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Pharmaceutics I Lesson Ten

Dr. Jun Shao

Lesson Ten I. Routes of Drug Administration and Dosage Forms A. Reasons for various routes and dosage forms Local: direct application of drug to desired site of action. Systemic: result from the entrance of the drug into the circulatory system and transport to the cellular site of its action. Long-term or short-term treatment Time allowed to exert effects Physical description! si"e! crystalline structure! melting point! solu#ility$%chemical structure!form!reactivity$ &iologic properties: relate to its a#ility to get to a site of action and elicit a #iologic su#stance 'rug Sta#ility in different routes Bioavailability/Bioequivalence &ioavaila#ility: The rate and extent of a drug #eing a#sor#ed and availa#le to the site of action. &ioe(uivalence: The comparison of #ioavaila#ilities of the same drug from different products. Pharmaceutical )(uivalent: drug products that contain identical amounts of the identical active drug ingredient! that is! the same salt or ester of the same therapeutic moiety! in identical dosage forms #ut not necessarily containing the same inactive Pharmaceutical Alternative: drug products the contain the identical therapeutic moiety%precursor #ut not the same amount! dosage form! or same salt%ester &ioe(uivalent 'rug Products: pharmaceutical e(uivalents or alternatives whose rate and extent of a#sorption do not show a significant difference when administered at the same dose A. *ral Route a. &ioavaila#le +raction f$ : may #e calculated #y comparison of the A,- after oral administration with that o#tained after intravenous administration + . A,-$oral% A,-$intravenous . A#sorption +raction x /- +$ +: +irst-pass meta#olism fraction #. Advantages%'isadvantages: safest! #ut slow drug response! chance of irregular a#sorption! destruction #y 01 en"ymes c. Possi#le dosage forms: ta#lets! capsules! suspensions! &. Rectal Route a. Advantages%'isadvantages: can a#sor# many solu#le drugs. Preferred for drugs destroyed%inactivated #y stomach environment. Also preferred when patient vomiting%unconscious. 2345 of drug a#sor#ed rectally #ypasses the liver. 6ay #e inconvenient%offensive. A#sorption irregular%difficult to predict #. +easi#le dosage forms: solutions! suppositories! ointments &. Parenteral Route a. Advantages%'isadvantages: rapid a#sorption emergencies$! #lood levels more predicta#le! unconscious patients. 'ifficult to remove drug after administration #. +easi#le dosage forms: done outside of intestine! in7ected through the follow of a fine needle into the #ody at various sites. c. 8 primary sites: -su#cutaneous: a( solutions%suspensions! small volumes. )x. 1nsulin. -intramuscular: greater volumes! long lasting. -intravenous: directly into vein. -an #e single! small volume or large volume drip. Allows desired #lood level to #e achieved in optimal manner. d. )ither a sterile suspension or solution or in a suita#le vegeta#le oil. 'rugs administered in a(ueous solution are a#sor#ed more rapidly than solid #%c no disintegration%dissolution$ Slow a#sorption . prolonged drug action depot! repository$. -. )picutaneous Route a. Advantages%'isadvantages #. +easi#le dosage forms: applied topically to the s9in.
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Pharmaceutics I Lesson Ten

Dr. Jun Shao

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