Rectal Delivery Part 1 Flashcards
define suppository?
solid, bullet-shaped mass of drug with a base of either cocoa butter or hi-mw-PEG manufactured by casting
Advantages of rectal admin for systemic therapy?
Drug-in-butt stability (DIBS)D – dysphagia/retainingI – irritationB – bypassS – stability
disadvantages of rectal admin?
1) poor acceptance2) variable bioavailability3) difficult to titrate dose
Function of rectum
continence & defecation (do not interfere with these)
what is the distance from anus across stratified squamous epithelium to columnar epithelium?
2.5 cm
describe rectal arterial blood supply
superior rectal artery (branch of inferior mesenteric artery)
venous return for superior rectal vein?
inferior mesenteric vein –> hepatic portal
venous return for middle/inferior rectal veins?
internal iliac –> IVC
describe tonicity, volume, & pH of rectal fluids
pH = 7.2tonicity: isotonic, can deal with slight changesvolume = 3mL, can hold 30-60mL additional
How much of rectal fluid is mucus?
1 - 2%
function of mucus in the rectal cavity
lubricant
describe properties of the two suppository vehicles
1) cocoa butter – melts @ 37C for slow, DR2) hi-mw-PEG – dissolves in fluids
describe properties of rectal gels
concentrated solution of hydrophilic polymerbioadhesive
how does suppository manufacture affect absorption?
1) manufactured – solution incorporated into melted base – drug moleculary dispersed in rectal cavity2) compounded – particles incorporated into melted base – drug particles dispersed in rectal cavity