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Nasal Dosage
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Nasal Dosage
Andi Nafisah Tendri Adjeng Mallarangeng
Struktur dan fungsi fisiologi dari organ hidungadalah:
1. Lubang (bukaan) hidung, merupakan jalur utama udara untuk masukke dalam rongga hidung. Lubang hidung dipisahkan oleh septum.
2. Rongga nasal terdiri atas 3 bagian terusan yang disebut denganturbinate (meatus):
Inferior tubinate (meatus bawah) Middle tubinate (meatus tengah) Superior turbinate (meatus atas)
Anatomi hidung
Sel Reseptor Saraf padaHidung adalah sel olfaktoriyang terletak pada jaringanepitel olfaktori di langit-langit
rongga hidung.
Di dalam sel-sel olfaktoriterdapat sekumpulan rambut
mikro atau silia.
Silia akan mendeteksipartikel-partikel pembawabau tertentu dari udara, yangmelewati hidung sehinggamendarat pada silia. Partikel-partikel ini larut dalam lapisanmukus. Silia berhubungandengan sel saraf olfaktoriyang membawa impuls sarafmenuju otak.
CHARACTERISTICS OFNASAL CELLS
The nasal epithelium exhibits relativelyhigh permeability, and only two cell layersseparate the nasal lumen from the dense
blood-vessel network in the laminapropria.
The respiratory epithelium is the majorlining of the human nasal cavity and is
essential in the clearance of mucus by themucociliary system.
This epithelium is composed of ciliatedand non-ciliated columnar cells, goblet
cells, and basal cells.
The respiratory epithelium is covered by amucus layer, which can be divided intotwo distinctive layers (the periciliary layer
and a more gel-like upper layer).The periciliary layer consists of a liquid of
lower viscosity.
Mucus is secreted from goblet cells ashighly condensed granules by exocytosis.The mucus layer is propelled by the ciliatoward the nasopharynx, and the functionof the mucociliary clearance is to removeforeign substances and particles from thenasal cavity, preventing them to reach the
upper airways.
The ciliated epithelium of the nasalpassage facilitates the movement of
the mucous layer. The mucuscontains lysozyme, glycoproteins,and immunoglobulins that act
against bacteria and protect againsttheir entry into the lungs. The ciliaryaction and the sneeze re ex addfurther defense against entry
The physical characteristics of compounds foroptimal intranasal absorption are the same as forother absorption routes. The drug must dissolvein the uids of the nasal mucosa and must besufciently lipophilic to cross the membranes ofthe nasal epithelium. Nasal absorption isfacilitated by the high permeability of smallvenules and capillaries associated with thenasal mucusa
NASALPHARMACOLOGY
Nasal administration producesrapid blood levels and rapid
responses that approach thoseobtained from intravenous
dosing.
the absorbed drug does notpass through the liver before
reaching the systemiccirculation, and, thus, rst-pass
metabolism is avoided.
In recent years, the nasal routehas received a great deal ofattention as a convenient andreliable route for the systemic
administration of drugs,especially those that are
ineffective orally and must begiven by injection.
Recently, butorphanol tartratewas introduced commercially in
a nasal spray dosage form(Stadol NS) for the relief of pain,such as migraine headache.
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Intranasaladministration may beused for local effects.Local effects include
treatment of nasalallergies,
rhinitis,
nasal congestion.
It would appear that thenasal route could be
considered for drugs thatmeet the following criteria:are
ineffectiveorally;
are usedchronically;
are usedin smalldoses;
aredesirableto have
rapid entryto thegeneral
circulation.
Syarat-syarat pembawatetes hidung
Memiliki pH pada range 5,5-7,5
Memiliki kapasitas buffer yang rendah
Isotonis atau mendekati isotonis
Tidak mempengaruhi viskositas normal mukusDapat cocok dengan pergerakan silia normal dan konsistensi ion
pada sekret hidungCocok dengan bahan aktif
Mengandung pengawet untuk menekan pertumbuhan bakteri yangada selama penggunaan tetes hidung
Nasal Dosageconsist of:
drops ne mist(aerosols)
nebulizers, solublematrices
Most nasalpreparations
are
Nasal drops:
are small volumeaqueous solutions.
are usually buffered topH of 6.8
are isotonic solutions.
These drops are usedlocally as antibiotics,anti-inammators, and
decongestants
TonisitasDigunakan larutandengan tonisitas yangmendekati atauisotonis, karena jikasangat encer atausangat pekat akanmenyebabkan iritasipada mukosa hidung
pHpH yang kearah alkalidapat menyebabkanrhinitis akut. Larutandengan sedikit asamcukup efektif, karenasediaan yang bersifatasam dapatmeningkatkankeasaman sekresiselain itu pH asam baikterhadap pertahananterhadap bakteri
ViskositasVsikositas yang terlaluberlebihan dapatmempengaruhipergerakan silia,namun bersifattemporaliy
intended fortopical
administrationadministration
into bodycavities
Administrationnasally as nesolid particles or
liquid miststhrough the
nasal passages
Nasal Aerosols are
solublematrices
Gels
intranasal vitamin B-12 gel, Nascobal (SchwarzPharma), is used as a dietary supplement. The gel
base is composed of a hydrophilic cellulosederivative. The gel is apparently odorless and non-
irritating, and adheres well to the mucousmembrane.
jelliesNeo-SynephrineViscous (Sano Winthrop) is a water-soluble nasal jelly formulated with methylcellulose; it
contains the decongestant phenylephrinehydrochloride.
The benets of nasallydelivered products are
rapid onset ofaction
Avoidance ofgastrointestinalbreakdown and
rst-passmetabolism.
Nasal drugscan be
administered ata lower dose,which also
means fewerside effects.
Disadvantage of nasal dosage
Thesophisticatedstructure andspecializedfunction ofairways andmembranes inthe nasal cavity,
The smallsurface area ofthis region,
May limit itscapacity fordrug delivery