Comparative Study of Compressibility, Disintegration and Dissolution

Introduction

Levofloxacin is a widely used broad-spectrum antibacterial drug, and several levofloxacin products in China have passed the consistency evaluation.

In the formulation studied here, the active pharmaceutical ingredient (API) accounts for a relatively high proportion of the tablet, while microcrystalline cellulose (MCC) is used as the main filler. The formulation is manufactured through a fluid-bed granulation and tablet compression process, making the performance of MCC particularly important for granulation, powder flow and tablet formation.

For this reason, levofloxacin tablets were selected as a model formulation to systematically evaluate the application performance and quality characteristics of MCC PH-101.

DESU^® MCC PH-101 is manufactured using Westpoint Pharma's proprietary spray-drying technology platform. By precisely controlling inlet and outlet temperatures, atomizer speed, feed rate and solid content, the manufacturing process enables controlled adjustment of moisture content, particle morphology, particle size distribution, density and porosity.

These structural characteristics can influence the flowability, compressibility, tabletability, disintegration and dissolution performance of MCC in oral solid dosage formulations.

In this study, levofloxacin tablets were prepared using a standard pharmaceutical manufacturing process, including fluid-bed granulation, sizing, blending and tablet compression. The performance of DESU^® MCC PH-101 was compared with commercially available MCC PH-101 products from Germany, Japan and the United States.

The effects of different compression pressures on tablet compressibility, disintegration and dissolution performance were also investigated.

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Experimental Methods

Levofloxacin Tablet Formulation

The formulation composition is shown below:

MCC PH-101 from different manufacturers was evaluated using the same formulation and processing conditions.

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Levofloxacin Tablet Manufacturing Process

4% HPMC E50 aqueous solution was used as the binder.

Fluid-Bed Granulation

The prescribed amounts of levofloxacin and MCC PH-101 were loaded into the fluid-bed granulator.

The 4% HPMC E50 aqueous solution was sprayed from the top as the granulation binder.

The main process parameters were:

• Inlet air temperature: 55°C
• Product temperature: 30°C
• Drying endpoint: Moisture content <3%
• Dried granules: passed through a 20-mesh sieve

Final Blending

Crospovidone was added externally and blended for 5 minutes.

Sodium stearyl fumarate was then added and blended for another 5 minutes.

Tablet Compression

Tablet compression parameters, including filling depth, pre-compression thickness, main compression thickness, feeder speed and production speed, were adjusted to obtain a target tablet weight of 314.50 mg.

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Tablet Quality Evaluation

Disintegration Time

Disintegration testing was performed according to General Chapter 0921, Disintegration Test, Chinese Pharmacopoeia 2025 Edition, Volume IV.

Tablet Weight Variation

Tablet weight variation was evaluated according to General Chapter 0101, Tablets, Chinese Pharmacopoeia 2025 Edition, Volume IV.

Friability

Tablet friability was evaluated according to General Chapter 0923, Friability Test for Tablets, Chinese Pharmacopoeia 2025 Edition, Volume IV.

Dissolution Profile

Dissolution testing was performed with reference to the pharmacopoeial method.

Two dissolution media were used:

• 0.1 mol/L hydrochloric acid, 900 mL
• pH 4.5 acetate buffer, 900 mL

The basket method was used at a rotational speed of 100 rpm.

Samples were collected at 5, 10, 15, 30 and 45 minutes, respectively, and the dissolution profiles were determined and plotted.

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Results and Discussion

How Does Different MCC PH-101 Affect Tablet Properties?

Different MCC PH-101 samples were evaluated in the same levofloxacin tablet formulation under the same compression parameters. The effect of different main compression pressures on tablet physical properties was investigated.

As shown in Table 1, the tablet weight variation of DESU^® MCC PH-101 was comparable to that of the commercially available MCC products.

Although the tablet hardness obtained with DESU^® was lower than that of the German and U.S. commercial products under the tested conditions, DESU^® showed a favorable friability performance.

Table 1. Physical Properties of Levofloxacin Tablets Prepared with Different MCC PH-101 Samples

How Does DESU^® MCC PH-101 Perform in Tablet Compressibility?

The compressibility results show that when tablet hardness reached more than 120 N, DESU^®, Japanese and German MCC PH-101 samples required approximately 13 kN of main compression pressure.

The U.S. commercial product required more than 14 kN under the tested conditions.

