Prochlorperazine buccal

Buccastem tablets are a form of prochlorperazine for buccal administration, containing 3 mg of prochlorperazine in a polysaccharide base. When placed in position the tablet softens over a period of a few minutes to form a gel which adheres to the gum and gradually releases the dmg. 

Prochlorperazine fulfils the criteria for efficient transmucosal delivery it is a highly lipid soluble base with a pKa of 8.1 and is therefore largely non-ionized at salivary pH. Because first-pass metabolism is avoided, the bioavailability via the buccal route is much higher than via the oral route (Figure 7.2). 

Figure 7.2 Mean plasma levels of prochlorperazine versus time in 12 volunteers for the buccal (Buccastem) or oral (Stemetil) delivery of prochlorperazine...

Compounds that are currently marketed or are being considered for buccal or sublingual routes include organic nitrates, barbiturates, papaverine, trypsin, prochlorperazine, benzodiazepines, buprenorphine, capto-pril, isoprenalin, oxytocin, and nifedipine. Oxytocin is currently the only peptide marketed in sublingual form. Sublingual steroids have been examined with moderate success. 

Examples of marketed mucoadhesive formulations are Attach buccal tablets (triamcinolone acetonide), Susadrin sublingual tablets (nitroglycerin Forest Laboratories, NY), and Buccastem buccal tablets (prochlorperazine maleate Reckitt and Colman, England). 

Prochlorperazine maleate buccal tablets are licensed for the non-prescription treatment of nausea and vomiting associated with migraine. 

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