Details of the Drug Formulation (DFM)

General Information of DFM (ID: F17659)
Name
Pravastatin 20 mg tablet
Company
RemedyRepack
Active Pharmaceutical Ingredient (API) Pravastatin API Info click to show the detail info of this API
Dyslipidaemia ICD-11: 5C81 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E0DB2E DIG Info Carbonic acid disodium salt Alkalizing agent ...
E03SQI DIG Info Carmellose sodium Disintegrant
E01UTP DIG Info Magnesium stearate lubricant
E0CX3L DIG Info Polyoxyl 35 castor oil Emulsifying agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            DBT Name: Cytochrome P450 3A (CYP3A) 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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 250 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity Inhibition (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_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 Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [3]
                    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 Carmellose sodium
                    Biological Activity Protein expression upregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Carmellose sodium
                    Biological Activity Protein expression upregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity EC50 = 306.5 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity IC50 = 600 uM (tested by experiment) [5]
                    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 Polyoxyl 35 castor oil
                    Biological Activity EC50 = 113.3 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Cytochrome P450 2C9 (CYP2C9) 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 Polyoxyl 35 castor oil
                    Biological Activity EC50 = 41.1 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity IC50 = 30 uM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_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 Polyoxyl 35 castor oil
                    Biological Activity EC50 = 36.1 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2CJ_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 Polyoxyl 35 castor oil
                    Biological Activity EC50 = 10.1 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A5_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            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 Polyoxyl 35 castor oil
                    Biological Activity EC50 = 1.1 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      Primary active transporter (PAT)
            DBT Name: Multidrug resistance protein 2 (ABCC2) 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 Polyoxyl 35 castor oil
                    Biological Activity Inhibition ratio = 51 % (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity Inhibition ratio > 73 % (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
            DBT Name: Multidrug resistance protein 1 (ABCB1) 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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 5 mg.mL-1 (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity Inhibition ratio = 61 % (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity Inhibition ratio > 100 % (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
            DBT Name: Urate exporter (BCRP) 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 Polyoxyl 35 castor oil
                    Biological Activity Inhibition ratio > 40 % (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ABCG2_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO1B1 (OATP-C) 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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.19 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.3 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B1_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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.0011 %(w/v) (tested by experiment) [11]
                    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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.0098 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
            DBT Name: Solute carrier SLCO1A2 (OATP-A) 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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.00054 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.00034 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_HUMAN
            DBT Name: Organic anion transporter 8 (OAT8) 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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.001 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B3_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.0047 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1B3_HUMAN
            DBT Name: Sodium/bile acid cotransporter (SLC10A1) 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 Polyoxyl 35 castor oil
                    Biological Activity IC50 = 2.8 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NTCP_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity IC50 = 0.012 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NTCP_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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyoxyl 35 castor oil
                    Biological Activity Chylomicron secretion downregulation (tested by experiment) [12]
                    Tested Species Homo sapiens (Human)
References
1 Nonionic surfactants are strong inhibitors of cytochrome P450 3A biotransformation activity in vitro and in vivo. Eur J Pharm Sci. 2009 Mar 2;36(4-5):401-11.
2 In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. iopharm Drug Dispos. 2004 Jan;25(1):37-49.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
5 Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
6 Inhibition of human efflux transporter ABCC2 (MRP2) by self-emulsifying drug delivery system: influences of concentration and combination of excipients. J Pharm Pharm Sci. 2014;17(4):447-60.
7 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.
8 Reversal of multidrug resistance by surfactants. Br J Cancer. 1992 Jul;66(1):62-8.
9 A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci. 2002 Sep;91(9):1991-2002.
10 Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release. 2007 Dec 4;124(1-2):1-5.
11 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.
12 The effects of pluronics block copolymers and Cremophor EL on intestinal lipoprotein processing and the potential link with P-glycoprotein in Caco-2 cells. Pharm Res. 2003 Jul;20(7):1085-92.

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