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Application Data
Most compatible disintegrants
The most compatible disintegrant with Neusilin® US2 was found to be Croscarmellose sodium (Ac-Di-Sol) followed by Crosslink polyvinylpyrrolidone (Kollidon-CL) and Carmellose calcium (ECG-505). The Characteristics (large surface area and porus nature) of US2 and the cross linking of Croscarmellose sodium act synergestically allowing the tablet to swell and absorb many times it weight in water leading to quick disintegration. Neusilin® US2 improves flowability and makes sufficiently hard tablets at low compression forces. Increase in hardness and compression pressure did not affect the disintegration time or tablet conformity when Croscarmellose sodium was used as a disintegrant.As most of the starch type disintegrants does not go well with Neusilin® US2, Croscarmellose sodium is your best choice when you choose Neusilin® US2 in your formulations. Oil to Powder
Free flowing powder of linseed oil (with Neusilin® US2)
Neusilin® US2 + 30% linseed oil, Dry at 50°C 
Linseed oil tablet, ∅11.3mm, 125N at 500kg/cm2 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)
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. 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
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
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)
