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 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 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: Solubility and dissolution rate Partition coefficient Stability and/or degradation rate in the physiological fluids Susceptability to metabolic inactivation 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.

Pendekatan metode/peralatan Pendekatan pro drug 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