Xiang, Tianyi, and Changquan Calvin Sun. International journal of pharmaceutics 649 (2024): 123636.
Magnesium stearate (MgSt) is widely employed as a lubricant in tablet manufacturing, particularly to mitigate punch sticking when compressing cohesive active pharmaceutical ingredients (APIs). However, recent investigations reveal that under low compaction pressures, external MgSt lubrication may paradoxically exacerbate punch sticking-a phenomenon critically dependent on the interplay of interfacial bonding areas (BA) and particle plasticity.
At low compaction pressures, the highly plastic MgSt undergoes greater deformation than the typically brittle APIs. This results in an extensive MgSt-API contact area, promoting stronger bonding between MgSt and API than between API particles themselves. Since MgSt is pre-applied as a dried suspension on punch tips, the adhesive force between MgSt and the punch remains constant. As a result, API particles preferentially adhere to the MgSt-coated surface, initiating sticking.
With increasing pressure, the bonding between API and MgSt intensifies, but so does API-API cohesion. At intermediate pressures, this leads to a peak in sticking behavior due to the dominant MgSt-API interactions. Only at higher compaction forces does the API-API bonding surpass the MgSt-API interaction, enabling the detachment of the MgSt layer and reducing punch sticking.
This study demonstrates the complex, pressure-dependent behavior of MgSt as a lubricant and underscores the importance of optimizing compaction force relative to API mechanical properties. Magnesium stearate's effectiveness is thus not universal but conditional, necessitating careful formulation and process design in tablet manufacturing.
He, Xianhong, et al. International Journal of Pharmaceutics 664 (2024): 124609.
Magnesium stearate (MgSt) is widely utilized in carrier-based dry powder inhaler (DPI) formulations for its ability to modulate interparticle interactions and improve aerosolization performance. In a recent study using fluticasone propionate (FP) as a model drug, MgSt was combined with lactose fines to investigate potential synergistic effects on powder properties and fine particle fraction (FPF).
Formulations containing 0.5% MgSt and varying lactose fine content (1-10%) demonstrated enhanced flowability and adhesion, which translated into improved FPF. The presence of MgSt significantly reduced the required amount of lactose fines to achieve comparable FPF performance. This synergistic effect is attributed to MgSt's ability to alter carrier surface energy and reduce cohesive forces, thereby facilitating better dispersion of API particles during inhalation.
Mixing order was also found to be critical: pre-mixing MgSt with the carrier before adding fines yielded a higher FPF compared to the reverse order. Rheological analysis further revealed a strong linear correlation between basic flowability energy (BFE), permeability, and FPF, highlighting the predictive value of powder flow properties.
In conclusion, magnesium stearate enhances DPI performance by working synergistically with lactose fines to optimize powder flow and dispersion characteristics, offering an effective strategy to improve drug delivery efficiency to the lungs. This work reinforces MgSt's role as a critical excipient in DPI design and formulation.
Kumar, Rohit, et al. Powder Technology 434 (2024): 119371.
Magnesium stearate (MgSt), a widely used pharmaceutical lubricant, plays a critical role in reducing particle-wall friction during tablet manufacturing. In a recent study examining a 50:50 microcrystalline cellulose (MCC) and lactose blend, MgSt was used in conjunction with colloidal silicon dioxide (CSD) to investigate their interactive effects on powder flow, compaction, and ejection performance.
The findings reveal a complex interplay between MgSt and nano-sized CSD. While CSD enhances flowability by forming porous coatings around host particles, it concurrently masks the surface exposure of MgSt. This reduction in exposed MgSt diminishes its lubricating efficiency, leading to increased particle-wall adhesion and elevated ejection and take-off forces. Notably, tablet picking-an undesirable defect-was linked to take-off forces exceeding 5 N, which became more likely at higher CSD levels due to reduced surface lubrication.
Moreover, the study demonstrated that while MgSt effectively reduces ejection force, its performance is compromised by excessive CSD, highlighting the need for a carefully optimized balance. CSD also significantly influenced bulk density and permeability, emphasizing its dominant role in powder bed structure and flow behavior compared to MgSt.
In conclusion, magnesium stearate is essential for controlling particle-wall friction in tablet formulations, but its functionality can be attenuated by the presence of glidants like CSD. A nuanced understanding of these excipient interactions is key to achieving optimal tablet compaction and minimizing manufacturing defects.
What is the molecular formula of Magnesium Stearate?
The molecular formula of Magnesium Stearate is C36H70MgO4 or Mg(C18H35O2)2.
What is the molecular weight of Magnesium Stearate?
The molecular weight of Magnesium Stearate is 591.2 g/mol.
What are some synonyms for Magnesium Stearate?
Some synonyms for Magnesium Stearate include Magnesium octadecanoate, Magnesium distearate, and Dibasic magnesium stearate.
When was Magnesium Stearate created and last modified?
Magnesium Stearate was created on 2004-09-16 and last modified on 2023-12-30.
What is the IUPAC name of Magnesium Stearate?
The IUPAC name of Magnesium Stearate is magnesium octadecanoate.
What is the InChI key for Magnesium Stearate?
The InChI key for Magnesium Stearate is HQKMJHAJHXVSDF-UHFFFAOYSA-L.
What is the Canonical SMILES representation of Magnesium Stearate?
The Canonical SMILES representation of Magnesium Stearate is CCCCCCCCCCCCCCCCCCC(=O)[O-].CCCCCCCCCCCCCCCCC(=O)[O-].[Mg+2].
What is the CAS number for Magnesium Stearate?
The CAS number for Magnesium Stearate is 557-04-0.
How many hydrogen bond acceptor count does Magnesium Stearate have?
Magnesium Stearate has 4 hydrogen bond acceptor counts.
What is the heavy atom count of Magnesium Stearate?
The heavy atom count of Magnesium Stearate is 41.