Boric acid

Identification

Name
Boric acid
Accession Number
DB11326
Type
Small Molecule
Groups
Approved
Description

Boric acid, also known as hydrogen borate, is a weak monobasic Lewis acid of boron with the chemical formula H3BO3. Boric acid is typically utilized in industrial processing and manufacturing, but is also used as an additive in pharmaceutical products, cosmetics, lotions, soaps, mouthwash, toothpaste, astringents, and eyewashes [4]. It is known to exhibit some antibacterial activity against infections such as bacterial vaginosis and candidiasis [1].

Structure
Thumb
Synonyms
  • ácido bórico
  • boracic acid
  • hydrogen borate
  • orthoboric acid
External IDs
E-284 / INS NO.284 / INS-284 / NSC-81726
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Acide BoriquePowderTopicalProduits Marc O (1987) Inc., Division Of Technilab Inc.1951-12-312000-08-24Canada
Boracic Acid PwrPowderTopicalStanley Pharmaceuticals, A Division Of Vita Health Products Inc.1972-12-312000-07-27Canada
Boric AcidPowder, for solutionTopicalDawson Traders Ltd.1985-12-312006-03-22Canada
Boric Acid Pwr 100%Powder100 %Nasal; Ophthalmic; TopicalRegal Pharms, Division Of Bradcan Corporation1978-12-311998-07-29Canada
Boric Acid Solution 2.5%Lotion2.5 %OphthalmicEverest Pharmaceuticals Ltd.1982-12-311999-07-14Canada
Eye Wash 2.5%Liquid2.5 %OphthalmicCanadian Custom Packaging Company1983-12-312009-07-06Canada
EyewashLiquid1.2 %OphthalmicRivex Ophthalmics Inc.1997-08-052000-08-03Canada
Gynox-softEmulsion7 mg/100mLTopicalSpai Sons Pharmaceutical International Cosmetics2012-06-30Not applicableUs
R.O.-eyewashLiquid1.2 %OphthalmicRichmond Pharmaceuticals1992-12-311997-08-11Canada
See Clean-One Eye DropsLiquid21.644 mg/14mLOphthalmicCho-A Pharm.Co.,Ltd.2017-12-29Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
British Army Foot PwrBoric acid (6 mg) + Formaldehyde (.75 mg) + Salicylic acid (3 mg) + Zinc oxide (6 mg)PowderTopicalRegal Pharms, Division Of Bradcan Corporation1980-12-312001-07-11Canada
Collyre Hygienique SokerBoric acid (11.1 mg) + Sodium borate (1.89 mg)LiquidOphthalmicProduits Francais Labs Inc.1978-12-311997-05-30Canada
Eye EzeBoric acid (1.11 %) + Sodium borate (.18 %)LiquidOphthalmicPharmavite Laboratories (1987) Inc.1958-12-312006-07-27Canada
Hemorro-dol SupBoric acid (226.7 mg) + Balsam of Peru (22.6 mg) + Belladonna (11.25 mg) + Benzocaine (50 mg) + Bismuth subcarbonate (86.4 mg) + Bismuth subnitrate (37.8 mg) + Ephedrine sulfate (2.5 mg) + Zinc oxide (226.7 mg)SuppositoryRectalProduits Francais Labs Inc.1981-12-311997-05-30Canada
Occu-cal DropsBoric acid (11.16 mg) + Phenylephrine hydrochloride (.2 mg) + Sodium borate (1.9 mg)Solution / dropsOphthalmicProduits Francais Labs Inc.1981-12-311997-05-30Canada
Occu-cal LotionBoric acid (11.1 mg) + Phenylephrine hydrochloride (.01 mg) + Sodium borate (1.896 mg)LotionOphthalmicProduits Francais Labs Inc.1981-12-311997-05-30Canada
Sha-lemBoric acid (0.95 g/30mL) + Bismuth subcarbonate (1.89 g/30mL) + Oleic Acid (14.5 g/30mL) + Palmitic Acid (7.25 g/30mL) + Stearic acid (7.25 g/30mL)OintmentTopicalShalem Products, Inc.1992-05-08Not applicableUs
Super SepticBoric acid (2 %) + Ethanol (40 %)LiquidTopicalEars R in Co Inc.1979-12-311999-07-13Canada
Thunas Eye DropsBoric acid (11.16 mg) + Sodium borate (1.9 mg)Solution / dropsOphthalmicThuna Herbal Remedies Ltd.1979-12-312002-10-16Canada
Trimo San Deodorant Vaginal JellyBoric acid (1.0 %) + Oxyquinoline sulfate (0.025 %) + Sodium borate (0.7 %)JellyVaginalMilex Products Ltd.1979-12-312005-07-25Canada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Recal DBoric acid (250 ug/1) + Calcium Carbonate (1342 mg/1) + Cholecalciferol (300 [iU]/1) + Cyanocobalamin (125 ug/1) + Folic Acid (1 mg/1) + Magnesium oxide (50 mg/1) + Pyridoxine hydrochloride (10 mg/1)WaferOralRiver's Edge Pharmaceuticals, LLC2009-01-142012-10-31Us
Categories
UNII
R57ZHV85D4
CAS number
10043-35-3
Weight
Average: 61.833
Monoisotopic: 62.017524428
Chemical Formula
BH3O3
InChI Key
KGBXLFKZBHKPEV-UHFFFAOYSA-N
InChI
InChI=1S/BH3O3/c2-1(3)4/h2-4H
IUPAC Name
boric acid
SMILES
OB(O)O

