Drug Formulations

&
Routes of
Administration

Ma. Minda Luz M. Manuguid, M.D.

 General Considerations
• Pharmaceutics – branch of Pharmacy
that deals with drug formulations
• Pharmaceutical products need to be
presented in a form that can be
administered to an organism
• Formulation takes into consideration
easy delivery as well as guaranteed
desired action (drug reaches target,
achieves therapeutic action)
 Oral Preparations
Pill – round or ovoid solid body; may be coated
with sugar or other substance
• Tablet – granulated powder containing one or
more medications, compressed into a disc; must
disintegrate in the GIT, so starch is often
incorporated; + sugar-/film- coating;
• Dragees – chewable tablets
• Enteric-coated tablets – coated with a
substance that is stable at acidic pH (will not
disintegrate in the stomach) but breaks down
rapidly at higher pH (small intestines)
 Oral Preparations
• Capsule – an outer “shell” holds the drug
inside
– Hard gelatin capsule – contains solid drug in
powder form; may be opened
– Soft gelatin capsule – contains the drug in liquid
or semi-liquid form; cannot be opened; useful
for drugs that are insoluble in water
• Sustained/Slow-release preparations – drug
is formulated in such a way that it releases
very slowly in the GIT; a single dose suffices
for delivery of the drug over a period of
hours, ensuring sustained action.
 Oral Preparations
Liquid preparations – for children & for
adults who have difficulty swallowing
pills; usually flavored to make them
palatable;
• Elixirs – drugs insoluble in water are
dissolved in Alcohol
• Syrups – sugared liquid preparations
• Suspension – drug in solid form, not
dissolved in Alcohol
• Emulsion – drug in liquid form, not
dissolved in Alcohol
 Topical Preparations
Topical – application of a drug to the skin/ mucosa
overlying the area to be treated
• Drops – isotonic solutions – ophthalmic, nasal,
otic (eardrops – formulated as oily solutions for
adherence to the aural cavity)
• Creams – water-based, poorly absorbed; drug is
left on skin surface as water evaporates
• Ointments – lipid-based, greasy appearance &
feel; drug penetrates deeply into tissues,
especially if with “occlusive” dressing
• Pastes – have a very high powder content;
water-repellent.
• Gels & Lotions – used on hairy parts of the body.
 Topical Preparations
• Intranasal sprays – often metered to
deliver precise doses of the drug; can be
absorbed systemically
• Transdermal patches – useful for
administering lipophilic drugs & those
that are active in very small amounts
• Suppositories – useful in nauseous or
vomiting patients, unconscious patients,
patients with difficulty of swallowing;
may be administered rectally or
vaginally (Pessaries)
 Parenteral Preparations
Parenteral – mode of drug administration that
avoids the GIT. Drug injections. Use of ASEPTIC
TECHNIQUE very very important!!
• Intravenous (IV) injections – fast action due to
avoidance of GI absorption
• Intradermal – injected into the dermis; very
slow absorption; only small quantities of the
drug can be given this way.
• Subcutaneous – just beneath the skin; very
slow route; poor blood supply
• Intramuscular – into the fleshy part of the
muscle: gluteus, deltoid, anterior thigh;
Routes of Administration
• Oral • Subcutaneous
• Sublingual • Intramusclar
• Mucosal
• Intravenous
• Transdermal
• Rectal • Intrathecal
• Vaginal • Intra-articular
• Epidural
Routes of Administration
Oral
• most convenient, most economical
• rate & extent of absorption determines onset of
drug action/effect
• usual site of absorption: small intestines
• nonionized lipid-soluble forms favor absorption
– weak acids are highly ionized in small intestinal alkaline pH
– weak acids are readily absorbed in the stomach
 Oral administration
• First pass effect:
– Drugs absorbed from the GIT passes through the portal
venous system, then through the liver before finally
reaching the systemic circulation, to the receptors &
target tissues
– Extensive hepatic metabolism/extraction results in
minimal drug delivery to the systemic circulation
(e.g.propranolol,Demerol, INH)
– poor liver extraction, ↑bioavailability e.g. diazepam,
warfarin
• Disadvantages
– emesis due to GIT irritation
– destruction of drug by gastric acid/ GI enzymes
– unreliable or inconsistent absorption
– metabolism of drug by intestinal flora
Transdermal administration
Advantages
• Sustained therapeutic plasma levels
• Reliable drug absorption
– Molecular wt < 1000
– pH range 5 – 9 in aqueous medium
– No histamine-releasing action
– Daily drug requirement < 10 mg
• Smaller doses, so lower incidence of side
effects
• Generally good patient compliance
• Examples: scopolamine, nitroglycerin,
nicotine
 Rectal administration
• Proximal rectum administration – absorption
into superior hemorrhoidal veins  portal
venous system - liver - systemic
circulation
• Low rectal administration – entry into the
systemic circulation without passing
through the liver
• Generally unpredictable pharmacological
responses
• Rectal mucosal irritation possible
• Examples: antipyretics, anticonvulsants
Parenteral administration
• Ensures active drug absorption
• More rapid drug delivery than Oral
• Only route acceptable for
unconscious patients, uncooperative
patients
• Systemic absorption depends on
capillary membrane surface area,
drug solubility in interstitial fluid
• Advantages:
– Rapid precise blood drug levels
– Irritant drugs more comfortably administered
– Drug is rapidly diluted
 Specialized Modes of
Administration
• Intrathecal – drug is introduced into the
CSF-filled space surrounding the spinal
cord; for giving of drugs directly into the
CNS, avoiding the blood-brain barrier
• Epidural – drug is introduced into the
space above the dura; useful in
administering local anesthetics for
surgical procedures in the pelvic area &
below
• Intra-articular – injection directly into
joint spaces
 The Drug Order /
Prescription
Contents of a Prescription:
• name of medication
• amount of medication to be given
(dose)
• route of administration
• frequency of administration
• other information: prescribing
physician’s name, signature, license
no., PTR no., S2 no. if applicable;
date; patient’s name, age, etc.,
frequency abbreviatio explanation
n
every day q. d. q. – Lat. – quisque =
every
d. – Lat – diem = day
every other q. o. d. o - other
day
every hour q. h. h – hora = hour
every 2 hrs q. 2h.
every 3 hrs. q. 3h.
etc. etc.
2x a day b. i. d. b. – bi = twice
3x a day t. i. d. t. – tri = thrice
4x a day q. i. d. q. – quad = four times
as much as q. s. q. – quantity
frequency abbreviatio explanation
n
every q. a. m. q. – every
morning a. – ante = before
m. – meridiem = noon
at h. s. h. – hora = hour
bedtime s. – somni = sleep
before a. c. a. – ante
meals c. - cibum = meal
after p. c. p. – post = after
meals c. – cibum = meal
as desired ad lib ad libitum = at one’s
pleasure
frequency abbreviatio explanation
n
as s. o. s. si opus sit = if it is
necessary
necessary

