Neusilin
The Neusilin is a synthetic amorphous form of Magnesium Alumino-metasilicate. It is a multifunctional excipient that can be used in both direct compression and wet granulation of solid dosage forms. Neusilin is widely used for improvement of the quality of tablets, powder, granules and capsules.
Neusilin does not develop gels with aqueous solutions unlike other Magnesium Aluminum Silicates. The different grades of Neusilin have been highly evaluated at home and abroad. It has a market presence of over 50 years in Japan.
What is Neusilin?
Neusilin® does not develop gels with aqueous solutions unlike other Magnesium Aluminum Silicates. It is available in various grades and two different pH options which makes it a versatile excipient for a wide variety of applications. With over 500 pharmaceutical preparations and a market presence of over fifty years in Japan, Neusilin® is well accepted by formulators world-wide as an aid for formulations containing antibiotics, oily actives, poorly water soluble APIs, herbal mixtures, vitamins, etc. Neusilin is also used as carrier for solid dispersions and self-micro emulsifying drug systems.
- Neusilin® occurs as a fine powder
or as granules of Magnesium Aluminometasilicate. - Neusilin® is represented by an empirical formula Al2O3·MgO·1.7SiO2·xH2O.
- Neusilin® is amorphous, possesses very large specific surface area and has high oil and water adsorption capacity.
- Neusilin® makes hard tablets at low compression forces compared to similar binders.
- Neusilin® increases the hardness synergy with other filler and binder excipients at low concentrations.
- Compounding with Neusilin® helps stabilize moisture sensitive as well as lipophilic API's.
- Neusilin® is stable against heat and has a long shelf life.
- Neusilin® is available in various grades. The grades differ in their bulk density, water content, particle size and pH.
"Multi-problem solver"
Neusilin® is amorphous and contains either tetrahedron or octahedron of Al, Octahedron of Mg and tetrahedron of Si which are randomly attached to form a complex three dimensional structure. Neusilin® does not possess repeating units of a defined monomer.
Experience granules of Magnesium Alumino metasilicate
General Properties of Neusilin®
Neusilin® Grades
Typical Properties
*1) BET surface area, nitrogen adsorption method
*2) Japanese Industrial Standard pigment test method (JIS K5101)
*3) Amount of 0.1N hydrochloric acid neutralized by 1g dried product (110°C. 7 hours)
*4) Weigh 2 g of sample, add water to make 50 ml. After stirring, allow to stand for 2 minutes, Measure pH using pH meter
Package Size
Samples are available upon request.
Please contact us to find out your nearest Gen Store distributor.
US Pharmacopoeia National Formular
Neusilin is manufactured under strict quality control at our FDA-GMP certified facilities Neusilin® meets all the requirements of the current USP/NF and JPC. An US DMF type IV filed in 1998.
Neusilin® is safe with no reports of adverse reactions and is an accepted ingredient by the US Pharmacopoeia/National Formulary and Japanese Pharmaceutical Codex. Based on the usage as an excipient in various formulations in Japan, Neusilin® up to 1.05 g can be used for oral uptake per day.*1 Neusilin® (Alkaline grades) is also approved as antacid active ingredient where the maximum dosage is 4g / day.*2 There are no established maximum oral intake limits specified by US-FDA.
*1) Encyclopedia of Pharmaceutical Additives, Japan, 2005
*2) Japanese approved list of manufacturing and import of gastrointestinal drugs
Neusilin® is a stable inorganic compound and meets JPC and NF specifications.
Data
Typical Application and Quantity Needed in Pharmaceutical Preparations
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
Oil adsorption capacity
Neusilin® US2 and UFL2 grades show higher oil adsorption capacity* when compared to MCC or Colloidal silica.
*Linseed oil direct adsorption
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)
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.
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Angle of repose after adding excipient to potato starch
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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Addition of 0.5% Neusilin® UFL2 prevents caking
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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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
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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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
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
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
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)
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37ºC, RH 53%
37ºC, RH 75%
37ºC, RH 92%
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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.
Cosmetic
in virtual reality.
Unique properties of Neusilin® grade, UFL2 makes it an ideal component of cosmetic preparations. UFL2 adsorbs both oil and water up to 300% and remain flowable. It functions as an efficient carrier of volatile compounds such as fragrances and liquids giving long shelf life and lasting effect. UFL2 gives very good mattifying effect, color uniformity and is an excellent cross-linker with polyacrylate resulting in smooth and stable gel sheets.
Facial care products including lotions, eye shadow, cleansers, powders,
facial treatment masks
Acne and Oily Skin treatments
Deodorants
Cosmetic Application
Neusilin® UFL2: Odor adsorption
UFL2 Application categorised
Comfort & Ease
Unique properties of Neusilin® grade, UFL2 makes it an ideal component of cosmetic preparations. UFL2 adsorbs both oil and water up to 300% and remain flowable. It functions as an efficient carrier of volatile compounds such as fragrances and liquids giving long shelf life and lasting effect. UFL2 gives very good mattifying effect, color uniformity and is an excellent cross-linker with polyacrylate resulting in smooth and stable gel sheets.
Facial care products including lotions, eye shadow, cleansers, powders,
facial treatment masks
Acne and Oily Skin treatments
Deodorants
Cosmetic Application
Neusilin® UFL2: Odor adsorption
UFL2 Application categorised
Pubmed publication
Joshi et al reported the successful development of a solid microemulsion preconcentrate (NanOsorb) of Artemether (ARM), an antimalarial agent with Neusilin® as an adsorption carrier. Excipients like dibasic calcium phosphate, lactose, microcrystalline cellulose, magnesium carbonate, calcium carbonate and Aerosil® 200 did not give desired results for solidification. NanOsorb significantly improved the therapeutic efficacy of ARM when compared to ARM solution and marketed formulation (Larither®) The acute and subacute toxicity studies successfully established the safety of the NanOsorb in animals.
Reference: Joshi M et al., Int J Pharm. 2008 Oct 1;362(1-2):172-8.
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