- In size reduction of dosage forms such as capsules, insufflations, suppositories, and ointments, particle size must be below 60 µm.
- The therapeutic effectiveness of certain drugs can be increased by reducing their particle size.
- The mixing of solid ingredients is easier if they are reduced to the same particle size.
- In the case of suspensions, particles being finer reduces the rate of sedimentation.
- The stability of emulsions is increased by decreasing the size of the oil globules.
- Particle size reduction in formulations such as ophthalmics and those meant for external application to the skin could help to reduce irritation of the skin area to which they are applied.
- The rate of drug absorption depends on particle size. The smaller the particle size, the quicker and greater the rate of absorption.
- The physical appearance of semisolids can be improved by reducing their particle size.
Advanced applications of size reduction are:
Properties of agglomerates: After milling, the breakage behavior of agglomerates aids in the investigation of the impacts of the formulation and mill settings. The breakage behavior is determined by the particle size before granulation as well as the amount of binder utilized. The strength of the granule to be milled is affected by several variables.
Bioavailability enhancement: The bioavailability of poorly soluble medications is frequently linked to the size of the drug particle. Pharmaceutical powders for inhalation must have a specific particle size. It specifies which parts of the respiratory system should be targeted in order for the product to be most effective. Micronization of solids reduces the size of a therapeutic ingredient to make it acceptable for inhalation formulations; it produces consistent results and is a low-cost method of producing small particle sizes.
Handling the powder: Powders have qualities that are similar to both solids and liquids, making handling and processing difficult. They are normally surrounded by air, and the amount of aeration has an impact on how the powder acts. Powder flow is responsible for a variety of production issues, including blending non-uniformity (segregation), under-or over-dosage, inaccurate filling, blockages, and stoppages. All of these issues can be mitigated by reducing the size of the object.
Supercritical fluid technology: Supercritical fluid technology offers the possibility to produce dry powder formulations suitable for inhalation or needle-free injection. It facilitates controlled particle formation in fine form at near-ambient temperatures and integrates particle formation and solvent removal into a single step.
Precipitation: Monodispersed ultrafine particles are produced by precipitation with compressed antisolvents. The medication is dissolved in a solvent before being combined with a miscible antisolvent. The way things are mixed varies a lot. When the solubility of the amorphous state is exceeded, precipitation of amorphous material may be favoured at high supersaturation. The antisolvent is supercritical carbon dioxide, but the solution jet is diverted by an ultrasonic-frequency surface, atomizing the jet into considerably smaller droplets. The advantage is that it can be used for the production of organic-solvent-free particles, has mild operating temperatures for processing biological materials, and is easier for microencapsulation of drugs for controlled release of the therapeutic agents.
Nanotechnology: Wet milling of active drugs in the presence of surfactant causes defragmentation. The obtained nanosuspension has an increased dissolution rate due to the larger surface area exposed, while the absence of Ostwald ripening is due to the uniform and narrow particle size range obtained, which eliminates the concentration gradient effect.
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