Benzothiazole Macrogol Glyceride Formulations for Dissolution

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Solution Overview

Problem

Current pharmaceutical formulations of benzothiazole derivatives face challenges in solubility and bioavailability, particularly in treating autoimmune disorders and inflammatory conditions, due to their poor dissolution rates and absorption profiles.

Innovation Solution

Development of macrogol glyceride pharmaceutical formulations, specifically stearoyl macrogol glyceride formulations containing benzothiazole derivatives, which include the use of excipients like Gelucire 50/13 and Poloxamer 188, enhancing solubility and bioavailability through methods such as melt granulation and spray chilling, resulting in improved drug loading and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Difficulty of detecting and measuring

If conventional pharmaceutical formulations are used, then manufacturing simplicity is maintained, but dissolution rate and bioavailability are poor

Engineering Contradiction:

Improvedissolution rateVSAvoidformulation complexity

Core Design Contradiction:

Difficulty of detecting and measuringVSEase of manufacture

Solution Approach 1:

The patent uses composite materials by combining benzothiazole derivatives with macrogol glycerides (specifically Gelucire 50/13) to create a formulation that improves dissolution rate. The macrogol glyceride acts as a solubility-enhancing excipient that forms a composite system with the drug, allowing better bioavailability while maintaining relatively simple manufacturing processes like melt granulation.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent applies parameter changes by modifying the physical state and solubility parameters of the benzothiazole derivative through formulation with macrogol glyceride. This changes the dissolution characteristics of the drug from poor to improved, enabling better absorption while keeping the formulation process manageable.

Inventive Principle:

Principle #35Parameter changes

2Productivity

If macrogol glyceride formulations are used, then dissolution rate increases, but formulation complexity increases

Engineering Contradiction:

Improvedissolution rateVSAvoidformulation complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent changes the solubility parameters of the benzothiazole derivative by formulating it with macrogol glyceride, which significantly improves dissolution rate and bioavailability. The macrogol glyceride modifies the physical-chemical parameters of the drug formulation, enabling faster dissolution while the process remains relatively simple.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent utilizes phase transitions in the macrogol glyceride excipient, which exhibits polymorphic transitions and melting point characteristics that facilitate drug dissolution. The phase behavior of macrogol glyceride during gastrointestinal transit enhances drug release and absorption, improving productivity without requiring complex formulation techniques.

Inventive Principle:

Principle #36Phase transitions

3Ease of operation

If oral administration is used, then ease of administration is improved, but absorption profile is poor

Engineering Contradiction:

Improveease of administrationVSAvoidabsorption profile

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent creates a composite material system combining benzothiazole derivatives with macrogol glyceride that maintains the ease of oral administration while significantly improving the absorption profile. The macrogol glyceride component enhances gastrointestinal absorption through its solubility-enhancing properties and interaction with biological membranes.

Inventive Principle:

Principle #40Composite materials

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 formulations significantly increase the dissolution rate and bioavailability of benzothiazole derivatives, leading to enhanced therapeutic effects in treating autoimmune disorders, inflammatory conditions, and other diseases by improving drug absorption and stability.

Implementation Method 1

The formulations significantly increase the dissolution rate and bioavailability of benzothiazole derivatives

Methodology Applied

Scientific EffectSolvation: Solvation

Implementation Method 2

adding a benzothiazole according to Formula (I) to a molten preparation of macrogol glyceride

Methodology Applied

Scientific EffectMelting: Melting

Implementation Method 3

enhancing solubility and bioavailability through methods such as melt granulation and spray chilling

Methodology Applied

Scientific EffectFreezing: Freezing

Data Source

PatentUS7838522B2Benzothiazole formulations and use thereof

Publication Date: 2010.11.23 ARES TRADING SA

AI summary

The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.