (c) an enteric coating layer in which one or more formulation components selected from the binder group and the separation layer are incorporating low-viscosity hydroxypropyl methylcellulose (HPMC) with a minimum clouding point of 45.6 and where the transmittance at the clouding point of the system is 45.6. The HPMC, which is incorporated into the sample, was dissolved at a concentration of 1.2% (w/w) in a mixed solution of 0.235 M phosphate buffer and gastric fluid simulated to pH 1.2 in a 4:5 ratio. The resulting pH of 6.75-6.85 was 96%. 2. Oral enteric coated formulations comprising (a) a core material incorporating an active ingredient selected from the group containing omeprazole, alkaline salts of omeprazole, (-)-enanziomer of omeprazole, and alkaline salts of (-)-enanziomer, and possibly a binder in the active ingredient mixture; (b) a separation layer; and (c) an enteric coating layer in which one or more formulation components selected from the binder group and the separation layer consist of low-viscosity hydroxypropyl methylcellulose (HPmC) with a minimum clouding point of 44.5 °C and where the transmittance at the clouding point of the system The HPMC, which is incorporated into the sample, was dissolved at a concentration of 1.0% (w/w) in a mixed solution of 0.235 M phosphate buffer and gastric fluid simulated to pH 1.2 in a 4:5 ratio, resulting in a pH of 6.75-6.85, equivalent to 95%. 3. A formulation pursuant to claim 1 or 2, in which the core material is further incorporated with an alkaline-reactive compound. 4. A formulation pursuant to claim 1 or 2, which contains an additional active ingredient in the mixture, along with a pharmaceutically acceptable base mixture selected from a group comprising surfactants, fillers, dispersants, alkaline additives, and mixtures of these. 5. The process for the manufacture of oral teric-coated pharmaceutical formulations under Patent 1 or 2, which comprises the following steps: (a) formation of a core material incorporating the active ingredient and possibly a selectable binder; (b) application of a segregation layer onto the core; and (c) application of an enteric coating layer onto the segregation-coated core, where one or more formulation structures are selected from groups containing the binder and the segregation layer composed of low-viscosity HPMC. 6. The process under claim 5, in which an alkaline-reactive compound is mixed with the active ingredient and a binder may be selected to form the core material. 7. A formulation under Patent 2 in which the separation layer consists of low-viscosity HPMC. 8. The formulation under Patent 2, in which the enterid coating consists of methacrylic acid polymer. 9. The formulation under claim 2, where the binder is low-viscosity HPMC. 10. A formulation pursuant to Patent 2 in which a low-viscosity HPMC has a viscosity less than 7.2 cps3 in a 2% aqueous solution. 11. The formulation under claim 2, where the active ingredient is omeprazole. 12. The formulation under claim 2, where the active ingredient is the magnesium salt of omeprazole. 13. The formulation under claim 2, where the active ingredient is the magnesium salt of (-)-enanchiomer. 14. A formulation under claim 1 or 2 where the separation layer is low-viscosity HPMC. 15. A formulation pursuant to claim 14 in which the anterid coating is composed of a methacrisic acid polymer. 16. A formulation pursuant to claim 1 or 2, where the binder is low-viscosity HPMC. 17. A formulation pursuant to claim 1 or 2 where low-viscosity HPmC has a viscosity less than 7.2 cps in a 2% aqueous solution. 18. A formulation pursuant to claim 1 or 2, where the active ingredient is omeprazole. 19. A formulation pursuant to claim 1 or 2 where the active ingredient is the magnesium salt of omeprazole. 20. A formulation pursuant to claim 1 or 2 where the active ingredient is a magnesium salt of (-)-enanchiomer.