Disodium Phosphocreatine Cyclodextrin Inclusion Complex
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Solution Overview
Problem
Existing creatine formulations face challenges with stability and bioavailability due to degradation in the acidic stomach environment and suboptimal transport across intestinal mucosal cells.
Innovation Solution
A formulation combining disodium phosphocreatine with cyclodextrin, co-granulated and coated with methacrylate copolymers, which protects creatine from gastric degradation and enhances intestinal uptake.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If creatine monohydrate is ingested orally, then it can be taken up by skeletal muscle to enhance performance, but it degrades rapidly in the stomach to form creatinine and is not fully solubilized in cold or room temperature water
Solution Approach 1:
Cyclodextrin serves as an intermediary host molecule that forms an inclusion complex with creatine. The cyclodextrin cavity encapsulates the creatine molecule, protecting it from degradation by gastric juices while maintaining solubility in cold or room temperature water. This host-guest complex prevents the harmful conversion of creatine to creatinine during gastric passage.
Solution Approach 2:
The invention creates a composite formulation combining creatine with cyclodextrin in a specific molar ratio (1:1 to 1:10). This composite material exhibits properties that neither component possesses alone: the cyclodextrin provides protection and solubility enhancement, while the creatine maintains its bioactive function. The composite structure stabilizes creatine against degradation while improving its physical properties.
2Reliability
If creatine is protected from degradation in the stomach, then stability is improved, but transport across intestinal mucosal cells remains suboptimal
Solution Approach 1:
The cyclodextrin inclusion complex changes the physical-chemical parameters of creatine, including its size, shape, and surface properties. This parameter modification enables the creatine-cyclodextrin complex to interact more effectively with intestinal mucosal cells, facilitating improved transport and absorption while maintaining protection from gastric degradation.
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 formulation significantly improves creatine bioavailability by protecting it from stomach acid and facilitating controlled release and absorption in the intestines, leading to enhanced muscle energy supply and potential benefits for muscle-wasting disorders.
Implementation Method 1
cyclodextrin...protects the creatine as it comes in contact with gastric juices
Implementation Method 2
coated with methacrylate copolymers, which protects creatine from gastric degradation and enhances intestinal uptake
Data Source
AI summary
Formulations of creatine, preferably phosphocreatine and most preferably disodium phosphocreatine, combined with cyclodextrin exhibit improved uptake across digestive mucosa, including intestinal, esophageal, and stomach mucosa. In particular, the formulations of the present invention are designed for protection of the cyclodextrin as it comes in contact with gastric juices so as to allow thereafter for unexpectedly improved site-specific intestinal release.