Pharmaceutical Technology II: Preformulation and Formulation

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Questions and Answers

What is the estimated development cost of a successfully marketed drug product?

$ 1.8 Billion (correct)

$ 100 Million

$ 856 Billion

$ 500 Million

What percentage of promising drug candidates never generate sufficient sales to recoup their development costs?

70 % (correct)

20 %

50 %

30 %

What is the main objective of preformulation?

To determine the solubility of a drug substance

To evaluate the compression properties of a drug substance

To investigate physical and chemical properties of a drug substance (correct)

To design a suitable assay for a drug substance

What is the growth rate of the pharmaceutical market from 2009 to 2010?

4.1 % Signup and view all the answers

What is the probability of a compound becoming a successfully developed drug product?

1 in 5,000 to 10,000 Signup and view all the answers

What is the primary goal of assay design?

To require minimum amounts of sample and allow determination of multiple parameters Signup and view all the answers

What is the main reason why physical and chemical drug-characterization is crucial?

To ensure the stability of a drug substance Signup and view all the answers

What information does a formulator obtain about potential drug candidates during preformulation?

Chemical identity, purity, assay, and quality Signup and view all the answers

What property of a compound is typically measured using UV, TLC, and HPLC assays?

LogP Signup and view all the answers

What is the sample requirement for measuring solubility using a UV assay?

Presence of a chromophore Signup and view all the answers

What type of assay is commonly used to measure the melting point of a compound?

DSC assay Signup and view all the answers

What is the purpose of measuring the pKa of a compound during preformulation?

To determine the solubility of the compound Signup and view all the answers

What property of a compound is typically measured using microscopy during preformulation?

Chemical identity Signup and view all the answers

What is the difference between LogP and LogD?

LogP is used for non-aqueous solubility, while LogD is used for aqueous solubility Signup and view all the answers

What is the lowest acceptable level of potency in a drug product?

90 % of the label claim Signup and view all the answers

What is the purpose of stability assessment during preformulation?

To challenge the compound by exposure to environmental stresses Signup and view all the answers

Which guidelines define the stability testing protocols?

ICH Guidelines Q1A(R2) Signup and view all the answers

What is the typical temperature range for long-term storage?

25 ± 2 ℃ Signup and view all the answers

What is the minimum duration of data required for regulatory approval for long-term storage?

12 months Signup and view all the answers

What is the purpose of stress conditions in stability testing?

To study the effect of oxidation and photolysis Signup and view all the answers

How many climatic zones are defined by the ICH?

4 Signup and view all the answers

What is the typical humidity range for accelerated stability testing?

75 ± 5 % RH Signup and view all the answers

What is the purpose of measuring hygroscopicity in an assay design?

To study the interaction of a drug candidate with water Signup and view all the answers

What is the reason for the popularity of UV spectrophotometry in drug analysis?

It is a cost-effective and widely available method that requires small quantities of material Signup and view all the answers

What is the term used to describe functional groups that absorb in the ultraviolet region?

Chromophores Signup and view all the answers

What is the relationship between the amount of light absorbed and the concentration of the solute in UV spectrophotometry?

The amount of light absorbed is directly proportional to the concentration of the solute Signup and view all the answers

What is the unit of measurement for the molar absorption coefficient (𝜀)?

L mol-1 cm-1 Signup and view all the answers

What is the significance of a higher molar absorption coefficient (𝜀)?

It results in higher absorbance Signup and view all the answers

What is the purpose of determining the stability of a drug candidate?

To identify potential degradation products Signup and view all the answers

What is the relationship between absorbance and concentration of the solute in UV spectrophotometry?

Absorbance is directly proportional to the concentration of the solute Signup and view all the answers

What is the primary reason why photostability testing is performed in solution?

To account for the possibility of light energy promoting oxidation and hydrolysis Signup and view all the answers

What is the relationship between light energy and wavelength?

Light energy is inversely proportional to wavelength Signup and view all the answers

What percentage of light is absorbed by plain glass in the 290-320 nm region?

80 % Signup and view all the answers

What is the typical size range of pharmaceutical powders?

1-3000 𝜇m Signup and view all the answers

What is the critical size range for effective pulmonary delivery?

2-5 𝜇m Signup and view all the answers

What is characterized by the repetition of atoms or molecules in a regular 3-D structure?

Crystal morphology Signup and view all the answers

How many crystal systems are there?

6 Signup and view all the answers

What is the purpose of light microscopy and electron microscopy in preformulation?

To characterize crystal morphology and particle size Signup and view all the answers

Study Notes

Introduction to Pharmaceutical Technology

The pharmaceutical market is large, with a value of $856 billion in 2010 and a growth rate of 4.1% from 2009.
Only 1 in 5,000 to 10,000 compounds with the potential to become drug substances will be successfully developed into a marketed drug product.
The estimated development cost of a drug is $1.8 billion.
Over 70% of promising candidates never generate sufficient sales to recoup their development costs.
Proper physical and chemical drug characterization is crucial in the development process.

Preformulation

Preformulation involves the investigation of physical and chemical properties of a drug substance, often newly discovered, alone or in combination with excipients.
The formulator obtains useful information on the identity, purity, assay, and quality of potential drug candidates.
Identity is determined using techniques such as UV, NMR, IR, TLC, and DSC.
Purity is determined by measuring moisture content, inorganic elements, heavy metals, and organic impurities.

Assay Design

Assay design involves developing a suitable assay to measure the properties of a drug substance.
An ideal assay should require minimum amounts of sample, allow the determination of multiple parameters, and be applicable to a range of compounds.
Properties measured during preformulation include solubility, pKa, logP, hygroscopicity, and stability.

Spectroscopy

UV spectrophotometry is a popular technique in preformulation due to its cost-effectiveness, availability, and requirement of small quantities of material.
Chromophores are functional groups that absorb in the ultraviolet region (190-390 nm).
Common chromophores include benzene, naphthalene, anthracene, ethylene, and ketone.

Stability

Stability assessment involves challenging the compound (possibly in combination with likely excipients) by exposure to a range of environmental stresses.
Stability testing protocols are defined in the ICH Guidelines Q1A(R2) and comprise long-term, intermediate, accelerated, and stress conditions.
Long-term storage conditions typically involve storage at 25 ± 2 ℃ and 60 ± 5 % RH for at least 12 months.
Intermediate storage conditions typically involve storage at 30 ± 2 ℃ and 65 ± 5 % RH for at least 6 months.
Accelerated stability assessment involves storage at 40 ± 2 ℃ and 75 ± 5 % RH for at least 6 months.

Microscopy

Microscopy is used to characterize crystal morphology, particle size, and surface properties of pharmaceutical powders.
Light microscopy and electron microscopy are the most common instruments used in preformulation.
Particle size is critical in pulmonary devices, with powders needing to be in the 2-5 𝜇m range for effective pulmonary delivery.

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Description

This quiz covers physico-chemical properties, assay design, and spectroscopy as part of pharmaceutical technology. It is a part of the SOPH 331 course at the University of Health and Allied Sciences.