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67 Cards in this Set
- Front
- Back
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What are suppositories?
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- solid dosage forms
- of various weights and shapes - usually medicated - for insertion into the rectum, vagina or the urethra - after insertion, suppositories soften, melt or dissolve in the cavity fluids |
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What are the different types of suppositories and what are their weights?
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- Rectal suppositories (weight ca. 2 g)
- Vaginal suppositories (weight ca. 5 g) - Urethral suppositories (cylindrical, 2 g female, 4 g male; unusual dosage form) |
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What are suppositories indicated for?
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- administering drugs to infants and small children, severely debilitated patients, those who cannot take medications orally
- administer drugs for either systemic or local application |
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What are the advantages over oral therapy?
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- Acidic pH of stomach or enzymes destroy drug
- Drugs irritating stomach - Drugs destroyed by first liver passage |
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What are the disadvantages of suppositories?
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- discomfort
- Variation of absorption - Irritation for mucous caused by some drugs or bases |
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What is the anorectal physiology?
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- ~10” long (20-30 cm)
- Nonmotile - 2-3 ml inert mucous fluid - No villi/microvilli - With blood and lymphatic vessels - pH: 7 to 8 |
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True/False
In local action suppositories, the suppository melts and releases the drug into the bloodstream. |
False
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What are some cases in which you would use local action suppositories?
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- Hemorrhoid (astringent, local anesthetic, vasoconstrictor, anti-pruritic, antiseptic)
- Fungal infection - Bacterial infection - Chronic inflammation - Constipation (Glycerin S.) |
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What percentage of the drug is absorbed in the blood circulation when using systemic action suppositories?
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50-70%
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What is the main blood circulation in system action suppositories?
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1. Inferior haemorrhoidal vein (HV)
2. Middle HV 3. Superior (upper) HV |
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What are some cases that you would use system action suppositories?
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- anti-emetic
- transquilizer - vasodilator - analgesic - hypnotic - antipyretic - anti-asthmatic |
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What are the Physicochemical Factors Affecting Rectal Absorption?
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- Lipid solubility (release from base)
- Particle size (dissolution rate, absorption) - Suppository vehicle |
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The ideal suppository base should have what properties?
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- be nontoxic, nonirritating, and easily formed by compression or molding.
- dissolve or disintegrate in the presence of mucous secretions. - melt at body temperature to allow for the release of the medication. - be stable on storage, not bind or otherwise interfere with release and absorption of drug substances |
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Suppository bases are classified according to what?
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their composition and physical properties
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What are the 2 classifications of suppository bases?
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1)Oleaginous (fatty) bases
2)Water soluble or miscible bases |
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What are suppositories composed of?
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- active ingredients
- additives - suppository base |
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What is the active ingredient in a suppository to treat antifungal (local)?
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clotrimazole
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What is the active ingredient in a suppository to treat antibacterial (local)?
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framycetin
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What is the active ingredient in a suppository to treat astringent (local)?
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bismuth subgallate
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What is the active ingredient in a suppository to treat anti-inflammation (local)?
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hydrocortisone
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What is the active ingredient in a suppository to treat low bioavailability (systemic)?
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propanolol HCL
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What is the active ingredient in a suppository to treat GI irritation (systemic)?
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indomethacin
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What is the active ingredient in a suppository to treat anti-emetic (systemic)?
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domperidone
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What is the active ingredient in a suppository to treat analgesic (systemic)?
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oxymorphone HCl
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What are some examples of pharmaceutical additives?
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plasticizer - Cetylalcohol, Propylene glycol
antioxidant, dispersant – Surfactant, Absorbance enhancer |
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What is the purpose of pharmaceutical additives?
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to improve quality
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____ is the fat obtained from the seed of Theobroma cacao (USP).
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cocoa butter
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What is cocoa butter also known as?
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Theobroma Oil
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What are the oil bases?
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1. Theobroma Oil or cocoa butter
2. Synthetic Triglycerides |
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All the acids are bonded to _______, forming an important number of triglycerides that result in Cocoa Butter
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glycerin
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Of the acids in cocoa butter, __% are disaturated triglycerides, of which __% are of the SOS type, __% POS, and the remaining __% are POP, meaning
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80;20;55;5
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What gives Cocoa Butter its physical and chemical behavior, mainly in its fusion and solidification properties ?
