Issues in contemporary drug delivery. Part VI: Advanced cardiac drug formulations

Daniel E. Hilleman, U. V. Banakar

Research output: Contribution to journalReview article

7 Citations (Scopus)

Abstract

Objective: To identify and discuss the clinical utility of new delivery systems and formulations of cardiac drugs. Data Sources: Studies describing or evaluating new drug delivery systems for cardiac drugs were identified through a MEDLINE literature search. Study Selection: All studies describing or evaluating new delivery systems for cardiac drugs were reviewed. Data Extraction: Data were abstracted and evaluated by each author independently. Data Synthesis: The most common oral sustained-release formulations include the wax-matrix system, the gastrointestinal therapeutic system (GITS), and the spheroidal oral drug absorption system (SODAS). The wax-matrix delivery system is limited by the occurrence of 'dose-dumping.' In a low-pH setting, the wax-matrix formulation may dissolve too rapidly, liberating the entire dose in a short period of time. The clinical relevance of this phenomenon is unknown. The GITS and SODAS formulations are less likely to be affected by pH and food. Nitroglycerin is available by many routes of administration. The topical patch forms are convenient to use, but are associated with the development of tolerance. A buccal formulation incorporates a relatively short onset of effect with a three- or four-times-daily dosing regimen. Although tolerance is less of a problem with buccal nitroglycerin than with topical nitrates, this formulation is less convenient to use because of buccal irritation and interference with eating and talking. A new spray formulation of nitroglycerin offers longer shelf-life storage stability and an easier mode of administration. The spray canister is stable for three years compared with 12 weeks for an opened bottle of sublingual nitroglycerin tablets. Sublingual administration of oral cardiac drugs offers the potential for a more rapid onset of effects. Although nifedipine is often given sublingually, objective data indicate that it is not absorbed buccally but rather in the stomach. It appears that the chew-and-swallow route is most appropriate for nifedipine. Captopril is absorbed sublingually but its efficacy has not been demonstrated. Transdermal clonidine improves compliance and is associated with fewer adverse effects than oral clonidine. Transdermal formulations of beta-blockers are currently being evaluated. Conclusions: Further advancements in the development of novel delivery systems for cardiac drugs are expected in the future.

Original languageEnglish
Pages (from-to)203-211
Number of pages9
JournalJournal of Pharmacy Technology
Volume8
Issue number5
StatePublished - 1992
Externally publishedYes

Fingerprint

Drug Compounding
Nitroglycerin
Cheek
Waxes
Drug Delivery Systems
Clonidine
Nifedipine
Pharmaceutical Preparations
Sublingual Administration
Swallows
Information Storage and Retrieval
Captopril
Deglutition
MEDLINE
Nitrates
Tablets
Compliance
Stomach
Eating
Food

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Issues in contemporary drug delivery. Part VI : Advanced cardiac drug formulations. / Hilleman, Daniel E.; Banakar, U. V.

In: Journal of Pharmacy Technology, Vol. 8, No. 5, 1992, p. 203-211.

Research output: Contribution to journalReview article

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abstract = "Objective: To identify and discuss the clinical utility of new delivery systems and formulations of cardiac drugs. Data Sources: Studies describing or evaluating new drug delivery systems for cardiac drugs were identified through a MEDLINE literature search. Study Selection: All studies describing or evaluating new delivery systems for cardiac drugs were reviewed. Data Extraction: Data were abstracted and evaluated by each author independently. Data Synthesis: The most common oral sustained-release formulations include the wax-matrix system, the gastrointestinal therapeutic system (GITS), and the spheroidal oral drug absorption system (SODAS). The wax-matrix delivery system is limited by the occurrence of 'dose-dumping.' In a low-pH setting, the wax-matrix formulation may dissolve too rapidly, liberating the entire dose in a short period of time. The clinical relevance of this phenomenon is unknown. The GITS and SODAS formulations are less likely to be affected by pH and food. Nitroglycerin is available by many routes of administration. The topical patch forms are convenient to use, but are associated with the development of tolerance. A buccal formulation incorporates a relatively short onset of effect with a three- or four-times-daily dosing regimen. Although tolerance is less of a problem with buccal nitroglycerin than with topical nitrates, this formulation is less convenient to use because of buccal irritation and interference with eating and talking. A new spray formulation of nitroglycerin offers longer shelf-life storage stability and an easier mode of administration. The spray canister is stable for three years compared with 12 weeks for an opened bottle of sublingual nitroglycerin tablets. Sublingual administration of oral cardiac drugs offers the potential for a more rapid onset of effects. Although nifedipine is often given sublingually, objective data indicate that it is not absorbed buccally but rather in the stomach. It appears that the chew-and-swallow route is most appropriate for nifedipine. Captopril is absorbed sublingually but its efficacy has not been demonstrated. Transdermal clonidine improves compliance and is associated with fewer adverse effects than oral clonidine. Transdermal formulations of beta-blockers are currently being evaluated. Conclusions: Further advancements in the development of novel delivery systems for cardiac drugs are expected in the future.",
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