Formulation development and scale-up of dutasteride liquisolid tablets.

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Formulation Science

Background:

• Liquisolid (LS) technology enhances dissolution and content uniformity for poorly water-soluble drugs, especially at low doses.
• Industrial-scale application of LS technology for drug formulation remains under-researched.
• Dutasteride (DTS) is a water-insoluble drug often requiring advanced formulation strategies.

Purpose of the Study:

• To develop and pilot-scale LS tablets containing 0.5 mg of dutasteride (DTS).
• To evaluate the feasibility of LS technology for industrial drug manufacturing.
• To assess key tablet quality attributes including dissolution and stability.

Main Methods:

• Two-stage study: placebo formulation development followed by pilot-scale LS tablet production with DTS.
• Utilized a high-shear granulator mixer with a spraying system for LS formulation.
• Comprehensive testing of manufactured tablets: mass uniformity, crushing strength, disintegration, dissolution, stability, and impurity profiling.

Main Results:

• A standard high-shear granulator mixer proved effective for LS formulation development and pilot-scale transfer.
• Successfully compressed the LS system into tablets meeting desired assay, content uniformity, and mechanical strength specifications.
• Achieved desired dissolution profiles for the dutasteride LS tablets.

Conclusions:

• The high-shear granulator mixer facilitates efficient LS formulation development and scale-up.
• LS technology is a viable industrial-scale approach for producing potent, low-dose drug tablets.
• The one-pot process approach enhances manufacturing safety for highly potent compounds.