Nasal Dosage

Andi Nafisah Tendri Adjeng Mallarangeng

Struktur dan fungsi fisiologi dari organ hidung

adalah:

1. Lubang (bukaan) hidung, merupakan jalur utama udara untuk masuk

ke dalam rongga hidung. Lubang hidung dipisahkan oleh septum.
2. Rongga nasal terdiri atas 3 bagian terusan yang disebut dengan
turbinate (meatus):

Inferior tubinate (meatus bawah)

Middle tubinate (meatus tengah)

Superior turbinate (meatus atas)

Anatomi hidung

Sel Reseptor Saraf pada

Hidung adalah sel olfaktori
yang terletak pada jaringan
epitel olfaktori di langit-langit
rongga hidung.

Di dalam sel-sel olfaktori

terdapat sekumpulan rambut
mikro atau silia.

Silia akan mendeteksi

partikel-partikel pembawa
bau tertentu dari udara, yang
melewati hidung sehingga
mendarat pada silia. Partikelpartikel ini larut dalam lapisan
mukus. Silia berhubungan
dengan sel saraf olfaktori
yang membawa impuls saraf
menuju otak.

CHARACTERISTICS OF
NASAL CELLS
The nasal epithelium exhibits relatively
high permeability, and only two cell layers
separate the nasal lumen from the dense
blood-vessel network in the lamina
propria.

The respiratory epithelium is covered by a

mucus layer, which can be divided into
two distinctive layers (the periciliary layer
and a more gel-like upper layer).

The respiratory epithelium is the major

lining of the human nasal cavity and is
essential in the clearance of mucus by the
mucociliary system.

This epithelium is composed of ciliated

and non-ciliated columnar cells, goblet
cells, and basal cells.

The periciliary layer consists of a liquid of

lower viscosity.

Mucus is secreted from goblet cells as

highly condensed granules by exocytosis.
The mucus layer is propelled by the cilia
toward the nasopharynx, and the function
of the mucociliary clearance is to remove
foreign substances and particles from the
nasal cavity, preventing them to reach the
upper airways.

The ciliated epithelium of the nasal

passage facilitates the movement of
the mucous layer. The mucus
contains lysozyme, glycoproteins,
and immunoglobulins that act
against bacteria and protect against
their entry into the lungs. The ciliary
action and the sneeze re ex add
further defense against entry

The physical characteristics of compounds for

optimal intranasal absorption are the same as for
other absorption routes. The drug must dissolve
in the uids of the nasal mucosa and must be
sufciently lipophilic to cross the membranes of
the nasal epithelium. Nasal absorption is
facilitated by the high permeability of small
venules and capillaries associated with the
nasal mucusa

NASAL
PHARMACOLOGY

Dont u
know?????

Nasal administration produces

rapid blood levels and rapid
responses that approach those
obtained from intravenous
dosing.

the absorbed drug does not

pass through the liver before
reaching the systemic
circulation, and, thus, rst-pass
metabolism is avoided.

In recent years, the nasal route

has received a great deal of
attention as a convenient and
reliable route for the systemic
administration of drugs,
especially those that are
ineffective orally and must be
given by injection.

Recently, butorphanol tartrate

was introduced commercially in
a nasal spray dosage form
(Stadol NS) for the relief of pain,
such as migraine headache.

treatment of nasal
allergies,

Intranasal
administration may be
used for local effects.
Local effects include

rhinitis,

nasal congestion.

It would appear that the

nasal route could be
considered for drugs that
meet the following criteria:
are
ineffective
orally;

are used
chronically;

are used
in small
doses;

are
desirable
to have
rapid entry
to the
general
circulation.

Syarat-syarat pembawa
tetes hidung
Memiliki pH pada range 5,5-7,5
Memiliki kapasitas buffer yang rendah
Isotonis atau mendekati isotonis
Tidak mempengaruhi viskositas normal mukus
Dapat cocok dengan pergerakan silia normal dan konsistensi ion
pada sekret hidung
Cocok dengan bahan aktif
Mengandung pengawet untuk menekan pertumbuhan bakteri yang
ada selama penggunaan tetes hidung

Nasal Dosage
consist of:

 drops
ne mist
Most nasal
(aerosols)
preparations
nebulizers,
are
soluble
matrices

are small volume

aqueous solutions.

are usually buffered to

pH of 6.8

Nasal drops:

are isotonic solutions.

These drops are used

locally as antibiotics,
anti-inammators, and
decongestants

Tonisitas

pH

Viskositas

Digunakan larutan
dengan tonisitas yang
mendekati atau
isotonis, karena jika
sangat encer atau
sangat pekat akan
menyebabkan iritasi
pada mukosa hidung

pH yang kearah alkali

dapat menyebabkan
rhinitis akut. Larutan
dengan sedikit asam
cukup efektif, karena
sediaan yang bersifat
asam dapat
meningkatkan
keasaman sekresi
selain itu pH asam baik
terhadap pertahanan
terhadap bakteri

Vsikositas yang terlalu

berlebihan dapat
mempengaruhi
pergerakan silia,
namun bersifat
temporaliy

Nasal Aerosols are

intended for
topical
administration

administration
into body
cavities

Administration
nasally as ne
solid particles or
liquid mists

through the
nasal passages

Gels

intranasal vitamin B-12 gel, Nascobal (Schwarz

Pharma), is used as a dietary supplement. The gel
base is composed of a hydrophilic cellulose
derivative. The gel is apparently odorless and nonirritating, and adheres well to the mucous
membrane.

jellies

Neo-SynephrineViscous (Sano Winthrop) is a watersoluble nasal jelly formulated with methylcellulose; it

contains the decongestant phenylephrine
hydrochloride.

soluble
matrices

The benets of nasally

delivered products are
rapid onset of
action

Nasal drugs
Avoidance of
can be
gastrointestinal administered at
breakdown and a lower dose,
rst-pass
which also
means fewer
metabolism.
side effects.

Disadvantage of nasal dosage

The
sophisticated
structure and
specialized
function of
airways and
membranes in
the nasal cavity,

The small
surface area of
this region,

May limit its

capacity for
drug delivery