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Drug Excipient Interaction Notes

Preformulation is the stage of drug development where the physicochemical properties of a drug substance are characterized to determine suitable formulations for studies. It involves understanding drug-excipient interactions, which can be physical, chemical, or physiological, and utilizes various analytical methods such as thermal, spectroscopic, and chromatographic techniques to assess compatibility. The ultimate goal is to create stable and effective dosage forms for preclinical and Phase-1 studies.

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626 views3 pages

Drug Excipient Interaction Notes

Preformulation is the stage of drug development where the physicochemical properties of a drug substance are characterized to determine suitable formulations for studies. It involves understanding drug-excipient interactions, which can be physical, chemical, or physiological, and utilizes various analytical methods such as thermal, spectroscopic, and chromatographic techniques to assess compatibility. The ultimate goal is to create stable and effective dosage forms for preclinical and Phase-1 studies.

Uploaded by

anishbanik.21
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We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd

Preformulation Concepts

The stage of development during which the physicochemical properties of drug substance are

characterized & established is known as Preformulation.

The knowledge of relevant physicochemical and biopharmaceutical properties determines the

appropriate formulation and delivery method for Pre-Clinical and Phase-1 studies.

Objectives of Preclinical Study - To develop elegant, stable, effective, and safe dosage forms by

establishing kinetic rate profiles, compatibility with other ingredients and establish physicochemical

parameters of new drug substances.

Drug - Excipient Interaction

What is an Excipient?

An inactive substance that serves as the vehicle or medium for a drug or other active substance is

called as an Excipient.

Types of Drug-Excipient Interactions

1. Physical Drug-Excipient Interactions:

- Common but difficult to detect.

- No new bonds formed; changes affect physical properties.

- Examples: Changes in dosage uniformity, solubility, flow properties.

- Tetracycline forms insoluble complex with calcium carbonate, reducing dissolution.

2. Chemical Drug-Excipient Interactions:

- Involves chemical degradation.

- Reactions like hydrolysis, oxidation, racemization, etc.

- Examples: Esters, amides, lactones undergo hydrolysis.


3. Physiological/Biopharmaceutical Drug-Excipient Interactions:

- Occur after administration.

- Excipients interact with physiological fluids.

- Example: Disintegrants in immediate release tablets.

Analytical Methods for Drug-Excipient Interactions

1. Thermal Techniques:

- Measure changes with temperature.

- Methods: DSC, Isothermal Microcalorimetry, DTA.

a) Differential Scanning Calorimetry (DSC):

- Compares thermal curves of pure vs. mixture.

- Detects compatibility based on enthalpy changes.

b) Isothermal Microcalorimetry:

- Measures heat from physical/chemical processes at constant temp.

c) Differential Thermal Analysis (DTA):

- Detects temperature changes due to exothermic/endothermic events.

2. Spectroscopic Techniques:

- Use electromagnetic radiation to analyze samples.

a) Vibrational Spectroscopy:

- Studies molecular vibrations (IR, Raman).


b) Fluorescence Spectroscopy:

- Measures emitted radiation to assess concentration & environment.

3. Chromatographic Techniques:

- Separate components based on adsorption.

a) Thin Layer Chromatography (TLC):

- Sample moves on a coated plate via capillary action.

- Identical Rf values indicate compatibility.

- Confirmative test after DSC.

Conclusion:

Analytical techniques help in identifying compatible excipients and troubleshooting formulation

issues.

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