The results indicate that DESU^® MCC PH-101 showed a comparable compression performance to the tested commercial products and required less compression pressure than the U.S. commercial sample under the same experimental conditions.

The compression performance of MCC is closely related to its particle structure, degree of polymerization and fibrillation characteristics.

The controlled spray-drying process used for DESU^® MCC PH-101 helps regulate the particle structure and enables MCC particles to form an interconnected network during compression. This structure contributes to tablet mechanical strength while maintaining favorable friability.

Figure 1. Compressibility curves of different MCC PH-101 samples in levofloxacin tablets.

Can MCC PH-101 Improve Tablet Disintegration?

Disintegration is an important quality attribute for immediate-release tablets because it affects the subsequent dissolution and release of the API.

As shown in the disintegration time–hardness profile, DESU^® MCC PH-101 showed a relatively broad operating range of disintegration time within the tested tablet hardness range.

Compared with the three imported MCC PH-101 samples, DESU^® provided flexibility in adjusting tablet hardness while maintaining the required disintegration performance.

This characteristic may be useful when formulation developers need to balance tablet mechanical strength and disintegration performance during formulation optimization.

Figure 2. Disintegration time versus tablet hardness of different MCC PH-101 samples.

Does DESU^® MCC PH-101 Affect Levofloxacin Tablet Dissolution?

The dissolution profiles showed that DESU^® MCC PH-101 provided rapid tablet disintegration while maintaining a dissolution profile generally comparable with the other tested MCC PH-101 samples.

The results indicate that the formulation prepared with DESU^® can achieve rapid tablet disintegration without introducing a significant difference in the overall dissolution behavior under the tested conditions.

For immediate-release formulations, maintaining consistent dissolution performance is particularly important because variations in tablet disintegration and wetting behavior may influence the dissolution profile.

Does DESU^® MCC PH-101 Improve Dissolution Consistency?

In addition to the dissolution profile itself, the relative standard deviation (RSD) of dissolution results can provide useful information regarding the consistency of drug release among tested samples.

At 15 minutes after the start of dissolution, the U.S. commercial MCC sample showed a relatively higher dissolution RSD compared with DESU^®.

The difference may be associated with variations in particle structure, crystallinity and surface hydrophilic characteristics, which can affect the wetting and water uptake behavior of MCC particles.

DESU^® MCC PH-101 is manufactured using a proprietary spray-drying technology platform designed to provide controlled particle morphology and physicochemical properties.

By controlling these characteristics during manufacturing, DESU^® aims to provide more consistent water uptake, wetting and swelling behavior within the same batch, supporting consistent dissolution performance.

What Do These Results Mean for MCC PH-101 Selection?

The results demonstrate that the selection of MCC PH-101 can influence several critical tablet quality attributes, including:

• Tablet compressibility
• Tablet hardness
• Friability
• Disintegration
• Dissolution consistency
• Compression process flexibility

In the levofloxacin tablet model formulation, DESU^® MCC PH-101 demonstrated comparable tablet weight variation and compression performance to the tested commercial MCC products.

At the same time, DESU^® showed favorable friability and disintegration performance, while its dissolution profile remained comparable with the other tested samples.

These results highlight the importance of considering not only pharmacopoeial compliance, but also the functional performance of MCC PH-101 in the actual tablet formulation and manufacturing process.

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Conclusion

This study evaluated the influence of different MCC PH-101 samples on the quality and performance of levofloxacin tablets.

Under the tested formulation and process conditions, DESU^® MCC PH-101 demonstrated favorable performance in tablet compression, friability and disintegration.

The compressibility results showed that DESU^® achieved tablet hardness above 120 N at approximately 13 kN of main compression pressure, while the dissolution profile remained generally comparable with the tested commercial MCC products.

The dissolution RSD results also indicated favorable consistency during the early stage of dissolution.

These results suggest that the particle structure and physicochemical properties of MCC PH-101 can play an important role in formulation development and tablet manufacturing.

Through its proprietary spray-drying technology, DESU^® MCC PH-101 is designed to provide controlled particle morphology, particle size distribution, density, porosity and moisture characteristics.

For pharmaceutical manufacturers developing immediate-release tablets, DESU^® MCC PH-101 can therefore be evaluated as a functional excipient for supporting tablet manufacturability and consistent tablet quality.

DESU^® MCC PH-101 — Beyond Compendial Compliance, Functional Performance.