Suppository, Inserts, and Sticks

Question 1

Suppository

Answer 1

Solid DF
One or more API dispersed in suitable base
Molded formed into shape for insertion
Insertion in orificies for systemic or local effects

Question 2

Inserts

Answer 2

Solid DF
insert naturally occurring body cavity other than rectum (w/ mouth or rectum)

Question 3

Medication Sticks

Answer 3

convenient form of administration

Question 4

Reasons for choosing rectal route:

Answer 4

• Patient cannot make use of the oral route
• The drug is not well suited for oral administration
• For localized treatment

Question 5

Reasons for not using route

Answer 5

• Cultural acceptance
• Slow and incomplete absorbance of drug
• Inter- and intra- drug level variations
• Difficult for large- scale production

Question 6

Why is water attracted with a resulting unpleassnt sensation ofor the patiens?

Answer 6

Due to osmotic effects

Question 7

Enzyme not present in rectum resulting to greater stability of peptide-like drugs

Answer 7

Esterase or Peptidase

Question 8

T/F. Penetration enhancers may be used in improve the absorption profile of the drugs

Answer 8

True.

Question 9

How is drug from the rectum absorbed?

Answer 9

Through passive diffusion

Question 10

Is the rate and extent of drug absorption in the rectum lower or higher than the oral route? Why?

Answer 10

Lower than oral Route due to small surface area of absorption

Question 11

What vein in the hepatic system causes the first-pass effect?

Answer 11

Superior Hemorrhoidal Vein

Question 12

What is the limitation of the use of surfactants in rectal drug delivery?

Answer 12

Surfactants may lead to irritation to the rectal mucosa

Question 13

This delivery contains low amount of fluid and has limited buffer capacity

Answer 13

Rectal Drug Delivery

Question 14

At what mL do rectally instilled preparations tend to be confined in the rectum or sigmoid colon? Then where does it travel after this?

Answer 14

About 50 mL, to the ascending colon if more mL

Question 15

T/F. Drugs in rectal drug delivery are erratically absorbed.

Answer 15

True. They are unpredictable or incompletely absorbed.

Question 16

Advantages of Rectal Administration

Answer 16

▶ First-pass effect
▶ Drug stability
▶ Large dose drugs
▶ Irritating drugs
▶ Unpleasant tasting or smelling drugs
▶ Pediatric use
▶ Unconscious, n/v
▶ Upper GIT disease
▶ Rapid drug effect system

Question 17

Disadvantages of Rectal Administration

Answer 17

▶ Lack of flexibility of the dosage
▶ Expensive (high demand)
▶ Exhibit variable effectiveness
▶ Erratic absorption
▶ Dose of drug may be greater than or less than the dose of the same drug given orally
▶ Factors affecting dosing (anatomic and physiologic factor and physicochemical factors)
▶ Physiologic Factors and Drug effect (i.e. Circulation route and pH and lack of buffering capacity of rectal fluids, colonic content)

Question 18

What factors affect the greater absorption in the rectum?

Answer 18

▶ fecal matter
▶ enema
▶ diarrhea
▶ colonic obstruction d/t tumor,
▶ tissue DHN

Question 19

In Lipid - Water Partition Coeffcient of the drug, the base consideration is an important decision. What base is suitable for a lipophilic drug?

Answer 19

Fatty base

Question 20

Physicochemical factors of the drug and base that affect rectal absorption

Answer 20

▶ lipid water solubility
▶ particle size
▶ lipid water partition coefficient in relation to suppository base

Question 21

What base is suitable for a water soluble or oil soluble drugs?

Answer 21

Water - soluble drugs

Question 22

Why are rectal suppositories have a thicker end?

Answer 22

To prevent expulsion when the sphincter contracts

Question 23

How should the rectal drug be inserted in the rectum?

Answer 23

Inserted base or blunt end up

Question 24

Absorption of rectum, a lipoidal system, is through the?

Answer 24

Superior vena cavaa

Question 25

Where is rectal drug delivery dependent?

Answer 25

Physicochemical properties of Drug Composition of Base

Question 26

What is a useful measure for drug absorption?

Answer 26

Partition between suppository base and rectal fluid

Question 27

How does uptake in rectal drug delivery occur?

Answer 27

Trancellular absorption via pH parition hypotheses

Question 28

Use of Surfactants in Rectal Drug Delivery

Answer 28

Modify membrane permeability enhance wetting and spreading of base dissolution of the drug

Question 29

What animal of choice is used in evaluation of rectal drug availability?

Answer 29

Dogs

Question 30

In the treatment of local conditions like hemorrhoids, what base is widely used for rectal drug delivery?

Answer 30

Fatty ointments

Question 31

What delivery forms are employed in the administration of drugs for systemic effects?

Answer 31

Tablets, capsules, microenemas

Question 32

Characteristics of rectal suppositories in adults include:

Answer 32

tapered at one or both ends weighing 2 g bullter torpedo or little finger 32 mm (1.5 in.) long

Question 33

What is the weight of pediatric rectal suppositories? What is its shape?

