Pharmaceutical preparation in the form of a paste comprising an acid-labile active ingredient
View Patent ↗The present invention relates to the field of pharmaceutical technology and describes a pharmaceutical preparation in the form of a paste comprising an acid-labile active ingredient, in particular an acid-labile proton pump inhibitor. The invention also relates to processes for producing the paste. The paste is particularly suitable for administering acid-labile active ingredients to animals or to people who have difficulty taking solid dosage forms such as tablets or capsules.
1. A pharmaceutical preparation in a water-based paste form with a viscosity between 1000 and 200000 mPa.s (determined with a rotational viscometer) for oral administration of an acid-labile active ingredient where a plurality of individual active ingredient units are dispersed in a water-based gel-like base composed of one or more pharmaceutical excipients, wherein the individual active ingredient units are microspheres, wherein the acid-labile active compound is the sole active ingredient and is selected from the group consisting of an acid-labile proton pump inhibitor, a salt of an acid-labile proton pump inhibitor with a base and a hydrate of a salt of an acid-labile proton pump inhibitor with a base, and is present in the individual active ingredient units in a matrix composed of a mixture comprising at least one solid paraffin and one or more substances from the group of fatty alcohol, triglyceride and fatty acid ester, and wherein an enteric coating is absent.
2. The pharmaceutical preparation in water-based paste form for oral administration as claimed in claim 1 , where the acid-labile active ingredient is present in the individual active ingredient units i) in a matrix composed of a mixture comprising at least one fatty alcohol and at least one solid paraffin, ii) in a matrix composed of a mixture comprising at least one triglyceride and at least one solid paraffin or iii) in a matrix composed of a mixture comprising at least one fatty acid ester and at least one solid paraffin.
3. The pharmaceutical preparation as claimed in claim 1 , which is a preparation ready for use.
4. The preparation as claimed in claim 1 , where an excipient selected from the group consisting of flavoring substances, buffer substances, preservatives and hydrophilic additives is present.
5. The preparation as claimed in claim 4 , where the hydrophilic additives are selected from the group consisting of glycerol, polyethylene glycols and propylene glycols.
6. The preparation as claimed in claim 1 , wherein pantoprazole, a salt of pantoprazole, a solvate of pantoprazole or a salt thereof is present as acid-labile proton pump inhibitor.
7. The preparation according to claim 1 , wherein the proton pump inhibitor is pantoprazole sodium sesquihydrate, (−)-pantoprazole sodium sesquihydrate, pantoprazole magnesium dihydrate, omeprazole magnesium, omeprazole or esomeprazole magnesium.
8. The preparation according to claim 1 , wherein the microspheres are monomodal microspheres and have a particle size range of 50-400 μm.
9. The preparation according to claim 1 , wherein, in the mixture, one or more further excipients, selected from the group consisting of polymers, sterols and basic compounds, is/are present in the matrix of the individual active compound units.
10. The preparation according to claim 9 , wherein the polymer is selected from the group consisting of povidone, vinylpyrrolidone/vinyl acetate copolymer, polyvinyl acetate, cellulose ethers, cellulose esters, methacrylic acid/methyl methacrylate copolymer, methacrylic acid/ethyl methacrylate copolymer and mixtures thereof.
11. The preparation according to claim 1 , wherein the fatty alcohol is selected from the group consisting of cetyl alcohol, myristyl alcohol, lauryl alcohol, stearyl alcohol and mixtures thereof.
12. The preparation according to claim 1 , wherein the solid paraffin is paraffinum solidum or ozocerite.
13. The preparation as claimed in claim 1 , where the water-based gel-like base comprises a gel former selected from the group consisting of sheet silicates, carrageenans, xanthan, gum acacia, alginates, alginic acids, pectins, carboxymethylcellulose, methylcellulose, hydroxypropylcellulose, methylhydroxypropylcellulose and poloxamers.
14. The preparation as claimed in claim 13 , wherein a mixture of two or more different gel formers are present.
15. The preparation as claimed in claim 13 , where the proportion of the gel former based on the preparation ready for use is from 0.05 to 20% by weight.
16. The preparation as claimed in claim 13 , where the proportion of the gel former based on the preparation ready for use is from 0.1 to 15% by weight.
17. The preparation as claimed in claim 13 , where the proportion of the gel former based on the preparation ready for use is from 0.4 to 10% by weight.
18. A process for manufacturing of a pharmaceutical preparation according to claim 13 , comprising introducing the individual active ingredient units into a dispersion of the gel former in water or introducing the gel former into a dispersion of the individual active ingredient units in water.