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Ceutics2 - Midterm 1 > 4 - Suppositories Theory > Flashcards

4 - Suppositories Theory Flashcards

1
Q

Solid dispersions or Solid Solutions

A

Drug phase is uniformly dispersed in a

WAXY or RUBBERY

solid dispersion medium

Suppositories - can also use orally if in capsules

Solid dispersions- typically form a RIGID SOLID MASS

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2
Q

Dispersions in a Gel Matrix

A

Drugs may be admin. topically in the form of

Dispersions in a Gel Matrix

Ointments / Transdermal drug deliv systems

Gels typically form a FLEXIBLE SOLID MASS

but may be liquified prior to application by either heating or shaking vigorously (thixotropic)

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3
Q

Type of gel that is formed by polymers cross-linked to one another by COVALENT BONDS

maintain structural INTEGRITY after drying in order to REMOVE solvent

A

Type 1 Gels

Derivatives of methacrylic acid

Used to manufacture:

Implants / Opthalmic Inserts / Contact Lenses

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4
Q

Implants to Deliver Antibiotics

ex. treat infections of middle ear or other non-accessible sites

A

Type 1 Gel

cross linked variety of agents that form dry powders that swell & form a gel on contact with water

agents:

dimethacrylate / methylenebisacrylamide

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5
Q

Soft Contact Lenses

Opthalmic controlled release drug delivery systems

A

Type 1 Gels

cross linked poly methacrylate

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6
Q

Disintigrant for Tablet formulations

A

Type 1 Gels

Use Croscarmellose sodium, that SWELLS on contact with water

= cross-linked carboxymethylcellulose sodium

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7
Q

Type of gel that is formed by polymers linked by

REVERSIBLY FORMED intermolecular bonds

like hydrogen bonds

can be recovered through melting / diluting with solvent

A

Type 2 Gel

Classiified by apparent # of phases & nature of interstitial solvent

unstable to changes in temperature ,stability affected by additives (salt / cosolvents)

every OTHER semisolid or solid dispersion solid solution drug delivery system

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8
Q

The taking up of liquid

WITHOUT measurable change in VOLUME

A

IMBIBITION

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9
Q

The taking up of liquid with an INCREASE IN VOLUME

A

SWELLING

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10
Q

Particles of dispersed phase interact SO STRONGLY

that the dispersing medium is SQUEEZED OUT

and forms a Seperate liquid phase

THE GEL ITSELF SHRINKS IN VOLUME

A

SYNERSIS

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11
Q

Reversible gel-sol (semisolid -fluid) formation with

NO CHANGE in

VOLUME or TEMPERATURE

usually triggered by SHEER FORCES

A

THIXOTROPY

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12
Q

Desolvated gel in which the

Framework remains INTACT

both Type 1 & Type 2 gels can be desolvated to become this

A

XEROGELS

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13
Q

Type of Gel Classification

Consist of macromolecules forming twisted / matted strands with the liquid phase in interstitial spaces

Usually formed by organic polymers such as

methacrylic acid (carbopol) = NOT CROSS LINKED

tragacanth / cellulose derivatives

A

ONE-Phase System

not 2-phase

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14
Q

Type of Gel Classification

Consists of FLOCCULES of small particles with distinct interparticular phase boundaries

Usually formed by INORGANIC materials:

Aluinum hydroxide gel / Bentonite magma

Milk of Magnesia

A

TWO-Phase System

not 1phase

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15
Q

Type of Gel Classification

Formed by HIGH concentrations of HYDROPHILIC COLLOIDS:

very common in drug delivery systems:

Colloidal Silica / Bentonite / ragacanth

Gelatin / Pectin / Acacia

Methylcellulose / Sodium Alginate

A

HYDROGELS

hence HYDRO-PHILIC = water love

Alumina / METHACRYLIC ACID / Gums

Starches

Maltodextrin

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16
Q

Type of Gel Classification

formed by HIGH concentrations of LIPOPHYLIC materials or

HYDROPHILIC POLYMERS that self-associate

LESS common ingredients

A

ORGANOGELS

Ex: Petrolatum / Plastibase

FATS - lard / cocoa butter

Aluminum Stearate

PEG / PVP / Cellulose derivatives

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17
Q

Most wildley used NATURAL polymer in pharmaceutical products

HYDROPHILIC Colloid = HYDROGEL

Used as:

Soft/hard ____ capsules

Tab granulations / coatings

Emulsions / Suppositories

A

GELATIN

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18
Q

Compounding with Gelatin

Hydrogel + Onephase (organic)

similars: Gums agar / irish moss (carrageenan) / pectin

tragcanth

A

Cold Water –> powder gelatin = gel on surface of particle

Hot Water –> DISSOLVE gelatin

colloidal dispersion will readily form with stirring

Cooling –> semi-rigid gel forms

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19
Q

Gelatin

Gel or Solid Dispersion?

