Syloid FP Silica - Grace - High-Performance …...The porous nature of Syloid® 244 FP silica and...
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Materials for Pharmaceutical Manufacturing synthesis intermediates purification technologies formulation and delivery formulation and delivery Syloid ® FP Silica Pharmaceutical Excipient Flow Data Technical Note Evaluation of Syloid ® 244 FP Silica and Other Glidants to Improve Flow Characteristics for APIs and Diluents Introduction In this study, we compared the flow improvement provided by Syloid ® 244 FP silica against other glidants such as fumed silica, precipitated silica and magnesium aluminum silicate. Various APIs and diluents were used to evaluate the flow properties upon addition of Syloid ® 244 FP silica and the other glidants in different amounts. Syloid ® 244 FP silica provides better flow improvement for both APIs and diluents. Both fine powders and coarser materials were included in the evaluation, and Syloid ® 244 FP silica performed better as a glidant in all cases. A glidant improves the flow characteristics of a powder mixture ■ Typically used at 0.25% - 2.0% levels ■ Optimum concentration coincides with amount needed to build a layer around the bulk powder ■ Allows for consistent feed from hopper ■ Efficient filling of die cavity Benefits of improved flow: ■ Decreased tablet weight variation ■ Increased content uniformity ■ Reduced friability and improved tablet hardness ■ Enables use of direct compression process in place of granulation processes in some cases Methods and Materials: The following materials were used in this study: APIs: Aspirin, Ascorbic acid and Paracetamol Diluents: Mannitol, Dextrose, Isomaltose, MCC PH 101, and MCC powder (MCCP) Glidants: Syloid ® 244 FP silica, Fumed silica (FS), Precipitated silica (PS), and Magnesium Aluminium Silicate (MAS) The porous nature of Syloid ® 244 FP silica and reduced dust due to its high density provide optimum flow characteristics for direct compression. Improved flow also reduces friability, decreases tablet weight variation, improves content uniformity and tablet hardness.
Transcript of Syloid FP Silica - Grace - High-Performance …...The porous nature of Syloid® 244 FP silica and...
Materials forPharmaceuticalManufacturing
synthesisintermediates
purificationtechnologies
formulationand delivery
formulationand delivery
Syloid® FP SilicaPharmaceutical Excipient
Flow Data Technical Note
Evaluation of Syloid® 244 FP Silica and Other Glidants to Improve Flow Characteristics for APIs and Diluents
Introduction
In this study, we compared the flow improvement provided by Syloid® 244 FP silica against other glidants such as fumed silica, precipitated silica and magnesium aluminum silicate. Various APIs and diluents were used to evaluate the flow properties upon addition of Syloid® 244 FP silica and the other glidants in different amounts.
Syloid® 244 FP silica provides better flow improvement for both APIs and diluents. Both fine powders and coarser materials were included in the evaluation, and Syloid® 244 FP silica performed better as a glidant in all cases.
A glidant improves the flow characteristics of apowder mixture
■ Typically used at 0.25% - 2.0% levels
■ Optimum concentration coincides with amount needed to build a layer around the bulk powder
■ Allows for consistent feed from hopper
■ Efficient filling of die cavity
Benefits of improved flow:
■ Decreased tablet weight variation
■ Increased content uniformity
■ Reduced friability and improved tablet hardness
■ Enables use of direct compression process in place of granulation processes in some cases
Methods and Materials:
The following materials were used in this study:
APIs: Aspirin, Ascorbic acid and Paracetamol
Diluents: Mannitol, Dextrose, Isomaltose, MCC PH 101, and MCC powder (MCCP)
Glidants: Syloid® 244 FP silica, Fumed silica (FS), Precipitated silica (PS), and Magnesium Aluminium Silicate (MAS)
The porous nature of Syloid® 244 FP silica and reduced dust due to its high density provide optimum flow characteristics for direct compression. Improved flow also reduces friability, decreases tablet weight variation, improves content uniformity and tablet hardness.
API Flow Improvement
Initially, we tested flow improvement with different amounts of the glidant. For fine powders, 1% of glidant was found to provide optimal results. For coarse powders, 0.5% of glidant was found to be sufficient to provide flow improvement.
Figure A: Aspirin flow properties at different amounts of glidant (fine powder passed through #40 mesh, and coarse powder retained on #40 mesh)
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0 0.5 1 1.5 2 2.5
% Syloid® 244 FP
Aspirin (Fine Powder)
An
gle
of
Rep
ose
(d
egre
es)
15
20
25
30
35
40
0 0.5 1 1.5 2 2.5
% Syloid® 244 FP
Aspirin (Coarse Powder)
An
gle
of
Rep
ose
(d
egre
es)
Ang
le o
f Rep
ose
(deg
rees
)A
ngle
of R
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egre
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Ang
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f Rep
ose
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rees
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Ang
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f Rep
ose
(deg
rees
)A
ngle
of R
epos
e (d
egre
es)
Ang
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f Rep
ose
(deg
rees
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% of Syloid® 244 FP Silica
% of Syloid® 244 FP Silica
Glidant Glidant
% of Syloid® 244 FP Silica
% of Syloid® 244 FP Silica
Figure B: Ascorbic acid flow properties at different amounts of glidant (fine powder passed through #40 mesh, and coarse powder retained on #40 mesh). We then proceeded to test the different APIs and shown below are the angle of repose values at optimized percentage of glidants.
