Oral Liquid Herbal Formulation for Berberine Solubility

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Solution Overview

Problem

Existing formulations of berberine for respiratory diseases face challenges in solubility, bioavailability, and stability, especially in solid oral dosage forms, and there is a need for stable syrup formulations that can combine multiple herbal extracts effectively.

Innovation Solution

A novel oral liquid pharmaceutical composition combining berberine or its pharmaceutically acceptable salt form with pelargonium sidoides and propolis, using a diluent system of propylene glycol and glycerin, along with additional herbal extracts and a buffer system to enhance solubility and stability, while controlling pH and toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If berberine is formulated in solid oral dosage forms, then it is easier to manufacture and administer, but its solubility and bioavailability are reduced

Engineering Contradiction:
Improveease of manufactureVSAvoidbioavailability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the physical state of berberine from solid to liquid formulation, and adjusts the pH parameter to 3-6 to enhance solubility and bioavailability while maintaining manufacturing feasibility

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite liquid formulation combining berberine with multiple herbal extracts (Pelargonium sidoides, propolis, and others) in a synergistic combination that improves both bioavailability and therapeutic effect

Inventive Principle:
Principle #40Composite materials

2Reliability

If multiple herbal extracts are combined in liquid formulation, then efficacy and bioavailability are improved, but solubility and stability become more difficult to maintain

Engineering Contradiction:
ImproveefficacyVSAvoidstability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent controls pH within the range of 3-6 to maintain stability of multiple herbal extracts in liquid form while preserving their therapeutic efficacy and solubility characteristics

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses excipients as intermediary substances to facilitate the compatibility and stability of multiple herbal extracts in the liquid formulation, preventing precipitation and degradation

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If berberine is formulated with higher concentration for better efficacy, then therapeutic effect is improved, but solubility and stability are compromised

Engineering Contradiction:
ImproveefficacyVSAvoidstability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent optimizes the concentration of berberine within specific ranges (0.1-10 mg/mL) and adjusts pH to 3-6 to achieve the maximum therapeutic effect while maintaining solubility and long-term stability of the formulation

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 composition achieves improved bioavailability, stability, and ease of administration, ensuring the active ingredients are properly dissolved and maintaining long-term stability, addressing the limitations of previous formulations.

Implementation Method 1

using a diluent system of propylene glycol and glycerin, along with additional herbal extracts and a buffer system to enhance solubility and stability

Methodology Applied
Scientific EffectSolubility enhancement through cosolvent system: Solvation

Implementation Method 2

using a diluent system of propylene glycol and glycerin, along with additional herbal extracts and a buffer system to enhance solubility and stability, while controlling pH and toxicity

Methodology Applied
Scientific EffectpH buffering:

Data Source

PatentEP2937077B1Oral liquid formulations comprising herbal extracts
Publication Date: 2021.10.06 MONTERO GIDA SANAYI VE TICARET

AI summary

The present invention relates to an herbal formulation comprising berberine and at least one more herbal extract for providing treatment in various respiratory diseases such as cold, cough, allergic asthma, seasonal allergic rhinitis, bronchitis, pharyngitis, laryngitis and pneumonitis.