SUPPOSITORIES Flashcards

1
Q
  • Solid dosage form in which one or more API’s are** dispersed** in a suitable base and molded into a suitable shape
  • Are solid dosage forms intended for insertion into the body orifices where they melt, soften, or dissolve and exert localized or systemic effects
A

SUPPOSITORIES

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2
Q

Suppositories used for nausea and vomiting

A

ONDANSETRON SUPPOSITORY

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3
Q

Suppositories used for nausea, vomiting tranquilizers

A

PROCHLORPERAZINE SUPP
CHLORPROMAZINE SUPP

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4
Q

Suppositories used for opioid analgesic

A

OXYMORPHONE SUPP

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5
Q

Suppositories used for Migraine

A

ERGOTAMINE TARTRATE SUPP

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6
Q

Suppositories used for NSAID

A

HYDROCORTISONE SUPP
MESALAMINE SUPP

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7
Q

Suppositories used for Analgesic-antipyretic

A

OPIGESIC SUPP

PARACETAMOL

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8
Q

Physiologic Factors affecting absorption of drugs from rectal suppositories

inside the body

A

circulation route
colonic contents
ph & lack of buffering capacity of the rectal fluids

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9
Q

Physicochemical Factors affecting absorption of drugs from rectal suppositories

product that you are preparing

A

lipid water solubility
particle size
nature of the base

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10
Q
  • Drugs absorbed in the rectum bypass the first pass effect in the liver instead of being absorbed into the general circulation
  • Lower hemorrhoidal veins surrounding the colon receive the absorbed drug and initiate its circulation throughout the body, bypassing the liver
A

CIRCULATION ROUTE

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11
Q

receive the absorbed drug and initiate its circulation throughout the body, bypassing the liver.

A

LOWER HEMORRHOIDAL VEINS

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12
Q

also assists in the absorption of rectally administered drugs

A

LYMPHATIC CIRCULATION

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13
Q

Rectal fluids are essentially neutral in pH (7.2-7.4) and have no effective buffer capacity, the form in which the drug is administered will not generally be chemically changed by the rectal environment

A

pH & lack of buffering capacity

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14
Q

Rectal fluids are essentially ____ in pH

A

NEUTRAL

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15
Q

pH of rectal fluids

A

7.2 - 7.4

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16
Q
  • It is more effective for a drug to absorbed systematically in an empty rectum than from one that is distended with fecal
  • Diarrhea, tissue dehydration can influence the rate and degree of absorption at the rectal site
A

COLONIC CONTENT

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17
Q
  • a lipophilic drug that is distributed in a fatty suppository base in low concentration has less of a tendency to escape to the surrounding aqueous fluid than does a hydrophilic substances in a fatty base.
  • the more drug a base contains, the more drug will be available for absorption
A

LIPID WATER SOLUBILITY

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18
Q
  • Smaller particle size the more readily the dissolution of the particle and the greater chance for rapid absorption
  • It is preferable to avoid a too fine particle size because of the high increase of the viscosity of the melted excipient that can result from the use of excessively small particles and possible difficulties in flow during production
A

PARTICLE SIZE

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19
Q
  • Base must be capable of melting, softening or dissolving to release its absorption
  • If the base interacts with the drug to inhibit its release , drug reaction will be impaired or prevented
  • If the base irritates the mucous membranes of the rectum, it may initiate a colonic response and prompt a bowel movement, eliminating the prospect of complete drug release and absorption
A

NATURE OF THE BASE

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20
Q

Most frequently used for rectal suppositories

A

FATTY BASE

oleaginous

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21
Q

3 classification of bases

A

FATTY OR OLEAGINOUS BASE
WATER SOLUBLE OR WATER MISCIBLE BASE
MISCELLANEOUS BASE

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22
Q

Mixture of oleaginous and Water soluble and water miscible

A

MISCELLANEOUS BASE

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23
Q
  • Theobroma cacao
  • Melts at 30-36°C
  • Ideal rectal suppository base
  • Disadvantage: bec of triglyceruide exhibit polymorphism=> crystals
  • Must be slowly and evenly melted in water bath to avoid crystallization
  • Phenol and chloral hydrate-lowers melting pt
  • Cetyl esters wax (20%) or beeswax (4%) (product will not solidify anymore)
A