Answer 33

half the wt and size of adult pencil shape

Question 34

The 2 g weight for rectal adult suppositories is based on what suppository base?

Answer 34

Cocoa butter base

Question 35

What indications of drug have systemic effect and administred rectally?

Answer 35

Sedatives, Tranquilizers, Analgesics

Question 36

the largest OTC rectal suppositories

Answer 36

Hemorrhoidal treatment

Question 37

classification of rectal suppository bases

Answer 37

fatty, water soluble, and water miscible

Question 38

Shell suppositories similar to soft - gel capsules

Answer 38

Rectal capsules

Question 39

They are of elongated shape and have a smooth external appearance that may be lubricated.

Answer 39

Rectal Capsules

Question 40

For capsules, to achieve a systemic effect, how is it usually filled with?

Answer 40

Solution of suspension of the durg in vegetable oil or liquid paraffin

Question 41

Why do rectal tablets have difficulty in disintegrating?

Answer 41

Due to low amount of water present in the rectum

Question 42

Have difficulty disintegrating due to low amount of water present in the rectum

Answer 42

Rectal Tablets

Question 43

Used to stimulate defecation

Answer 43

Effervescent rectal tablet preparations

Question 44

Substances in liquid form designed for rectal administration

Answer 44

Enemas

Question 45

Component of Enemas

Answer 45

Vehicle or One or more active substance dispered in sutiable solvents

Question 46

Solvents used in enemas for active substances

Answer 46

Water Glycerol Macrogols (PEGs)

Question 47

Stabilizers and excipients help enemas through?

Answer 47

Improvement of dissolution rate

Question 48

Contains small volume (approx. 3mL) rectal DF which can release drug immediately without melting and dissolution if the vehicle is water

Answer 48

Microenemas

Question 49

Rectal Powders are used for

Answer 49

Solutions

Question 50

Why are rectal powders lyophilized?

Answer 50

To have a porous product that has a large surface area and dissolves rapidly

Question 51

These are inserted in the lower part of the rectum for a limited time and removed.

Answer 51

Rectal tampons

Question 52

What is the dose of vaginal administration if local action is only intended?

Answer 52

smaller doses with reduced absorptionand systemic distribution toxicity

Question 53

Antifungals used mentioned that can be applied in?

Answer 53

Clotrimazole, Miconazole, Clindamycin

Question 54

Miconazole can treat

Answer 54

vaginal infection

Question 55

What influences passive drug absorption?

Answer 55

Absorption site physiology Absorption site pH solubility and partitioning characterisitcs of he drug

Question 56

Why is vaginal fluid in the women's body acidic?

Answer 56

Due to the presence microflora consisting lactobacilus

Question 57

What size of the particles in VDD can cause irritation in the human body

Answer 57

Insoluble, 50 micrometer

Question 58

T/F. Vaginal pH increases with menstrual, cervical, and uterine secretions

Answer 58

True

Question 59

Important charac of an ideal vaginal

Answer 59

should be long acting, reducing the frequency of administration * should be stable in a range of climatic conditions * should not lead to any irritation, burning or itching * should not cause any leakage * should not cause staining or discolouring of under garments * the formulation should be colourless and odourless * the formulation should not adversely affect sexual activity * women should be able to use it without the knowledge of a male partner * should be easy to insert and/or apply, without the need for an applicat

Question 60

DDS that is usually oviform and may weigh 1 to 5 grams

Answer 60

Vaginalsupp. or pessaries

Question 61

What base is usually used in preparing pessaries

Answer 61

glycerol - gelatin bases

Question 62

vaginal semisolids can cause

Answer 62

problems of drugs that are prone to hydrolysis

Question 63

Thin layers of polymeric material for single- dose

Answer 63

Vaginal film

Question 64

Bioadhesives utilized to minimize leakage and improve retention in vagina

Answer 64

Xanthan gum Carbapol

Question 65

Solid, single- dose preparations *Ovoid (other shapes are available) tablets that may or may not be coated *Preferred for drugs that are prone to hydrolysis, and in countries that are tropica

Answer 65

Vaginal Tablet

Question 66

controlled release, and prolonged delivery

Answer 66

Vaginal ring

Question 67

What entraps the polymer network present in flexible and vainal renig ?

Answer 67

flexible, circular netowrk eg. estring

Question 68

General Specifications of Supposiroty Bases

Answer 68

base is nontoxic and nonirritating to mucous membranes. *The base is compatible with a variety of drugs and should be pharmacologically inert. *The base melts or dissolves in rectal fluids. *The base should be stable on storage; it should not bind or otherwise interfere with release or absorption of drug substances.

Question 69

Bases used in suppository bases

Answer 69

Cocoa butter Cocoa butter substiute glycerinated gelatin halogenated vegtableoil mixtures of PEg fatty acid esters of PEG

Question 70

What is the rate of spreading and transportation based n?