Pharmacology

Indication

No FDA- or EMA-approved therapeutic indications on its own.

Pharmacodynamics

Boric acid exhibits minimal bacteriostatic and antifungal activities [4]. Boric acid is likely to mediate antifungal actions at high concentrations over prolonged exposures [3].

Mechanism of action

Information regarding the mechanism of action of boric acid in mediating its antibacterial or antifungal actions is limited. Boric acid inhibits biofilm formation and hyphal transformation of Candida albicans, which are critical virulence factors [3]. In addition, arrest of fungal growth was observed with the treatment of boric acid [3].

Absorption

Boric acid is well absorbed from the gastrointestinal tract, open wounds, and serous cavities but displays limited absorption in intact skin [4]. Following intraperitoneal injection in mice, the peak concentration was reached in about 1.0-1.5 hr in the brain whereas the value was 0.5 hr in other tissues [4].

Volume of distribution

Volume of distribution ranges from 0.17 to 0.5 L/kg in humans, where large amounts of boric acid are localized in brain, liver, and kidney [4].

Protein binding

No protein binding reported.

Metabolism

No metabolic pathways reported.

Route of elimination

Regardless the route of administration, boric acid predominantly undergoes rapid renal excretion of >90% of total administered dose as unchanged form. Small amounts are also excreted into sweat, saliva, and feces. Following administration as ointment, urinary excretion of boric acid accounted for only 1% of the administered dose [4].

Half life

According to human cases of poisoning, the elimination half-life of boric acid ranges from 13 to 24 hours [2, 4].

Clearance

A case report of acute boric acid poisoning following oral ingestion of 21 g of boric acid presents the total body clearance of 0.99 L/h before hemodialysis [2].

Toxicity

Acute oral LD50 is 2660 mg/kg in rat [MSDS]. Individuals are likely to be exposed to boric acid from industrial manufacturing or processing. Local tissue injury from boric acid exposure is likely due to caustic effects. Systemic effects from boric acid poisoning usually occur from multiple exposures over a period of days and involve gastrointestinal, dermal, CNS, and renal manifestations. Gastrointestinal toxicity include persistent nausea, vomiting, diarrhea, epigastric pain, hematemesis, and blue-green discoloration of the feces and vomit [4]. Following the onset of GI symptoms, a characteristic intense generalized erythroderma follows [4]. Management of mild to moderate toxicity should be supportive. In case of severe toxicity, dialysis may be required in addition to supportive treatment.

