NAV

Hydroxypropyl cellulose

Identification

Summary

Hydroxypropyl cellulose is a cellulose ether used to treat dry eyes.

Brand Names
Lacrisert
Generic Name
Hydroxypropyl cellulose
DrugBank Accession Number
DB00840
Background

Hydroxypropyl cellulose is an ether of cellulose where some of the hydroxyl groups of the cellulose have been hydroxypropylated forming -OCH2CH(OH)CH3 groups. Lacrisertis a formulation of hydroxypropyl cellulose that is used for artificial tears. It is used to treat syndromes characterized by insufficient tear production (keratoconjunctivitis sicca), recurrent corneal erosions, decreased corneal sensitivity, exposure and neuroparalytic keratitis, and as a lubricant for artificial eyes. As a food additive, hydroxypropyl cellulose is used as a thickener and as an emulsion stabilizer.

Type
Small Molecule
Groups
Approved
Synonyms
  • Cellulose hydroxypropyl ether
  • Cellulose, 2-hydroxypropyl ether
  • Hiprolosa
  • Hydroxypropyl cellulose
  • Hydroxypropyl cellulose (type H)
  • Hydroxypropylcellulose
  • Hyprolose
  • Hyprolosum
  • Modified cellulose
External IDs
  • E 463
  • E-463
  • Ins no.463
  • INS-463

Pharmacology

Indication

Used to relieve dryness and irritation caused by reduced tear flow that occurs in certain eye diseases (keratoconjunctivitis sicca), recurrent corneal erosions, decreased corneal sensitivity, exposure and neuroparalytic keratitis, and as a lubricant for artificial eyes.

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Associated Conditions
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Pharmacodynamics

Hydroxypropyl cellulose (cellulose, 2-hydroxypropyl ether) is a derivative of cellulose with both water solubility and organic solubility. Hydroxypropyl cellulose acts to stabilize and thicken the precorneal tear film and prolong the tear film breakup time which is usually accelerated in patients with dry eye states. Hydroxypropyl cellulose also acts to lubricate and protect the eye. Hydroxypropyl cellulose usually reduces the signs and symptoms resulting from moderate to severe dry eye syndromes, such as conjunctival hyperemia, corneal and conjunctival staining with rose bengal, exudation, itching, burning, foreign body sensation, smarting, photophobia, dryness and blurred or cloudy vision. Progressive visual deterioration which occurs in some patients may be retarded, halted, or sometimes reversed.

Mechanism of action

Hydroxypropyl cellulose is a derivative of cellulose that is soluble in both water and organic solvents. It is particularly good at trapping water and producing a film that serves as a barrier to water loss. Hydroxypropyl cellulose possesses good surface activity but does not gel as it forms open helical coils. In general Hydroxypropyl cellulose is a water-soluble thickener, emulsifier and film-former often used in tablet coating.

Absorption

Studies conducted in rats fed 14 C-labeled hydroxypropyl cellulose demonstrated that when orally administered, hydroxypropyl cellulose is not absorbed from the gastrointestinal tract and is quantitatively excreted in the feces.

Volume of distribution

Not Available

Protein binding

None

Metabolism

Hydroxypropyl cellulose is a physiologically inert substance. In a study of rats fed hydroxypropyl cellulose or unmodified cellulose at levels up to 5% of their diet, it was found that the two were biologically equivalent in that neither was metabolized.

Route of elimination

Studies conducted in rats fed 14C-labeled hydroxypropyl cellulose demonstrated that when orally administered, hydroxypropyl cellulose is not absorbed from the gastrointestinal tract and is quantitatively excreted in the feces.

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

LD50=10200 mg/kg (oral, rat)

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
No interactions found.
Food Interactions
No interactions found.

Products

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International/Other Brands
A-Gel (Fresenius Kabi)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
LacrisertPellet5 mg/1OphthalmicAton Pharma, Inc.1981-06-012016-09-21US flag
LacrisertInsert5 mg / insertOphthalmicBausch Health, Canada Inc.2004-05-25Not applicableCanada flag
LacrisertInsert5 mg/1ConjunctivalMerck Sharp & Dohme Limited1981-06-012009-05-31US flag
LacrisertInsert5 mg/1OphthalmicBausch & Lomb Incorporated1981-06-01Not applicableUS flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
RFW2ET671P
CAS number
9004-64-2
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

Synthesis Reference

Seiji Orii, Yukio Sasagawa, Akinori Ito, Maruyama, Hiromi, Yoshiteru Sakai, "Process of producing hydroxypropyl cellulose." U.S. Patent US4292426, issued April, 1964.

US4292426
General References
  1. Wander AH: Long-term use of hydroxypropyl cellulose ophthalmic insert to relieve symptoms of dry eye in a contact lens wearer: case-based experience. Eye Contact Lens. 2011 Jan;37(1):39-44. doi: 10.1097/ICL.0b013e3181f84f92. [Article]
  2. McDonald M, D'Aversa G, Perry HD, Wittpenn JR, Nelinson DS: Correlating patient-reported response to hydroxypropyl cellulose ophthalmic insert (LACRISERT(R)) therapy with clinical outcomes: tools for predicting response. Curr Eye Res. 2010 Oct;35(10):880-7. doi: 10.3109/02713683.2010.495811. [Article]
  3. Luchs JI, Nelinson DS, Macy JI: Efficacy of hydroxypropyl cellulose ophthalmic inserts (LACRISERT) in subsets of patients with dry eye syndrome: findings from a patient registry. Cornea. 2010 Dec;29(12):1417-27. doi: 10.1097/ICO.0b013e3181e3f05b. [Article]
KEGG Drug
D01536
PubChem Substance
46508483
RxNav
27291
ChEMBL
CHEMBL1201471
PharmGKB
PA164746492
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Hydroxypropyl_cellulose
FDA label
Download (187 KB)
MSDS
Download (73.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Unknown StatusSupportive CareDry Eyes1

Pharmacoeconomics

Manufacturers
  • Aton pharma inc
Packagers
  • Aton Pharma Inc.
  • Medisca Inc.
  • Merck & Co.
Dosage Forms
FormRouteStrength
InsertConjunctival5 mg/1
InsertOphthalmic5 mg / insert
InsertOphthalmic5 mg/1
PelletOphthalmic5 mg/1
Prices
Unit descriptionCostUnit
Lacrisert 60 5 mg Insert Box281.99USD box
Lacrisert 5 mg eye insert3.68USD insert
Hydroxypropylcellulose powd0.51USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Drug created at June 13, 2005 13:24 / Updated at August 14, 2022 00:07