Gelling agent-based dosage form
The present invention generally relates to dosage forms for oral administration including one or more gelling agents. In particular, the present invention is directed to gelling agent-based dosage forms that are easily administered and taken, or swallowed. The present invention is also directed to gelling agent-based dosage forms that exhibit relatively low syneresis, are thermally stable, exhibit substantially constant active ingredient concentration, and/or exhibit one or more advantageous rheological properties. In particular, the present invention is directed to such gels containing one or more omega-3 fatty acids. The gelling agent-based dosage forms of the present invention are suitable for administration of a relatively large dose of active ingredient. The gelling agent-based dosage forms of the present invention are also suitable for administration of multiple active ingredients. Dosage forms of the present invention also provide tamper resistance and, thus, prevent recovery or diversion of active ingredients contained therein. The gelling agent-based dosage forms are also suitable for use as gastro-retentive and sustained release dosage forms.
1. An aqueous deformable gel emulsion composition, the emulsion comprising a lipophilic phase dispersed within a gelled aqueous phase, and an emulsifier, wherein the lipophilic phase comprises a lipophilic active ingredient, and the gelled aqueous phase comprises water and one or more gelling agents, wherein:
water constitutes from about 30 wt % to about 60 wt % of the composition;
the gelling agents consist essentially of xanthan gum, locust bean gum, iota-carrageenan, and gum tragacanth;
each of xanthan gum, locust bean gum, iota-carrageenan, and gum tragacanth constitutes from about 0.5 to about 1.5 wt % of the composition; and
the composition further comprises a source of calcium ions selected from the group consisting of calcium acetate, calcium chloride, calcium carbonate, calcium ascorbate, and combinations thereof in a proportion of from about 0.1 to about 1 wt %.
2. The composition of claim 1 wherein the weight ratio of the lipophilic phase to the aqueous phase is from about 0.25:1 to about 0.8:1.
3. The composition of claim 1 wherein the emulsifier is a non-ionic emulsifier selected from the group consisting of whey protein, lecithin, sorbitan mono-oleate, polyoxyethylene sorbitan mono-oleate, and combinations thereof.
4. The composition of claim 1 wherein the gel (i) has a Young's modulus (Pa/% strain) of from about 10 to about 95; and/or (ii) the gel has a Young's modulus (Pa/% strain) per unit composition surface area of from about 0.25 Pa/cm 2 to about 10 Pa/cm 2 .
5. The composition of claim 1 wherein the gel strength per unit composition surface area is from about 0.1 to about 1.75 kPa/cm 2 .
6. The composition of claim 1 wherein the gel has an extensibility of from about 50% to about 90%.
7. The composition of claim 1 wherein syneresis of the composition during storage under ambient conditions for 90 days is less than about 10%.
8. The composition of claim 1 wherein syneresis of the composition during storage under ambient conditions for 90 days is less than about 7%.
9. The composition of claim 1 wherein the composition exhibits a gel strength at its rupture point of at least 1 kPa.
10. The composition of claim 1 wherein the composition exhibits a gel strength at its rupture point of at least 10 kPa.
11. The composition of claim 1 wherein the composition exhibits a gel strength at its rupture point of from about 20 kPa to about 50 kPa.
12. The composition of claim 1 wherein the composition exhibits a melting point of at least 40° C.
13. The composition of claim 1 wherein the composition exhibits a gel strength at its rupture point of about 1 kPa and a melting point of at least 40° C.
14. The composition of claim 1 wherein the composition has a shape selected from the group consisting of cylindrical, spherical, oval, rectangular, and square.
15. The composition of claim 1 wherein water constitutes from about 30 wt % to about 50 wt % of the composition.
16. The composition of claim 1 wherein the source of calcium ions is calcium chloride.
17. The composition of claim 16 wherein calcium chloride is present in a proportion of from about 0.2 to about 0.6 wt %.
18. An aqueous deformable gel emulsion composition, the emulsion comprising a lipophilic phase dispersed within a gelled aqueous phase, and an emulsifier, wherein the lipophilic phase comprises a lipophilic active ingredient, and the gelled aqueous phase comprises water and one or more gelling agents, wherein:
water constitutes from about 30 wt % to about 60 wt % of the composition;
the gelling agents consist essentially of xanthan gum, locust bean gum, iota-carrageenan, and gum tragacanth, each of xanthan gum, locust bean gum, iota-carrageenan, and gum tragacanth constituting from about 0.5 to about 1.5 wt % of the composition;
the composition further comprises calcium chloride in a proportion of from about 0.1 to about 1 wt %; and
the composition exhibits a gel strength at its rupture point of at least 1 kPa and a melting point of at least 40° C.