1
Q
main transportation route of the semi solid dosage forms
A
SKIN
2
Q
ROUTES OF DRUG MOLECULES
- across lipids
- considered the major route of penetration
A
INTERcellular
2
Q
ROUTES OF DRUG MOLECULES
across corneocytes
A
INTRAcellular
3
Q
ROUTES OF DRUG MOLECULES
via skin appendages
A
appendageal
4
Q
FACTORS INFLUENCING DRUG ABSORPTION
drugs with both water and lipid solubility are favorably absorbed through skin
A
PARTITION COEFFICIENT of DRUGS THROUGH THE SKIN
5
Q
FACTORS INFLUENCING DRUG ABSORPTION
- found in the stratum corneum layer of the epidermis
- prevents the Natural Moisturizing Factor from being stripped from the skin
A
MOISTURE BALANCE in the skin
6
Q
FACTORS INFLUENCING DRUG ABSORPTION
prevents the skin from drying out, even during excessive contact of the skin with water
A
NATURAL MOISTURIZING FACTOR
7
Q
FACTORS INFLUENCING DRUG ABSORPTION
- the skin constantly releases water in the skin surface, which evaporates quickly without being noticed
- when the surrounding environment has a high moisture content, the rate of evaporation of sweat is slowed down, and the person becomes aware of the clammy moist sensation on his skin
A
INSENSIBLE PERSPIRATION
8
Q
FACTORS INFLUENCING DRUG ABSORPTION
- Moisture Balance in the Skin
- Insensible Perspiration
A
MOISTURE & TEMPERATURE IN THE ENVIRONMENT OF THE SKIN
9
Q
FACTORS INFLUENCING DRUG ABSORPTION
skin penetration has been enhanced by abrasions or when the skin is stripped of its barrier layer
A
PATHOLOGICAL INJURY TO THE SKIN
10
Q
FACTORS INFLUENCING DRUG ABSORPTION
- penetration of drug substances may be enhanced by the use of suitable semi solid base
- the vehicle may help increase the rate of penetration of drug substances into the skin
- it serves as a carrier for the API
A
TYPE OF VEHICLE USED SKIN
11
Q
STARTING MATERIALS
- most widely used substances in semisolids next to water
A
PETROLATUM & MINERAL OIL
12
Q
STARTING MATERIALS
Petrolatum
Mineral Oil
A
Hydrocarbons
13
Q
STARTING MATERIALS
HYDROCARBONS:
* a complex mixture of semisolids containing hydrocarbon aliphatic, cyclic, saturated, unsaturated, branched and unbranched substances varying proportions
A
PETROLATUM
14
Q
STARTING MATERIALS
HYDROCARBONS:
* derived from petroleum acid
* less tacky and with lower viscosity
A
MINERAL OIL
15
Q
STARTING MATERIALS
- help increase the VISCOSITY of hydrocarbons such as petrtolatum and mineral oil
- prevent separation of hydrocarbons from the ointment
- examples: paraffin, beeswax, ceresin wax
A
HYDROCARBON WAXES
16
Q
STARTING MATERIALS
HYDROCARBON WAXES:
* mixture of paraffin and ozokerite
A
CERESIN WAX
17
Q
STARTING MATERIALS
- vegetable fixed oils which contain glycerides of mixtures of saturated and unsaturated fatty acids
- these are employed for its EMOLLIENT and SKIN-LUBRICATING effects
- examples: fixed oils of peanut, olive, sesame, cottonseed, coconut, corn
A
OLEAGINOUS SUBSTANCES
18
Q
STARTING MATERIALS
- functions as AUXILIARY EMULSIFIERS and as VISCOSITY-BUILDERS
- examples: stearic acid, stearyl/cetyl alcohols
A
FATTY ACIDS and ALCOHOLS
19
Q
STARTING MATERIALS
FATTY ACIDS & ALCOHOLS:
* emulsifiers in water-removable creams
A
STEARIC ACID
20
Q
STARTING MATERIALS
FATTY ACIDS & ALCOHOLS:
* emollients, provides the firmness/softness in consistency of creams
A
STEARYL / CETYL ALCOHOLS
21
Q
STARTING MATERIALS
- substances that prevent COALESCENCE and act as product STABILIZERS
- examples: triethanolamine stearate (TEA), SPANS, TWEENS, CARBOWAX
