Click to Visit Pharmapproach Marketplace Click to Visit Pharmapproach Marketplace Click to Visit Pharmapproach Marketplace
  • About Us
  • Contact Us
  • Advertise With Us
Sunday, January 24, 2021
Pharmapproach.com
  • Home
  • Post Categories
    • Pharmaceutical Technology
    • Clinical Pharmacy
    • Pharmaceutical Microbiology
    • Pharmacology
    • Pharmaceutics
    • Pharmacy Management
    • Pharma Companies
    • Articles
    • Pharmatips
    • Pharmaceutical Machines
  • Pharma MarketplaceNew!
Post Ads For Free
Pharmapproach.com
  • Home
  • Post Categories
    • Pharmaceutical Technology
    • Clinical Pharmacy
    • Pharmaceutical Microbiology
    • Pharmacology
    • Pharmaceutics
    • Pharmacy Management
    • Pharma Companies
    • Articles
    • Pharmatips
    • Pharmaceutical Machines
  • Pharma MarketplaceNew!
Post Ads For Free
Pharmapproach.com
No Result
View All Result

Preformulation Studies: Bulk Characterization

by Pharmapproach
July 19, 2020
in Pharmaceutical Technology
0
0
SHARES
4.3k
VIEWS
Share on FacebookShare on Twitter

The development of an efficient dosage form usually starts with preformulation studies. These studies are designed to investigate and deliver all necessary data useful to the formulator in developing an optimum drug delivery system that can be mass produced.  In this post, the discussion is focused on bulk characterization of candidate drug molecules in a drug discovery setting.

Bulk characterization of drug molecules involves the characterization of various solid-state properties that could change during process development. Variability of bulk characteristics, such as particle size, shape and surface area, powder flow properties, bulk and tapped density etc., significantly dictate many subsequent events and approaches in drug development processes. Bulk characterization testing includes:

Contents

  • 1 1. Particle size and surface area
  • 2 2. Powder flow properties
  • 3 3. Density
  • 4 4. Compressibility
  • 5 5. Crystallinity
  • 6 6. Polymorphism
  • 7 7. Hygroscopicity
  • 8 References

1. Particle size and surface area

Powders are likely the least predictable of all materials with respect to flowability. This is because there are a whole lot of factors that can change their flow properties. In tablet formulation, particle size distribution and shape influence mixing efficiency and flow properties of powders and granules. 

In addition to the effects of particle size distribution and shapes on various physicochemical properties of a drug substance, the biopharmaceutical behaviours of drug substances are equally affected. For instance, the bioavailability of a poorly soluble drug showing a dissolution rate limiting step in the absorption process can be enhanced when administered in a finely divided state rather as a coarse material.

2. Powder flow properties

Flow properties of powders can be influenced by changes in particle size, shape and density as well as electrostatic charges and adsorbed moisture. Flow properties depend on frictional force and force of cohesion between one powder particle and another. Thus, an in-depth knowledge of the flow properties of powders is essential for an efficient mixing and tabletting process.

Also, there is need to establish as early as possible how the flow properties of a powder may affect formulation and efficacy especially when the expected dose of the drug is large. Powder flow properties are characterized by determining the angle of repose, compressibility index also called Carr’s index, Hausner ratio etc.

3. Density

Bulk and tapped density are measures of densification pattern and packing or arrangement of any powder. These two parameters play a role in packing and particle arrangement of powders, the volume occupied by a given powder bed and the ease with which the powder will flow under a given condition.

It is important to understand these parameters as they are very essential in forming some ideas about the size of the final dosage form.

4. Compressibility

Compressibility is a measure of the relative volume change of powders, that is, its ability to decrease in volume or deform under pressure. This property is useful in selecting appropriate formulation ingredients.

5. Crystallinity

This refers to the unique arrangement of constituent atom or molecules of solids in a regular, periodic pattern. Most candidate drug molecules exist as solid with very few existing as liquids and even less in gaseous form. When dissolved in different solvent under different processing conditions, crystalline substances losses its crystal nature and its polymorphic state modified in addition to change in character or composition of the recrystallized particles.

The degree of crystallinity of drug substances has marked effect on its hardness, density, transparency and diffusion. This influences both the choice of the delivery system and activity as determined by the rate of delivery.

6. Polymorphism

This is the ability of a solid material to crystallize forming at least two different crystalline species with distinct internal lattice. These different molecular arrangements disappear in liquid and vapor states.

Polymorphs differ from one another with respect to their physical properties (e.g., solubility, melting point, optical and electrical properties, hardness, compression properties, density, etc.,) and of great concern is their stability and solubility.

The need to identify the most stable polymorph at room temperature can never be overemphasized.

7. Hygroscopicity

Many drug substances usually absorb or lose moisture from the atmosphere to achieve equilibrium with the water in the atmosphere. The amount of moisture absorbed or lost by a given quantity of a drug substance can vary significantly and continually depending on the relative humidity and air temperature.

These cyclic changes lead to constant variations in the moisture content of unprotected drug substances and excipients and in turn affect the stability, flow properties, compatibility, etc., of drug substances.

