High loading and fast disintegration film for fast drug absorption
Inventors
XU, Jinjie • KWOK, Sau Kuen Connie • CHEUK, Wah Kit • Li, Ying • LAU, Pak Ho
Assignees
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Publication Number
US-11096892-B2
Publication Date
2021-08-24
Expiration Date
Abstract
A film forming composition comprises a film forming component and a solvent, wherein the film forming component comprises 0-50 wt % of a first water soluble polymer, 0.3-40 wt % of a second water soluble polymer, 0-15 wt % of plasticizer and 50-70 wt % of active ingredient. The first and second water soluble polymers have a Tg of −52° C. to 216° C., and difference of Tg values of the first and second water soluble polymer is 62-268° C. The film formed by the film forming composition capable to load high content of active ingredient and lead to fast absorption of active ingredient is provided.
Core Innovation
The invention relates to an oral topical orodissolving film composition for buccal or sublingual delivery. The film formulation uses a film forming component and a solvent to form a porous, thicker dry film that disintegrates fast and supports absorption.
The film forming component contains pullulan as a first water soluble polymer and PEO 200K as a second water soluble polymer, together with plasticizer. The film forming component has a defined Tg in the range of 20°C to 30°C, where pullulan has a Tg greater than 150°C and PEO 200K has a Tg less than 52°C.
The weight ratio of the first water soluble polymer to the second water soluble polymer is 34-35:1, and the plasticizer is present at 2.4-5.2% by weight, enabling the resulting film forming component Tg of 20°C to 40°C with reduced plasticizer content. The formulation further includes a filler selected as silk fibroin and at least one of disintegrating agent, sweetener, surfactant, and antifoaming agent.
A resulting film is formed such that its dry thickness is approximately 30-35% of the wet thickness, with controlled solvent content and a dry film thickness above about 265 µm. The described film structure and composition are supported by dissolution and disintegration performance, and comparative pharmacokinetic results are reported in Beagle dogs versus commercial oral tablets.
Claims Coverage
The document includes one independent claim directed to a film forming composition and specifies major quantitative relationships among the polymers, plasticizer, metoprolol tartrate, solvent ratio, and Tg; it also requires specific filler and film thickness behavior. Inventive features are defined by these quantified composition and film-formation parameters.
Tg-defined film forming component with pullulan and PEO 200K
A film forming component having a Tg of 20°C to 30°C, wherein the first water soluble polymer is pullulan with a Tg greater than 150°C, the second water soluble polymer is PEO 200K with a Tg less than 52°C, and the ratio of the first water soluble polymer to the second water soluble polymer is 34-35:1.
Quantified composition amounts including metoprolol tartrate
A film forming composition comprising a film forming component and a solvent, wherein the film forming component comprises 30-35% by weight of a first water soluble polymer, 0.5-1% by weight of a second water soluble polymer, 2.4-5.2% by weight of plasticizer and 50%-70% by weight of metoprolol tartrate.
Film forming component to solvent weight ratio
A film forming composition wherein the weight ratio of the film forming component to the solvent is 1:0.5-3.
Filler and at least one adjuvant selected among disintegrating agent, sweetener, surfactant and antifoaming agent
The film forming component further comprises a filler and at least one of disintegrating agent, sweetener, surfactant and antifoaming agent.
Silk fibroin filler
Wherein the filler is silk fibroin.
Dry-to-wet thickness relationship
Wherein a resulting film has a dry thickness in approximately 30-35% of a wet thickness thereof.
Overall, claim coverage is focused on a Tg-defined film forming component that combines pullulan and PEO 200K in a specified ratio, contains quantified plasticizer and metoprolol tartrate, specifies the film forming component-to-solvent ratio, includes silk fibroin with at least one of several adjuvants, and requires that the resulting film dry thickness is approximately 30-35% of the wet thickness.
Stated Advantages
Enables high active ingredient loading while maintaining fast disintegration and absorption.
Provides fast disintegration and dissolution performance for an orodissolving film.
Shows improved pharmacokinetic performance versus commercial oral tablets in Beagle dogs, including faster absorption and higher plasma levels/AUC.
Documented Applications
Oral topical delivery in a buccal or sublingual form of an orodissolving film.
Buccal/sublingual administration for delivery of active ingredients including metoprolol tartrate and ibuprofen, as described in the provided content.
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