Hypromellose

Identification

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Name
Hypromellose
Accession Number
DB11075
Type
Small Molecule
Groups
Approved
Description

Hypromellose, or hydroxypropyl methylcellulose (HPMC) 8, is a semisynthetic, inert, and viscoelastic polymer that forms a colloid solution when dissolved in water. It acts as a thickening agent, coating polymer, bioadhesive, solubility enhancer in solid dispersions, and binder in the process of granulation and in modified release formulations 2. It is a commonly used as a delivery component in oral pharmaceutical products that provides the release of a drug in a controlled fashion, effectively increasing the duration of release of a drug to prolong its therapeutic effects 1. Hypromellose is also found in eye drops as a lubricant 3.

Synonyms
  • Cellulose hydroxypropyl methyl ether
  • Cellulose, 2-hydroxypropyl methyl ether
  • Hipromelosa
  • Hydroxypropyl methylcellulose 2208
  • Hydroxypropyl methylcellulose 2910
  • Hydroxypropyl methylcellulose 4000
  • Hydroxypropyl methylcelluloses
  • Hydroxypropylmethylcellulose
  • Hypromellose
  • Hypromelloses
Product Ingredients
IngredientUNIICASInChI Key
Hypromellose 2208 (100 mpa.s)B1QE5P712KNot AvailableNot applicable
Hypromellose 2208 (15000 mpa.s)Z78RG6M2N2Not AvailableNot applicable
Hypromellose 2906 (4000 mpa.s)5EYA69XGATNot AvailableNot applicable
Hypromellose 2906 (50 mpa.s)612E703ZUQNot AvailableNot applicable
Hypromellose 2910 (15 mpa.s)36SFW2JZ0WNot AvailableNot applicable
Hypromellose 2910 (15000 mpa.s)288VBX44JCNot AvailableNot applicable
Hypromellose 2910 (3 mpa.s)0VUT3PMY82Not AvailableNot applicable
Hypromellose 2910 (4000 mpa.s)RN3152OP35Not AvailableNot applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EntrocelSolution18 mg/1mLOralMallinckrodt2009-06-012012-10-31Us
GoniotaireSolution25 mg/1mLOphthalmicAltaire Pharmaceuticals Inc.2002-01-18Not applicableUs
Mc Methylcellulose Solution 1%Solution1 gRectalE Z Em, Inc.1982-12-312009-08-04Canada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Artelac Lubricant Eye DropsSolution.32 %OphthalmicBausch & Lomb Inc2005-03-252008-07-28Canada
Corneo HypromelloseSolution0.3 %OphthalmicOrimed Pharma Corporation2015-09-16Not applicableCanada
GentealSolution3 mgOphthalmicNovartis1997-10-17Not applicableCanada
Genteal GelGel0.3 %OphthalmicAlcon, Inc.2002-10-232016-05-30Canada
GenTeal MildLiquid0.002 L/1LOphthalmicNovartis2009-09-14Not applicableUs
GenTeal Mild to ModerateLiquid0.003 L/1LOphthalmicNovartis2009-09-14Not applicableUs
GenTeal SevereGel.003 g/1gOphthalmicNovartis Pharmaceuticals Corporation2009-09-14Not applicableUs
GoniosoftLiquid25 mg/1mLOphthalmicO Cu Soft, Inc.1989-10-02Not applicableUs
