PEARLITOL® 200 GT Mannitol: Harnessing the Potential of Higher Active Ingredient Content for Smaller, More Convenient Tablets

INTRODUCTION

Mannitol is the first intention excipient for oral solid forms, designed for APIs having stability problems. Mannitol is not hygroscopic and presents a high chemical stability; therefore, it is considered compatible with almost all drugs.

To combine its high stability properties with a cost-effective production process, textured mannitol powders have been developed for the manufacturing of tablets by direct compression.¹

During tablet production, capping may occur depending on the API properties and ratio, the tablet shape (as convex tablets), the compression pressure, and the tablet production speed. Several solutions are proposed to decrease or suppress capping, as precompression step, lower production speed, lower compression force. But often, it appears necessary to decrease the API content to produce conform tablets at an acceptable production output.

PEARLITOL® 200 GT is a new pure beta mannitol grade for direct compression which powder properties have been optimized to limit the occurrence of capping. It was demonstrated that the high powder density of this new and innovative directly compressible mannitol explains its unique behavior of suppressing capping or moving it to higher compression force and/or higher tableting speed.²

OBJECTIVES

This study aimed to demonstrate that PEARLITOL® 200 GT gives effectively access to higher API content, and consequently smaller tablet size, compared to two well-known directly compressible mannitol products: Mannitol SD-A, a spray-dried mannitol and Mannitol G-B, a granulated mannitol.

Sitagliptin was used as a drug model as its powder properties favors the occurrence of capping. The objective was to formulate tablets of 400 mg weight and 100 N hardness.

A compression simulator STYLCAM 200R from MEDELPHARM (France) was used, and a production at 140,000 tablets/hour on a KORSCH XL400 was simulated. Increased ratio of sitagliptin were tested until capping was observed.

MATERIALS AND METHODS

Materials

PEARLITOL® 200 GT mannitol from Roquette Frères (Lestrem, France)

Mannitol SD-A: spray-dried mannitol

Mannitol G-B: low density granulated mannitol

Sitagliptin phosphate monohydrate powder (Starpharm, China)

Vegetal magnesium stearate (Roquette Magnesium Stearate)

RESULTS

The TADES powder properties quotation system was used to predict the behavior of the blends in the tablet press and assure that the feeding was good enough to produce tablets with constant properties.

Sitagliptin itself has poor powder properties (see fig. 1) and is not usable on a rotary press. Indeed, it was not possible to produce any tablet on the compression simulator. All blends with 25% sitagliptin and mannitol present powder properties ensuring stable tablet production (all properties’ quotations being higher than the limit of 5, represented by the red dotted line). PEARLITOL® 200 GT presents the best behavior, with all properties’ quotations being higher than 6.

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Source: Roquette, website PEARLITOL® 200 GT Mannitol: Access to Smaller Tablet for the Same Active Ingredient Content (roquette.com)