Injectable Gabapentin Formulation for Consistent Pain Relief
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Solution Overview
Problem
The oral administration of gabapentin for pain treatment is limited by dose-dependent bioavailability and uncertainties related to gastrointestinal function and oral intake, leading to inconsistent plasma concentrations and reduced effectiveness for post-procedural pain relief.
Innovation Solution
Development of an injectable pharmaceutical formulation comprising gabapentin or its derivatives, optionally combined with non-opioid pain drugs like acetaminophen, in an aqueous carrier, which can be administered via parenteral routes to ensure consistent and effective pain management, including pre-procedure, peri-procedure, and post-procedure pain relief.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral administration of gabapentin is used for pain treatment, then the medication can be easily administered, but the bioavailability is dose-dependent and inconsistent due to saturable L-amino acid transport mechanism in the intestine
Solution Approach 1:
The patent changes the route of administration from oral to parenteral (intravenous or intramuscular injection), fundamentally altering how the drug enters the system. This bypasses the saturable intestinal transport mechanism and achieves consistent, predictable plasma concentrations regardless of dose, while maintaining ease of administration through standardized injection protocols
2Quantity of substance
If high doses of gabapentin are administered orally to achieve therapeutic plasma concentrations, then pain relief effectiveness improves, but the bioavailability decreases due to saturation of the L-amino acid transport mechanism
Solution Approach 1:
The patent changes the route of administration from oral to parenteral, which fundamentally alters the pharmacokinetic parameters. This bypasses the saturable intestinal transport mechanism, allowing for predictable plasma concentrations at any dose level without the bioavailability degradation that occurs with oral high-dose administration
3Force
If oral administration is used for pre-procedural pain management, then the medication can be given in advance, but the effectiveness is uncertain due to variable gastrointestinal function and oral intake restrictions
Solution Approach 1:
The patent changes the route of administration from oral to parenteral injection, which eliminates the variability introduced by gastrointestinal function and oral intake restrictions. This ensures predictable plasma concentrations and reliable pre-procedural pain management, as the drug is absorbed directly into the bloodstream through the injection route
Data Source
AI summary
Formulations, methods of manufacturing, methods of stabilizing, kits, and uses as medicament are provided, for example for the treatment of pain. The formulations can comprise gabapentin optionally combined with at least one non-opioid pain drug in an aqueous carrier. The pharmaceutical formulation can have a pH of about 2.0 to about 10.0. The at least one non-opioid pain drug can be acetaminophen. The components can be included in any amount suitable for purposes of obtaining properties desirable for an injectable infusion, for example an intravenous infusion.