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The triglyceride composition:
Stearic Acid Palmitic Acid Oleic Acid |
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Theobroma Oil is a mixture of liquid triglycerides entrapped in what?
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a network of crystalline, solid triglycerides
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At 15-25 degrees C, theobroma oil is in what form?
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hard, amorphous solid
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At 30-35 degrees C (body temperature), what happens to theobroma oil?
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melts to a bland, nonirritating oil
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True/False
In warm clients, you must keep suppositories refrigerated. |
True
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True/False
It is okay to heat theobroma oil over 35 degrees C. |
False
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Because theobroma is a _______ compound, if overheated it will convert to a ______ structure that melts in the ____ degrees C range.
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polymorphic; metastable; 25-30
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What are the 4 forms of cocoa butter crystal and what are their melting points?
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1. beta crystal (mp 34-36 °C)
2. beta’ crystal* (mp 27 °C) 3. alpha crystal* (mp 22 °C) 4. gamma crystal* (mp 18 °C) |
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Synthetic triglycerides consist of what?
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hydrogenated vegetable oils
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True/False
Synthetic triglycerides exhibit polymorphism. |
False
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Which are more expensive: theobroma oils or synthetic triglycerides?
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synthetic triglycerides
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What is an example of a synthetic triglyceride?
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fattybase
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The triglycerides in synthetic triglycerides are derived from what?
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palm, palm kernel, and coconut oils
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What are the characteristics of synthetic triglycerides?
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- stable with a low irritation profile
- needs no special storage conditions - exhibits excellent mold release characteristics - solid with a melting point of 35-37°C |
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What are the water soluble/miscible bases?
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1)Glycerinated Gelatin
2)Polyethylene Glycol (PEG) polymers |
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What is glycerinated gelatin composed of?
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70% glycerin, 20% gelatin, 10% water
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Why should glycerinated gelatin be packaged in tight containers?
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they are hygroscopic
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Are glycerinated gelatins good rectal suppository bases? Why or why not?
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No, because they may exert an osmotic effect and a defecation reflex
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Glycerinated gelatin is a useful suppository base particularly for ____ suppositories.
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vaginal
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What is the appearance of glycerinated gelatin?
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translucent
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What are polyethylene glycol (PEG) polymers incompatible with?
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silver salts, tannic acid, aminopyrine, quinine, aspirin, benzocaine, and sulfonamides
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True/False
PEG's can be formulated by either molding or compression. |
True
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Are PEG's stable? What are they miscible with?
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- They are chemically stable
- Miscible with water and mucous secretions |
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Why can you not store PEG's in a polystyrene prescription vial?
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the polyethylene glycol will adversely interact with polystyrene (use glass containers)
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What is the major disadvantage of PEG's?
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incompatible with a large number of drugs
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An oil-soluble drug will have what kind of release with an oily base?
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slow release
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An oil-soluble drug will have what kind of release with a water soluble/miscible base?
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moderate release
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A water-soluble drug will have what kind of release with an oily base?
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rapid release
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A water-soluble drug will have what kind of release with a water soluble/miscible base?
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moderate release, based on diffusion
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What are the different methods of suppository preparation?
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- Rolled (Hand-Shaped) Suppositories
- Compression-Molded (Fused) Suppositories - Fusion or Melt Molding |
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True/False
Compression-molded (fused) suppositories are formed without heat, only pressure. |
True
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Since the components of suppositories are measured by weight, but compounded by volume, what is required to provide accurate doses?
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density calculations and mold calibrations
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What is used to determine how much of a base will be displaced by a drug?
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density factor
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Density Factor =
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(weight of drug) / (weight of base displaced)
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When the density factor is not known, what is used to experimentally determine it?
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double casting technique
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What are the steps to the double casting technique?
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1) Mix all of the drugs with a portion of the base and use the mixture to partially fill each of the suppository mold cavities
2) Use plain base to overfill each cavity 3) Let cool, then remove excess base from top of mold. Remove suppositories, remelt, and recast to evenly distribute the drug. |
