Oral Dosage Form with Drying Agent for Intestinal Bioavailability
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Solution Overview
Problem
Oral dosing of certain active agents, such as poorly absorbed or high molecular weight agents, is ineffective due to enzymatic degradation and limited transport across the intestinal epithelium, leading to insufficient blood concentration.
Innovation Solution
A pharmaceutically acceptable oral dosage form containing an active agent and a drying agent, with a protective coating, providing a drying effect at the intestinal site to enhance bioavailability, and a fluid uptake capacity of at least 20 g fluid per dosage form.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral dosing is used for poorly absorbed or high molecular weight active agents, then ease of administration and patient compliance are improved, but bioavailability and blood concentration are insufficient due to enzymatic degradation and limited transport
Solution Approach 1:
The drying agent is incorporated into the dosage form in advance to create a localized drying effect at the intestinal site upon administration. This preliminary preparation of the delivery system enables the drying effect to occur automatically when the dosage form reaches the intestine, addressing the bioavailability problem without requiring additional patient actions
Solution Approach 2:
The drying agent acts as an intermediary substance that mediates between the active agent and the intestinal environment. By absorbing excess fluid at the intestinal site, the drying agent creates favorable conditions for active agent absorption while protecting against enzymatic degradation, thus improving bioavailability without compromising ease of administration
2Reliability
If the intestinal environment is altered to improve absorption, then bioavailability increases, but the complexity of the dosage form increases
Solution Approach 1:
The drying agent is formulated to exert its effect locally at the intestinal site rather than systemically. This localized action creates the necessary drying environment precisely where needed for improved absorption, while the rest of the dosage form maintains simple characteristics suitable for oral administration
Solution Approach 2:
The drying agent modifies the physical parameter of fluid content in the intestinal environment locally. By changing the hydration state from wet to dry at the specific site of action, the system enhances absorption without requiring complex modifications to the overall dosage form structure or administration process
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The oral dosage form significantly increases the bioavailability of active agents by creating a localized drying effect, improving their absorption and reducing degradation, thereby achieving effective blood concentration.
Implementation Method 1
at least one drying agent capable of drying an area about the intestinal site... providing a drying effect in an area about the intestinal site where the active agent is to be delivered
Data Source
AI summary
A pharmaceutically acceptable oral dosage form for delivery of an agent to an intestinal site has one or more active agent regions having an active agent to be delivered to the intestinal site, one or more drying agent regions having at least one drying agent therein capable of drying an area about the intestinal site, the one or more drying agent regions being separate from the one or more active agent regions, and a protective coating at least partially covering a surface of the form. The dosage form has a fluid uptake capacity as measured for the entire dosage form when immersed in a fluid media according to a Dosage Form Fluid Uptake Assay of at least about 20 g fluid per dosage form.