Dapagliflozin Propylene Glycol Hydrate Immediate Release Formulation
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Solution Overview
Problem
Current treatments for type II diabetes, characterized by hyperglycemia due to excessive hepatic glucose production and peripheral insulin resistance, lack effective solutions for consistent control of plasma glucose levels, leading to potential diabetic complications.
Innovation Solution
Development of an immediate release pharmaceutical formulation containing dapagliflozin (S)-propylene glycol hydrate, combined with bulking agents, binders, disintegrants, glidants, and lubricants, formulated as stock granulation for capsules or tablets, to enhance glucose excretion in urine and improve insulin sensitivity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If dapagliflozin is formulated as immediate release pharmaceutical formulation with bulking agents, binders, disintegrants, glidants and lubricants, then the drug delivery effectiveness is improved, but the formulation complexity increases
Solution Approach 1:
The formulation is segmented into distinct functional components: active ingredient (dapagliflozin), bulking agents (for volume and flow), binders (for granulation integrity), disintegrants (for tablet breakdown), glidants (for flow improvement), and lubricants (for friction reduction). Each component performs a specific function, allowing the complex formulation to be managed through modular design where each ingredient addresses a particular challenge in drug delivery.
Solution Approach 2:
Several excipients in the formulation serve multiple functions. For example, microcrystalline cellulose acts as both a bulking agent providing volume and structural support, and as a binder contributing to granulation integrity. Lactose monohydrate serves as both a bulking agent and a disintegrant when used in certain forms. This multi-functionality reduces the total number of ingredients needed while maintaining formulation effectiveness.
2Reliability
If dapagliflozin propylene glycol hydrate is used as the active ingredient, then the therapeutic efficacy for type II diabetes is improved, but the manufacturing process complexity increases
Solution Approach 1:
The dapagliflozin is pre-formed as a propylene glycol hydrate solvate with defined stoichiometry (1:0.4 to 1:0.6 molar ratio) before formulation. This preliminary crystallization step establishes a stable, predictable starting material with controlled solubility and dissolution characteristics. The pre-formed hydrate structure ensures consistent therapeutic efficacy while simplifying subsequent formulation steps, as the active ingredient is already in its optimal physical form for drug delivery.
Data Source
AI summary
Pharmaceutical formulations are provided which are in the form of capsules or tablets for oral use and which include dapagliflozin propylene glycol hydrate is: Formula (Ia) or Formula (Ib) and a pharmaceutical acceptable carrier therefor, which formulation is designed for immediate release. The formulations are used for the treatment of diabetes and related diseases.