LACTITOL MONOHYDRATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C12H24O11.H2O
Molecular Weight	362.3276
Optical Activity	UNSPECIFIED
Defined Stereocenters	9 / 9
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.OC[C@H](O)[C@@H](O)[C@H](O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O)[C@H](O)CO

InChI

InChIKey=LXMBXZRLTPSWCR-XBLONOLSSA-N

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

HIDE SMILES / InChI

Description
Sources: http://www.angelini.it/wps/wcm/connect/it/home/prodotti/farmaci/portolac-polvere-10g
Curator's Comment: description was created based on several sources, including: https://health.mail.ru/drug/importal_n/ | http://www.druginfosys.com/drug.aspx?drugcode=2283&type=1 | https://medikamio.com/fr-ch/medicaments/importal-sachets-de-poudre-10-g/pil | http://www.tabletwise.com/medicine/lactitol-monohydrate

Lactitol is a sugar alcohol. This ingredient has been determined to be GRAS for specified uses as a direct food additive and foods containing lactitol are eligible for a health claim related to dental caries. Lactitol is used as an oral powder or solution in the management of hepatic encephalopathy and in case of short-term treatment of occasional constipation. Intestinal flora of large intestine is metabolize lactitol to low-molecular organic acid, which leads to an increase in osmotic pressure in intestine, increase in volume of fecal masses bowel function normalization. This drug might cause abdominal discomfort, especially flatulence and abdominal pain rarely or sometimes abdominal distension. These effects tend to diminish or disappear after a few days of regular intake of the drug. Since 'antacids and neomycin can neutralize ' acidifying effect of lactitol on stool, they should not be co-administered with lactitol in cirrhotic patients with hepatic encephalopathy; however both substances do not alter the 'laxative effect in patients with constipation.

Originator

Approval Year

Conditions

Condition	Modality	Targets	Highest Phase	Product
Constipation 112 Sources: https://medikamio.com/fr-ch/medicaments/importal-sachets-de-poudre-10-g/pil http://en.pharmacodia.com/web/drug/1_11996.html	Primary		Approved 8429	Importal Approved Use It is recommended for the treatment of occasional constipation, stool regulation and chronic hepatic encephalopathy.
Hepatic encephalopathy 5 Sources: https://health.mail.ru/drug/importal_n/ https://www.ncbi.nlm.nih.gov/pubmed/7569287	Primary		Approved 8429	Importal Approved Use It is recommended for the treatment of occasional constipation, stool regulation and chronic hepatic encephalopathy.

C_max

Value	Dose	Analyte	Population
776 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	20 g single, oral dose: 20 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
2780 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211281Orig1s000MultidisciplineR.pdf	21 g single, oral dose: 21 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
776 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211281Orig1s000MultidisciplineR.pdf	21 g single, oral dose: 21 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

AUC

Value	Dose	Analyte	Population
6.019 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	20 g single, oral dose: 20 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
14941 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211281Orig1s000MultidisciplineR.pdf	21 g single, oral dose: 21 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
6019 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211281Orig1s000MultidisciplineR.pdf	21 g single, oral dose: 21 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

T_1/2

Value	Dose	Analyte	Population
2.4 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	20 g single, oral dose: 20 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
2.16 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211281Orig1s000MultidisciplineR.pdf	21 g single, oral dose: 21 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
2.43 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211281Orig1s000MultidisciplineR.pdf	21 g single, oral dose: 21 g route of administration: Oral experiment type: SINGLE co-administered:	LACTITOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

