Deformulation analysis/ Reverse Engineering

Deformulation analysis (also known as reverse engineering) is a process of analyzing the components of a product to identify the ingredients and their ratios. It involves understanding the chemical and physical properties of the product and its components.

This method is often used in the Pharmaceutical, Food, and Beverage industry to determine the exact ingredients and their ratios used in a product. It is also used in the pharmaceutical industry to determine the active ingredients in a drug and the inactive ingredients used to stabilize the drug. This process can be used to reverse engineer a product (RLD) to replicate the original formulation.

Deformulation can also be used to identify adulterants in food products, improve quality control, and investigate the production of counterfeit products. It is also used to compare the composition of a product to its label claims and to investigate legal disputes between rivals.

Pharmaceutical Deformulation can be used for:

  • Competitive product characterization.
  • Development of generic drug products.
  • Identification of batch-to-batch variations.
  • Comparative analysis of "good" and "bad" samples.
  • Patent infringement or trade secret investigations.

Deformulation involves instrumental techniques and conventional extraction methods to identify and quantify the components of a complex mixture. A judiciously performed reverse engineering exercise can facilitate the decision-making process at various stages of product development. Proactive solid-state characterization of the API in the RLD would reduce risks along the developmental pathway, especially for products containing molecules in which the bioavailability is sensitive to dissolution.

Deformulation analysis/Reverse Engineering is very useful in the pharmaceutical industry because it can help to ensure that products are safe, effective, and of high quality. Particle-size reduction or micronization is a common method used by pharmaceutical companies to improve the dissolution rate of poorly water-soluble drugs (BCS Class II and IV). API particle-size distribution—which directly affects bioavailability and dissolution rate—helps ensure a bioequivalent formulation, especially for drugs having dissolution-sensitive bioavailability. Thus, the information generated from the API's particle-size distribution in the innovator product is critical in ensuring dissolution and bioequivalence. The challenge herein lies in determining the API's particle size in the presence of other excipients. Routine particle-sizing techniques based on light obscuration and laser scattering will not be applicable because of their inability to differentiate between the API and excipient particles. The only feasible technique is microscopy.

Microscopy can differentiate APIs from excipients based on characteristics such as particle shape and birefringence patterns. Under polarized light, crystalline drugs exhibit birefringence patterns whereas many excipients are non-crystalline and therefore do not exhibit a birefringence pattern. Thus, identifying and characterizing the original drug's API at the molecular and particle levels accelerates decision-making and minimizes developmental and regulatory approval time. The tablet can be put in a petri dish containing water, and the disintegration pattern can be examined under a low-power optical microscope. Tablets prepared using direct compression disintegrate into individual particles, whereas tablets prepared by wet or dry granulation disintegrate into particle agglomerates (granules).

Cost and speed to market are keys to success for a generic pharmaceutical company. Achieving bioequivalence to the RLD is a critical part of development, and the chance of bio-failures must be reduced. Reverse engineering is a useful tool for developing generic products to better ensure bioequivalence. A sound reverse-engineering strategy that encompasses the decoding of the RLD's quantitative formula, the solid-state characterization of the API, and the manufacturing process may reduce development timelines and costs.

For effective solid-state characterization of the API ImageProVison is offering a 21CFR Part 11 compliant Microscope Image Analysis system.

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