RXCIPIENTS® FM 1000 – A versatile excipient for orally disintegrating tablet (ODT) formulations
1. Introduction
Certain patient groups, specifically elderly and infant
patients, experience difficulties with swallowing oral
dosages of medication. Orally disintegrating tablets (ODTs) are one approach to ease the intake, helping patients to comply with their prescription plans.
A conventional disintegrant pulls water into the tablet and swells, resulting in the delamination of the tablet. Evonik new excipient RXCIPIENTS® FM 1000 boosts the function of the disintegrant, causing the tablet to breakdown into small particles rather than to just delaminate.
By adjusting the concentration of RXCIPIENTS® FM 1000 in combination with the disintegrant, formulators can target different disintegration times of the ODT.
RXCIPIENTS® FM1000 calcium silicate can thereby be combined with a broad range of other ingredients.
2. Mode of action and advantages
RXCIPIENTS® FM 1000 channels moisture to the disintegrant due to its hydrophobic nature. The disintegrant absorbs that moisture, swells and thereby breaks the tablet.
Typically, 5–15 wt.-% of RXCIPIENTS® FM 1000 are used in the formulation.
Advantages of using RXCIPIENTS® FM1000 include:
- Promotion of faster tablet disintegration, breaking the tablet down into easy to swallow fine particles
- Durability of tablets, with low friability even at low
compression forces - Support of bulk packing instead of expensive blister
packing - High level of flexibility in formulation due to compatibility
with many different disintegrants and fillers
3. Case studies (example 1-3)
The following examples illustrate the benefits of RXCIPIENTS® FM 1000.
3.1 Example 1 – Placebo ODT formulation
Formulation
Mixing
- All components except magnesium stearate were passed through a sieve (840 µm)
- Mixing in a V blender for 10 min at 27 rpm
- Addition of magnesium stearate after passing through a sieve (400 µm)
- Mixing in V blender for 5 min at 27 rpm
Tabletting
- SMI – Piccola rotary press, Model 8
- Turret speed: 30 rpm
- Compression force: 5–9 kN
- Tablet diameter: 10 mm
- Tablet mass: 450 mg
Results
RXCIPIENTS® FM 1000 drastically reduced the disintegration time at a low concentration and at the same time improved compressibility of the formulation leading to tablets with equivalent mechanical stability at a significantly lower compression force. The following pictures illustrate the quick disintegration.
3.2 Example 2 – Acetaminophene ODT formulation
3.3 Example 3 – COX-2 inhibitor ODT formulation
(see more in the technical information)
4. Chemical identity, regulatory and registration information
Calcium silicate, physical and chemical properties
See the full technical information on “RXCIPIENTS® FM 1000 – by Evonik” here
(click the picture to download the technical information)
Source: Evonik technical information “RXCIPIENTS® FM 1000 – by Evonik”