Sodium tetraborate decahydrate could be utilized as pharmaceutical excipients, such as preservatives and mordants. Pharmaceutical excipients or pharmaceutical auxiliaries refer to other chemical substances other than drug ingredients used in the pharmaceutical process. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients can also affect the absorption, distribution, metabolism, and elimination (ADME) processes of concomitant medications.

Physicochemical Properties

Molecular Formula	B4H20NA2O17
Molecular Weight	381.37
Exact Mass	382.086
CAS #	1303-96-4
PubChem CID	16211214
Appearance	White, monoclinic crystals Hard crystals, granules or crystalline powder; efflorescent in dry air, the crystals often being coated with white powder Crystalline granules or crystalline powder White, crystalline solid [Note: Becomes anhydrous at 608 degrees F]
Density	1.73 g/mL at 25 °C(lit.)
Boiling Point	320°C
Melting Point	75 °C
Hydrogen Bond Donor Count	10
Hydrogen Bond Acceptor Count	17
Rotatable Bond Count	0
Heavy Atom Count	23
Complexity	121
Defined Atom Stereocenter Count	0
SMILES	B1([O-])OB2OB([O-])OB(O1)O2.[Na+].[Na+].O.O.O.O.O.O.O.O.O.O
InChi Key	CDMADVZSLOHIFP-UHFFFAOYSA-N
InChi Code	InChI=1S/B4O7.2Na.10H2O/c5-1-7-3-9-2(6)10-4(8-1)11-3;;;;;;;;;;;;/h;;;10*1H2/q-2;2*+1;;;;;;;;;;
Chemical Name	disodium;3,7-dioxido-2,4,6,8,9-pentaoxa-1,3,5,7-tetraborabicyclo[3.3.1]nonane;decahydrate
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ADME/Pharmacokinetics	Absorption, Distribution and Excretion A 1 mL oral dose of borax solution was given orally to male Wistar rats at eleven concentrations (0, 100, 200, 300, 400, 500, 600, 700, 800, 900, 1000 mg boron/L). Twenty four hour urine samples were analyzed and the reported recovery was 99.6 +/- 7.9%. These compounds /boric acid and borax/ may enter body by inhalation, ingestion or by skin absorption through mucous membranes or skin burns. Absorption through damaged skin is rapid and almost complete; absorption also occurs through undamaged skin but not to sufficient extent to cause poisoning. Following absorption, there is a rise in concentration of boron in cerebrospinal fluid, but highest concentrations are found in brain tissues, liver and adipose tissue. Repeated doses have cumulative effect with retention ... greatest in bone tissue. ... Elimination is mainly in urine but also to a lesser extent in feces, milk and sweat. ... Absorption and transportation greatest via roots; moves to growing parts of plant. In a carefully conducted human in vivo study, found that only 0.23, 0.21, and 0.12% of a saturated dose of boric acid, borax, and disodium octaborate tetrahydrate, respectively were absorbed. For more Absorption, Distribution and Excretion (Complete) data for BORAX (9 total), please visit the HSDB record page. Biological Half-Life ... Readily absorbed from the gastrointestinal tract and excreted in the urine with a half-life of about 24 hours. ... A group of rats (n = 10) was dosed intravenously with borax at 0.4 mg boron/100 g of body weight. The following kinetic parameters were reported: elimination half life was 4.64 hr; total clearance was 0.359 mL/min per 100 g body weight.
Toxicity/Toxicokinetics	Interactions Alteration of borate toxicity has been demonstrated in young, 4 to 6 wk old mice by simultaneous administration of d-glucose with borax. Least toxic were molar ratios of 1:1.5 and 1:2 borax-d-glucose, which reduced mortality from 100% to 45 and 37.5% ... Borax ... complexes with polyhydroxy compounds in aqueous solution, resulting in altered toxicities. Non-Human Toxicity Values LD50 Rat oral 396-689 mg boron/kg LD50 Rat oral 5.66 g/kg (SRP: 5,660 mg/kg) LD50 Mouse oral 2000 mg/kg LD50 Mouse ip 2711 mg/kg For more Non-Human Toxicity Values (Complete) data for BORAX (12 total), please visit the HSDB record page.
References	[1]. Pharmaceutical excipients - quality, regulatory and biopharmaceutical considerations. Eur J Pharm Sci. 2016 May 25;87:88-99.
Additional Infomation	Borax is a mineral with formula of Na2B4O5(OH)4·8H2O. The IMA symbol is Brx. See also: Sodium Borate (annotation moved to). Therapeutic Uses Borax has a feeble bacteriostatic action similar to that of boric acid. It is not used internally. Applied externally it is mildly astringent and was formerly used as a gargle or mouthwash in the treatment of aphthous ulcers and stomatitis, as a lotion in bromidrosis and inflammatory conditions of the eye, and as a nasal douche. Borax Glycerin and Honey of Borax were formerly used as paints for the throat and tongue and to alleviate dryness of mouth but excessive use may cause toxic effects, they should not be used. /Borax Glycerin and Honey of Borax/ Borax was used for treatment of 31 patients suffering from skeletal fluorosis. The amount administered was gradually increased from 300-1100 mg/day during a three month period, with one week resting period each month. Experimental criteria included observation of symptoms, of physical signs such as movement of joints, and urinary excretion of fluoride and boron tetrafluoride. Findings in patients given borax were compared with data obtained from controls to whom no borax was administered. Borax appeared to be effective. Clinically, sodium borate and boric acid have been used as irrigants, dressings, antiseptics, buffers, and preservatives. EXPTL THER: Sodium borate and boric acid are used or have been tested for medical purposes in many foreign countries. /In Japan,/... 5% sodium borate is sprayed on the skin following application of analgesic agents to form a transparent, flexible, water-resistant film. ...In India, a formulation of "indigenous Indian drugs" and 25% sodium borate is reported to be a long-acting (4 months) oral contraceptive; it has been reported that the drug acts by inhibiting endometrial alkaline phosphatase and preventing ovum implantation. ...In Russia, sodium borate is administered orally to patients with hepatocerebral dystrophy to remove accumulated pathological quantities of copper from the body. Drug Warnings Borax and boric acid used in powders and ointments have resulted in serious poisonings and death.

Solubility Data

Solubility (In Vitro)

H2O: 50 mg/mL (131.11 mM)

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6221 mL	13.1106 mL	26.2213 mL
	5 mM	0.5244 mL	2.6221 mL	5.2443 mL
	10 mM	0.2622 mL	1.3111 mL	2.6221 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.