The BCS is a system that was developed to differentiate drugs on the basis of their:

• Solubility, and
• Permeability

Also, dissolution rate plays a role.

Solubility class boundaries are based on the highest dose strength of an immediate release (IR) product. The drug is considered highly soluble when the highest dose strength is soluble in 250 mL or less of an aqueous media of a pH in the range of 1 to 7.5. This quantity of 250 mL is commonly used in bioequivalence studies where subjects take the study drug with a "glass" of water (generally 8 ounces).

Determined by:

• pH-solubility profile
• Shake-flask method
• Analysis by a validated stability-indicating assay

Permeability class boundaries are based upon a comparison to intravenous infusion. The basis is indirectly on the extent of absorption of a drug in humans and directly on the measurement of rates of mass transfer across human intestinal membrane. In addition, in some cases it can be based on non-human systems that can predict drug absorption in humans, including some in-vitro culture methods. A drug is highly permeable when 90% or more of the administered oral dose is absorbed.

Determined by:

• Absorption extent in humans
  • Mass-balance pharmacokinetic studies
  • Absolute bioavailability studies
• Intestinal permeability methods
  • In vivo intestinal perfusion studies in humans
  • In vivo or in situ intestinal perfusion studies in animals
  • In vitro permeation experiments with excised human or animal intestinal tissue
  • In vitro permeation experiments across epithelial cell monolayers

Dissolution class boundaries consider a drug to be rapidly dissolving when at least 85% of the drug dissolves within 15 minutes in USP Dissolution Apparatus 1 or 2 under prescribed conditions.

Determined by:

• USP apparatus I (100 rpm) or II (50 rpm)
• Dissolution media (900 mL): 0.1 N HCl or simulated gastric fluid, pH 4.5 buffer, and, pH 6.8 buffer or simulated intestinal fluid
• Compare dissolution profiles of test and reference products using a "similarity" factor (f₂)

Next week, we will look at BCS Classes I through IV and their characteristics

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

Opioid addiction too costly; communities deciding who should be saved

• In towns across Ohio, debates are emerging as legislators ponder both the fiscal and emotional costs of an opioid epidemic that killed nearly 4,000 people in the state in the last year.
  
  
• Larry Mulligan Jr., Mayor of Middletown, said the city has spent $100,000 on Narcan in the first six months of the year, a tenfold increase from what the town spent during all of last year.
  
  
• A city council member, has proposed a controversial three-strikes policy in which first responders wouldn't administer Narcan to repeated overdose victims.
  
  
• In 2016, Ohio EMS units administered at least 19,570 doses of Naloxone, according to state records covering the first nine months of the year.
  
  
• Two doses of Evzio Injection, cost $4,500, up from $690 in 2014. The price of other forms of the drug, including the nasally administered Narcan, typically range from $70 to $150 per dose, officials say.
  
  
• Further complicating the costs, the potency of the newest batches of opioids often means first responders must administer multiple doses of naloxone to revive patients. Health officials say powerful additives to the illicit market-such as fentanyl and carfentanil-are to blame.
  
  
• Even if saved, an opioid user often is back on drugs within days, if not hours, officials say. Here in Ohio, first responders say it's not uncommon for overdose victims to have previously been revived with naloxone at least a half-dozen times.
  
  
• Some officials and residents are starting to ask how a community can bear to try to help those who do not appear to want to help themselves.
  
  
• State and local officials say it might be time for "tough love": pushing soaring medical costs back onto drug abusers or even limiting how many times first responders can save an individual's life.
  
  
• In Maryland, concerns about funding also have forced the Baltimore Department of Health to ration its dwindling naloxone supplies, providing kits to areas where the need is greatest.
  
  
• The state of Kentucky's Office of Drug Control Policy reports 1,404 overdose deaths last year.
  
  
• People in the nation's heartland, Jones said, are fed up with "enabling these people" amid a surge in drug-related
  • foster care cases
  • property crimes
  • emergency room visits

https://www.washingtonpost.com/world/as-opioid-overdoses-exact-a-higher-price-communities-ponder-who-should-be-saved/2017/07/15/1ea91890-67f3-11e7-8eb5-cbccc2e7bfbf_story.html

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Did You Know ...

�Life from the seat of a tractor�?

Tip of the Week

-Your fences need to be horse-high, pig-tight, and bull-strong.
-Keep skunks and bankers at a distance.
-Good judgment comes from experience, and a lot of experience comes from bad judgment!

Looking Back

Don't try passing,
On a slope,
Unless you have,
A periscope!
     Burma Shave