Pharmatrans TAP Tartaric Acid Pellet applications

In pharmaceutical production of oral solid dose (OSD) medicines, functional starter pellets are used to interact with the active pharmaceutical ingredient to achieve the targeted drug release profile. Functional starter pellets perform a different function from neutral beads that are non-interactive with API.

Functional starter cores can use a variety of acidic or basic carriers, that are ideally suited to modulating the micro- environmental pH and thereby enhance API solubility, especially in sustained- release formulations, where they act as pH-modifiers of weakly basic APIs.

Tartaric Acid uses

For the pharma industry, the main use of tartaric acid has been as a nontoxic and nonirritant material that can be incorporated into pharmaceutical formulations with bicarbonates, as the acid component of effervescent granules, powders, and tablets.

Tartaric acid pellets used as functional starter cores provide a suitably acidic environment to encourage more rapid dissolution of weak basis APIs at higher pH value.

Typically, a formulation with tartaric acid pellets (TAPs) in the OSD’s, enhances the dissolution rate in higher pH environments, such as the lower gastrointestinal tract (GIT). Once the highly soluble tartaric acid reached the GIT, it dissolves, decreasing the pH and facilitating API dissolution.

Tartaric acid excipients used as starter pellets has enabled formulators to design and improve delivery methods and profiles of API.

Tartaric acid pellets are likely to grow and are sought as specific and innovative solutions to overcome different formulation challenges. At the same time, process techniques have evolved beyond the well- known extrusion-spheronization and granulation technologies. These newer processes provide a reliable means of manufacturing API-matrix and pure API pellets.

TAP pellet functional starter cores

TAP provides a new gold standard for formulator designers working with drugs showing pH dependent solubility and therefore require an acidic environment to improve dissolution rate, release, and absorption. The TAP pellets used as cores are highly functional in creating the acidic microenvironment required to make pH dependent drugs successful, such BSC class IV drugs, where use of a tartaric core is almost essential. By dissolving, the tartaric acid provides several functions as an acidic pH-level provider, assisting the dissolution, and increasing the bioavailability of the drug in the GIT.

Since tartaric acid is so fast dissolving (typically within 90 seconds), it allows to prepare smart drug release formulations with best time release of API at the desired point in the GIT.

The main function of the tartaric acid TAP core is to act as a pH-lowering agent, exploiting high tartaric acid solubility to suit drugs that have low solubility at higher pH-values. Poorly soluble drugs in intestinal fluids at higher pH-values may induce a poor bioavailability as a significant problem. Such drugs include,among the others, dabigatran, dypiridamol, and verapamil.

In these cases, the tartaric TAP core can enhance the drug release, speed dissolution, and improve bioavailability.

Pharmatrans TAP® pellets

Pharmatrans Sanaq offers specialized range of TAP with customized particle size distribution and others starter pellets to aid design of various types of solid dosage forms.

The product range, beside TAP, has been extended from standard types of microcrystalline cellulose, such as neutral starter cores CELLETS®, purely made of microcrystalline cellulose and MCELL 100%; to Sugar Spheres; to Mannitol pellets and to Calcium carbonate pellets.

Pharmatrans Sanaq’s TAP® are formulated for superior coating and layering properties for more reproducible product characteristics and to improve the dissolution profile in extended release tartaric pellet formulations.

The sphericity of TAP core acts as a functional starter and it can be layered with the API drug substance, with subsequent polymer film coating to achieve extended-release profile.

The Tartaric acid excipient TAP pellets offered by Pharmatrans Sanaq are manufactured with proprietary technology and assure highly spherical form with narrow particle size distribution (PSD) between 200 and 800 microns.

TAP® advantages

Pharmatrans Sanaq TAP® Tartaric Acid Pellets are formed from particles that are highly optimized to support coating and layering processes to achieve reproducible product characteristics.

In extended-release pellet formulations TAP® pharma tartaric acid starter cores can be integrated to reduce the pH-dependency of the drug release and therefore achieve the desired dissolution profile.

TAP pellets conform with current Ph. Eur./USP standards and are available in two different formats:

• TAP 200 (100µm-350µm particle size)
• TAP 400 (300µm-500µm particle size)

Resources

Click on Pharmatrans Sanaq TAP^® tartaric acid pellets  for product details.
Click on Starter pellets: Materials, manufacturing methods, and applications for further information.