COCOA BUTTER

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24
Q

most commonly used fatty or oleaginous base

A

COCOA BUTTER

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25
* triglycerides of **saturated** fatty acids (**lauric acid**) * triglycerites of saturated fatty acids C12-C18 with varied portion of corresponding partial glycerides)
WITEPSOL BASES
26
Triglycerides **derived** from **coconut oil**
WECOBES BASES
27
**Commercially available** triglycerides from palm, palm kernel, and coconut oils with **self emulsifying** glyceryl monostearate and polyoxyl stearate
FATTIBASE
28
* Most frequently used in the preparation of **vaginal suppositories** * Gelatin (**20%**) glycerin (**70%**) Medication (**10%**) * Tends to **absorb** moisture, has **dehydrating effect** and **irritates** tissue upon insertion (moist prior to insertion)
GLYCERINATED GELATIN BASE
29
components of **glycerinated gelatin base**
Gelatin (20%) glycerin (70%) Medication (10%)
30
Gelatin (**60%**) glycerin (**20%**) Medication (**20%**)
URETHRAL SUPPOSITORIES
31
* are **polymers** of ethylene oxide and water prepared to various chain lengths, molecular weighs and physical state. * Having average molecular weights of **300**, **400** and **600** clear, colorless liquids, while those with molecular weighs of 600-1000 are semisolids * **Do not melt at body temperature** but rather dissolved slowly in the body’s fluid * Do not leak from **orifices**
PEG SUPPOSITORIES
32
**oldest** and **simplest** method, by **rolling** the suppository into the desired shape. The mass is then rolled into a **cylindrical rod** of desire length and diameter
MOLDING FROM A MELT
33
**cold mass** of the base containing the drug is **compressed** into suppositories by using **compression** into the desired shape
COMPRESSION
34
If **Glycerinated gelatin** will be used as the **base**. The mold should be **lubricated** with ______
MINERAL OIL
35
If suppositories are stored in **extreme dryness** it may lose ____ and become
LOSE MOISTURE BECOME BRITTLE
36
If suppositories are stored in **high humidity** it will **absorb moisture** and tends to become ____
SPONGY
37
**Cocoa butter** should be stored inside the ____
REFRIGIRATOR
38
**Glycerinated gelatin** should be placed in ____
CONTROLLED ROOM TEMPERATURE
39
PEG should be placed in ____
USUAL ROOM TEMPERATURE
40
A **single-use** medicated **transurethral system** for the delivery of alprostadil to the **male urethra** * Treatment of Erectile dysfunction
MUSE
41
* Adv: **easy** to manufacture; **more stable**; **less messy** * Usually **ovoid** packed **with inserter** * Prepared by **tablet compression** * **Lactose** - filler/diluent * **Starch** - disintegrant * **Polyvinylpyrrolidone** - Dispersing agent * **Magnesium Stearate** - lubricant
VAGINAL INSERTS
42
more preferred than vaginal suppositories
VAGINAL INSERTS / VAGINAL TABLET
43
* Administering **topical** drugs * **Cylindrical** in shape ranging from 5 to 25g * Packed in an **applicator tube** for topical administration and the applicator can be **adjusted** to continually exposed new fresh sticks How to prepare: * Same as preparing supp except that melt is **poured** into the **administering device** or tube * Local anesthetics, sunscreens, oncology products, antiviral and antibiotics
MEDICATION STICKS
44
**Opaque** bases inclues
WAXES OILS PEGS
45
**Clear** bases included
SODIUM STEARATE GLYCERIN
46
# SIZE Rectal (adult)
32mm (1.5 in)
47
# SIZE Rectal (**infant** and **children**)
16mm
48
# SIZE URETHRAL MALE
3 - 6 mm
49
other name for **vaginal** suppositories
PESSARIES
50
other name for **urethral male supp**
BOUGIES
51
# WEIGHT Rectal (**adult**)
2g
52
# WEIGHT Rectal (**infant** and **children**)
1g
53
# WEIGHT Vaginal
5g
54
# WEIGHT Urethral Male
4g
55
**long**, **cylindrical**, one or both ends **tapered**
RECTAL ADULT
56
**pencil-like** shape
RECTAL INFANT & CHILDREN
57
**globular**, **oviform**, or **cone** shape
VAGINAL
58
**slender**, **pencil-shaped**
URETHRAL MALE & FEMALE
59
# SIZE Urethral Female
70mm
60
# WEIGHT URETHRAL MALE
4g
61
# WEIGHT URETHRAL FEMALE
2g
62
Latin name for suppositories
SUPPONERE
63
***supponere*** means
TO PLACE UNDER
64
**avoiding** the **breakdown** of certain drugs that are susceptible to
GASTRIC DEGRADATION
65
the ____ of the **rectum** and **vagina** **permits the absorption** of many soluble drugs
MUCOUS MEMBRANE