Suppositories, Inserts, Medication Sticks and Drug Delivery System for Vaginal Administration Flashcards
Absorption into the _____ causes first- pass effect
Superior Hemorrhoidal Vein
No esterase or peptidase activity is present in the _____, resulting in a much greater stability of peptide-like drugs
Rectum
Absorption may be directly into the _______, and bypass the liver
Superior Vena Cava
Uptake is via _____ via _____
transcellular absorption; pH-partition
hypothesis
For the treatment of local conditions, like haemorrhoids, ____ are used widely
fatty ointments
Largest single-use category OTC
Haemorrhoidal treatment
Rectal suppository bases can be classified broadly into two types:
fatty and water soluble or water
miscible
Have difficulty disintegrating due to low amount of water present in the rectum
Rectal Tablets
Blood drainage from the vagina is via the vaginal vein. From here the blood moves into the ______ and thus avoids the ____, i.e. the drugs absorbed through vaginal wall bypasses first-pass metabolism in liver
inferior vena cava; hepatic portal system
Vaginal suppositories (pessaries) are most often
prepared with ______. _______- are less common since they are said to promote irritation. ______ are little used, since they promote discomfort on the side of the patient
Glycerol-gelatin bases; Polyethylene glycols; Fatty excipients
May be a problem for drugs that are prone to hydrolysis. Require an applicator, applicators are messy in use and delivering an accurate dose is difficult. Single-dose preparations (3-5mL) are preferred
Vaginal semisolids
Preferred for drugs that are prone to hydrolysis, and in countries that are tropical
Vaginal tablets
Left in the vagina typically for longer periods than vaginal medicated tampons
Vaginal rings
Local action, Irrigation, or Diagnostics
excipients may be added for enhanced stability
Vaginal solutions, emulsions, and suspensions
The functional length of the urethra (from the bladder neck) in females is approximately _ cm; in the male, approximately _ to _ cm
3; 4 to 5
*diameter: __;
*length: __ female, __ male;
*weight: __ female, __ male.
5 mm;
50 mm; 125 mm;
2 g; 4 g;
There is reluctance with _____ as a rectal suppository base because of its relatively slow dissolution
glycerinated gelatin
The rate of spreading and the rate of transportation to the rectal fluid is partially based on
viscosity
It should be stated as a general rule that __ emulsion-type suppositories are strongly discouraged as the probability of drug transfer to the inner phase is high, and drug absorption may become reduced.
w/o
Most commonly used method for production of
suppository on both small & large scale.
Pour molding
