SYLOID® FP Silica

Multifunctional Excipients for the Nutraceutical and Pharmaceutical Industry

GRACE Talent | Technology | Trust

Formulation Challenges

Formulating nutraceutical and vitamin products poses numerous challenges driven by a multitude of factors. These formulations typically contain a diverse range of active ingredients, which introduce formulation difficulties due to disparities in particle size, flowability, compressibility, moisture sensitivity, and inter-ingredient interactions. For instance, some active ingredients are available in granular form, while others only exist as fine powders. This results in a wide distribution of particle sizes within the blended mixture, leading to inhomogeneous dispersion of actives and significant tablet-to-tablet variability in dosage. Additionally, botanically derived ingredients exhibit lot-to-lot variations in physical properties, further complicating the formulation process. Moreover, oily or sticky raw materials are notoriously difficult to incorporate into solid dosage forms, with the challenge exacerbated when fine powdered ingredients are present in the formulation.

Hygroscopicity

Plant extracts are inherently hygroscopic and tend to absorb moisture from the surrounding environment. This moisture absorption leads to the formation of sticky agglomerates that adhere to other powdered ingredients and manufacturing equipment. The severity of this issue is dependent on the ambient Relative Humidity (RH) and the critical RH threshold at which the ingredient loses its free-flowing characteristics.

SYLOID® FP silicas are high-porosity, micronized silica powders. When incorporated into formulations, they can adsorb substantial amounts of moisture, ensuring active ingredients remain dry and free-flowing throughout processing and storage.

Stability

Beyond enhancing powder flowability, SYLOID® FP porous silica gels also improve the stability of moisture-sensitive ingredients such as natural products and vitamins. By adsorbing moisture during both the manufacturing process and the storage of the final product, these silicas prevent ingredient degradation and extend the product's shelf life.

Dosage Size Constraints

The high load of active ingredients, combined with dosage size limitations, often leaves minimal space for excipients in the formulation. A typical nutraceutical formulation contains 70-90% active ingredients, with only 10-30% allocated for excipients. This low excipient loading, coupled with the diversity of actives in a single formulation, makes it challenging to achieve key formulation targets such as good flowability, optimal disintegration time, adequate tablet hardness, and reduced friability.

SYLOID® FP silicas are highly efficient, multifunctional excipients that can meet multiple formulation requirements simultaneously. Furthermore, their high bulk density means they contribute minimally to the final dosage size. Grace’s SYLOID® FP silicas effectively mitigate or resolve these core formulation challenges.

Key Properties of Silica

Pore Size Distribution

SYLOID® silicas feature a precisely controlled, narrow pore size distribution, offering formulators additional advantages including superior moisture control and uniform interaction between the silica and adsorbed substances.

Adsorptive Capacity

Pore size exerts a significant influence on the moisture adsorption behavior of silica. Small-pore silica can adsorb moisture at low relative humidity, acting as an effective desiccant. In contrast, wide-pore silica adsorbs large quantities of water at higher relative humidity levels, making it ideal for high-humidity environments.

Case Study

Study Description

SYLOID® 244FP silica was evaluated against precipitated and pyrogenic (fumed) silica at an optimized loading of 1% in a multivitamin formulation. Powder flowability was characterized by the angle of repose, and the blended powders were subsequently compressed into tablets to assess tablet performance attributes.

Baseline Formulation

| Ingredients | % Composition |

|---------------------------|---------------|

| Vitamin A | 2.0 |

| Vitamin B1 | 2.0 |

| Vitamin B2 | 2.0 |

| Vitamin B3 | 4.0 |

| Vitamin B6 | 0.4 |

| Vitamin B12 | 0.001 |

| Biotin | 0.01 |

| Folic acid | 0.2 |

| Vitamin C | 15.0 |

| Vitamin D3 | 0.003 |

| MCC | 61.8 |

| AcDiSol | 6.0 |

| PVP K30 | 5.0 |

| SYLOID® FP Silica - Glidant | 1.0 |

| Mg Stearate | 0.5 |

| **Total** | **100.0** |

Powder flowability is a critical factor in tablet manufacturing; poor flowability impairs tablet weight uniformity and process efficiency. Glidants are added to formulations specifically to enhance the flow properties of powder blends.

