Nasal Dosage

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Nasal Dosage Andi Nafisah Tendri Adjeng Mallarangeng

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Nasal Dosage

Transcript of Nasal Dosage

  • 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