What does adding/removing water do?

A

HydroGEL

with enough HOT water –> can be formed into shapes by molding or film casting then DEHYDRATING until you reach the desired rigidity

MORE WATER –> MORE FLEXIBLE

Less water = less rigid

EVEN LESS WATER = Brittle Plastic

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20
Q

Gelling agents that

REQUIRE HEAT

during compounding

A

Gelatin

Natural Gums

21
Q

Gelling agents that are

ADVERSELY AFFECTED

by OVERHEATING

A

COCOA BUTTER

22
Q

Define

Dispersions or Solutions of a drug substance prepared by HEATING a SOLID dispersing medium (organogel) above its melting point

Then dispersing the DRUG particles in the molten medium

sometimes with aid of a surfactant or emulsifier

A

SOLID DISPERSIONS

typically a organogel (fat / high MW polymer)

Result AFTER COOLING is a coarse/fine dispersion of the drug in a solid matrix

23
Q

Define

Formed by dissolving a drug substance in a

MOLTEN solid solvent

have a VARIABLE MELTING POINT, based on composition

A

Solid SOLUTION

(molecular dispersion = solution)

Result after cooling is microcrystals of the drug substance in a SOLID matrix

may or may NOT be crystalline

24
Q

Define

Mixture of 2 Solids that have a SHARP MELTING POINT

A

EUTECTICS

E = Eutectic Point

When the 2 compositions (drug in molten medium) reach this point, the remaining liquid crystallizes as a

MIXED CRYSTAL MASS

containing both A + B microcrystals

altered solubility properties!

25
Q

Eutectics might have a

MORE RAPID DISSOLUTION

due to:

A

Increased DRUG Solubility

Solubilization by carrier

Prevention of Aggregation of drug particles

Altered Wettability

production of Metastable solid forms

26
Q

TRUE Solid Solutions

Variable Melting Point, based on composition

A

NO eutectic is observed

Commonly observed for METAL ALLOYS

molecule of B is replaced by molecule of A in the crystal lattice of the solid

27
Q

CONTINUOUS Solid Solutions

Variable Melting Point, based on composition

A

uncommon in pharmaceutical applications

2 components are MISCIBLE WITH EACH OTHER

in all proportions in the liquid/molten state

28
Q

AMORPHOUS Solid Solution

Common with Gel-Forming Polymers as the SOLVENT component for the drug

PEG / PVP / Cellulose Derivatives

A

Solute molecules are ​DISPERSED MOLECULARLY

BUT IRREGULARLY within the Amorphous solvent

drug loading may be a problem,

Solubility in PEG for poorly water soluble drugs can be <10%

29
Q

PEG

Amorphous Solid Solution

A

Polymer that contain BOTH

Microcrystalline + Amorphous Regions

Drug may dissolve in the Amorphous PEG which

PREVENTS Crystallization of the drug

30
Q

Rectal Suppositories used for?

A

Used to administer drugs for systemic effects for patients

unable to take medication by mouth

or

for LOCAL action in the PERIANAL Area

ex. cathartic suppositories - produce peristalsis

hemorrhoid suppositories

31
Q

Rectal Absorption of Drugs

Suppositories

A

Mucosa of the rectum/anus are LIPOID BARRIERS

Solid dosage forms typically soften / melt @ body temp

Partitioning effects control bioavailbility

32
Q

Formulation of a Suppository

A

Coarse Dispersion of drug particles in a BASE of:

low-melting AMORPHOUS solid matrix

(cocoa butter / similar fats)

or

semi-CRYSTALLINE solid matrix

slowly-dissolving water-soluble polymers

(PEG / Glycerinated Gelatin)

33
Q

Formulation of VAGINAL Suppositories

have a local dehydrating Effect;

MOISTEN with WATER before use & STORE DRY

A

MOST use HYDROPHILIC BASES

(PEG +/- Surfactants / Glycerinated Gelatin)

