Technology

High-Precision agitation of the very small amount of solutions. Contribution to the development of low-cost and efficient high-dissolution test methods.

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MICROPADDLE can directly stir samples on a 96 well plate

Principal scientist Mr. Kenichi Sakai, production engineering research department of CHUGAI PHARMACEUTICAL CO., LTD., developed a high-throughput formulation screening (HTFS) system based on the concept of rapid and efficient formulation design of candidate compounds. 1)

Our precise microplate paddle mixer MICROPADDLE played a part in developing the system.

MICROPADDLE is a system that can directly agitate individual samples on a 96 well plate. Twelve agitation conditions can be set in one plate. We asked Mr. Sakai about an application of this product, which can agitate various kinds and a trace amount of samples with high precision and high speed.

1)Sakai K., et al., 2016 AAPS Annual Meeting and Exposition(Denver),37T1030(2016)

The number of elution samples that are evaluated in one day increased from 12 to 1200

In recent years, there is a growing number of pharmaceutical candidate compounds that are poorly soluble. In the early stages of drug development, such as after lead optimization, the limited drugs can be used for formulation, so it is necessary to design the formulation efficiently in a small amount for Phase 1. CHUGAI PHARMACEUTICAL CO., LTD established HTFS system with the keyword "multiple simultaneous high-speed developments".

MICROPADDLE is used to evaluate the dissolution behavior of solid dispersions (SD). The ability to evaluate with high accuracy has a significant impact on the success of formulation design.

When a vessel is used for dissolution tests, the number of samples that can be evaluated at one time is limited due to space limitations. On the other hand, when the evaluation is performed using a microplate, a shaker is required. However, this method does not perform agitation uniformly, so there is a high possibility of overestimation or underestimation.

The efficient evaluation of the kinetic dissolution from the start to the end of dissolution has been required in HTFS to speed up the development of SD formulations.

MICROPADDLE which agitates on a microplate highly accurately achieved this.

MICROPADDLE can be applied to standard 96 well plates, and its simple operation allows high precision agitations. After the installation of MICROPADDLE, the number of samples that are evaluated daily increased from 12 to 1,200. The compound consumption per one sample was reduced to 1/1,000. The agitation of MICROPADDLE is comparable to that using a vessel.
MICROPADDLE has less unevenness of agitation than the shaker method. "It's highly accurate so that you can speed up the development. It is innovation." Mr. Sakai said.

The application in the dissolution test was introduced this time, but Mr. Sakai stated that MICROPADDLE is also useful for the membrane permeability test of formulations, which is a unique technology of CHUGAI PHARMACEUTICAL CO., LTD. Also, he mentioned the possibility that it can be used in all cases where high-precision agitation with a small amount of solution is required.

Realization of the needs and ideas of a pharmaceutical company.

The development of MICROPADDLE started with a word from Mr. Sakai.
When he saw that an intermolecular interaction analyzer was stirring a small amount of solution (ULVAC has been handling the intermolecular interaction analyzer, and agitation of the trace solution is a part of its function), Mr. Sakai said that "I wish we had a stirrer that can stir such a small amount of liquid precisely." His word was delivered to the person in charge, and then the development of MICROPADDLE started.

High precision is the most critical factor in the dissolution test. It is essential for stable results that the paddle and well positions remain constant as well as the control of rotation. Also, there was a particular request for easy operability of positioning this paddle. The person in charge of the development of ULVAC had a hard time to meet the requirements.

Mr. Sakai said, "Everyone uses MICROPADDLE simply by putting it on( a microplate), but it means that you developed a product that everyone can use it without any stress", and praised the highly finished MICROPADDLE.

Mr. Sakai said contentedly, " The equipment manufacturer ULVAC realized our needs. As it was the introduction of a new product, we were worried about initial failures, but they investigated the cause of the failure and reported it accurately, and fix the problem quickly. Thanks to this, we were able to launch HTFS system quickly."

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