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. Iavazzo C, Gkegkes ID, Zarkada IM, Falagas ME: Boric acid for recurrent vulvovaginal candidiasis: the clinical evidence. J Womens Health (Larchmt). 2011 Aug;20(8):1245-55. doi: 10.1089/jwh.2010.2708. Epub 2011 Jul 20. [PubMed:21774671]
  2. Teshima D, Morishita K, Ueda Y, Futagami K, Higuchi S, Komoda T, Nanishi F, Taniyama T, Yoshitake J, Aoyama T: Clinical management of boric acid ingestion: pharmacokinetic assessment of efficacy of hemodialysis for treatment of acute boric acid poisoning. J Pharmacobiodyn. 1992 Jun;15(6):287-94. [PubMed:1432568]
  3. De Seta F, Schmidt M, Vu B, Essmann M, Larsen B: Antifungal mechanisms supporting boric acid therapy of Candida vaginitis. J Antimicrob Chemother. 2009 Feb;63(2):325-36. doi: 10.1093/jac/dkn486. Epub 2008 Dec 4. [PubMed:19059942]
  4. BORIC ACID - National Library of Medicine HSDB Database- Toxnet - NIH [Link]
  5. Boric Acid - National Toxicology Program - NIH [Link]
External Links
Human Metabolome Database
HMDB0035731
KEGG Compound
C12486
PubChem Compound
7628
PubChem Substance
347827967
ChemSpider
7346
BindingDB
39817
ChEBI
33118
ChEMBL
CHEMBL42403
HET
BO3
Wikipedia
Boric_acid
ATC Codes
S02AA03 — Boric acid
PDB Entries
1a95 / 1a96 / 1a97 / 1e3j / 1oj7 / 1s3t / 2j9t / 2y8s / 2y8t / 3r2v
show 13 more
MSDS
Download (49 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2Not Yet RecruitingTreatmentDermatitis, Eczematous1
2, 3CompletedTreatmentBacterial Vaginosis (BV)1
2, 3CompletedTreatmentChronic Periodontitis With Mandibular Degree 2 Furcation Defects1
4CompletedTreatmentEndocrine ophthalmopathy1
Not AvailableCompletedTreatmentOtomycosis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
PowderTopical
Powder, for solutionTopical
PowderNasal; Ophthalmic; Topical100 %
LotionOphthalmic2.5 %
PowderTopical
LiquidOphthalmic
LiquidOphthalmic2.5 %
EmulsionTopical7 mg/100mL
SuppositoryRectal
LotionOphthalmic
LiquidOphthalmic1.2 %
WaferOral
LiquidOphthalmic21.644 mg/14mL
OintmentTopical
LiquidTopical
Solution / dropsOphthalmic
JellyVaginal
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)169MSDS
boiling point (°C)300MSDS
water solubilitySoluble in hot water, partially soluble in cold waterMSDS
Predicted Properties
PropertyValueSource
logP-0.51ChemAxon
pKa (Strongest Acidic)8.7ChemAxon
pKa (Strongest Basic)-5.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area60.69 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity7.69 m3·mol-1ChemAxon
Polarizability5.15 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of inorganic compounds known as miscellaneous borates. These are inorganic compounds in which the largest metallic oxoanion is borate, to which either no atom or a non metal atom is bonded.
Kingdom
Inorganic compounds
Super Class
Mixed metal/non-metal compounds
Class
Miscellaneous mixed metal/non-metals
Sub Class
Miscellaneous metallic oxoanionic compounds
Direct Parent
Miscellaneous borates
Alternative Parents
Metalloid salts / Inorganic salts
Substituents
Borate / Inorganic salt / Inorganic metalloid salt
Molecular Framework
Not Available
External Descriptors
boric acids (CHEBI:33118) / an anion (BORATE)

Drug created on December 03, 2015 09:52 / Updated on November 03, 2018 15:39