Enterically Coated Solid Dosage Forms for Targeted Small Intestine Release

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Solution Overview

Problem

Current pharmaceutical dosage forms lack efficient targeting and release mechanisms in the small intestine, leading to suboptimal therapeutic efficacy and physiological effects, particularly when administering bacterial agents or microbial extracellular vesicles.

Innovation Solution

Development of enterically coated solid dosage forms, such as capsules, tablets, and minitablets, that allow controlled release of pharmaceutical agents in the small intestine, utilizing enteric coatings like polymethacrylate-based copolymers and methacrylic acid ethyl acrylate copolymers to target immune cells and epithelial cells, enhancing therapeutic efficacy and reducing doses required.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If non-enterically coated dosage forms are used, then the dosage form is simpler to manufacture, but therapeutic efficacy is reduced

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoiddosage form structure

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The enteric coating is applied in advance to the solid dosage form core before administration. This preliminary protective layer prevents premature release of the pharmaceutical agent in the stomach, ensuring the agent reaches the small intestine intact for optimal therapeutic effect.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The enteric coating acts as an intermediary layer between the pharmaceutical agent and the gastrointestinal environment. This coating material selectively permits passage only under specific conditions (intestinal pH), mediating the release of the active ingredient at the appropriate location.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If higher doses of pharmaceutical agent are administered, then therapeutic efficacy may be improved, but the dose required is higher

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoiddose of pharmaceutical agent

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The invention changes the environmental parameter (pH) at which the pharmaceutical agent is released. The enteric coating is designed to remain intact in acidic stomach conditions and dissolve at the higher pH of the small intestine, thereby changing the release parameters to achieve better therapeutic outcomes at lower doses.

Inventive Principle:

Principle #35Parameter changes

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 enterically coated solid dosage forms achieve 10-fold or more increased therapeutic efficacy and physiological effects compared to non-enterically coated forms, allowing for targeted delivery and systemic effects outside the gastrointestinal tract with reduced doses.

Implementation Method 1

enterically coated solid dosage forms... that allow controlled release of pharmaceutical agents in the small intestine

Methodology Applied

Scientific EffectpH-dependent solubility:

Implementation Method 2

enteric coatings like polymethacrylate-based copolymers and methacrylic acid ethyl acrylate copolymers to target immune cells and epithelial cells

Methodology Applied

Scientific Effectcontrolled dissolution:

Data Source

PatentUS20230355689A1Solid dosage forms containing bacteria and microbial extracellular vesicles

Publication Date: 2023.11.09 EVELO BIOSCIENCES INC

AI summary

Enterically-coated solid dosage forms containing a pharmaceutical agent which includes bacteria and/or microbial extracellular vesicles (mEVs) are provided. Methods of treatment using such solid dosage forms are also provided.