Progesterone Cocrystals Solubility Bioavailability
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Solution Overview
Problem
Progesterone, a crucial hormone for gestation and treatment of infertility and secondary amenorrhea, has low bioavailability and poor solubility when taken orally, limiting its effectiveness in pharmaceutical forms.
Innovation Solution
The development of cocrystals of progesterone with coformers such as vanillic acid, benzoic acid, salicylic acid, and cinnamic acid, which alter physicochemical properties like solubility and stability, enhancing bioavailability and dissolution rates.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If progesterone is formulated as oral capsules, then it is convenient for administration, but bioavailability is low and solubility is poor
Solution Approach 1:
The patent creates cocrystals by combining progesterone with coformers (such as organic acids or bases) to form a composite crystalline material. This cocrystal structure modifies the physicochemical properties of progesterone, specifically improving its solubility and dissolution rate while maintaining the oral capsule formulation for convenient administration.
Solution Approach 2:
The patent changes the physical and chemical parameters of progesterone by forming cocrystals with different stoichiometric ratios and crystal structures. This alters the solubility profile and dissolution characteristics of the drug, enabling improved bioavailability while maintaining oral administration convenience.
2Ease of operation
If progesterone is administered orally, then it is easy to administer, but solubility in water is poor limiting absorption
Solution Approach 1:
The patent forms cocrystals combining progesterone with coformers to create a composite material with enhanced aqueous solubility. The cocrystal structure allows better interaction with aqueous environments in the gastrointestinal tract, improving dissolution and absorption while maintaining oral administration ease.
Solution Approach 2:
The coformer acts as an intermediary substance that mediates between the hydrophobic progesterone molecule and the aqueous environment. The coformer's molecular structure facilitates better solvation and dissolution of progesterone in water, enabling improved absorption without compromising administration ease.
3Reliability
If cocrystals are formed to improve solubility, then bioavailability increases, but the formulation complexity increases
Solution Approach 1:
The patent segments the formulation development into systematic steps: selecting appropriate coformers based on compatibility criteria, determining optimal cocrystal stoichiometry, and establishing characterization methods. This segmented approach manages formulation complexity while achieving improved bioavailability through cocrystal formation.
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 cocrystals of progesterone with specific coformers improve bioavailability and sustained progesterone concentration, addressing the limitations of existing oral formulations by increasing solubility and stability, thereby enhancing therapeutic efficacy.
Implementation Method 1
Cocrystals of progesterone have been disclosed in the literature... Cocrystals have the potential alter physicochemical properties. More specifically, cocrystals have been reported to alter aqueous solubility and/or dissolution rates
Data Source
AI summary
The present invention relates to a cocrystal of progesterone and a coformer selected from the group consisting of vanillic acid, benzoic acid, salicylic acid, cinnamic acid, and vanillin. The present invention also relates to a pharmaceutical composition comprising a cocrystal of the present invention and at least one pharmaceutically acceptable carrier. The present invention further relates to a method of supplementing progesterone in women. This method involves administering to a female subject in need thereof a pharmaceutical composition of the present invention.