Angle of Repose

SYLOID® 244FP silica and PERKASIL® SM 660 silica delivered superior flowability of the tablet blend, as indicated by the lowest angle of repose values (a lower angle denotes better flow). This enhanced flowability results in:

- Uniform distribution of active ingredients

- Improved tablet weight consistency

- Reduced production time

Tablet Hardness

Tablets manufactured with SYLOID® 244FP silica exhibited superior hardness compared to those made with pyrogenic (fumed) and precipitated silica. This increased hardness prevents tablet breakage during processing, packaging, and transportation.

Tablet Weight Variation

Tablet weight variation is a common issue in tablet compression and directly impacts the accurate delivery of active ingredients per dose. Utilizing SYLOID® 244FP silica as a glidant resulted in the lowest tablet weight variation among all tested silica materials, ensuring consistent dosage delivery.

Performance in Powder Nutritional Supplements

Grace’s SYLOID® and PERKASIL® silicas are uniquely suited for formulating powder-based nutritional supplements. In bulk powder applications, maintaining free-flowing behavior during processing is critical to minimizing production downtime and ensuring product quality and homogeneity. Free flow is defined as the ability of a powder to maintain its flow velocity once in motion.

In this regard, Grace’s SYLOID® and PERKASIL® silicas act as high-performance free-flow agents, performing the following key functions:

- Prevent particle packing and act as a physical barrier during compaction

- Coat and smooth the surfaces of bulk powder particles, reducing inter-particle friction

- Adsorb excess atmospheric moisture before it is absorbed by the bulk powder

- Adsorb moisture and oil that migrate out of the bulk powder matrix

Grace’s silicas are manufactured to high purity standards, are chemically inert, and deliver exceptional performance in ensuring free flow – even for the most challenging powdered supplement formulations.

Benefits of SYLOID® FP Silica Excipients for Moisture Control and Adsorption

- Enhanced product uniformity during blending

- Improved manufacturing efficiency

- Low usage levels, resulting in lower formulation costs

- High load-carrying capacity for active and excipient ingredients

- Effective protection against moisture pick-up

- Reduced dust generation during production

- Minimized tablet weight variation

- Lower tablet friability and improved hardness

- Increased production rates

- Enables direct compression processing, eliminating the need for granulation

Benefits of SYLOID® 72FP Silica and SYLOID® G 156F* Silica for Glidant Applications

SYLOID® 72FP and SYLOID® G 156F* silicas are specifically designed as cost-effective glidants for pharmaceutical formulations, offering the following advantages:

- Enhances flowability for both standard and challenging formulations

- Reduced dust generation, lowering the potential for cross-contamination

- Low bulk density, enabling easier handling and storage

*Only available in the Americas

Summary

Selecting the right excipient is a critical decision that can significantly improve production efficiency, product quality, and formulation development validation time – while overcoming the common challenges associated with nutraceutical and vitamin formulations.

Incorporating SYLOID® silica excipients into formulations addresses many of the key challenges in nutraceutical and vitamin manufacturing. These silicas drastically improve the flow properties of powder blends, enabling formulators to achieve consistent flow that translates to better product uniformity, enhanced tablet strength, and minimal tablet weight variation.

Regulatory Compliance

SYLOID® FP silica products are manufactured and certified to meet the test requirements outlined in the latest editions of:

- USP-NF for silicon dioxide

- JPE for hydrated silicon dioxide

- EP for colloidal hydrated silica and dental-type silica

- Chinese National Standard GB25576-2010 Class III

All FP products also comply with global food additive standards, including:

- Food Chemical Codex (FCC)

- EU Directive No. 231/2012 for E551

- Japanese Specification and Standards for Food Additives D326

- JECFA requirements for Amorphous Silicon Dioxide

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

Grace Corporate Headquarters

W. R. Grace & Co.

7500 Grace Drive

Columbia, Maryland 21044 USA

Tel.: +1 410.531.4000

Regional Locations

**Latin America**

São Paulo, Brasil

Tel: +55.15.3141.4100

**Asia Pacific**

Shanghai, China

Tel: +86.21.3325.8288

**Europe**

Worms, Germany

Tel.: +49.6241.40300

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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 cannot 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®**, **PERKASIL®**, 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 2023 W. R. Grace & Co.-Conn. All rights reserved.

GRACE

Talent | Technology | Trust

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