A
EMULSIFIERS
22
Q
STARTING MATERIALS
- used as HUMECTANTS, prevents DEHYDRATION and “CRUSTING” on top of creams and ointments in jars
- examples: glycerin, PG, Sorbitol 70%, PEG (lower MW)
A
POLYOLS
23
Q
STARTING MATERIALS
- these must be uniformly dispersed throughout the semisolid vehicle to assure product homogeneity
- these solids must be impalpable to touch
- particles less than 74 microns (equivalent to 200 mesh) is said to be (eequivalent to 200 mesh)
A
INSOLUBLE POWDERS
24
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
* prepared from mixtures of **high** and **low MW PEG**
* **NO WATER** is required in its preparation
* **water soluble**, due to many polar groups and ether linkages
* suitable combinations og **high & low MW PEG** yield products having **ointment-like consistency**, which **soften or melt** when applied topically
WATER SOLUBLE / GREASELESS BASES
25
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
WATER-SOLUBLE/GREASELSS BASES:
* **LOW MW PEG**
liquids
26
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
WATER-SOLUBLE/GREASELESS BASES:
* **MODERATELY HIGH MW PEG**
UNCTUOUS
27
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
WATER-SOLUBLE/GREASELSS BASES:
* **VERY HIGH MW PEG**
SOLIDS
28
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
* these are **O/W emulsions** referred to as **creams**
* upon application, there is **little or no evidence** of **its presence** onto the skin
* best for **moist skin lesions**, since its O/W character tend to **adsorb serious discharges**
* examples: **vanishing creams**, **foundation creams**, **shaving creams**
WATER-REMOVABLE/WASHABLE BASE (O/W)
29
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
WATER-REMOVABLE/WASHABLE:
* relief of **inflammatory dermatoses**
Fluocinolone acetonide cream (SYNALAR)
30
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
WATER-REMOVABLE/WASHABLE:
* for **osteoarthritic joint pain**
Capsaicin cream (ZOSTRIX)
31
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
* these are **hydrophilic mixtures** formed by the **addition** of substances that possess **polar groupings** (sulfates, carboxyl, hydroxyl, or ether linkagaes) to a **hydrocarbon base**
* **Lanolin**, **Cholesterol**, **Sorbitan monostearate/monooleate** are added to hydrocarbon bases to make it hydrophilic
* These bases are of **W/O** type
ABSORPTION / EMULSIFIABLE BASE (W/O)
32
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
ABSORPTION/EMULSIFIABLE BASE (W/O):
* **Commercially available**
AQUAPHOR
EUCERIN
33
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
ABSORPTION/EMULSIFIABLE BASE (W/O):
* a **50% W/O emulsion**
EUCERIN
34
# **TYPES OF SEMISOLID VEHICLES (NON-MEDICATED BASES)**
* typically **lipophilic**
* spreads **easily** onto the skin
* **difficult to remove**
* act as **occlusive dressings**, since the normal evaporation of insensible perspiration is inhibited
* examples: **white petrolatum**, **mineral oil**, **white/yellow ointment**, **USP**
HYDROCARBON BASES
35
# **METHODS FOR OINTMENT PREPARATION**
* **ANHYDROUS ointments** are manufactured by this process, which is made by **dissolving the APIs** in the **previously melted FATS & WAXES**
* the **melted mass** must be **mixed while cooling** to ensure the homogenous distribution of the ingredients
FUSION METHOD
36
# **FUSION METHOD**
if a **PERFUME** or **VOLATILE OIL** is added, at what temperature is it best done?
