Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23533)
Name
Ranitidine Hydrochloride eq 15 mg base/mL syrup
Company
Teligent
Active Pharmaceutical Ingredient (API) Ranitidine API Info click to show the detail info of this API
Gastric ulcer ICD-11: DA60 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E05GFF DIG Info Butylparaben Antimicrobial preservative
E06YUO DIG Info Disodium hydrogenorthophosphate Buffering agent ...
E0SF4Y DIG Info Ethanol Antimicrobial preservative ...
E0T4YW DIG Info Hypromellose Coating agent
E0V4HH DIG Info Potassium phosphate monobasic Buffering agent
E0X6QO DIG Info Propylparaben sodium Antimicrobial preservative
E04NIZ DIG Info Saccharin sodium anhydrous Flavoring agent
E0T4TW DIG Info Sodium chloride Diluent ...
E0G5FT DIG Info Sorbitan tristearate Dispersing agent ...
E0H2SC DIG Info Water Solvent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Muscarinic receptor M1 (ACM1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 12 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACM1_HUMAN
            DBT Name: Alpha-1A adrenoceptor (ADA1A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 16.4 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA1A_HUMAN
            DBT Name: Thromboxane A2 receptor (TBXA2R) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 19 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TA2R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Prostaglandin G/H synthase 2 (COX-2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 > 3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity Protein expression upregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity Protein expression downregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
            DBT Name: Cytochrome P450 2E1 (CYP2E1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity IC50 = 253.5 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity EC50 = 211.8 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2CJ_HUMAN
            DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity EC50 = 159.3 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2D6_HUMAN
            DBT Name: Cytochrome P450 3A5 (CYP3A5) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity IC50 = 19.4 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A5_HUMAN
      Hydrolase (HDase)
            DBT Name: Intestinal alkaline phosphatase (IAP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Potassium phosphate monobasic
                    Biological Activity IC50 = 2410 nM (tested by experiment) [4]
                    Tested Species Bos taurus (Bovine)
                    UniProt ID PPBI_BOVIN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase I (CA1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Saccharin sodium anhydrous
                    Biological Activity Ki = 18540 nM (estimated based on the structural similarity with CHEMBL310671 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.970873786
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH1_HUMAN
            DBT Name: Cholesterol 25-hydroxylase (CYP1A2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity EC50 = 106.7 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Dopamine transporter (DAT) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 19 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A3_HUMAN
            DBT Name: Norepinephrine transporter (NET) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 20 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A2_HUMAN
            DBT Name: Solute carrier SLCO2B1 (OATPB) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity Inhibition ratio = 73.5 % (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity Ki = 44.3 uM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
            DBT Name: Monoamine transporter VAT2 (VMAT2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity Ki = 6.6 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID VMAT2_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Sodium channel alpha Nav1.5 (SCN5A) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity Ki = 33 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SCN5A_HUMAN
      Nuclear receptor (NR)
            DBT Name: Estrogen receptor alpha (ESR1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 1420 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylparaben sodium
                    Biological Activity EC50 = 38200 nM (estimated based on the structural similarity with CHEMBL15841 ) [8]
                    Structural Similarity Tanimoto coefficient = 0.946428571
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity IC50 = 3.5 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
            DBT Name: Oxysterols receptor LXR-beta (NR1H2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Butylparaben
                    Biological Activity Ki = 66000 nM (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NR1H2_HUMAN
      Cell line (CELL)
            DBT Name: Colon cancer Caco-2 cells (Caco-2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity Promotion ratio > 18 % (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity Promotion ratio > 27 % (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4 Synthesis, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines. Eur J Med Chem. 2014 May 6; 78:167-77.
5 Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamides. Bioorg Med Chem. 2009 Jul 15; 17(14):5054-8.
6 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
7 Disconnecting the Estrogen Receptor Binding Properties and Antimicrobial Properties of Parabens through 3,5-Substitution. ACS Med Chem Lett. 2017 Dec 15; 9(1):51-55.
8 Discovery of natural estrogen receptor modulators with structure-based virtual screening. Bioorg Med Chem Lett. 2013 Jun 1; 23(11):3329-33.
9 Identify liver X receptor modulator building blocks by developing a fluorescence polarization-based competition assay. Eur J Med Chem. 2019 Sep 15; 178:458-467.
10 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.

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