Goniovisc Ophthalmic LubricantSolution / drops25 mg/1mLOphthalmicHub Pharmaceuticals2011-11-10Not applicableUs
HylaTearsLiquid3 mg/10mLOphthalmicHyalogic Llc2018-02-12Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Advanced Eye Relief/ Redness Maximum ReliefHypromellose (5 mg/1mL) + Naphazoline hydrochloride (0.3 mg/1mL)Solution / dropsOphthalmicPreferreed Pharmaceuticals Inc.2010-09-02Not applicableUs
Advanced Eye Relief/ Redness Maximum ReliefHypromellose (5 mg/1mL) + Naphazoline hydrochloride (0.3 mg/1mL)Solution / dropsOphthalmicBauch & Lomb Incorporated2010-09-02Not applicableUs
Artificial TearsHypromellose (0.002 mg/1mg) + Glycerin (0.002 mg/1mg) + Polyethylene glycol 400 (0.01 mg/1mg)Solution / dropsOphthalmicGeri-Care Pharmaceuticals, Corp2018-06-01Not applicableUs
Artificial TearsHypromellose (0.2 %) + Glycerin (0.2 %)SolutionOphthalmicTeva2011-04-19Not applicableCanada
Artificial TearsHypromellose (0.3 %) + Dextran (0.1 %)SolutionOphthalmicAlcon, Inc.2005-03-162009-02-24Canada
Artificial TearsHypromellose (2 mg/1mL) + Glycerin (2 mg/1mL) + Polyethylene glycol 400 (10 mg/1mL)LiquidOphthalmicAmerican Sales Company2010-09-06Not applicableUs
Bion TearsHypromellose 2910 (4000 mpa.s) (3 mg/1mL) + Dextran 70 (1 mg/1mL)Solution / dropsOphthalmicALCON LABORATORIES, INC.1992-10-19Not applicableUs
Bion Tears - Liq OphHypromellose (0.3 %) + Dextran 70 (0.1 %)Solution / dropsOphthalmicAlcon, Inc.1996-10-282016-10-20Canada
CAREALL Artifical TearsHypromellose (2 mg/1mL) + Glycerin (2 mg/1mL) + Polyethylene glycol 400 (10 mg/1mL)Solution / dropsOphthalmicNew World Imports, Inc2014-01-01Not applicableUs
CAREALL Lubricating Eye DropsHypromellose 2910 (4000 mpa.s) (.3 mg/1mL) + Dextran 70 (.1 mg/1mL)Solution / dropsOphthalmicNew World Imports2014-06-01Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
EntrocelHypromellose (18 mg/1mL)SolutionOralMallinckrodt2009-06-012012-10-31Us
Gonak HypromelloseHypromellose 2906 (4000 mpa.s) (25 mg/1mL) + Hypromellose 2906 (50 mpa.s) (25 mg/1mL)SolutionOphthalmicAkorn1997-01-01Not applicableUs
Gonak HypromelloseHypromellose 2906 (4000 mpa.s) (25 mg/1mL) + Hypromellose 2906 (50 mpa.s) (25 mg/1mL)SolutionOphthalmicAkorn1997-01-01Not applicableUs
GoniosoftHypromellose (25 mg/1mL)LiquidOphthalmicO Cu Soft, Inc.1989-10-02Not applicableUs
GoniotaireHypromellose 2906 (4000 mpa.s) (25 mg/1mL)SolutionOphthalmicAltaire Pharmaceuticals Inc.2002-01-18Not applicableUs
International/Other Brands
Hymelose / Hyprosol / Ikleen / Intavis / Irimist / Melose / Melose Drop / Methocel / Naifa / Optichlor / Takflur
Categories
UNII
3NXW29V3WO
CAS number
9004-65-3
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Protectant (ophthalmic) 4

