Preformulation Studies Pdf

The speed or rate at which drug substance dissolves in a medium is called dissolution rate. It is hydrolyzed by the acid in stomach to liberate the free base which is active. Crystallization of drug in a metastable form after solidification from fused solution, which has high solubility. Two methods are available for determination are as follow.


Every drug has intrinsic chemical and physical properties which has been consider before development of pharmaceutical formulation. The melt is then cooled and solidified rapidly in an ice bath with vigorous stirring. The structure of a solid compound refers as crystallinity and these structures disappear in the liquid and vapor states.

Usually these commence with probing experiments to confirm decay at the extremes of pH and temperature e. To increase the solubility of sparingly soluble solute. So, it is more important factor for product storage than the formulation. To facilitate faster solidification, the homogenous melt is poured in the form of a thin layer onto stainless steel plate and cooled by flowing air or water on the opposite side of the plate. Thermal Analysis It is used to study the physico-chemical interactions of two or more components.

Stability Testing of Pharmaceutical Products is first quantitative assessment of chemical stability of new drug. It also influence the flow and the mixing efficacy of powders and granules. This method is frequently used to study the influence of particle size, surface area, and excipients upon the active agent.

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Cosolvancy To enhance the solubility of poorly soluble materials, the water miscible solvents are used in which the drug has good solubility. One polymorph which is unstable at all temp.

However, the formation of a soluble complex with a low association constant results in increased rates of dissolution and absorption. Solubilization may lead to enhanced absorption and increased biological activity. Amorphous form of Novobiocin is well absorbed whereas crystalline form results in poor absorption. Cartensen published by technomic publishing Co.

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Solvent Method They are prepared by dissolving a physical mixture of two solid components in a common solvent, followed by evaporation of the solvent. It has faster dissolution and absorption rates than crystalline form. Phenobarbitone is insoluble in water. Obviously, this parameter is very critical for drugs of low potency, which may constitute the bulk of the final granulation or table.


In suspension phase transformation from unstable form to more stable polymorph can cause changes in crystal size and caking. Exothermic substances give off heat in the process of dissolution.

Basically reduction in particle size increase contact surface area of the particle, there by ultimately it increase rate of solubility of drug. Drug absorption from ointment bases and suppositories also increased. Solubility determination, pKa determination, Partition coefficient, Dissolution behavior, Common ion effect, Membrane permeability.

Pre formulation aspects of pharmaproducts Ch. To stabilize unstable drugs. Many drug substances exhibit a tendency to absorb moisture. Erythromycin Estolate Prodrug of erythromycin is inactive and tasteless. Impurities may make a compound toxic or render it unstable.

The presentation is successfully added In Your Favorites. To formulate sustained release dosage or prolonged release regimens of soluble drugs by using poorly soluble or insoluble carriers. By using glident we can alter the flow properties. Taste may be acidic, bitter, bland, intense, sweet and tasteless.

These studies are advisable to evaluate samples of toxicology preparations for stability and potential homogeneity problems. Potential Bulk characterization Volatility, optical activity, solvate formation Crystallinity and polymorphism.

During preformulation, john mill utilitarianism pdf it is important to identify the polymorph that is stable at room temperature. Presentation Description The ppt explains the preformulation studies in details and in a very representative manner. Preformulation Preformulation is branch of Pharmaceutical science that utilizes biopharmaceutical principles in the determination of physicochemical properties of the drug substance. Compatibility studies The knowledge of drug excipients interaction is useful for the formulation to select appropriate excipients.

Dielectrical Constant is the effect that substances has, when it acts as a solvent on the case with which it separates oppositely charged atoms. During the pre-formulation evaluation of the drug substance, therefore, its flow ability characteristic should be studied, especially when the anticipated dose of the drug is large. Once past initial toxicity, phase I clinical toxicology begins for actual formulations. Mostly, the unionized form of the drug is the one absorbed.

Preformulation Studies