as needed p. r. n. pro re nata = as

occasion
requires

immediatel stat statim - immediately

y
with c cum = with
before a ante = before
abbreviatio explanation
n
p.o. per orem = by mouth
iv intravenous
im intramuscular
subQ; sq subcutaneous
mg milligram
mcg microgram
IU International units
 Drug Dosage
• units of measurement: units/hr.; mg./hr.;
mg./min.; mcg/min.; mcg/kg/min
• formula : dose = rate x concentration
• nonparenteral meds –
– capsules & unscored tablets are rounded to the nearest
whole tablet
– Scored tablets are rounded to the nearest ½ tablet
– Liquid meds are rounded to one decimal place (tenth)
• parenteral meds
– Intradermal inj – 0.1 ml. or less
– Subcutaneous – 1.0 ml or less
– Intramuscular – 1.0 ml or less for older infants & young
children; 2.0 ml or less for elderly thin adults & children; up
to 3.0 ml in large muscles in well-developed adults
 Dosage calculations
• Rate – always in ml./hr.
• Ratio & Proportion – equations
containing ratios of equal value
separated by colons or written as
fractions. e.g. 2 : 6 = 4 : 12 – the
two inner numbers, 6 & 4, are the
“means”; the two outer numbers, 4
& 12, are the “extremes”. The
product of the means must equal
the product of the extremes.
 Calculations
• Intravenous calculations – drop factor
– macrodrop – factor of 10, 15, or 20 drops per ml
– microdrip – 60 gtts/ml
• Formula for calculating iv flow rate:
V1/T1 = V2/T2 where V1 – volume to infuse;
T1 – time to infuse;

V2 – drop factor;
T2 - time in minutes
 Pediatric Calculations
• Based on body surface area
– BSA is determined from a normogram
– Formula: child’s BSA /1.7 sq. m. x adult dose
• Based on body weight:
– Convert child’s weight to kg. (1 kg. = 2.2 lb)
– Calculate the medication dose, then the daily dose, then
divide the daily dose by the number of doses/day