Orlistat Acarbose Fixed-Dose Combination for Weight Loss

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Solution Overview

Problem

Current pharmaceutical products for obesity and overweight management, such as orlistat and acarbose, are limited by modest efficacy and significant gastrointestinal side effects, leading to poor patient compliance and limited long-term weight loss.

Innovation Solution

A modified release composition of orlistat and acarbose, designed with specific release patterns in different parts of the gastrointestinal tract, to achieve a synergistic effect enhancing weight loss and improving quality of life by minimizing side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If orlistat and acarbose are used separately for weight loss, then weight loss effect is achieved, but gastrointestinal side effects occur

Engineering Contradiction:
Improveweight lossVSAvoidgastrointestinal side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent combines orlistat (a lipase inhibitor) and acarbose (an alpha-glucosidase inhibitor) into a single fixed-dose combination product. This merging allows both drugs to work synergistically for weight loss while enabling coordinated release patterns that reduce gastrointestinal side effects. The combination product has demonstrated superior weight loss efficacy compared to individual drugs, while the synchronized modified-release formulation mitigates the GI adverse effects associated with each drug when used separately.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent employs modified-release technology to change the release parameters of both orlistat and acarbose. By controlling the release rate and timing of each drug component, the formulation achieves sustained therapeutic effects for weight loss while reducing peak concentrations that cause gastrointestinal side effects. This parameter modification transforms the delivery characteristics of both drugs simultaneously.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If conventional release formulations are used, then drug delivery is simple, but weight loss efficacy is limited and side effects are not minimized

Engineering Contradiction:
Improveweight loss efficacyVSAvoidformulation complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent divides the combination formulation into distinct functional components with different release characteristics. The modified-release formulation segments the delivery of orlistat and acarbose, allowing each drug to be released at optimized rates and timings. This segmentation enables sophisticated control over drug release patterns while maintaining a manageable formulation structure that achieves superior weight loss efficacy.

Inventive Principle:
Principle #1Segmentation

3Quantity of substance

If single-drug treatments are used, then formulation is simpler, but synergistic weight loss effect is not achieved

Engineering Contradiction:
Improveweight loss effectVSAvoidcombination formulation complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent merges orlistat and acarbose into a single fixed-dose combination product with coordinated modified-release mechanisms. This merging captures the synergistic weight loss effect of combining a lipase inhibitor with an alpha-glucosidase inhibitor, while the integrated formulation design manages the complexity through unified release control strategies.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS20240226024A1Synergistic effects on weight loss, improved quality of life and reduced gastro-intestinal side effects with a composition of orlistat and acarbose
Publication Date: 2024.07.11 EMPROS PHARMA AB
  • US20240226024A1 patent drawing
  • US20240226024A1 patent drawing
  • US20240226024A1 patent drawing

AI summary

The invention relates to a composition of orlistat and acarbose for use in improving quality of life. The combination is administered orally to obtain a synergistic effect. The synergistic effect is obtained after 13 weeks or more such a after 14 weeks or more. after 15 weeks or more. after 16 weeks or more. after 17 weeks or more. after 18 weeks or more. after 19 weeks or more. after 20 weeks or more. after 21 weeks or more. after 22 weeks or more. after 23 weeks or more. after 24 weeks or more. after 25 weeks or more of after 26 weeks or more of treatment. The synergistic effect gives improved weight loss.