Parameters in Preformulation Studies

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What are the Parameters of Research in
Preformulation Studies?
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Preformulation Study

• Preformulation study the term is frequently
  heard in a pharmaceutical industry. But, what is
  it exactly?
• A Preformulation study is an investigation of the
  physical, chemical, and mechanical properties of
  a drug substance to develop a safe, effective,
  and stable dosage form. Thus, it forms an
  integral part of the drug development process.

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Just like any research study is carried out to
accomplish a particular goal, the main objective
of  Preformulation studies is to accomplish the
following

• To establish the physicochemical properties of
  the new drug substance
• To determine its kinetic profile and stability
• To determine its compatibility with inactive
  ingredients or excipients
• To know the methods of drug processing and storage

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In order to accomplish these goals,
certain Preformulation parameters of the drug
substance are investigated. Lets see what these
parameters are
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1.Organoleptic properties of the
drug

• Organoleptic properties are the aspects that can
  be experienced through ones senses like
• taste, smell, sight, and touch.
• Thus, it includes a recording of the colour,
• odour, and taste of the drug.

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2.Bulk characters of the drug

• This includes
• Crystallinity and Polymorphism
• Hygroscopicity
• Fine particle characterization
• Powder flow properties

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Crystallinity and Polymorphism

• Crystallinity refers to the outer appearance and
  internal structure of the drug molecule
• and can affect its physicochemical
• properties.
• Polymorphism is the ability of a
• compound to crystallise in different shapes with
  different internal structure.

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Hygroscopicity

• Hygroscopicity is the measure of the
• tendency to adsorb atmospheric moisture by the
  drug substance.
• It characterizes the drug stability with
• respect to the environmental humidity.

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Fine particle characterization

• The size of the drug particle can influence its
  dissolution rate, suspendability and other
• properties.
• Thus, it becomes important to classify the
• drug substances as coarse, moderately coarse,
• very coarse, fine, and very fine.

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Powder flow properties

• Since the majority of active pharmaceutical
  ingredients are delivered as powders, either as a
  
• pill or for dissolution, understanding and
• controlling the powder behaviour of drugs are
• extremely important.
• Powder flow properties help you understand
• the ease with which the drug powder will flow
• under a set of specific conditions like humidity,
  pressure etc.

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3.Solubility analysis

• Ionization constant- pKa is the measurement of
  the acidity of the compound. Its determination
  helps in understanding the solubility, protein
  binding, and permeability of the drug substance
  to characterize its properties like absorption,
  distribution, metabolism and excretion from the
  body.
• pH solubility profile helps to understand the
  influence of pH on drug solubility, stability,
  and absorption.
• Common ion effect (Ksp) determines the solubility
  of the drug substance when a soluble compound
  having a common ion with the drug is added to the
  test solution.

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• Thermal effects help to evaluate the drug
  solubility with respect to the changes in the
  temperature of the solvent.
• Solubilization is the method of increasing the
  solubility of sparingly soluble drug substance by
  various techniques like adding a co-solvent,
  changing the pH and temperature, adding a
  surfactant, reducing the particle size etc.
• Partition co-efficient is the measurement of the
  drug lipophilicity or ability to cross a cell
  membrane.
• Dissolution is the process of resolving the drug
  substance into its individual components and
  characterizing their properties.

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4.Stability analysis
The stability of the drug is studied with respect
to various factors like

• Stability in toxicology formulations
• Solution stability
• pH-rate profile
• Solid state stability
• Bulk stability
• Compatibility

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Thus, by investigating the above parameters of a
new drug molecule, scientists can formulate the
drug substance into a stable, safe, and
effective dosage form that can be easily taken
by the patient to cure his illness.
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