Innovative dosage forms for targeted formulations

Why are pharmaceutical pellets innovative dosage forms for targeted formulations? Pharmaceutical pellets are an advanced and versatile drug delivery form that is becoming increasingly important in the pharmaceutical industry. These spherical starter cores offer a wide range of benefits and applications, ranging from targeted drug delivery to improving patient compliance.

Pellets can have different size distributions, often ranging from 60 µm to 1,400 µm. The use of pellets allows precise control of the release kinetics of the active substance in the body, which leads to improved therapeutic effectiveness. One classifies according to inert pellets (sugar, MCC pellets) or functional pellets (acid pellets, e.g. tartaric acid pellets).

The manufacturing process of pellet formulations involves the spraying and coating techniques where the active ingredient and functional excipients are layered onto the pellet. A key advantage of pharmaceutical pellets lies in their ability to combine different active ingredients with different release profiles in a single dosage form. This is particularly useful in the treatment of diseases where a combination of multiple drugs is required or where sustained or targeted drug release is required. By precisely controlling the rate of release, pellets can help minimize unwanted side effects and maximize the effectiveness of therapy.

Another plus point is improved patient acceptance. Pellets can be filled into capsules, embedded in tablets, or even mixed into foods, making them more convenient for patients, especially those who have difficulty swallowing pills. This can increase therapy adherence and positively influence the outcome of the treatment. Also in pediatrics – medicines for newborns, babies and small children – pellet formulations offer the great advantage of adapting the dosage to the needs of these patient groups. Complex re-formulations very often become obsolete.

Advantage of pharmaceutical pellets in innovative dosage forms

Pros of Pharmaceutical Pellets

  • Precise Drug Release:

    Pellets allow for controlled and targeted drug release, ensuring optimal therapeutic effects and minimizing side effects, such as dose dumping.

  • Versatile Formulation:

    Pellets can combine multiple active ingredients with varying release profiles in a single dosage form, enabling effective combination therapies.

  • Improved Patient Compliance:

    Smaller pellet sizes and various administration methods (e.g., capsule, tablet embedding) make them more palatable, increasing patient acceptance and adherence to treatment.

  • Enhanced Bioavailability:

    Pellets can improve drug solubility and absorption, leading to enhanced bioavailability and therapeutic efficacy.

  • Flexible Dosage Adjustment:

    Pellets allow for easy dose adjustments, making them suitable for pediatric, geriatric, and patients with special needs.

  • Reduced Side Effects:

    Controlled drug release minimizes peak plasma concentrations, reducing the risk of adverse reactions.

  • Targeted Therapies:

    Pellets can be designed for site-specific drug delivery, beneficial for conditions affecting specific areas of the body.

Myths about Pharmaceutical Pellets

  • Complex Manufacturing?

    Manufacturing processes are often considered as challenging, especially the scale-up from development scale to pilot and production scale. Proven and established scale-up concepts for pellet layering and coating applying the Wurster technology are well discovered.

  • Scale-Up

    Some people believe complex scale-up issues. In reality, that’s not the case, as pellet formulations are easily scalable with the right process technologies.

  • Micropellets

    State-of-the-art production processes are applied for coating micropellets with sizes at 100 µm, such as fluidized bed processes. Avoiding particulate aggregation issues during coating of small particles.

  • high drug load

    With one drug-layering step, a pellet drug load of up to 60 % is usually achievable. For a higher drug load of up to 80 %, a batch split must be applied most likely [1].

  • Not sticking on myths

    Get in touch with CDMOs for pharmaceutical formulation of oral dosage forms, e.g. Glatt Pharmaceutical Services. Having professionals on-board will target your formulations goals with strong benefits.

Remember that the pros and myths can vary based on the specific drug, patient population, and therapeutic goals. It’s important to carefully consider these factors when deciding for using pharmaceutical pellets in Innovative dosage forms. With the best partnering CMDO, your drug formulation will take profit for all aspects.

Summary

Finally, pharmaceutical pellets represent a significant innovation in drug formulation. Their multiple advantages in terms of precise release, combination of active ingredients, and patient acceptance help increase drug efficacy and improve therapy outcomes. With continuous advances in pharmaceutical technology, we can’t wait to see how this formulation technique will evolve in the future.

References

[1] Pharm. Ind. 84, Nr. 12, 1440–1450 (2022)

Pharmaceutical pellets: Innovative dosage forms