Oral Dosage Forms Using Cyclodextrin and Bicarbonate for Bioavailability
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Solution Overview
Problem
There is a need for dosage forms that improve the pharmacokinetic properties and/or bioavailability of active pharmaceutical agents, particularly those with poor aqueous solubility.
Innovation Solution
The use of cyclodextrins and/or bicarbonates in dosage forms, such as oral formulations, to enhance the solubility and bioavailability of drugs through inclusion complexes and pH adjustment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional dosage forms are used for drugs with poor aqueous solubility, then the formulation is simple, but the bioavailability and dissolution rate are poor
Solution Approach 1:
The patent uses cyclodextrins as intermediary substances that form inclusion complexes with poorly water-soluble drugs. The cyclodextrin cavity encapsulates the hydrophobic drug molecule, while the hydrophilic outer surface of cyclodextrin interacts with water, thereby improving dissolution and bioavailability without fundamentally changing the drug structure
Solution Approach 2:
The patent modifies the physical-chemical parameters of the drug formulation by changing the molecular environment of the drug through cyclodextrin inclusion. This alters the solubility parameter, dissolution rate, and pharmacokinetic properties of the drug without changing the drug's chemical structure
2Reliability
If the drug dosage is increased to achieve therapeutic effect, then the therapeutic effect is improved, but the side effects and toxicity increase
Solution Approach 1:
By improving the dissolution rate and bioavailability through cyclodextrin inclusion complexes, the patent enables achievement of therapeutic plasma concentrations with lower doses. This parameter change in drug delivery efficiency directly reduces the dosage required and consequently minimizes dose-dependent side effects and toxicity
3Productivity
If the dissolution rate is increased to improve bioavailability, then the Cmax and AUC are improved, but the formulation complexity increases
Solution Approach 1:
Cyclodextrins serve as a versatile intermediary that can be incorporated into various dosage forms (tablets, capsules, injections) with relatively simple formulation processes. The inclusion complex formation occurs spontaneously under mild conditions, avoiding complex manufacturing steps while achieving enhanced dissolution rates
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 proposed dosage forms increase the bioavailability of drugs by improving dissolution and reducing Tmax, with potential reductions in drug dosage and enhanced Cmax and AUC, while providing pain relief and therapeutic effects.
Implementation Method 1
a cyclodextrin (optionally as an inclusion complex of the drug and the cyclodextrin)
Implementation Method 2
a bicarbonate, and methods of treatment using the dosage form
Data Source
AI summary
Disclosed herein are dosage forms comprising a combination of: 1) an active pharmaceutical ingredient (API), 2) a cyclodextrin, and 3) a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the drug for the treatment of conditions such as pain.