Tears (artificial) 4

Lubricant (ophthalmic) 4

Diagnostic aid (contact lens procedures; gonioscopy) 4

Pharmacodynamics

Hypromellose is the most commonly used in hydrophilic matrix fabrication. It allows for controlled release of drug substances, increasing duration of therapeutic effects 3. The physical characteristics of this drug resemble natural tears, providing lubrication to the ocular surface and maintaining corneal hydration in dry eye syndromes 7.

Hypromellose is considered an inert substance as it has no direct pharmacological activity. The viscosity promoting properties of hypromellose prolong the retention time and improve adhesion of synthetic tears to the cornea and conjunctiva. As a result, the tear film breakdown time is prolonged and/or the tear film stability is enhanced. A stable tear film protects the cornea from dryness and epithelial cells 6.

Hypromellose is a methyl and hydroxypropyl mixed ether of cellulose. It is utilized as artificial tears to prevent conjunctival and corneal damage due to impaired lacrimal secretions. It is also used as a visco-elastic promoting agent by maintaining a deep, viscous chamber and allowing for easier manipulation, helping the vitreous surface to be pushed back, thus preventing the formation of a postoperative flat chamber 5.

Mechanism of action

Promotes corneal wetting by the stabilization and thickening the precorneal tear film and prolonging the tear film breakdown time, which is usually shortened in dry eye conditions. Hypromellose also acts to lubricate and protect the eye 6.

The surface active properties of the vehicles found in artificial tears solutions act to stabilize the tear film and increase tear viscosity to prevent delay tear evaporation and delay tear drainage 4.

In the intact eye, the corneal surface is moistened primarily by the mucin that is produced in the conjunctiva. Mucin is adsorbed on the corneal surface and forms a hydrophilic surface. This creates a moisture barrier. In the typical dry eye, and particularly in case of mucin deficiency, the application of artificial tear fluid is highly recommended. Both its surface activity and its adsorptive capacity make hypromellose optimal for this use. Hypromellose has a physical-chemical action and leads to, in an aqueous solution, a reduced surface tension as well as an increased level of viscosity. Hypromellose adheres well to the cornea and conjunctiva and provides ample moisture. Irritation symptoms caused by blinking, which occur in the case of tear fluid deficiency, are therefore decreased and symptoms of epithelial desiccation are also alleviated 6.

TargetActionsOrganism
UEpithelial cell adhesion moleculeNot AvailableHumans
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Not systemically absorbed 6.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity

LD 50 (Rat): > 5 g/kg MSDS.

Hypromellose is considered low toxicity to non-toxic 8.