Hygroscopic (absorb moisture from the AIR) & require protection from moisture

34
Q

Uses for Vaginal Suppositories

A

ANTIBIOTICS

clindamycin = bacterial infections

Miconazole nitrate = antifungal / yeast infections

CONTRACEPTRION

nonoxynol-9

35
Q

Urethral Suppositories

A

UNCOMMON

OG made from cocoa butter, but need SMALL DIAMETER

so PEG-Based are now PREFFERED, have resistance to breaking

36
Q

Type of Suppository Base

Mixture of Crystalline Polymorphs that MELT in the range of 30-36*C

Suppositories need to be SOLID @ room temp,

but readily dissolved @ body temp

A

COCOA BUTTER

(Theobroma Oil)

MELT @ 30-36*

melting point can be CONTROLLED using additives

37
Q

Type of Suppository Base (dispersing medium) that

DISSOLVES,

rather than MELT

Suppositories need to be SOLID @ room temp,

but readily dissolved @ body temp

A

PEG (Carbowax)

PEG 1000 = 37-40*C

PEG 3350 = 54-58*C

PEG 4600 / 6000 = 60+

Hygroscopic / releases much slower

38
Q

Type of Suppository Base (dispersing medium) that

Softens & Dissolves SLOWLY,

rather than MELT

Suppositories need to be SOLID @ room temp,

but readily dissolved @ body temp

A

GLYCERINATED GELATIN

softens / dissolves slowly

mainly for Vaginal Inserts

MORE HYGROSCOPIC

may irritate tho if NOT pre-moistened

39
Q

Cocoa Butter Formulation

From a Mixture of Triglycerides from Theobroma Cacoa

major component of CHOCOLATE

A

Adding Fat-Soluble Drugs–> can lower melting point

SO we can HIGHER the MP by adding:

waxes / spermaceti to adjust the MP to reach 36*C

  • HydroPHILIC drugs are INSOLUBLE in cocoa butter*
  • they form solid dispersions*
40
Q

Fattibase

(TG’s from PALM + COCONUT oils w/ glycerol…)

Wecobee Bases

(Coconut oil TGs)

Witopsol Bases

A

COMPETING PRODUCTS

of cocoa butter

41
Q

Cocoa butter is from a mixture of TG’s from Theobroma cacao, which forms Multiple Crystalline Polymorphs, which has a

_Melting point of ~36*C?_

A

Beta - Polymorph

PREFERRED POLYMORPH

Alpha polymorphs will slowly convert into Beta over several days

42
Q

Cocoa butter is from a mixture of TG’s from Theobroma cacao, which forms Multiple Crystalline Polymorphs, which has a

_Melting point of <30*C?_

A

Metastable

Alpha-Polymorph

Formed if heated ABOVE 60* and is RAPIDLY CHILLED

UNUSABLE as a suppository

will convert to Beta over several days

43
Q

In order to PREVENT formation of the Alpha-Polymorph (instead of the Beta-Polymorph) what must you do?

Cocoa Butter Suppository Base

A

heat/melt BELOW <50*C

use slow cooling of melt

44
Q

PEG = Carbowax

Formulation / Composition

Base for Suppositories

A

DISSOLVE in body fluids rather than melt

May form Solid Solutions / Dispersions

hygroscopic (absorb moisture)

Partitioning Effect =

Hydrophilic drugs may release MORE SLOWLY

use cocoa butter for rapid onset of action

45
Q

Glycerinated Gelatin

Formulation / Composition

Base for Suppositories

A

20 parts gelatin + 70 parts glycerol + 10 parts water/drug

Used mostly for Vaginal Inserts

Softens SLOWLY, provides a DELAYED RELEASE

Hygroscopic

(more than PEG, may IRRITATE if not premoistened)

46
Q

Method of Compounding Suppositories

Like making BREAD!

  1. Titurate drug into fine powder
    1. add grated cocoabutter/base
  2. Incorporate drug into base using pestle
  3. Place between sheets of filtered paper
  4. kneed + roll into CYLINDER
  5. cut to length
A

COLD ROLLED

Traditional method

w/ mortar & Pestle

47
Q

Method of Compounding Suppositories

Similar to Cold-Rolled but

Place initial compact mass in a

PRESS & FORCE INTO MOLD

A

COMPRESSION MOLDED

48
Q

Method of Compounding Suppositories

  1. Melt the base
    1. use SLOW heating w/ cocoa butter
      1. avoid completing melting to preserve Beta polymorph seed crystals
  2. ​​Add Drug & dissolve or disperse in molten base
  3. Pour into mold
    1. allow to cool,
      1. use SLOW COOLING to force crystallization as Beta polymorph
A

Fusion

or

Hot Melt Molding

Ceutics2 - Midterm 1 (7 decks)

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