Modified Amylopectin Enteric Capsule for Intestinal Drug Delivery
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Solution Overview
Problem
Existing oral capsule technologies fail to effectively protect active ingredients from gastric juice degradation, leading to reduced therapeutic efficacy, as they lack targeted release mechanisms for the intestine and require organic solvents in capsule formation.
Innovation Solution
A modified amylopectin with replaced hydrogen atoms and an acid value of 35-180 mg KOH/g is developed, which is pH-sensitive and intestinal-enzyme-biodegradable, allowing for controlled drug release in the intestine by mixing an anhydride derivative with amylopectin, eliminating the need for organic solvents in capsule formation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional capsule materials are used, then capsule formation is simple, but active ingredients are damaged by gastric juice before absorption
Solution Approach 1:
The patent modifies the chemical structure of amylopectin by introducing carboxyl groups through reaction with anhydride derivatives, changing its solubility parameters to achieve pH-sensitive behavior. The modified amylopectin remains insoluble at gastric pH (1.2-3.0) but dissolves at intestinal pH (6.0-7.5), providing targeted protection and release of active ingredients without requiring organic solvents.
Solution Approach 2:
The patent creates a composite material system where modified amylopectin forms an enterosoluble capsule shell that combines the properties of natural polysaccharide biodegradability with pH-sensitive synthetic polymer behavior. This composite structure provides both protection against gastric juice and controlled release in the intestine through the unique properties of the chemically modified amylopectin.
2Reliability
If pH-sensitive synthetic polymers are used for intestine-target capsules, then protection against gastric juice is improved, but organic solvents are required in capsule formation
Solution Approach 1:
The patent changes the solubility parameters of natural amylopectin through chemical modification to achieve pH-sensitive behavior without requiring organic solvents. By introducing carboxyl groups, the modified amylopectin transitions from being water-soluble to pH-dependent solubility, enabling capsule formation in aqueous environments while maintaining intestinal targeting functionality.
Solution Approach 2:
The patent replaces expensive and environmentally problematic organic solvent-based systems with a water-based system using modified natural polysaccharide. The modified amylopectin capsule shell can be formed and dissolved using only water, eliminating the need for toxic organic solvents while maintaining the required protective and release functions.
3Ease of manufacture
If natural polysaccharide polymer is used as capsule material, then biodegradability is improved, but pH-sensitive properties are insufficient
Solution Approach 1:
The patent modifies the chemical parameters of natural amylopectin by introducing carboxyl groups through anhydride derivative reaction. This chemical modification changes the pH sensitivity profile of the natural polysaccharide, enabling it to remain stable at gastric pH and dissolve at intestinal pH, while preserving its biodegradability and eliminating the need for organic solvents.
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 modified amylopectin material provides enhanced protection against stomach acid and controlled release in the intestine, improving therapeutic efficacy and eliminating the use of organic solvents in capsule formation, thus offering a more effective and environmentally friendly intestine-targeted delivery system.
Implementation Method 1
The enterosoluble and intestinal-enzyme-biodegradable material with pH-sensitive properties is prepared by chemical modification of a natural polysaccharide polymer
Implementation Method 2
The enterosoluble and intestinal-enzyme-biodegradable material is developed. The enterosoluble and intestinal-enzyme-biodegradable material with pH-sensitive properties is prepared by chemical modification of a natural polysaccharide polymer (e.g., amylopectin) capable of degradation by intestinal enzymes
Implementation Method 3
at least one of hydrogen atoms is replaced by —CO—(CH2)n—COOH (n is 2-4) and the modified amylopectin has an acid value of 35-180 mg KOH/g or 36-178 mg KOH/g
Data Source
AI summary
An enterosoluble and intestinal-enzyme-biodegradable material is provided. The enterosoluble and intestinal-enzyme-biodegradable material includes a modified amylopectin, wherein at least one of hydrogen atoms is replaced by —CO—(CH2)n—COOH (n is 2-4) and the modified amylopectin has an acid value of 35-180 mg KOH/g. The disclosure also provides a method for preparing an enterosoluble and intestinal-enzyme-biodegradable material.