MEGGLE researchers demonstrate superior water uptake for CombiLac®

Wasserburg, Germany: – Pharmaceutical lactose specialist MEGGLE Excipients &Technology (MEGGLE) has performed a research study demonstrating how its new co-processed excipient CombiLac® is characterized by improved water uptake behavior via Dynamic Vapor Sorption (DVS).

The study was authored by a multinational team of MEGGLE researchers, comprising; Dr. Mirjam E. Dogru, Dr. Vera Fichtner, Ilona L. Pescher, Dr. Christian Nowak and Dr. Franz K. Penz at the MEGGLE Excipients & Technology laboratories at Wasserburg, Germany, assisted by Joseph A. Zeleznik from MEGGLE USA, Inc.

Study objectives

The purpose of the study was to demonstrate the impact of appropriate excipient selection in significantly reducing or preventing the water uptake than can lead to changes in the physical form, functional performance, or chemical stability of many APIs through effects such as degradation by hydrolysis.

These changes can impact API performance during solid dosage form development and manufacture.

The study focused on examining the water sorption characteristics of CombiLac® as a new, co-processed, directly compressible excipient that comprises α-lactose monohydrate (70 %), MCC (20 %) and native maize starch (10 %), in comparison to various physical admixtures (PAMs) having equivalent composition.

Gravimetric monitoring

The team used Dynamic Vapor Sorption to gravimetrically monitor moisture up-take by of different samples over a range of temperatures and relative humidifies (R.H.).

Each sample was dried at 0 % R.H. until constant mass was reached. Two cycles were performed on each sample steadily increasing R.H. up to 90 %.

The team examined a range of materials including three CombiLac® batches and a variety of physical admixtures (PAMs) of equivalent composition: including spray- dried (SD) lactose, pregelatinized starch, milled lactose grade and native maize starch.

Reproducible results

They observed consistent moisture uptake reproducibility (30, 50, 90% R.H.) in the three co-processed lactose-based excipient (CombiLac®) lots with maximum RSD of less than 3%.

A performance comparison showed that co-processed excipient demonstrated superior moisture uptake capacity compared to the PAMs. This effect was clearly evident over the entire water sorption range investigated using equilibrium and non-equilibrium conditions. “This was attributed to the individual component physical properties, including particle size. Kinetics in dm [%] after leaving equilibrium conditions have been recorded and fitted for various relative humidities,” the study observes.

Greater API stability

In conclusion, the team comments:

“DVS results showed that co-processing lactose, MCC, and maize starch was successful in creating an excipient having improved moisture sorption properties superior to a physical admixture having equivalent composition. Water sorption behavior may be tailored to enhance the protective performance of an excipient, which may provide greater API stability.”

The study is available to download from the MEGGLE Excipients & Technology website (see Resources below).

About MEGGLE Wasserburg

Bavarian-based MEGGLE Wasserburg is one of the world’s experts in lactose based excipients and powder technology.

From its roots as a dairy operation in the late 1880s, MEGGLE has become one of the world’s leading manufacturers of pharmaceutical lactose, supplying the pharma market segment with a broad-based and unique lactose product portfolio.

MEGGLE Excipients & Technology has harnessed outstanding product quality and intelligent innovation to become a global leader in the manufacture of lactose-based excipients, focusing on products for direct tableting and dry powder inhalation.

A multidisciplinary team of committed and highly qualified people allows MEGGLE clients to benefit from pioneering experience and innovative drive in industrial milk and whey processing. The company constantly strives to develop high-tech, functional products for solid dosage form applications, where they can deliver maximum performance.

The company has introduced several pioneering products, notably Tablettose®, the world’s first agglomerated lactose for direct tableting, Cellactose® 80, a pioneering co-processed excipient based on cellulose-lactose for outstanding compression and flow properties and RetaLac®, the first direct compressible co-processed excipient using a hypromellose-lactose base for modified release formulations.