Adverse events may include blurred vision and contact dermatitis 4. Hypersensitivity and intolerance reactions may occur (for example, eye burning, pain, increased lacrimation, a sensation of foreign body, conjunctival hyperemia, eyelid swelling, pruritus). The stickiness sensation of the eyelids, the decreased sense of smell, photosensitivity 6.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Li CL, Martini LG, Ford JL, Roberts M: The use of hypromellose in oral drug delivery. J Pharm Pharmacol. 2005 May;57(5):533-46. [PubMed:15901342]
  2. Al-Tabakha MM: HPMC capsules: current status and future prospects. J Pharm Pharm Sci. 2010;13(3):428-42. [PubMed:21092714]
  3. BION TEARS [Link]
  4. Hypromellose [Link]
  5. MIMS Hypromellose [Link]
  6. SUMMARY OF PRODUCT CHARACTERISTICS [Link]
  7. SUMMARY PRODUCT ASSESSMENT [Link]
  8. Hydroxypropyl methyl cellulose [Link]
External Links
PubChem Substance
347911105
Wikipedia
Hypromellose
ATC Codes
S01KA02 — Hypromellose
AHFS Codes
  • 52:13.00* — Artificial Tears
  • 52:92.00 — EENT Drugs, Miscellaneous
  • 36:89.00* — Other Diagnostics
MSDS
Download (229 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentDry Eye Syndrome (DES)1
2CompletedTreatmentConjunctivitis, Seasonal Allergic1
2CompletedTreatmentEye Dryness1
2CompletedTreatmentMacular Edema (ME) / Retinopathy, Diabetic1
2RecruitingTreatmentHerpes Zoster Keratitis1
2RecruitingTreatmentThyroid Eye Disease1
2TerminatedTreatmentDry Eye Syndromes1
2, 3CompletedTreatmentConjunctivitis, Viral1
3CompletedTreatmentConjunctivitis, Viral1
3CompletedTreatmentExfoliation Syndrome / Glaucoma, Primary Open Angle (POAG)1
3CompletedTreatmentEye Dryness2
3Unknown StatusTreatmentAdenovirus / Conjunctivitis1
4CompletedNot AvailableEndothelial Graft Rejection1
4CompletedNot AvailableEye Dryness1
4CompletedNot AvailableMyopia1
4CompletedPreventionChronic Allergic Conjunctivitis1
4CompletedPreventionConjunctivitis, Seasonal Allergic1
4CompletedTreatmentAnterior Uveitis (AU) / Cystoid Macular Edema1
4CompletedTreatmentConjunctivitis, Seasonal Allergic4
4CompletedTreatmentCorneal Edema / Intraocular Pressure1
4CompletedTreatmentCorneal Epithelium Defect1
4CompletedTreatmentDry Eye Syndrome (DES)1
4CompletedTreatmentDry Eye Syndromes2
4CompletedTreatmentEye Dryness3
4CompletedTreatmentGlaucoma1
4CompletedTreatmentGlaucoma, Primary Open Angle (POAG) / Ocular Hypertension1
4CompletedTreatmentGlaucoma / Ocular Hypertension3
4CompletedTreatmentKeratoconjunctivitis Due to Adenovirus / Viral Shedding1
4CompletedTreatmentOpen-angle Glaucoma (OAG)1
4Unknown StatusDiagnosticEye Dryness1
4Unknown StatusTreatmentEye Dryness1
4WithdrawnTreatmentDry Eye Syndrome (DES)1
Not AvailableCompletedPreventionEye Dryness1
Not AvailableCompletedSupportive CarePain NOS2
Not AvailableCompletedTreatmentDry Eye Syndrome (DES)3
Not AvailableCompletedTreatmentEye Dryness1
Not AvailableCompletedTreatmentEye Dryness / Lipid Layer / Liposic / Tear Film / Tears Naturale Forte1
Not AvailableCompletedTreatmentGlaucoma1
Not AvailableCompletedTreatmentGlaucoma, Primary Open Angle (POAG) / Pseudoexfoliation Syndrome1
Not AvailableCompletedTreatmentIntraocular Pressure1
Not AvailableCompletedTreatmentKeratoconjunctivitis Sicca1
Not AvailableRecruitingSupportive CarePain NOS1
Not AvailableRecruitingTreatmentAdenoviral Conjunctivitis / Conjunctivitis1
Not AvailableRecruitingTreatmentAge-related Cataract1
Not AvailableRecruitingTreatmentEye Dryness1
Not AvailableRecruitingTreatmentMeibomian Gland Dysfunction (MGD) / Sjögren's Syndrome2
Not AvailableTerminatedTreatmentMigraine1
Not AvailableUnknown StatusTreatmentGlaucoma / Ocular Surface Disease1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
SolutionOphthalmic.32 %
SolutionOphthalmic
LiquidOphthalmic
SolutionOphthalmic0.3 %
SolutionOral18 mg/1mL
SolutionOphthalmic3 mg
GelOphthalmic0.3 %
LiquidOphthalmic0.002 L/1L
LiquidOphthalmic0.003 L/1L
GelOphthalmic
GelOphthalmic.003 g/1g
LiquidOphthalmic25 mg/1mL
SolutionOphthalmic25 mg/1mL
Solution / dropsOphthalmic25 mg/1mL
LiquidOphthalmic3 mg/10mL
SolutionOphthalmic5 mg/1mL
Solution / dropsOphthalmic1 %
Solution / dropsOphthalmic0.5 %
SolutionRectal1 g
Solution / dropsOphthalmic
Solution / dropsOphthalmic4 mg/1mL
Kit; solutionIntraocular; Irrigation
Solution / dropsOphthalmic; Topical3 mg/1mL
LiquidOphthalmic3.5 mg/1mL
Solution / dropsOphthalmic10 mg
GelOphthalmic3 mg/1g
Solution / dropsOphthalmic17 mg/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
PropertyValueSource
water solubilitySoluble https://www.sigmaaldrich.com/catalog/product/usp/1330005?lang=en®ion=CA
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein complex binding
Specific Function
May act as a physical homophilic interaction molecule between intestinal epithelial cells (IECs) and intraepithelial lymphocytes (IELs) at the mucosal epithelium for providing immunological barrier...
Gene Name
EPCAM
Uniprot ID
P16422
Uniprot Name
Epithelial cell adhesion molecule
Molecular Weight
34932.005 Da
References
  1. Geerling G, Daniels JT, Dart JK, Cree IA, Khaw PT: Toxicity of natural tear substitutes in a fully defined culture model of human corneal epithelial cells. Invest Ophthalmol Vis Sci. 2001 Apr;42(5):948-56. [PubMed:11274071]

Drug created on December 03, 2015 09:51 / Updated on July 16, 2019 06:23