Hydroxypropyl cellulose

Identification

Name
Hydroxypropyl cellulose
Accession Number
DB00840  (APRD01023)
Type
Small Molecule
Groups
Approved
Description

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.

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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LacrisertPellet5 mg/1OphthalmicAton Pharma, Inc.1981-06-012016-10-13Us
LacrisertPellet5 mg/1OphthalmicBauch & Lomb Incorporated1981-06-01Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LacrisertInsert5 mgOphthalmicAton Pharma Inc Division Of Valeant Pharmaceuticals North America Llc2004-05-25Not applicableCanada
International/Other Brands
A-Gel (Fresenius Kabi)
Categories
UNII
9XZ8H6N6OH
CAS number
9004-64-2
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

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.

Structured Indications
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
Toxicity

LD50=10200 mg/kg (oral, rat)

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
No interactions found.
Food Interactions
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. [PubMed:21178699]
  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. [PubMed:20858108]
  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. [PubMed:20847657]
External Links
KEGG Drug
D01536
PubChem Substance
46508483
ChEMBL
CHEMBL1201471
PharmGKB
PA164746492
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Hydroxypropyl_cellulose
AHFS Codes
  • 52:13.00* — Artificial Tears
FDA label
Download (187 KB)
MSDS
Download (73.5 KB)

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
  • Aton pharma inc
Packagers
Dosage forms
FormRouteStrength
InsertOphthalmic5 mg
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

Taxonomy

Classification
Not classified

Drug created on June 13, 2005 07:24 / Updated on December 10, 2017 17:18