Teknologi Farmasi Sediaan

Padat
Pendahuluan
Deni Rahmat

 Obat : senyawa yang aktif secara fisiologi yang

digunakan untuk pengobatan penyakit dalam
manusia (Ansel).
Senyawa obat mungkin didapat dari mineral,
tumbuh-tumbuhan, binatang atau merupakan
produk dari sintesis kimia organik atau
biosisntesis.
Senyawa obat dikombinasikan dengan bahanbahan farmasetik tidak aktif secara fisiologi
dalam penyiapan berbagai bentuk sediaan
obat.

 USP berisi monograpi yang detil tentang

senyawa obat dan bentuk sediaan sementara
National Formulary berisi monograpi mengenai
bahan-bahan farmasetik.
Harus dicatat bahwa banyak produk farmasetik
di pasaran tidak dicantumkan dalam monograpi.
Bentuk sediaan dari suatu obat mungkin
bervariasi, dengan berbagai rute pemberiannya.
Hal ini karena perbedaan rates and extents
dari absorpsi dari berbagai cara pemberian obat.

 Obat-obat yang diberikan secara intravena

memasuki aliran darah secara langsung
dan karenanya obat seluruhnya ada dalam
darah.
Pemberian secara oral mempunyai barriers
biologi, kimia dan fisika.
Dosis injeksi parenteral akan lebih rendah
dibandingkan dengan dosis oral untuk
mencapai konsentrasi obat dan efek terapi
yang sama.

 Absorpsi dapat terjadi di berbagai tempat di

dalam tubuh yang dapat dicapai dari rektum,
saluran cerna, di bawah lidah dan dari tempattempat lain.
Karenanya, masing-masing obat harus dipelajari
secara individual untuk menentukan rute
terbaik dari pemberiannya dan selanjutnya
bentuk sediaan yang sesuai untuk memenuhi
persyaratan klinik yang diinginkan.
Penakaran dosis pada sediaan cair adalah
fleksibel dibandingkan dengan sediaan padat.

 Obat-obat jarang diberikan sendiri tetapi

bersama dengan satu atau lebih bahan
pembantu yang mempunyai berbagai fungsi.
Melalui penggunaan secara selektif bahan
pembantu/eksipien/pharmaceutic ingredients
bisa dihasilkan berbagai bentuk sediaan.
Eksipien itu dapat : melarutkan,
mensuspensikan, mengentalkan,
mengencerkan, mengemulsikan, menstabilkan,
mengawetkan, mewarnai, memberikan rasa
kepada zat aktif.

Mengapa perlu dibuat bentuk sediaan?

Penghantaran dosis yang akurat secara
aman dan nyaman.
Perlindungan zat aktif dari pengaruh yang
merusak dari udara (oksigen) dan lembab.
Perlindungan zat aktif dari pengaruh yang
merusak dari asam lambung setelah
pemberian oral.
Menyembunyikan rasa yang tidak enak dari
zat aktif (kapsul, tablet salut, sirup manis).

 Menyediakan sediaan cair dari zat yang

tidak larut atau tidak stabil dalam pembawa
yang diinginkan (suspensi).
Menyediakan bentuk sediaan cair yang larut
dalam pembawa yang diinginkan (sirup).
Menyediakan aksi obat yang diperpanjang
melalui mekanisme controlled release
(berbagai sediaan tablet, kapsul dan
suspensi controlled release).

 Menyediakan aksi obat yang optimal dari

tempat pemberian secara topikal (salep,
cream, patch transdermal, sediaan untuk
diberikan di hidung, telinga dan mata).
Menyediakan pemberian obat ke dalam
celah di tubuh (suppositoria dan ovula).
Menyediakan pemberian obat langsung ke
dalam aliran darah (injeksi).
Menyediakan aksi obat yang optimal
melalui terapi inhalasi (inhalasi aerosol).

Rute Pemberian Obat

Oral |mulut
Sublingual|di bawah lidah
Parenteral|selain melalui saluran cerna
(dengan injeksi)
intravena|vena
intraarteri|arteri
intracardiac|hati
subkutan|di bawah kulit

intramuskular|otot
Transdermal|permukaan kulit
Konjungtival|konjungtiva
Intranasal|hidung
Aural|telinga
Rektal|rektum
Vaginal|vagina
Uretal|uretra

Bentuk Sediaan Padat:

Oral|tablet, kapsul, serbuk
Sublingual|tablet
Rektal|suppositoria
Vaginal|suppositoria, tablet

Powder
In compounding, "powder" refers to a
dosage formulation that is solid in
physical state.
But the formulation may be
composed of only the active drug or
may be a mixture of the active drug
and other ingredients.

