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Lactitol monohydrate

Alias: Lactitol monohydrate; D-Lactitol monohydrate; Lactitol (monohydrate); Lactitol hydrate; UH2K6W1Y64; DTXSID6047028
Cat No.:V29230 Purity: ≥98%
Lactitol monohydrate (CCRIS6315; Lactit;Lactosit Miruhen; NSC-231323;pizensy), the monohydrated form of lactitol and a disaccharide analogue of lactulose, is a naturally occuring sweetener and gastrointestinal agent as well asan osmotic laxative used for the treatment of chronic idiopathic constipation (CIC) in adults.
Lactitol monohydrate
Lactitol monohydrate Chemical Structure CAS No.: 81025-04-9
Product category: Bacterial
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
5g
10g
Other Sizes

Other Forms of Lactitol monohydrate:

  • Lactitol
Official Supplier of:
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Product Description
Lactitol monohydrate (CCRIS6315; Lactit; Lactosit Miruhen; NSC-231323; pizensy), the monohydrated form of lactitol and a disaccharide analogue of lactulose, is a naturally occuring sweetener and gastrointestinal agent as well as an osmotic laxative used for the treatment of chronic idiopathic constipation (CIC) in adults. It was approved in 2020 for medical uses as an oral solution to help produce bowel movements. In addition, it is also a reduced calorie sweetener derived from natural milk sugar, and has been used in a various sweetening applications.
Lactitol monohydrate (CAS 81025-04-9) is a disaccharide analogue of lactulose. It is a sugar alcohol used as a replacement sweetener in low-fat foods, sugar-free candies, cookies, chocolate, and ice cream. Clinically, Lactitol has been investigated for use as an osmotic laxative and, along with other non-absorbable disaccharides such as lactulose, in the treatment of hepatic encephalopathy in patients with cirrhosis. It was approved in 2020 for medical use as an oral solution to help produce bowel movements, specifically for the treatment of chronic idiopathic constipation (CIC) in adults.
Biological Activity I Assay Protocols (From Reference)
Targets
Lactitol monohydrate does not have a classic "target" in the sense of a receptor or enzyme. Its mechanism of action is osmotic. As a non-absorbable disaccharide, it is not digested in the small intestine and passes into the colon, where it is fermented by colonic bacteria. This fermentation produces short-chain fatty acids and gases, which lower the colonic pH and increase osmotic pressure. The resulting osmotic gradient draws water into the intestinal lumen, softening the stool and stimulating peristalsis, thereby producing a laxative effect. In hepatic encephalopathy, its mechanism involves acidifying the colonic contents, which traps ammonia (NH3) as ammonium (NH4+), reducing its absorption and thereby lowering systemic ammonia levels.
ln Vitro
In vitro, Lactitol monohydrate is used as a research tool to study osmotic effects and the metabolism of non-absorbable sugars. It is not typically used in cell-based assays for pharmacological activity, as its primary mechanism is physical and osmotic rather than receptor-mediated. Its stability and lack of metabolism in the small intestine are key properties that make it effective as an osmotic laxative.
ln Vivo
In vivo, Lactitol monohydrate is an effective osmotic laxative used for the treatment of chronic idiopathic constipation (CIC). It is also used in the management of hepatic encephalopathy. Its efficacy in these conditions is well-documented in clinical studies. It produces bowel movements by drawing water into the intestines, softening the stool, and stimulating peristalsis. Its effects are mild and generally occur within 24 to 48 hours after oral administration.
Enzyme Assay
For in vitro assays, the primary studies involving Lactitol monohydrate focus on its stability and lack of metabolism. It is not used in standard cell-free enzyme/receptor binding assays, as its mechanism of action is osmotic. However, its fermentation by colonic bacteria can be studied in vitro using anaerobic culture systems to measure gas production and changes in pH.
Cell Assay
Lactitol monohydrate is not typically used in standard cell-based pharmacological assays, as its mechanism of action is physical and osmotic. However, its effect on intestinal epithelial cells can be studied in vitro by measuring changes in cell volume or ion transport in response to osmotic stress. Its lack of cellular toxicity is often confirmed in such studies.
Animal Protocol
In vivo efficacy is evaluated in animal models of constipation or in clinical trials. In animal models, the compound is administered orally, and endpoints include time to first bowel movement, stool frequency, stool consistency, and intestinal transit time. In clinical studies, its efficacy as a laxative is assessed by patient-reported outcomes, such as the number of complete spontaneous bowel movements per week.
ADME/Pharmacokinetics
Lactitol monohydrate has a molecular formula of C12H24O11·H2O and a molecular weight of 362.33 g/mol. Its CAS number is 81025-04-9. It is a white, crystalline powder that is highly soluble in water. It is stable and can be stored at room temperature. Its purity is typically >98%.
Toxicity/Toxicokinetics
Lactitol monohydrate has a very low toxicity profile. As a non-absorbable sugar alcohol, it is generally well-tolerated. The most common side effects are gastrointestinal, including flatulence, abdominal cramping, and diarrhea, particularly at higher doses. These effects are generally mild and transient. No significant systemic toxicity has been reported.
References

[1]. Continuous combined intake of polydextrose and lactitol stimulates cecal fermentation and salivary IgA secretion in rats. J Oral Sci. 2017;59(4):603-610.

[2]. Lactitol or lactulose in the treatment of chronic constipation: result of a systematic. J Indian Med Assoc. 2010 Nov;108(11):789-92./a >

Additional Infomation
See also: lactitol (note moved to).
Lactitol monohydrate is an FDA-approved medical food and over-the-counter laxative for the treatment of chronic idiopathic constipation. It is marketed under the brand name Pizensy. It is also used as a food additive and sugar substitute. Its mechanism of action involves its osmotic effect in the colon. It is not a drug in the traditional sense but a medical food and laxative.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H26O12
Molecular Weight
362.33
Exact Mass
362.142
CAS #
81025-04-9
Related CAS #
Lactitol;585-86-4
PubChem CID
3067270
Appearance
White to off-white solid powder
Density
1.69 g/cm3
Boiling Point
788.5ºC at 760 mmHg
Melting Point
95-98ºC
Flash Point
430.7ºC
Index of Refraction
1.634
Hydrogen Bond Donor Count
10
Hydrogen Bond Acceptor Count
12
Rotatable Bond Count
8
Heavy Atom Count
24
Complexity
343
Defined Atom Stereocenter Count
9
SMILES
O([C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1)[C@H]([C@H](O)CO)[C@H](O)[C@@H](O)CO.O
InChi Key
LXMBXZRLTPSWCR-XBLONOLSSA-N
InChi Code
InChI=1S/C12H24O11.H2O/c13-1-4(16)7(18)11(5(17)2-14)23-12-10(21)9(20)8(19)6(3-15)22-12;/h4-21H,1-3H2;1H2/t4-,5+,6+,7+,8-,9-,10+,11+,12-;/m0./s1
Chemical Name
(2S,3R,4R,5R)-4-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyhexane-1,2,3,5,6-pentol;hydrate
Synonyms
Lactitol monohydrate; D-Lactitol monohydrate; Lactitol (monohydrate); Lactitol hydrate; UH2K6W1Y64; DTXSID6047028
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)
Solubility Data
Solubility (In Vitro)
H2O : ~120 mg/mL (~331.19 mM)
DMSO : ~100 mg/mL (~275.99 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 25 mg/mL (69.00 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7599 mL 13.7996 mL 27.5991 mL
5 mM 0.5520 mL 2.7599 mL 5.5198 mL
10 mM 0.2760 mL 1.3800 mL 2.7599 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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