Merck KGaA

Novel Pharmaceutical Salt Forming Counterions with Increased Dissolution Rates and Supersaturation

Posted by Merck KGaAResponsive · Innovative Products and Technologies · Germany

Summary of the technology

One of the major obstacles in developing promising New Chemical Entities (NCEs) as Active Pharmaceutical Ingredients (APIs) is their low solubility and therefore poor bioavailability.

Merck has developed a novel class of salt forming anions as counter-ions for protonated free base APIs which result in an accelerated dissolution rate and increased solubility by supersaturation of the NCE.

The invention is based on a systematic thermodynamic and molecular engineering approach to design the above mentioned anions resulting in crystal lattices of API salts with weak Coulomb interactions.

Merck KGaA
Merck KGaA

 

 

Fig. 1: Illustration of different anion packing in a pharmaceutical salt with strong (left) and weak (right, increased dissolution rate and supersaturation) charge attraction in the crystal lattice.

 

 

 

Fig. 2: Effect of increased dissolution rate and supersaturation (red) of novel anions compared to standard salt (blue).

 

State of the Art


One of the major obstacles in developing promising New Chemical Entities (NCEs) as Active Pharmaceutical Ingredients (APIs) is their low solubility and therefore poor bioavailability.


The growing need for nano-molar activity with high specificity and low side effects of APIs increased this problem over the last decades. Different pharmaceutical formulation technologies do already exist but have their specific drawbacks in obtaining an optimized drug product meeting all requirements.


Innovation


Merck has developed a novel class of salt forming anions as counter-ions for protonated free base APIs which result in an accelerated dissolution rate and increased solubility by supersaturation of the NCE.
The invention is based on a systematic thermodynamic and molecular engineering approach to design the above mentioned anions resulting in crystal lattices of API salts with weak Coulomb interactions.

The molecular fragments based approach for the molecular design uses toxicologically known building blocks. In-silico toxicity and Ames test were negative. The novel technology offers choice in salt selection and greatly improves the solubility of APIs and allows further optimization of counter-ions for specific free base NCEs.

Advantages 

  • Highly increased dissolution rate
  • Multiple concentration by supersaturation

  • Improved solid state properties

  • IP for life cycle extension of existing APIs

  • More efficient discovery process

  • Application as Enabling technology for novel NCEs

 

Intellectual property status

A patent application on novel anions and their pharmaceutical salts was filed.

Desired business relationship

Merck is seeking partners for licensing or transfer and further development of this technology.

Terms

  1. Fast track partnering
  2. Signing fee: 50,000€
  3. Transfer of entire IP package and experimental report on salt forming anions as counter-ions for protonated free base API.
  4. Royalties on net sales: 2 %

 

    Technology Owner

    Merck KGaA

    Large Enterprise

    Related keywords

    • Medicine, Human Health
    • Clinical Research, Trials
    • Medical Research
    • Pharmaceutical Products / Drugs
    • Therapeutic
    • Pharmaceuticals/fine chemicals
    • pharmaceutical salt

    About Merck KGaA

    Large Enterprise from Germany

    Merck KGaA, Darmstadt, Germany is a leading company for innovative and top-quality high-tech products in healthcare, life science and performance materials. Around 39,000 employees work in 65 countries to improve the quality of life for patients, to further the success of our customers and to help meet global challenges.

    Legal Disclamer

    There are two different, unaffiliated companies that use the name MERCK. Merck KGaA, Darmstadt, Germany, which operates this website, uses the firm name “Merck KGaA, Darmstadt, Germany,” in the United States and Canada, and also uses “EMD Serono” in biopharma, “MilliporeSigma” in life science and “EMD Performance Materials” in materials business. The other company, Merck & Co., Inc. holds the rights in the trademark MERCK in the United States and Canada. Merck & Co. is not affiliated with or related to Merck KGaA, Darmstadt, Germany, which owns the MERCK trademark in all other countries of the world. To reflect such fact and to avoid any confusion, certain logos, terms and business descriptions of the publications on this website have been substituted or modified, such as by referring to “Merck KGaA, Darmstadt, Germany” instead of “Merck” standing alone. Publications on this webpage, therefore, slightly deviate from the otherwise identical versions accessible outside the United States and Canada.

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