Nitrofurantoin: Two Particle Sizes and a Gel!

Continuing this week with our discussion of nitrofurantoin formulations (Furadantin, Macrodantin, MacroBid), we will look at another formulation that was developed to aid those patients that experienced nausea when taking the Furadantin tablets. The company related the occurrence of nausea to the rapid absorption of the nitrofurantoin. We discussed last week how the "macro" particles were developed to slow the rate of dissolution and absorption.

Another approach was to develop a dual-release capsule that contained 25 mg of nitrofurantoin macrocrystals and 75 mg of nitrofurantoin monohydrate. The nitrofurantoin macrocrystals have a slower dissolution and absorption rate than the nitrofurantoin monohydrate, but the nitrofurantoin monohydrate is contained in a powder blend that forms a gel matrix when in contact with gastric or intestinal fluids. As a result, the drug slowly releases over time, slowing the rate of absorption.

So, in this formulation, there are two different approaches to minimize or slow down the absorption rate of the drug:

1. A large particle size for 25 mg of nitrofurantoin to retard the dissolution rate, and
2. 75 mg of regular size nitrofurantoin monohydrate in combination with a gel-forming excipient to form a gel and slow the diffusion of the nitrofurantoin to the mucosal surface after it dissolves.

This is an example where dissolution and absorption can be affected by the use of a larger particle size and a smaller particle size inside a gel matrix.

Loyd V. Allen, Jr., PhD, RPh
Editor-in-Chief
International Journal of Pharmaceutical Compounding
Remington: The Science and Practice of Pharmacy Twenty-second edition

News

QuVa Pharma Acquires 503B Manufacturing Facility from Healix
QuVa Pharma, Inc., a newly formed sterile compounding pharmacy led by two industry executives, announces it has completed the acquisition of the assets of the 503B Compounding Pharmacy Services Division of Healix, Inc., including its state-of-the-art manufacturing facility. The modern manufacturing facility acquired by QuVa Pharma is the Healix facility that is located in Sugar Land, Texas. QuVa Pharma expects to retain all current employees and to grow the capacity and staff of the facility over time. The management team is led by Stuart Hinchen, co-founder and CEO, and Peter Jenkins, co-founder. Both executives bring to QuVa Pharma the experience and track records built during their tenure at JHP Pharmaceuticals and Mayne Pharma.
http://www.fiercepharmamanufacturing.com/press-releases/quva-pharma-new-sterile-compounding-pharmacy-services-company-acquires-503b

Rectal Medication Administration Device in Emergency and Critical Care Settings
Hospi Corporation, a medical device company, has announced an alternative for rapid administration of medication and fluids in the acute setting with the use of a novel device, called the Macy Catheter, in the emergency room or intensive-care unit. Designed for the administration of medications and liquids rectally, it has proved easy to use without the need to reposition the patient multiple times and has greatly expanded the number of pharmaceuticals that can be provided to patients lacking oral or intravenous routes. This device is both a clinically effective and cost-effective way to administer medications when patients are unable to swallow.
http://www.fiercemedicaldevices.com/press-releases/study-describes-first-uses-novel-medication-administration-device-emergency

(Editor's Note: Another opportunity for compounding?)

Allergan Recalls Ophthalmics
Allergan has announced that it is conducting a voluntary recall down to consumer level of specific lots of its REFRESH Lacri-Lube� 3.5 g and 7 g for dry eye, REFRESH P.M. 3.5 g for dry eye, FML (fluorometholone ophthalmic ointment) 0.1% (sterile ophthalmic ointment topical anti-inflammatory agent for ophthalmic use, 3.5 g), and Blephamide (sulfacetamide sodium and prednisolone acetate ophthalmic ointment, USP) 10%/0.2% sterile topical ophthalmic ointment combining an antibacterial and a corticosteroid, 3.5 g. This results from a small number of customer complaints which reported a small black particle at the time of use, related to part of the cap of the container.
http://www.fiercepharma.com/press-releases/allergan-issues-voluntary-nationwide-recall-us-specific-lots-refresh-lacri

IJPC Now on Facebook and Youtube

Become a fan of the IJPC Facebook page and share ideas, photos, and keep up to date with the latest compounding information - http://www.facebook.com/IJPCompounding

Learn about the Journal's new multi-media features and view our growing collection of educational and training videos at www.ijpc.com/video or by subscribing to our Youtube channel at https://www.youtube.com/user/IJPCompounding.

Did You Know ...

...that it is amazing the influence that celebrities have on the actions and thought processes of many individuals? After hearing rhetoric for a while, some individuals start thinking it is FACT and start acting like it. Wake up! They live in a dream world!

Tip of the Week

In reality, most celebrities are not good role models, but they have been contributing to changing societies' values and morals over the years; just look at where we are today. The lowering of standards in movies and television shows continues unabated. Wake up and encourage values based on good character, good morals, considerate actions, and what is absolute, not relative!

Looking Back

Shaving brush,
Don't you cry!
You'll be a shoe dauber,
By and By!
     Burma Shave