Intranasal

Intranasal can be used for
local & sytemic

3 nasal regions (**VRO)

 

Vestibular

 

Respiratory

 

Olfactory

Vestibular=nasal vestibule & valve

 

Respiratory= extends 6-8cm backwards.inc SA &turbulence

[3 turbinates Inferior,Middle,Superior]

 

Olfactory= Roof of nasal canal

[poorly ventilated, close to CNS. Potential for Rx delivery to brain. Very Small SA]

Which nasal region is major region for rx absorption
Respiratory Region
Nasal Mucosa 2 parts

Anterior=1/3 resp region(varying epithelia)

 

 

Posterior=2/3 resp region(gud for abs due to only have 1 cell layer)

[ciliated pseudostratified epithelium,mucociliary clearance]

 

Mucociliary clearance

Mucus

 

 

Cilia

 

occurs in posterior of resp reg

 

Mucus=protects epi,trap/transports substances(especially rx and undsolved stuff) pH 6.3

 

Cilia= function in coordination ot move mucus[mucus moved posteriorly]

clearanc 15- 20 mins for inhaled sub

one of most important factors physiologically affecting nasal drug absorption

Mucociliary clearance

[less enzyme act than intestines]

Nasal blood supply is _______ and not drained to _____

highly vascularized(can absorb large molecules)

 

hepatic portal system

Synarel (Rx)

Naferelin (generic)[peptide]

for central precocious puberty, nasasl cavity contains fenestrated caps

Nasal associated lymphoid tissue vaccine used intranasal
Flumist
nasal complicated by these conditions

Physiologic=rhinitis,asthma,hay fever,nasal polyps

 

environmental=humidity,temp,some rx dry nasal secretion

Dose form design concepts(***POVPD)

pH=4-8(ciliary beat best at 7-10)

Osmolarity=isotonic liquids preferred

Viscosity = affects drug fate(high slows clearance)

Preservation= Antimicrobial preservatives are usually included in the formulation

dRUG DISPOSITION=form spray vs drop()

Spray=deposited in anterior

 

Drop= generally get greaer coverage 

sprays=metered dosed aerosol pressurized
SPRAY considerations=

Description=pressurized aerosol vs mechanical pump

 

Particle size= 8-20 um in diameter impact the nasal cavity

 

Spray bottle design= designed to reach nasal valve

STADOL (Rx)

 

butorphanol tartrate(generic)

 

nasal spray=used for pain relief(systemic)

extensive first pass

aqueous sol

Rhinocort Nasal Inhaler

budesonide 

used for allergic rhinitis(local inflammation)

20% reaches sys absorption

metered dosedpressurized inhaler

(micronized budesonide suspended in propellants)

Bactroban Nasal

Mupirocin calcium

 

ointment 2% nasal colonizaion of MRSA 

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