Featured Research

from universities, journals, and other organizations

Drug development: Clever crystals

Date:
August 20, 2012
Source:
The Agency for Science, Technology and Research (A*STAR)
Summary:
Water plays a key role in the co-crystallization of active pharmaceutical ingredients, researchers have found.

Water plays a key role in the co-crystallization of active pharmaceutical ingredients, researchers have found.

There is much more to drug development than simply identifying a potent active pharmaceutical ingredient (API). Scientists must ensure that the API can tolerate the production process, remain stable during storage and distribution, and behave appropriately inside the patient's body after administration. One emerging technique for improving the performance of APIs with non-ideal physicochemical properties is to co-crystallize them with a second compound that modulates their behavior. Srinivasulu Aitipamula and co-workers at the A*STAR Institute of Chemical and Engineering Sciences have now developed a novel route for preparing such co-crystals.

The researchers have discovered that adding water droplets can help to form co-crystals of caffeine, a compound known to act as a central nervous system stimulant and a muscle relaxant. Caffeine is inherently unstable to humidity -- a property that can be improved by forming co-crystals with biocompatible compounds such as 4-hydroxybenzoic acid (4HBA). Computer models predict that co-crystals of caffeine and 4HBA in the ratio of 1:1 should form the most stable structure. To date, however, researchers have only been able to produce 2:1 and 1:2 co-crystals.

Aitipamula and his team have now successfully formed 1:1 co-crystals of caffeine and 4HBA, in the form of a monohydrate. By grinding together a 1:1 mixture of the two components along with two drops of water, a crystal structure was formed in which each pair of crystallization partners is partly held together by a water molecule.

According to Aitipamula, the key to water's ability to produce the 1:1 co-crystal is its capacity to both donate and accept hydrogen bonds -- the intermolecular force that holds co-crystals components together. "In the case of the caffeine-4HBA co-crystal hydrate, unused hydrogen bond acceptors and donors are satisfied by forming hydrogen bonds with the water molecule," he says. Without water, the number of hydrogen bond donors and acceptors is unbalanced, resulting in the preferential formation of the 2:1 and 1:2 crystals instead.

The process also works for other APIs, as the researchers have found. They have generated a 1:1 co-crystal hydrate of 4HBA with piracetam, a drug used to treat memory and balance problems. The results suggest that forming hydrates offers an alternative way to generate co-crystals with particular ratios of constituents, expanding the options for forming pharmaceutical materials.

The researchers are currently focused on developing new co-crystals for APIs and studying their physicochemical properties. "Our primary emphasis is to target APIs that pose problems in pre-formulation and dissolution," Aitipamula says.


Story Source:

The above story is based on materials provided by The Agency for Science, Technology and Research (A*STAR). Note: Materials may be edited for content and length.


Journal Reference:

  1. Srinivasulu Aitipamula, Pui Shan Chow, Reginald B. H. Tan. Co-crystals of caffeine and piracetam with 4-hydroxybenzoic acid: Unravelling the hidden hydrates of 1 : 1 co-crystals. CrystEngComm, 2012; 14 (7): 2381 DOI: 10.1039/C2CE25080B

Cite This Page:

The Agency for Science, Technology and Research (A*STAR). "Drug development: Clever crystals." ScienceDaily. ScienceDaily, 20 August 2012. <www.sciencedaily.com/releases/2012/08/120820121224.htm>.
The Agency for Science, Technology and Research (A*STAR). (2012, August 20). Drug development: Clever crystals. ScienceDaily. Retrieved September 30, 2014 from www.sciencedaily.com/releases/2012/08/120820121224.htm
The Agency for Science, Technology and Research (A*STAR). "Drug development: Clever crystals." ScienceDaily. www.sciencedaily.com/releases/2012/08/120820121224.htm (accessed September 30, 2014).

Share This



More Matter & Energy News

Tuesday, September 30, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Do Video Games Trump Brain Training For Cognitive Boosts?

Do Video Games Trump Brain Training For Cognitive Boosts?

Newsy (Sep. 29, 2014) More and more studies are showing positive benefits to playing video games, but the jury is still out on brain training programs. Video provided by Newsy
Powered by NewsLook.com
CERN Celebrates 60 Years of Science

CERN Celebrates 60 Years of Science

Reuters - Business Video Online (Sep. 29, 2014) CERN, the European Organisation for Nuclear Research, celebrates 60 years of bringing nations together through science. As Joanna Partridge reports from inside the famous science centre it's also planning to turn the Large Hadron Collider particle accelerator back on after an upgrade. Video provided by Reuters
Powered by NewsLook.com
This 'Invisibility Cloak' Is Simpler Than Most

This 'Invisibility Cloak' Is Simpler Than Most

Newsy (Sep. 28, 2014) Researchers from the University of Rochester have created a type of invisibility cloak with simple focal lenses. Video provided by Newsy
Powered by NewsLook.com
New Corvette Can Secretly Record Convos And Get You Arrested

New Corvette Can Secretly Record Convos And Get You Arrested

Newsy (Sep. 28, 2014) The 2015 Corvette features valet mode – which allows the owner to secretly record audio and video – but in many states that practice is illegal. Video provided by Newsy
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:

Breaking News:

Strange & Offbeat Stories


Space & Time

Matter & Energy

Computers & Math

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile: iPhone Android Web
Follow: Facebook Twitter Google+
Subscribe: RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins