Application Data

Typical Application and Quantity Needed in Pharmaceutical Preparations

Typical Application and Quantity Needed in Pharmaceutical Preparations

Pharmaceutical Application

I. Oils and extracts to powder

The most suitable grade for converting oil to powder is Neusilin® US2. When the oil load is comparatively high, an addition of 0.5 to 2% UFL2 will improve flowability substantially. Neusilin® UFL2 alone at 0.5% can resolve sticking issues of oily formulations.

Schematic flow

Schematic flow

Oil adsorption capacity

Oil adsorption capacity Neusilin® US2 and UFL2 grades show higher oil adsorption capacity* when compared to MCC or Colloidal silica.
*Linseed oil direct adsorption

Oil to Powder

Free flowing powder of linseed oil (with Neusilin® US2)

Neusilin® US2 + 30% linseed oil, Dry at 50°C Neusilin® US2 + 30% linseed oil, Dry at 50°C
Neusilin® UFL2 Powder (x 20,000) Linseed oil tablet, ∅11.3mm, 125N at 500kg/cm2

Tablets of Scopolia extract and soybean oil (with Neusilin® UFL2)

Tablets of Scopolia extract and soybean oil (with Neusilin® UFL2) A mixture containing 25% Scopolia extract or Soybean oil and 25% UFL2 was compounded with equal amount of Lactose. This mixture was subjected to static compression and tabletting. We found no adhesion to pestle and mortar and the compressibility was good. The tablet did not exude the extract or oil on storage.

Tablets of Vitamin E (with Neusilin® US2)

Tablets of Vitamin E (with Neusilin® US2) An ethanol solution of tocopherol acetate (VE) 20-50% was compounded with proportional amount of Neusilin® and mixed well. To this mixture, 3% Croscarmellose sodium and 1% Magensium stearate was added before tabletting. High quality tablets with a load of up to 30% Vitamin E can be prepared with Neusilin® US2.
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II. Improve flow

Angle of repose after adding excipient to potato starch

Angle of repose after adding excipient to potato starch

Neusilin® UFL2 particle stick to the surface and aid flow

Potato starch (x 1,000) Potato starch
(x 1,000)
Potato starch (x 10,000) Potato starch
(x 10,000)
Potato starch + Neusilin® (x 1,000) Potato starch + Neusilin®
(x 1,000)
Potato starch + Neusilin® (x 10,000) Potato starch + Neusilin®
(x 10,000)
Electron micrograph showing Neusilin® UFL2 particles sticking to the starch surface. On addition to starch, the UFL2 particles stick to the surface and facilitate flow as in a 'roller blade' model. A 0.5% addition of UFL2 to potato starch vastly improves flowability.
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III. Anti caking

Addition of 0.5% Neusilin® UFL2 prevents caking

Addition of 0.5% Neusilin® UFL2 prevents caking

Neusilin® UFL2 prevents caking at high humidity conditions

Sodium L-aspartate at 45°C, 75% RH, 2 days Sodium L-aspartate at 45°C, 75% RH, 2 days
Sodium L-aspartate with 0.5% UFL2 at 45°C, 75% RH, 2 days Sodium L-aspartate with 0.5% UFL2 at 45°C,
75% RH, 2 days
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IV. Compressibility

Neusilin® UFL2 increases lactose tablet hardness

Neusilin® UFL2 increases lactose tablet hardness Compounding Lactose with 10% Neusilin® UFL2 results in higher hardness when compared to 15% microcrystalline cellulose. Neusilin® US2 at similar levels can also be used to improve hardness of tablets.

High quality tablets at low compression pressure

High quality tablets at low compression pressure Tablet hardness of cornstarch/lactose based tablets compounded with either using Neusilin® US2, colloidal silica or calcium silicate. Corn starch, lactose and excipient were mixed thoroughly. Magnesium stearate as lubricant was added prior to tabletting. Compression with Neusilin® US2 or Neusilin® UFL2 generally gives harder tablets compared to colloidal silica.
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V. Solid dispersion

Formulating poorly water soluble drugs by solid dispersion leads to a remarkable improvement in dissolution and bioavailability. Neusilin® can potentially resolve problems associated with tabletting and improve efficiency of solid dispersion.

Three methods to apply adsorbent carriers in different solid dispersions

Three methods to apply adsorbent carriers in different solid dispersions

V(i). Key advantages of Neusilin® as an adsorbant

  • Improve flow
  • High quality tablets at low compression forces
  • High specific surface area
  • High adsorption capacity
  • Higher API load
  • Restricts reversion of amorphous form to crystalline state
  • Inert core material

V(ii). Solid dispersion

Published examples

In developing a solid dispersion system for the BAY 12-9566, Gupta et al,1,2 prepared ternary dispersion granules using hot-melt granulation. First, the candidate drug BAY 12-9566 was added to a molten solid dispersion carrier, Gelucire® 50/13 maintaining a temperature of 90°C. Neusilin® US2 was preheated to 80°C in a granulator for 15 min with stirring at 300 rpm. The molten mixture was then added drop-wise over a period of one minute to Neusilin® with continued stirring. Hot melt granulation was performed at an increased stirring speed of 600 rpm for one more minute to obtain ternary dispersion granules of drug, Gelucire® 50/13 and Neusilin® US2. The dispersion granules were allowed to come to room temperature by air cooling followed by sieving through mesh #18 BSS. The free flowing granules of the dispersion were processed into tablets.

1) Gupta et al, Pharm Dev Tech, 6: 563- 72, 2001
2) Gupta et al, Pharmaceutical Research, 19:1663-72, 2002


Gupta et al, Pharmaceutical Research, 19:1663-72, 2002

Dissolution profile of solid dispersion granule

Dissolution profile of solid dispersion granule Comparison of drug dissolution (after 30 min) from initial and stored solid-dispersion granules using USP Type II apparatus at 50 rpm. Data are shown for drug dissolution (% of initial) from solid-dispersion granules after storage at 40°c/75% RH (Gupta et al, 2002)

2) SMEDDS (Self Micro Emulsifying Drug Delivery Systems)
Catarzi et al, 6th world meeting on Pharmaceutics, BioPharmaceutics and Pharmaceutical Technology, 2008

Glyburide Preparation:
SME formulation was prepared by adding under continuous stirring Tween 20 and Labrafac Hydro WL (oil phase) and then distilled water to Glyburide solubilized in Transcutol. Glyburide tablets were prepared by direct compression. The preparation with Neusilin® US2 resulted in improved flow, compact tablets and improved dissolution profile.

Dissolution profile of glyburide preparation

Dissolution profile of glyburide preparation Glyburide (GLY) dissolution profile from the different tablet formulations (Ref. Tablet – commercial GLY formulation; SME tablet – Glyburide SME formulation consisting of Labrafac Hydro® as oil phase, Tween 20 as surfactant and Transcutol® as co-surfactant; TC tablet – Glyburide formulation consisting of Transcutol (TC). (Catarzi et al, 2008)
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VI. Hygroscopic velocity curve of Neusilin®

1) at 37 °C, RH 53%

37ºC, RH 53%

2) at 37°C, RH 75%

37ºC, RH 75%

3) at 37°C, RH 92%

37ºC, RH 92%
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VII. Hygroscopic equilibrium curve of Neusilin®

Hygroscopic equilibrium curve of Neusilin® The Hygroscopic velocity curve of different grades of Neusilin® indicate that Neusilin® is stable and do not absorb moisture up to 70% RH. Neusilin® remains flowable even after absorbing moisture up to 250% of its weight.
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