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2025
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Summary of the "Universal Pharmaceutical Excipient" in Pharmaceutical Preparations
As excipients and additives in pharmaceutical production and formulation preparation, pharmaceutical excipients not only serve as shaping agents and carriers, improve pharmaceutical stability, but also have functions such as solubilization, dissolution promotion, and controlled/sustained release.
1. Basic Properties of Pharmaceutical Excipients and Silica
1.1 Importance of Pharmaceutical Excipients
As excipients and additives in pharmaceutical production and formulation preparation, pharmaceutical excipients not only serve as shaping agents and carriers, improve pharmaceutical stability, but also have functions such as solubilization, dissolution promotion, and controlled/sustained release. They directly affect the quality, safety, and efficacy of pharmaceuticals.
1.2 Characteristics of Silica
With a chemical formula of mSiO₂·nH₂O, it is a white powder with good fluidity, high purity, and non-pollution. It has small particle size, large specific surface area, and abundant pores. The surface silanol groups endow it with good adsorption performance, which can improve the quality and performance of pharmaceutical preparations (especially tablets) and enhance the market competitiveness of pharmaceuticals.
2. Traditional Applications of Silica in Pharmaceutical Preparations
| Application Scenario | Function and Effect |
| Lubricant | Used in capsules, dispersible tablets, and other pharmaceuticals; can prevent pellet adhesion, accelerate the dissolution rate of dispersible tablets in water, improve dispersion uniformity, and ensure controllable quality. |
| Glidant | Suitable for the wet granulation and tableting process (for relatively stable pharmaceuticals); solves the problems of insufficient fluidity, compressibility, and drug release characteristics of most pharmaceuticals, reduces sticking during tableting, lowers friction between particles and between tablets and die walls, and ensures good tablet formation and taste. |
| Anti-adherent | Applied in gel patches; helps this dosage form achieve the advantages of high drug loading, good transdermal effect, good skin compatibility, and no irritation, promoting it to become a new direction and potential new preparation in the transdermal drug delivery system. |
| Adsorbent | Used in solid preparations; significantly improves the in vitro dissolution rate of drugs and solves the problem of low bioavailability of traditional drugs. |
| Antistatic Agent | Aiming at the problem of powder electrostatic adsorption during fluidized bed particle preparation; its surface hydrophilic groups can absorb moisture in the air to form an electrophilic film, or reduce surface resistance through proton transfer, eliminating static electricity. |
3. New Applications of Silica in Pharmaceutical Preparations
3.1 Crystalline Form Stability Promoter
The crystalline form stability of drugs is a basic guarantee for pharmaceutical quality (including its own stability in different environments and the stability of the dominant crystalline form in preparations with excipients during clinical application). Through the action of amorphous excipients such as silica, active pharmaceutical ingredients (APIs) like clopidogrel bisulfate can obtain better crystalline form stability and drug compatibility.
3.2 Grinding Aid
When modifying and extracting drugs in dispersible tablets, it can significantly enhance the water absorption capacity of drugs and shorten the disintegration time. When co-ground with APIs, it can promote the crushing and refinement of APIs, form co-ground materials with high porosity, accelerate water penetration, and strengthen the disintegration effect of dispersible tablets.
3.3 Excipient for Colon-Targeted Preparations
In line with the advantages of the colon-targeted drug delivery system, such as "small dosage, high efficacy, low side effects, and convenient administration," mesoporous silica can load a large amount of poorly soluble drugs and endow the lipid layer with mechanical stability, ensuring that drugs are not destroyed in the gastrointestinal tract and are released to exert efficacy after reaching the ileocecal region.
3.4 Excipient for Sustained-Release Preparations
It helps sustained-release preparations achieve the characteristic of "slow and non-constant drug release in the specified medium after oral administration." Compared with ordinary preparations, it reduces the frequency of administration, improves patient compliance, and lowers drug side effects. At the same time, it has the dual effects of increasing lipolysis rate, promoting drug absorption, and delaying the in vitro release rate of some drugs.
3.5 Other Fields
Two types of modified products have emerged: self-structure modification and blending modification. For example:
3.Mesoporous silica nanoparticles: With customizable pore structure and ultra-high surface activity, they can be used as drug delivery carriers for therapeutic agents to optimize pharmaceutical packaging and transportation.
4.Silicified microcrystalline cellulose (prepared by mixing microcrystalline cellulose and silica in a certain proportion and spray drying): Can be used as a functional diluent for direct compression, solving the problem of uneven distribution of active ingredients in tablets, and suitable for the preparation of tablet cores, orodispersible tablets, and dispersible tablets.
5.Nano-silica: With strong adsorption, hydrophilicity, biocompatibility, and surface polyhydroxyl properties, it can be made into high-quality biosensors and biomarking/detection materials after modification.
4. Current Development Status and Future Trends
4.1 Current Requirements
With the improvement of pharmaceutical safety and efficacy, and the advancement of the consistency evaluation of generic drugs and original drugs, higher requirements are put forward for the quality of silica.
4.2 Future Trends
Modifying silica to obtain better performance is the main direction. However, some new research technologies are not yet mature. For example, mesoporous silica nanoparticles are mostly in the cell experiment stage in the medical field, with few animal experiments and no clinical trials involved. The further development of silica in the pharmaceutical field requires joint efforts from the materials industry and medical research.
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