References

  • Aulton M. E and Taylor M. (2013). Aulton’s Pharmaceutics: The Design and Manufacture of Medicines. Amsterdam, Netherlands: Churchill Livingstone Elsevier.
  • Chaurasia G. (2016). A Review on Pharmaceutical Preformulation Studies in Formulation and Development of New Drug Molecules. International Journal of Pharmaceutical Science and research, 7(6): 2313-2320.
  • Gibson, M. (2004). Pharmaceutical Preformulation and Formulation: A Practical Guide from candidate Drug Selection to Commercial Dosage Form. Florida: CRC Press LLC.
  • Kulkarni, S., Sharma, S. and Agrawal, A. (2015). Preformulation – A Foundation For Formulation Development. International Journal of Pharmaceutical, Chemical And Biological Sciences, 5(2): 403-406.
  • Kumar, P., Vaishnavi, G., Divya, K. and Lakshmi, U. (2015). An Overview on Preformulation Studies. Indo American Journal of Pharmaceutical Science, 2(10): 1399-1407.
  • Leo, A., Hansch C., and Elkins D. (1971). Partition Coefficients and Their Uses. Chemical Reviews, 71(6): 525-616.
  • Onyishi, I. V. (2015). Lecture on Personal Collection of Onyishi, University of Nigeria, Nsukka, Enugu State.

People whop read this article titled ‘bulk characterization’ also searcced for: bulk characteristics definition, bulk density, solubility analysis in preformulation, partition coefficient in preformulation, crystallinity and polymorphism Related Keywords: What is bulk characterization? What is Preformulation in pharmacy? Why preformulation studies are important? What are physicochemical properties of drugs? What is Preformulation? bulk characterization slideshare, preformulation studies, preformulation studies slideshare, preformulation parameter, drug preformulation, preformulation studies Wikipedia, ph solubility profile in preformulation, preformulation studies of tablets pdf

Tags: Preformulation studies
Previous Post

11 Factors Promoting Counterfeit Drug Production, Sales and Demand

Next Post

The Role of a Social Psychologist in a Pharmaceutical Company

Related Posts

Featured image for Types of Emulsions predictions
Pharmaceutical Technology

Types of Emulsions

January 4, 2021
Featured image for Advantages and Disadvantages of Pharmaceutical Emulsions
Pharmaceutical Technology

Advantages and Disadvantages of Pharmaceutical Emulsions

December 18, 2020
Featured image for Problems Encountered During Trituration and Possible Solutions
Pharmaceutical Technology

Problems Encountered During Trituration and Possible Solutions

November 13, 2020
Featured image for Mechanisms involved in the mixing pharmaceutical powders
Pharmaceutical Technology

Mechanisms Involved in the Mixing of Pharmaceutical Powders

November 13, 2020
Featured image for Mixing of Pharmaceutical Powders
Pharmaceutical Technology

Mixing of Pharmaceutical Powders in Small-Scale Operations

November 13, 2020
Featured image for Effervescent salts
Pharmaceutical Technology

Effervescent Salts

November 11, 2020

Leave a Reply Cancel reply

Your email address will not be published. Required fields are marked *

Post Flash

Pharmaceutical Marketing: 3 Ways to Boost Sales Team Performance

Drug Delivery Systems: An Overview

Factors Influencing Pharmaceutical Plant Layout

Fluidized Bed Dryer

Prescription Drugs and Over-The-Counter Drugs: Do You Know the Difference?

List of Pharmacy Schools in The United States

Standards Organisation of Nigeria (SON) State Offices and Contact Details

Sweetening Agents Used In Oral Pharmaceutical Suspensions

Regulations, Guidelines and Clinical Trials

Drugs, Chemical and Herbal Regulations
Drugs, Herbal, and Chemical Guidelines
Clinical Trials

Important Links

Drug Manufacturing Companies in Nigeria
National Agency for Food & Drugs Admin & Control
Pharmacists Council of Nigeria
Pharmaceutical Society of Nigeria
Journal of Pharmaceutical Development and Industrial Pharmacy
Job Opportunities for Pharmacists

Subscribe via Email

Enter your email address to subscribe to this blog and receive notifications of new posts by email.

Join 812 other subscribers

Submit Articles

Click to Submit Your Article

Archives

  • About Us
  • Advertise With Us
  • Terms and Conditions
  • Privacy Policy
  • Contact Us

© 2021 Pharmapproach Limited. All Rights Reserved .

No Result
View All Result
  • Home
  • Post Categories
    • Pharmaceutical Technology
    • Clinical Pharmacy
    • Pharmaceutical Microbiology
    • Pharmacology
    • Pharmaceutics
    • Pharmacy Management
    • Pharma Companies
    • Articles
    • Pharmatips
    • Pharmaceutical Machines
  • Pharma Marketplace

© 2021 Pharmapproach Limited. All Rights Reserved .

x
This website uses cookies. By continuing to use this website you are giving consent to cookies being used. Visit our Privacy and Cookie Policy.