Doses

Dose	Population	Adverse events
20 g 1 times / day steady, oral Recommended Dose: 20 g, 1 times / day Route: oral Route: steady Dose: 20 g, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	unhealthy, 18-87 years n = 298 Health Status: unhealthy Condition: chronic idiopathic constipation Age Group: 18-87 years Sex: M+F Population Size: 298 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	Other AEs: Urinary tract infection, Abdominal pain... Other AEs: Urinary tract infection (5%) Abdominal pain (3%) Hypersensitivity reaction Rash Pruritus Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf
20 g 1 times / day steady, oral Recommended Dose: 20 g, 1 times / day Route: oral Route: steady Dose: 20 g, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	unhealthy, 18-88 years n = 291 Health Status: unhealthy Condition: chronic idiopathic constipation Age Group: 18-88 years Sex: M+F Population Size: 291 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf	Disc. AE: Flatulence, Diarrhea... Other AEs: Upper respiratory tract infection, Flatulence... AEs leading to discontinuation/dose reduction: Flatulence (1%) Diarrhea (1%) Blood creatine phosphokinase increased (1%) Increased blood pressure (1%) Other AEs: Upper respiratory tract infection (9%) Flatulence (8%) Diarrhea (4%) Blood creatine phosphokinase increased (4%) Abdominal distension (3%) Increased blood pressure (3%) Diarrhea (grade 3, 1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211281s000lbl.pdf
130 g 1 times / day single, oral Highest studied dose Dose: 130 g, 1 times / day Route: oral Route: single Dose: 130 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3552029/	healthy, 23-48 years n = 21 Health Status: healthy Age Group: 23-48 years Sex: M+F Population Size: 21 Sources: https://pubmed.ncbi.nlm.nih.gov/3552029/	Sources: https://pubmed.ncbi.nlm.nih.gov/3552029/
74 g 1 times / day single, oral MTD Dose: 74 g, 1 times / day Route: oral Route: single Dose: 74 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3552029/	healthy, 23-48 years n = 21 Health Status: healthy Age Group: 23-48 years Sex: M+F Population Size: 21 Sources: https://pubmed.ncbi.nlm.nih.gov/3552029/	DLT: Diarrhea, Gastrointestinal symptom NOS... Dose limiting toxicities: Diarrhea (15 patients) Gastrointestinal symptom NOS (severe, 4 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/3552029/

AEs

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:75323	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:75323
ChemicalBook	CB5363096	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB5363096
ChemicalBook	CB6668853	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB6668853
MolPort	MolPort-006-069-327	https://www.molport.com/shop/molecule-link/MolPort-006-069-327
ZINC	ZINC000005225520	http://zinc15.docking.org/substances/ZINC000005225520
eMolecules	26985447	https://www.emolecules.com/cgi-bin/more?vid=26985447