Ascorbic Acid (Fine Powder)
An
gle
of
Rep
ose
(d
egre
es)
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0 0.5 1 1.5 2 2.5
% Syloid® 244 FP
An
gle
of
Rep
ose
(d
egre
es)
% Syloid® 244 FP
Ascorbic Acid (Coarse Powder)
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0 0.5 1 1.5 2 2.5
Chart 1. Flow improvement in Aspirin (fine powder passed through #40 mesh, and coarse powder retained on #40 mesh)
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Syloid®
244 FPPS FS
Aspirin (Fine Powder)
No Glidant
1.0% Glidant
No Glidant
0.5% Glidant
Syloid®
244 FPPS FS
Aspirin (Coarse Powder)
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25
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40
Chart 2. Flow improvement in Ascorbic Acid(fine powder passed through #40 mesh, and coarse powder retained on #40 mesh)
Ang
le o
f Rep
ose
(deg
rees
)A
ngle
of R
epos
e (d
egre
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Ang
le o
f Rep
ose
(deg
rees
)
Ang
le o
f Rep
ose
(deg
rees
)A
ngle
of R
epos
e (d
egre
es)
Ang
le o
f Rep
ose
(deg
rees
)
Glidant
Glidant
Glidant
Glidant
% of Syloid® 244 FP Silica% of Syloid® 244 FP Silica
No Glidant
1.0% Glidant
Syloid®
244 FPPS FS
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22
24
26
28
30
32
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Ascorbic Acid (Fine Powder)
No Glidant
0.5% Glidant
Syloid®
244 FPPS FS
Ascorbic Acid (Coarse Powder)
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Chart 3. Flow improvement in Paracetamol (fine powder passed through #60 mesh, and coarse powder retained on #40 mesh)
No Glidant
1.0% Glidant
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Syloid®
244 FPPS
Paracetamol (Coarse Powder)
No Glidant
1.0% Glidant
Syloid®
244 FPPS FS
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Paracetamol (Fine Powder)
Diluents flow improvement
Figure C: Diluent flow properties at different amounts of glidant
% Syloid® 244 FP
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0 0.5 1
MCC PH 101 MCC Powder
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0 0.5 1 1.5 2 2.5
% Syloid® 244 FP
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Want More Information on Syloid® FP Silica?
Visit: www.SyloidFP.com
Chart 4. Flow improvement in MannitolA
ngle
of R
epos
e (d
egre
es)
Ang
le o
f Rep
ose
(deg
rees
)A
ngle
of R
epos
e (d
egre
es)
Ang
le o
f Rep
ose
(deg
rees
)A
ngle
of R
epos
e (d
egre
es)
GlidantGlidant
Glidant
20
25
30
35
40
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50
55
Syloid®
244 FPPS FS MAS
Mannitol
No Glidant
1% of Glidant
No Glidant
1% of Glidant
Syloid®
244 FPPS FS MAS
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25
30
35
40
Dextrose
No Glidant
0.5% of Glidant!
MCC PH 101
Syloid®
244 FPPS FS MAS
3234
3638
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Chart 5. Flow improvement in Dextrose
Chart 6. Flow improvement in MCC pH 101 (DC grade) Chart 7. Flow improvement in Isomaltose
Chart 8. Flow improvement in MCC powder
Syloid®
244 FP
No Glidant
0.5% of Glidant
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37.5
Isomaltose
FS
Glidant
Glidant
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25
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50
Syloid®
244 FP
No Glidant
1.5% of Glidant
MCC Powder
FS
Conclusions
Porous silica gel, such as Syloid® 244 FP silica, is advantageous for flow improvement compared to other glidants because of its porous nature and reduced dust due to its high density. It is especially effective as it not only coats the particles in the bulk powder, but also adsorbs moisture from the API or from a humid environment, thus ensuring a free-flowing powder.
The information presented herein is derived from our testing and experience. It is offered for your consideration and verification. Since operating conditions vary significantly, and are not under our control, we disclaim all warranties on the results that may be obtained from the use of our products. W. R. Grace & Co.-Conn. and its subsidiaries can not be held responsible for any damage or injury occurring as a result of improper installation or use of its products. GRACE® and SYLOID® are trademarks, registered in the United States and/or other countries, of W. R. Grace & Co.-Conn. This trademark list has been compiled using available published information as of the publication date of this brochure and may not accurately reflect current trademark ownership or status. Alltech Associates, Inc. is a wholly owned subsidiary of W. R. Grace & Co.-Conn. Grace Materials Technologies is a business segment of W. R. Grace & Co.-Conn., which now includes all product lines formerly sold under the GRACE DAVISON brand. ©Copyright 2012 Alltech Associates, Inc. All rights reserved.
