Biofarmasetika

Nur Illiyyin Akib

Latar Belakang
Not as pure chemical drug substances but are
formulated into finished dosage forms (drug
products),
Formulated drug products active drug
substance and selected ingredients (excipients)
Drug products are designed to deliver drug for
local or systemic effects.
The design and formulation of drug products
requires a thorough understanding of the
biopharmaceutic principles of drug delivery

Sediaan obat molekul obat

absorbsi fraksi obat jaringan
MEC-MIC aksi
Sifat kimia
fisika obat

Bentuk
Formula

Pengujian in vitro dan in

vivo

Fis

io
lo

gi
s

Definisi
Biopharmaceutics is the study of the in-vitro
impact of the physicochemical properties of
drugs and drug products on drug delivery to the
body under normal or pathologic conditions.
Bioavailability refers to the measurement of the
rate and extent of active drug that becomes
available at the site of action.
Because the systemic blood circulation delivers
therapeutically active drug to the tissues and to
the site of action of the drug, changes in
bioavailability affect changes in the
pharmacodynamics and toxicity of a drug.

Pengertian Biofarmasetika
Mempelajari hubungan sifat fisika kimia bahan
aktif dan formulasi sediaan obat terhadap
bioavailabilitasnya.
Sifat Fisikokimia obat dipelajari dalam Ilmu
Kimia Fisika dan Farmasi Fisika
Formulasi sediaan obat dipelajari dalam kuliah
Farmasetika
Bioavailabilitas obat dipelajari dalam ilmu
Farmakokinetika,
Bioavailabilitas (F): kecepatan dan jumlah obat
yang mencapai sirkulasi sitemik.

Materi Kuliah
pengantar biofarmasetika
transport lintas membran
faktor kimia fisika obat bioavailabilitas
faktor formulasi obat bioavailabilitas
Faktor fisiologis pasien bioavailabilitas
biofarmasetika sediaan oral, transdermal, dan
okular
7. Pengujian bioavailabilitas dan bioekivalensi
8. Studi absorbsi obat
9. Studi disolusi obat
1.
2.
3.
4.
5.
6.

 Absorpsi sistemik dipengaruhi:

1. Anatomik dan fisiologik tempat
absorpsi
2. Fisika kimia obat atau sediaannya.
. Memilih rute pemberian obat dan
rancangan bentuk sediaan obat
bioavailabilitas obat dapat
dikendalikan.

Faktor Fisika Kimia

pH dan pKa
Ukuran partikel
Koefisien partisi
Polimorfisme
Hidrat/anhidrat
Bentuk kristal

Faktor Anatomi-Fisiologi

Kecepatan pengosongan lambung

Motilitas usus waktu transit
Perfusi darah ke saluran cerna
Interaksi OM
Metabolisme lintas pertama

Bentuk Sediaan

Sediaan padat
Sediaan cair
Rute pemakaian
Pembawayang ideal

Tujuan Mempelajari Biofarmasetika

adjust the delivery of drug from the drug product in such
a manner as to provide optimal therapeutic activity and
safety for the patient
Biofarmasetika bertujuan untuk mengatur pelepasan obat
sedemikian rupa ke sirkulasi sistemik agar diperoleh
pengobatan yang optimal pada kondisi klinik tertentu
(Shargel, 2005).
Rational design of drug products based on:
(1) the physical and chemical properties of the drug substance
(2) the route of drug administration, including the anatomic and
physiologic nature of the application site (eg, oral, topical,
injectable, implant, transdermal patch, etc
(3) desired pharmacodynamic effect (eg, immediate or prolonged
activity)
(4) toxicologic properties of the drug

Each route of drug application special

biopharmaceutic considerations in drug product
design

Contoh:
a vaginal tablet formulation for the treatment
of a fungal infection ingredients
compatible with vaginal anatomy and
physiology
An eye medication appropriate pH,
isotonicity, sterility, local irritation to the
cornea, draining by tears, and concern for
systemic drug absorption

Each route of drug application special

biopharmaceutic considerations in drug product
design

Contoh:
intramuscular injection drug local
irritation, drug dissolution, and drug
absorption from the intramuscular site
The systemic absorption of a drug from an
extravascular site is influenced by the
anatomic and physiologic properties of the
site and the physicochemical properties of
the drug and the drug product.

 The rate of drug release from the product

and the rate and extent of drug absorption
are important in determining the distribution,
onset, intensity, and duration of drug action.

By choosing the route of drug administration

carefully and properly designing the drug
product
biopharmaceutic studies the drug product
does not irritate, cause an allergic response,
or allow significant systemic drug absorption

Proses Absorbsi Obat Padat

(1)disintegration of the drug product
and subsequent release of the drug
(2)dissolution of the drug in an
aqueous environment
(3)absorption across cell membranes
into the systemic circulation.

Tugas
Jelaskan definisi, uraikan mekanismenya,
jelaskan di mana terjasinya, dan sebutkan
senyawa obat untuk jenis transport lintas
membran berikut ini:
1. Difusi pasif
2. Difusi terfasilitasi
3. Osmosis
4. Transport pasangan ion
5. Transport konvektif
6. Pinositosis

FISIKA KIMIA BAHAN OBAT

pH dan pKa optimum stability and solubility
of the final product
Partikel Size solubility of the drug and
therefore the dissolution rate of the product
Polymorphism The ability of a drug to exist in
various crystal forms may change the
solubility of the drug. Also, the stability of
each form is important, because polymorphs
may convert from one form to another.
Hygroscopicity Moisture absorption may
affect the physical structure as well as
stability of the product

FISIKA KIMIA BAHAN OBAT

Partition coefficient May give some
indication of the relative affinity of the drug
for oil and water. A drug that has high
affinity for oil may have poor release and
dissolution from the drug product.
Excipient interaction The compatibility of
the excipients with the drug and sometimes
trace elements in excipients may affect the
stability of the product. It is important to
have specifications of all raw materials.

Faktor Formulasi
Excipients provide certain functional
properties to the drug and dosage form:
improve the compressibility of the active
drug
improve stabilize the drug against
degradation,
decrease gastric irritation
control the rate of drug absorption from the
absorption site
increase drug bioavailability

Faktor Formulasi
Excipients affect the dissolution kinetics of the drug by
altering the medium in which the drug is dissolving or by reacting
with the drug itself.
suspending agents increase the viscosity of the drug vehicle -->
diminish the rate of drug dissolution from suspensions.
Tablet lubricants repel water and reduce dissolution when used
in large quantities.
Coatings will crosslink upon aging and decrease the dissolution
rate.
surfactants low concentrations of surfactants decrease the
surface tension and increase the rate of drug dissolution. Higher
surfactants concentrations tend to form micelles with the drug
and thus decrease the dissolution rate.
High compression of tablets without sufficient disintegrant may
cause poor disintegration of a compressed tablet.

Pertimbangan biofarmasetika: safety dan

efficacy
Pertimbangan farmakodinamika: release
the drug rapidly atau slowly nirogliserin
for angina pektoris dan asma
Pertimbangan senyawa obat:
physicochemical properties influence the
type of dosage form and the process for
the manufacture of the dosage form

 Pertimbangan bentuk sediaan obat:

sediaan oral, sediaan bukal dan
sublingual, sediaan nasal, sediaan
rektal dan vaginal, sediaan
parenteral, sediaan inhalasi, sediaan
transdermal