Formulation Aspects of Sublingual Technology

In today’s fast-paced world, people demand medications that act swiftly and effectively. Sublingual technology or tablets have become a key solution, offering a rapid onset of action that is crucial for managing various medical conditions. The term “Sublingual,” meaning ‘under the tongue,’ indicates how this technology works: the medication directly reaches the bloodstream. Their unique formulation not only enhances efficacy but also makes them a preferred choice for specific patient groups.

Understanding Sublingual Tablets

Sublingual tablets dissolve under the tongue, allowing active ingredients to absorb directly into the bloodstream through the mucosal tissues. This contrasts with traditional oral tablets, which must be swallowed and passed through the digestive system before the drug is absorbed into the bloodstream.

Mechanism of Action:
When patients place a sublingual tablet under the tongue, it dissolves quickly due to the rich blood supply in the sublingual area. This rapid dissolution facilitates faster therapeutic effects compared to oral tablets which undergo a slower digestive process.

Types of Sublingual Tablets:

There are two primary types of sublingual tablets:

1. Molded Sublingual Tablets: Manufacturers form these tablets by molding a paste that contains the active ingredient and excipients.
2. Compressed Sublingual Tablets: Similar to traditional oral tablets, these tablets undergo compression techniques. While they also dissolve quickly, they may have different textural properties.

Formulation Aspects of Molded Sublingual Tablets

Ingredients and Excipients:

• Soluble excipients such as lactose, dextrose, sucrose, and mannitol enhance tablet dissolution.
• Finely divided powders ensure rapid disintegration.
• Solvents like alcohol and water mixtures create a paste with the required consistency.

Preparation Process:

• Blend active ingredients with excipients and moisten the mixture with solvents to form a paste.
• Mold the paste into tablets, optimizing the blend to ensure rapid solubility and disintegration.

Enhance Stability:

• Add antioxidants to prevent oxidation of the active ingredient.
• Use buffers to maintain the tablet's pH and ensure stability.
• Apply techniques such as compression and coating to increase tablet hardness and reduce erosion during handling.

Formulation Aspects of Compressed Sublingual Tablets

• Manufacturing Methods:
  • Wet Granulation Method: This method mixes the drug with excipients and a granulating fluid to form granules, which are then compressed into tablets.
  • Direct Compression Method: This simpler technique compresses the drug and excipients directly into tablets without granulation.
• Key Components:
  • Use directly compressible soluble excipients like microcrystalline cellulose and croscarmellose sodium.
  • Incorporate super disintegrates like sodium starch glycolate to ensure rapid disintegration.
  • Add lubricants like magnesium stearate to improve tablet flow during compression.
  • Utilize sugar-based excipients for taste-masking and a pleasant mouthfeel.

Innovations in Compression:
The Flash Tab technology promotes the rapid disintegration and dissolution of compressed tablets. This advancement helps balance the tablet’s mechanical strength with the need for fast-acting disintegration, optimizing both performance and user experience.

Evaluation of Sublingual Tablets

Physical Evaluation:

• Conduct quality control tests for weight variation, drug content, hardness, and friability. Ensure proper hardness to guarantee optimal drug absorption and stability, maintaining the tablet's integrity and effectiveness.

Disintegration Time (DT):

• Measure the disintegration time to confirm that the tablet dissolves quickly under the tongue. Adhere to USP standards to maintain the medication's effectiveness.

Wetting Time (WT) and Friability:

• Assess wetting time to ensure the tablet begins to dissolve promptly. Perform friability tests to evaluate the tablet’s durability during handling, ensuring it remains intact until use.

‍

In Vivo and In Vitro Evaluation of Sublingual Tablets

Pharmacokinetic Data Analysis:

• Measure key pharmacokinetic parameters such as Cmax (maximum concentration), Tmax (time to reach maximum concentration), and AUC (area under the curve) to evaluate the drug's bioavailability.

Permeation Studies:

• Conduct ex vivo studies using porcine oral mucosa to gain insights into drug permeation and absorption. Use techniques like diffusion cells and Franz diffusion cells for these studies.

Recent Developments in Sublingual Formulations

Sublingual formulations continue to evolve with promising advancements. One of the latest innovations is:

Nitroglycerin Sublingual Aerosols:

• Recent developments feature nitroglycerin-delivering sublingual sprays, which manage conditions like hypertension. These sprays offer rapid relief and enhance patient compliance by providing a convenient and effective delivery method.

The medical world requires constant updates to address new challenges and improve existing solutions. Advancing sublingual technology effectively meets these needs.

The formulation aspects of sublingual tablets play a vital role in creating effective, fast-acting medications. By understanding ingredients, manufacturing processes, and evaluation methods, healthcare professionals and pharmaceutical scientists can develop innovative sublingual formulations, such as Oral Thin Film technology, that cater to various patient needs. As research and technology progress, new developments in sublingual formulations will likely improve therapeutic outcomes and patient satisfaction.

About ZIM Laboratories Limited

ZIM Laboratories Limited is a therapy-agnostic &  innovative drug delivery solution provider focusing on enhancing patient convenience and treatment adherence to drug intake. We offer a range of technology-based drug delivery solutions and non-infringing proprietary manufacturing processes to develop, manufacture, and supply innovative and differentiated generic pharmaceutical products to our customers globally. At ZIM Labs, we provide our customers with a comprehensive range of oral solid value-added, differentiated generic products in semi-finished and finished formulations. These include granules, pellets (sustained, modified, and extended-release), taste-masked powders, suspensions, tablets, capsules, and Oral Thin Films (OTF).

‍