Grace Materials Technologies

Application Note

SYLOID® FP Silica Pharmaceutical Excipients

Benefits for the Oral Dry Suspension of Antibiotics
SYLOID® Silica’s Unique Morphology Helps: Study Results Show Stability and Flow
• Protect antibiotic formulations from moisture Formulation A Formulation B
Ingredients
• Enhances storage stability and shelf life Quantity (mg/5mL)
Amoxicillin (Equivalent) 600 200
• Improves the flow and liquid dispersion properties of powder
formulations Clavulanic acid (Equivalent) 42.9 28.5
SYLOID® AL1-FP silica 42.9 28.5
Xanthan gum 5 5
Internal
Carboxy Methyl Cellulose Na 15 15
Surface Area
Sweetening agent 5 5
SYLOID 244FP silica
®
5 3.5
Strawberry Flavor q.s q.s

Note: Care should be taken while dispensing the ingredients to prevent

hygroscopic materials from absorbing excess moisture which can lead
to stability problems.

In a study, Grace compared SYLOID® AL1-FP silica and SYLOID® 244FP

mesoporous silica gel excipients with other pharamceutical grade
excipients from leading manufacturers.

External Equivalent amounts of Amoxicillin and Clavulanic acid were mixed with
Surface Area the remaining excipients to get dry powder suspension as shown in the
table here. The formulation was evaluated for assay, content uniformity,
dispersability, flowability, pourability, and viscosity of final liquid
Solving the Moisture Challenge suspension.

Beta-lactam antibiotics such as Amoxicillin, Cefuroxime, and
Cefixime are often formulated with Potassium Clavulanate to avoid
degradation from β-lactamase enzymes. Potassium Clavulanate is
highly hygroscopic in nature and is hydrolyzed in the presence of
moisture, which ultimately affects the efficiency of the antibiotics. As
a result, manufacturers of β-lactam antibiotics look to dry powder
formulations which can be easily converted to liquid suspension
before administration.
SYLOID® AL1-FP silica’s surface area and highly active surface work as
a very effective desiccant. This helps to protect the highly hygroscopic
Potassium Clavulanate from hydrolysis and provides continued
stabilization of β-lactam antibiotics. With a high absorption capacity for
water vapor at low relative humidity SYLOID® AL1-FP silica’s surface
area and active surface work as a very effective desiccant to protect the
highly hygroscopic Potassium Clavulanate from hydrolysis and provide
continued stabilization of β-lactam antibiotics.

The challenge is to stabilize the antibiotics in this powder form.
Grace’s SYLOID® AL1-FP silica works as a uniquely effective moisture
absorbent that helps maintain stability while SYLOID® 244FP silica
is commonly used to maintain powder flow, uniformity, and to help
prevent caking.
The high absorption capacity allows the silica to help maintain a very
low humidity microenvironment near powder particles, reducing water
available to degrade the ingredients. In a formulation, the ratio of
SYLOID® AL1-FP silica to Potassium Clavulanate is optimized at 1:1.
SYLOID® 244FP silica helped ensure content uniformity, powder flow
property, to avoid agglomeration of powder and as a suspension aid.
Over a period of one month at room temperature and at 40°C with

1
75% relative humidity, we found no significant change in both Potassium
Clavulanate and Amoxicillin drug content. The combination of SYLOID®
AL1-FP silica and SYLOID® 244FP silica was ideal for stabilizing dry powder
formulations containing highly hygroscopic compounds.

Amoxicillin and Potassium Clavulanate Stability Data

100
% Drug Content in the Formulation

80

60

40

20

0
Amoxicillin Potassium Clavulanate

Initial 2 Weeks 1 Month

Control Parameters Observations

Moisture Control Effective desiccant action was observed in the formulation.
Stability No degradation of API in the formulation.
Anti-caking Formulation was observed free flowing without any lumps.
Content Uniformity Uniform drug content was found throughout the formulation.

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Tel: +1.410.531.4000

For more information about SYLOID® FP silica, visit: SYLOIDFP.com

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 reserves the right to change prices and/or specifications without prior notification. GRACE® and SYLOID® are trademarks, registered in the United
States and/or other countries, of W. R. Grace & Co.-Conn. TALENT TECHNOLOGY TRUST™ is a trademark 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. © Copyright 2017 W. R. Grace & Co.-Conn. All rights reserved.