Parteck® MXP Excipient – Mix. Melt. Perform.
Parteck® MXP Excipient
The hot melt extrusion difference
Poor solubility of APIs is a critical challenge in drug development. One formulation technique to increase solubility and, consequently, improve bioavailability of drugs is hot melt extrusion (HME). With this technology, the API is dispersed, often down to the molecular level, into a polymer matrix to form an amorphous solid dispersion. It is a solventfree process that is applicable to a broad range of poorly soluble APIs, making it suitable for various solid dosage formulations.
Our new Parteck® MXP is specifically designed for application in HME. The polyvinyl alcoholbased enhances the solubility of a wide range of APIs with low solubility. The polymer used in Parteck® MXP has a long safety record related to its usage in drugs and is generally recognized as safe (GRAS) by the U.S. Food and Drug Administration. Parteck® MXP excipient complies with United States Pharmacopoeia (USP), European Pharmacopoeia (Ph Eur), and Japanese Pharmacopoeia for excipient (JPE) monographs.
Fast dissolution. High solubility. Long stability.
Using a fixed API load of 30 %, a dissolution of extruded Parteck® MXP and other polymers for HME was assessed in a performance study of itraconazole extrudates. Parteck® MXP demonstrated a faster dissolution time and a higher maximal solubility value when compared to marketed polymers under the same conditions (Fig. 1).
Longterm stability of extrudates at a higher API load can be a major concern for the stability of the drug product. Milled itraconazole: Parteck® MXP extrudates were stored under various conditions for six months. Stability was assessed using HPLC (API chemical stability), DSC (assessment of recrystal lization from amorphous state), and repeat dissolution. As seen in Fig. 2, the extrudate was stable under all conditions.
Enhanced solubility. High API load. Broad range of APIs.
For the APIs assessed in our studies, using Parteck® MXP significantly enhanced solubility with no detectable degradation of the API.
Parteck® MXP has excellent thermocapacity which can lead to increased solubilization of the API. Due to its high degradation temperature, extrusion above 200 °C shows no degradation of the polymer thereby making it applicable to APIs across a wide range of melting temperatures (Tm). Parteck® MXP can achieve a minimum API load of 30% in the majority of APIs that were tested.
Dissolution studies were performed using recommended conditions from the FDA.
*Plasticizer is required to make the extrusion feasible or easier
Flexible release kinetics. Variety of dosage forms.
Once the challenges of solubility enhancement have been overcome, difficulties in the final oral formulation can arise. These may vary based on the intended final release kinetics, final dosage form, and inherent properties of the polymer itself (e.g., poor aqueous solubility).
Using the same extrudate, Parteck® MXP can be easily formulated into a variety of final oral dosage forms with immediate or sustained release kinetics, without the need to fine-tune the polymer.
Furthermore, some dosage forms in our studies, pending on the desired release kinetics, had little to no additional excipients added to optimize the formulation and feature a high API load. Tablets (direct-shaped or compressed) are very strong (>200 N) and are resistant to alcohol, thus leading to reduced dose dumping and side effects.
See the full white paper on “Parteck® MXP Excipient – Mix. Melt. Perform.” here
(click the picture to download the white paper)
Source: Merck white paper “Parteck® MXP Excipient – Mix. Melt. Perform.”
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