 Pharmaceutical powders are formulated to be exist

as fine particles.
The powders are then smooth to the touch and
nonirritating to the skin.
Powders generally range from 0.1 to 10 micron in
size.
The size of the particles are often expressed as a
number which corresponds to the mesh screen size
of a sieve.
The screen size indicates the number of openings
in the mesh screen per inch.
For example, a # 40 sieve has 40 openings per
inch in the screen mesh. Particles that can sift
through that mesh are said to be "40 mesh" size.

Comminution
Reducing the particle size of a
powder will result in an uniform
distribution of particle sizes.
The process of reducing the particle
size is called comminution.

Capsule
The word capsule is derived from the latin
capsula meaning a small box.
In pharmacy, the word capsule is used to
describe an edible package made from gelatin
which is filled with medicines to produce a unit
dose, mainly for oral use.
There are two types of capsule, differentiated by
adjectives hard and soft.
The hard capsule consists of two pieces, a cap
and a body, that fit one inside the other.

 They are produced empty and are filled in a

separate operation.
The soft gelatin capsule is a capsule which is
manufactured and filled in one operation.
The raw material used in manufacture are similar
for both hard and soft capsules.
The first stage of the process is to prepare a
gelatine solution in demineralized water or a
mixture of demineralized water and glyserol. To this
are added, colorants, preservatives and process aid
depending upon the type of capsule required.

Tablet
The compressed tablet is the most popular dosage
form in use today.
About two-thirds of all prescriptions are dispensed as
solid dosage forms, and half of these are compressed
tablets.
A tablet can be formulated to deliver an accurate
dosage to a specific site; it is usually taken orally, but
can be administered sublingually, rectally or
intravaginally.
It is just one of the many forms that an oral drug can
take such as syrups, elixirs, suspensions, and
emulsions.
It consists of an active ingredient with biologically inert
excipients in a compressed, solid form.

 Tablets can be made in virtually any shape, although

requirements of patients and tabletting machines mean
that most are round, oval or capsule shaped.
Tablet diameter and shape are determined a
combination of a set of punches and a die. The
thickness is determined by the amount of tablet
material and the position of the punches in relation to
each other during compression.
Once this is done, we can measure the corresponding
pressure applied during compression. The shorter the
distance between the punches, thickness, the greater
the pressure applied during compression, and
sometimes the harder the tablet. Tablets need to be
hard enough that they don't break up in the bottle, yet
friable enough that they disintegrate in the gastric tract.

 The tablet is composed of the Active Pharmaceutical

Ingredient (that is the active drug) together with
various excipients.
These are biologically inert ingredients which either
enhance the therapeutic effect or are necessary to
construct the tablet.
The filler or diluent (eg lactose or sorbitol) is a bulking
agent, providing a quantity of material which can
accurately be formed into a tablet.
Binders (eg methyl cellulose or gelatin) hold the
ingredients together so that they can form a tablet.
Lubricants (eg magnesium stearate or
polyethylene glycol) are added to reduce the friction
between the tablet and the punches and dies so that
the tablet compression and ejection processes are
smooth.
Disintegrants (eg starch or cellulose) are used to
promote wetting and swelling of the tablet so that it
breaks up in the gastro intestinal tract; this is
necessary to ensure dissolution of the API.

 Tableting methods consist of granulation and direct

compression.
Granulation may be defined as a size enlargement
process which converts small particles into
physically stronger & larger agglomerates.
Granulation method can be broadly classified into
two types: Wet granulation and Dry granulation.
Powders that can be mixed well and therefore do
no require granulation and can be compressed in to
tablet through Direct Compression.

Suppositories
Suppositories are solid preparations which may contain one or more
active pharmaceutical ingredient(s) intended for rectal application.
They are normally used for local action or systemic absorption of the
active ingredient(s).
They usually melt, soften, or dissolve at body temperature.
Suppositories are usually prepared from excipients or bases such as
cocoa butter, glycerinated gelatin and macrogols.
They may also contain additives, such as adsorbents, surface-active
agents, viscosity-influencing agents, antioxidants, antimicrobials, and
authorized colouring agents.
Any excipients used for the preparation of suppositories must be
proven through product development studies not to affect adversely
either the stability of the final product or the availability of the active
ingredient(s) at the site of action; incompatibility between any of the
components of the dosage form should be avoided.

Ovula
Vagina is route for administration for
contraceptives, antifungals,
antimicrobials.
It is used for the achievement of
local or for systemic absorption.
The vaginal wall is very well suited
for the absorption of drugs for
systemic use.
As it contains a vast network of blood