Answer 70

partially based viscous

Question 71

Glycerinated gelatin

Answer 71

slow dissolution

Question 72

What type of emulsions suppository that increases the propbabiity of drug transfer to the inner phase?

Answer 72

o/w emulsions

Question 73

What can be used for insufficient air displacement and agglomeration that can affect dissolution of drug particles and increase producing a w/o emulsions system?

Answer 73

Surfactants

Question 74

Increasing viscosity causes agglomeration, name viscosity enhancing additives that can slow down the release of drugs?

Answer 74

colloidal silicon dioxide aluminum monostearte

Question 75

lecithin addition causes what to high amount solid drugs?

Answer 75

decreases the attraction between the drug particles, enhancing the flow properties of the dispersion

Question 76

reasons why cocoa butter is not used as a base?

Answer 76

*polymorphic behaviour, *insufficient contraction during cooling, *low softening point, *chemical instability, *poor water-absorptive power, and its price`

Question 77

parameter that refers directly to the amount of mono- and di-glycerides present in the fatty base

Answer 77

hydroxyl number of these bases

Question 78

advantage of high OH bases

Answer 78

larger melting capacity and solidifying ranges

Question 79

Other name for cocoa butter

Answer 79

theobroma oil

Question 80

content of unsaturated FA in theobroma oil

Answer 80

40%

Question 81

Cocoa butter melts at

Answer 81

body temperature, temperature dependent

Question 82

What should be added to avoid eutexia when adding theobroma oil and another substnace?

Answer 82

addition of higher melting wax i.e. white ewax and synthetic spermaceti

Question 83

Examples of CB substitutes

Answer 83

Palm Kernel Oil Cottonseed Oil Stearic Acid Palmitic Acid Glycerol Monopalmitate Glycerol MonostearteAdva

Question 84

Advantages of CB substie over CB

Answer 84

decrease potential for rancidity and phase transition behavior

Question 85

Why must glycerinated gelatin be moistened prior to insertion?

Answer 85

It absorbs mositure as a results of hygroscopic properties of glycerin. It can have dehydrating effect and irritate tissue skin.

Question 86

Examples of water soluble bases

Answer 86

Glycerinated gelatin a Polyethylene glycol (macrogol)

Question 87

Purpose of glycerol-gelatin base

Answer 87

laxative

Question 88

What is prepared easily from unlubricated molding, but not so from handrolling

Answer 88

PEG suppositories

Question 89

What does cooling to near the melting point prevent?

Answer 89

Prevent fissuring caused by crystallization

Question 90

Components of glycerinated gelatin

Answer 90

Glycerin - 70% Gelatin - 20% Drug 10%

Question 91

What does a higher proportion of gelatin indicate in the glycerinated gelatin based?

Answer 91

The base will be rigid and more long acting

Question 92

What base is usually used for vaginal supp instead of rectal?

Answer 92

Glycerinated gelatin, it can cause osmotic laxative effect in rectal supp.

Question 93

How to decrease induced irritation of the rectum for PEG?

Answer 93

addition of at least 20% water and moistening before insertion

Question 94

Why should PEG bases be stored in tightly packed containers?

Answer 94

To avoid the development of peroxides in the base

Question 95

How are suppositories produced?

Answer 95

Hand molding Molding (fusion) Cold Compression

Question 96

It is the 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.

Answer 96

Hand molding

Question 97

Elegant suppository can be made by compression the cold-grated mass into the desired shape . It is simple and more elegant appearance than hand molding. It avoids the possibility of sedimentation of the insoluble solids in the suppository base.

Answer 97

Compression Molding

Question 98

Most commonly used method for production of suppository on both small & large scale. First, the base is melted on water bath, and then the drugs are either emulsified or suspended in it. Then, the mass is pour into cooled metal molds, which are usually chrome or nickel plated.

Answer 98

Pour Molding

Question 99

The molding operation (pouring, cooling & removal) can be performed by machine . The output of a typical rotary machine, range from 3500 to 6000 suppositories per hour

Answer 99

Automatic Molding Machine

Question 100

PEG bases are incompatible with

Answer 100

Silver salts Tannic Acids Aminopyrine Quinine Icthammol Aspirin Benzocaine Sulphonamides

Question 101

Softerns PEG

Answer 101

high concentration of salicylic acid

Question 102

What is added to improve consistency of suppositories?

Answer 102

Stearyl, cetyl, myristyl alcohols, stearic acid

Question 103

What makes syntheic fat bases more brittle?

Answer 103

high degree hydrogenation high stearate content higher solid contents

Question 104

contraction facilitate the removal of the suppository from the mold , eliminating the need for mold release agents

Answer 104

Good mold release

Question 105

Mold Releasing agents

Answer 105

mineral oil aq soln of sls alcohols silicones soap

Question 106

It results from the autoxidation and subsequent decomposition of unsaturated fats into low & medium molecular weight saturated & unsaturated aldehydes, ketones and acids, which have strong unpleasant odor

Answer 106

Rancidity