Multiparticulates: Beads, Granulation and Drug Layering

Multiparticulate dosage forms, such a beads, microspheres, or engineered granules, can be used to provide a wide range of drug release patterns to meet n array of drug delivery needs. Multiparticulates can be designed to provide extended release, delayed release, pulsatile or bi-phasic release, or even site-specific release of drugs.

Formex has the capability for bead manufacture through wet-mass extrusion and spheronization, and granule manufacture though high-shear granulation and melt-granulation processes. Beads and granules can be coated using aqueous- and organic based processes to apply functional and aesthetic coatings. Beads can also be coated with drug-containing layers to provide certain release profiles; to improve solubility through increased surface area of drug releasing particles; and to stabilize the drug in an amorphous form.

Beads can be made containing drug in a controlled release matrix, can be coated with release modifying polymer layers (such as enteric polymers or diffusion controlling polymers), or can serve as a substrate for drug-containing polymer coatings for drug-layering applications. Granules can be made from drug particles and binding polymers to generate modified release granules.

Multiparticulate formulations can have several advantages over single-unit controlled release dosage forms. They tend to exhibit more uniform gastric emptying as compared to single-unit dosage forms, which can be important for dosage forms with time-based release mechanisms. Multiparticulates also have significantly lower risk of dose-dumping than do single unit dosage forms, because the dose is distributed among many drug delivery units rather than being constrained to one unit.

Multiparticulates also can provide more complex and customized release profiles, such as bi-phasic release using two populations of multiparticulates in a single dosage form.

Liquid Solutions

Liquid/semi-solid in capsule and in bottle solutions provide an innovative approach which enables small molecule developers to exploit the potential of lipid-based formulations to overcome poor aqueous solubility and improve compound bioavailability.

The relative advantages of the option are short development time, elimination of challenging API characteristics (poor flow, taste, etc.), potential content uniformity issues, and increase bioavailability of particularly poorly soluble compounds. The Option can form a solid dispersion/solution in hot melt process that can be filled into hard capsules before sealing/banding for either clinical phase or commercial manufacturing.

The presence in traditional capsule provides improved stability, faster feasibility, reduced cost, and broader access to expertise/contract providers.

Novel Dosage Forms

Many drugs are more successfully administered by routes other than being swallowed, where absorption into the blood stream occurrs in the gastrointestinal tract.

Formex has developed or manufactured several non-standard dosage forms.

These include:

  • Fast-dissolving tablets or granules that dissolve in the mouth for very rapid drug absorption.
  • Oral films that also release drug in the mouth.
  • Buccal films that adhere to and release drug through the buccal tissue in the mouth. This route of administration delivers drugs that are not stable or well absorbed from the intestine.
  • Thin-films to administer drugs through the skin (trans-dermal dosage forms).
  • Solid, drug releasing monoliths and other shapes to deliver drugs though non-oral routes.

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