kelasB

Sistem Penghantaran
Obat
Endang Diyah Ikasari

Materi kuliah...
Introduction
Influence of drug properties and routes of drug
administration
Theory of mass transfer
Polymer in controlled release
Transdermal therapeutic system
Microparticulate drug carries: liposom,
micropheres, cells
Prodrug delivery system
gastroretentive

Definisi....
A drug delivery system (DDS) is
defined as a formulation or a device
that enables the introduction of a
therapeutic substance in the body and
improves its efficacy and safety by
controlling the rate, time, and place of
release of drugs in the body

Aims of DDS Development

1.
2.
3.
4.
5.
6.

Improvement of drug safety and efficacy

Improved compliance
Chronopharmacological benefits
Reduction of cost of drug development
Life extension of the products
Reduction of risk of failure in new product
development

Sistem penghantaran obat (DDS)

kompleksitas penghantaran obat.
Optimasi obat sampai lokasi target
Aspek temporal (berkaitan dengan waktu)
Aspek spasial (berkaitan dengan tempat)

Struktur molekul obat

(bobot/besar molekul)

Absorpsi obat

Sifat fisikokimia

Suhu lebur
pKa
Kelarutan
Koefisien partisi
pH stabilitas
kristal

Perilaku dalam GIT

Jendela absorpsi
Transport aktif/pasif
Abs. Limfatik
farmakokinetika

Dosage form design:

A Physicochemical Approach
In enhancing the safety and therapeutic
efficacy
A rational approach to designing any
dosage form requires a complete
understanding of its physicochemical and
biopharmaceutical properties
The physicochemical and
biopharmaceutical properties of the drug
can have a tremendous impact on its BA
and hence on its efficacy and toxicity
profile

Sifat fisikokimia dan biofarmasetika

yang perlu diperhatikan:
1. Solubility and dissolution rate
2. Partition coefficient
3. Stability and/or degradation rate in the
physiological fluids
4. Susceptability to metabolic inactivation
5. Mechanism of transport through biological
membranes.

Poor aqueous solubility is not always

limitation

Contoh:
Sediaan SR p.o dapat dicapai apabila suatu
obat dikombinasi dengan zat yang memiliki
kelarutan dalam air rendah, sehingga dapat di
abs. GIT
Sediaan SR parenteral dapat dicapai setelah
pemberian i.m pada obat yang telah
dilarutkan dalam air/suspensi/ sediaan dalam
bentuk reservoir/depot dalam minyak.

Once the physicochemical and

biopharmaceutical properties of the drug are
determined and the desired plasma
concentratiom profile is defined, an efficacious
dosage form can be selected and developed
bay utilizing some approach:

Pendekatan formulasi
Pendekatan metode/peralatan
Pendekatan pro drug
Pendekatan dengan alternatif cara
pemberian