PubMed

Title	Date	PubMed
Intestinal permeability in children: variation with age and reliability in the diagnosis of cow's milk allergy.	2001 May	11430707
Structural changes in natural actomyosin and surimi from ling cod (Ophiodon elongatus) during frozen storage in the absence or presence of cryoprotectants.	2001 Oct	11600013
Interaction of methylparaben preservative with selected sugars and sugar alcohols.	2002 Jul	12115834
Sugar alcohols enhance calcium transport from rat small and large intestine epithelium in vitro.	2002 Jun	12064809
Tributyrin and lactitol synergistically enhanced the trophic status of the intestinal mucosa and reduced histamine levels in the gut of nursery pigs.	2002 Mar	11890403
Comparison of rifaximin and lactitol in the treatment of acute hepatic encephalopathy: results of a randomized, double-blind, double-dummy, controlled clinical trial.	2003 Jan	12480560
Effects of lactulose and lactitol on coliform bacteria and bacterial translocation in the caecum during 72-h starvation in rats.	2003 Jul	12927899
Chemoenzymatically synthesized glycoconjugate polymers.	2003 Mar-Apr	12625739
[Compressibility of directly compressed forms of lactitol].	2003 Sep	14619701
Antagonistic activity of lactic acid bacteria as probiotics against selected bacteria of the Enterobaceriacae family in the presence of polyols and their galactosyl derivatives.	2004 Feb	15055768
Effect of sugar alcohols on gut function and body composition in normal and cecectomized rats.	2004 Jul	15297710
Lactose derivatives are inhibitors of Trypanosoma cruzi trans-sialidase activity toward conventional substrates in vitro and in vivo.	2004 Jul	15070857
Oxalate degradation by intestinal lactic acid bacteria in dogs and cats.	2004 Jul 14	15223120
Combination of polydextrose and lactitol affects microbial ecosystem and immune responses in rat gastrointestinal tract.	2004 Jun	15182394
Non-absorbable disaccharides for hepatic encephalopathy: systematic review of randomised trials.	2004 May 1	15054035
[Intestinal function tests].	2005 Sep 14	16193906
Management of hepatic encephalopathy: focus on antibiotic therapy.	2006	16498257
Carbohydrate preference, acid tolerance and bile tolerance in five strains of Bifidobacterium.	2006 Apr	16553741
[The diagnostics and therapy of hepatic encephalopathy. Recommendations of of the working group on portal hypertension in the Czech Hepatology Society and the J. E. Purkinje Czech Medical Society].	2006 Jan	16526204
Threshold for transitory diarrhea induced by ingestion of xylitol and lactitol in young male and female adults.	2007 Feb	17484374
The trans-sialidase from Trypanosoma cruzi efficiently transfers alpha-(2-->3)-linked N-glycolylneuraminic acid to terminal beta-galactosyl units.	2007 Nov 26	17765882
[A case of recurrent pneumatosis cystoides intestinalis associated with recurrent pneumoperitoneum].	2007 Sep	17885285
Effect of oral lactulose on clinical and immunohistochemical parameters in patients with inflammatory bowel disease: a pilot study.	2007 Sep 4	17784949
Prophylactic antibiotic treatment is superior to therapy on-demand in experimental necrotising pancreatitis.	2008	19014609
Xylitol-supplemented nutrition enhances bacterial killing and prolongs survival of rats in experimental pneumococcal sepsis.	2008 Mar 11	18334022
Treatment of minimal hepatic encephalopathy.	2008 Nov	19125944
Polyols as filler-binders for disintegrating tablets prepared by direct compaction.	2009 Jun	19274511
Some putative prebiotics increase the severity of Salmonella enterica serovar Typhimurium infection in mice.	2009 Nov 30	19948011
Freeze-drying of proteins with glass-forming oligosaccharide-derived sugar alcohols.	2010 Apr 15	20097277
Pharmacotherapy for hepatic encephalopathy.	2010 Jun 18	20518580
Lactitol or lactulose in the treatment of chronic constipation: result of a systematic.	2010 Nov	21510584
Current and emerging strategies for treating hepatic encephalopathy.	2010 Sep	20691385

Patents

Sample Use Guides

In Vivo Use Guide

Initial dose - 20 g at once during 4-5 days. Next, 10 g per day.

Route of Administration: Oral

In Vitro Use Guide

The species of bifidobacteria, which were detected in vessel of each fermentation after adaptation to an Lactitol 1% (wt/vol): Bifidobacterium adolescentis, B. bifidum, B. longum, B. dentium and B. catenulatum. B. angulatum, B. breve and B. infantis were not detected.

Name

Type

Language

LACTITOL MONOHYDRATE

Common Name

English

LACTITOL HYDRATE [JAN]

Common Name

English

D-LACTITOL MONOHYDRATE

Common Name

English

BLI-400

Code

English

D-GLUCITOL, 4-O-.BETA.-D-GALACTOPYRANOSYL-, MONOHYDRATE

Common Name

English

NSC-759131

Code

English

Lactitol monohydrate [WHO-DD]

Common Name

English

LACTITOL MONOHYDRATE [EP MONOGRAPH]

Common Name

English

PIZENSY

Brand Name

English

LACTITOL MONOHYDRATE [MI]

Common Name

English

LACTITOL MONOHYDRATE [II]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C283