40-43C
37
STEPS IN **FUSION METHOD**
1. preparation of the **oil phase**
2. **hydration** of the ingredients in the aqueous phase
3. **foaming** the emulsion
4. **dispersion** of the APIs
38
# **FUSION METHOD**
**heating** is required to **melt** some ingredients (waxes), usually at what temperature
70 - 75C
39
# **FUSION METHOD**
this may be required to **accelrate hydration**
heating
40
# **FUSION METHOD**
the aqueous and oil phases are **blended** under ____ to **form emulsion**
vigorous agitation
41
# **FUSION METHOD**
these are done to **minimize foam formation** after the product has emulsified
defoaming
42
a **heterogenous system** of **2 immiscible liquids**
EMULSIONS
43
**ointments** and **other semisolid preparations** are packaged either in ____ or in ____
large-mouth ointment jars
metal/plastic tubes
44
MICROBIAL SCREENING for semisolid preparations
Staphylococcus aureus
Pseudomonas aeruginosa
45
# **MINIMUM FILL**
for product weighing **60 g or mL**
NOT LESS THAN 90% of the labeled amount
46
# **MINIMUM FILL**
for product weighing **60g or mL - 150g or mL**
NLT 95% of the labeled amount
47
STANDARD ASSAYS
%Purity
%Content
48
STERILITY TEST
Membrane Filtration Technique
Test Tube Inoculation Method
49
studies applicable to:
* antifungals
* antivirals
* corticosteroids
* antibiotics
* topicals for vaginal use
DERMATOPHARMACOKINETIC STUDIES (DPS)
50
# **EVALUATION AS PER NON-USP REQS**
affects the:
* **physical** stability
* **chemical** stability
* **microbial** stability
Water content
(Karl Fischer Method)
51
# **EVALUATION AS PER NON-USP REQS**
usual **water limit**
0.5% - 1%
52
# **EVALUATION AS PER NON-USP REQS**
Usual **water content** for oinments containing:
* **Bacitracin**
* **Chlortetracycline HCl**
* **Nystatin**
NMT 0.5%
53
# **EVALUATION AS PER NON-USP REQS**
usual **water content** for ointments, creams, or gels containing:
* **Erythromycin**
* **Gentamycin sulfate**
* **Neomycin sulfate**
* **Tetracycline HCl**
NMT 1%
54
# **EVALUATION AS PER NON-USP REQS**
* mandatory for **OPHTHALMIC OINTMENTS** ONLY
METAL PARTICLE DETECTION TEST
55
# **EVALUATION AS PER NON-USP REQS**
* mandatory for **ophthalmic ointments** filled in **collapsible tubes**
* by classical **blotting paper method**
LEAKER TEST
56
METHODS OF FILLING OPHTHALMIC OINTMENTS
Blow Fill Seal Method (BFS)
Form Fill Seal Method (FFS)
57
# **METHODS OF FILLING OPHTHALMIC OINTMENTS**
Blow Fill Seal Method (BFS) Sequence
1. Fabrication of containers
2. Filling the Product
3. Sealing
58
# **METHODS OF FILLING OPHTHALMIC OINTMENTS**
the **conventional method** of filling ophthalmic ointments
FORM FILL SEAL METHOD (FFS)
59
* these are added to semisolids whenever **oxidative deterioration** is anticipated
* examples: **BHA**, **BHT**, and **propyl gallate**
ANTIOXIDANTS
60
this may be used in **ophthalmic ointments** against **bacterial/fungal contamination**
BORIC ACID
61
# **USE OF INGREDIENTS**
* **counterirritant**
* provides **cooling sensation**
MENTHOL
62
# **USE OF INGREDIENTS**
* **mild analgesic**
* **nasal decongestant**
Camphor
63
# **USE OF INGREDIENTS**
* **expectorant**
* provides **soothing aroma**
eucalyptus oil
64
# **USE OF INGREDIENTS**
* **counterirritant**
* stimulates **circulation**
turpentine oil
65
# **USE OF INGREDIENTS**
* **stiffening** agent
* **consistency modifier**
PARAFFIN
66
# **USE OF INGREDIENTS**
* **analgesic**
* **anti-inflammatory**
Methyl Salicylate
67
# **USE OF INGREDIENTS**
* **base**
* **emollient**
* **protective**
petroleum jelly
68
what is the **key excipient** in the chest rub ointment that acts as the **base**, serves as an **emollient**, **occlusive**, and **carrier** for the API
petroleum jelly
69
what are the API for the **chest rub ointment**
MENTHOL
CAMPHOR
METHYL SALICYLATE
70
# **OTHER BASES OF OPHTHALMIC OINTMENTS**
* sterelized by **gamma radiation** or sterilization by **filtration**
LANOLIN
71
# **OTHER BASES OF OPHTHALMIC OINTMENTS**
* possess **emollient** properties suitable for **eye ointment formulation**
Lanolin alcohol
72
# **METHODS FOR OINTMENT PREPARATION**
* used for **HEAT-LABILE** or **VOLATILE** substances
* the API can be incorporated into the base by:
* **Micronization**
* **Levigation**
* **Geometric dilution**
INCORPORATION METHODS
73
# **METHODS FOR OINTMENT PREPARATION**
INCORPORATION METHODS:
* **reduces particle size** to eliminate grittiness
MICRONIZATION
74
# **METHODS FOR OINTMENT PREPARATION**
INCORPORATION METHODS:
* examples: **mineral oil** - used to form **smooth paste**
LEVIGATING AGENT
levigation
75
# **METHODS FOR OINTMENT PREPARATION**
INCORPORATION METHOD:
* ensures **even distribution** of API
GEOMETRIC DILUTION
76
# **METHODS FOR OINTMENT PREPARATION**
* **refines particle size** and ensure **uniform dispersion** of the drug
* **prevents agglomeration** and improves **content uniformity**
HOMOGENIZATION
Manuf LAB
flashcards
Decks in class (5)
# Cards
