Table 1

   PHYSICOCHEMICAL PROPERTIES OF CHOLYLSARCOSINE AND CHOLYLGLYCINE

               Property                                                        Cholylsarcosine     Cholylglycine          Reference                                        

Molecular weight, daltons (sodium salt)                                502                      488                           62

Solubility of protonated acid, mM                                           2.4                         0.6                            62

Ionization properties, pK_a                                                        3.7                         3.9                            62

Critical micellization pH (CMpH)^a                                          3.7                         4.8                            62

Ion product of calcium salt, (mol/L)³                           1 x 10^-7                        6 x 10^-7                           62,76

Critical micellization concentration (CMC), mM^b      10-11                          9-10                               62

Surface pressure at CMC, dynes/cm                                    21                    21                                   62

CMC in presence of 1-monoolein, mM^b                                5                      5                                     62

Solubilization capacity for monoolein^c                                   2                      1.6                                  62

^aThe critical micellization pH is defined as that pH value at which the solubility of the compound undergoes a marked increase.  This occurs when the concentration of the monomer reaches the CMC of the system (77).

^bThe value for the CMC and CMpH were determined in the presence of Na⁺concentration of 0.15 M.

^bThe solubilization capacity is defined as ()monoolein solubilized / )bile acid concentration at a bile acid concentration exceeding the CMC)

  Table 2.

BIOLOGICAL PROPERTIES IN THE RAT OF CHOLYLSARCOSINE AND CHOLYLGLYCINE (OR CHOLYLTAURINE)

                                                                           Cholylsarcosine                 Cholylglycine          Reference

I.  Hepatic physiology

     Hepatic biotransformation                                                 None                           None                        61

  T_maxof biliary secretion, µmol/min-kg                                 22                                15 (CT)                    61

               Effect on bile flow, L, ACA^a, µL/µmol                      15                                15                            78

      Effect on biliary phospholipid secretion, PL/BA             0.17                            0.17                         78       

  Effect on biliary cholesterol secretion, Cholesterol/PL      0.17                            0.17                          78

II.  Intestinal Physiology

  Effect on triglyceride absorption                             Promoting                  Promoting (CT)                  62

  Ileal transport, ml/20 cm--min                                               1.8                               1.8                           61

Bacterial metabolism                                                          

     Deconjugation-dehydroxylation                                          None                           Rapid                       61
                                                     

^a The apparent choleretic activity is defined as the )bile flow / )bile acid recovered in hepatic bile

  Table 3.

BIOLOGICAL PROPERTIES IN THE HUMAN  OF CHOLYLSARCOSINE AND CHOLYLTAURINE

                                                                                       Cholylsarcosine                 Cholylglycine       Reference

I.  Hepatic Physiology             

   Hepatic biotransformation                                                   None                           None                         64

   Effect on bile flow, L, ACA, µL/µmol                                   19                                15                             64

    Effect on biliary phospholipid secretion, PL/BA*             0.19                            0.12                             64

   Effect on biliary cholesterol secretion, Cholesterol/PL     0.4                               0.4                             64

II.  Intestinal Physiology

   Effect on triglyceride absorption                             Promoting                  Promoting                           68,69,72,73

   Ileal transport, T_{max ,} µmol/kg-min                                         0.2                            0.2                                65                                      

Bacterial Metabolism

Deconjugation-dehydroxylation                                              None                           Rapid                       64,69

Table IV

EFFECT OF     CHOLYLSARCOSINE (CS) OR MIXED CONJUGATED BOVINE BILE ACIDS (MBBA) ON FAT ABSORPTION AND FECAL WEIGHT IN ILEAL RESECTION OR SBS PATIENTS.

Age,Sex   Jejunum, cm.  CBA, gm/day   Fat absorption, gm/day  Fat absorption, %  Fecal wt,g/day  Reference 

                                                               Control            CBA                Control  CBA          Control  CBA

I.  Patients lacking a colon                                                                 

35M            150             CS, 1.5                  26.3         57.1                26.3    42.9            1.9          1.1                  68

57F             150             CS, 1.5                  24.1        84.3                  20.1     70.2            2.9           2.2              

57F            200             MBBA, 6                47             83                    37.9     66.9             1.8    1.8                      69

                                       MBBA, 12             47           95                     37.9     76.6             1.8      2.1

                                       CS, 6                     61           82                     49.2     66.1             1.7      1.9

                                       CS, 12                   61           93                      49.2     75.0             1.7      2.0

     (pooled data, n=4)   CS, 6                                                              78        99                                                    73

  

Patients with a colon

58F        180              CS, 4                                                              65        98                                                     73

48F        150              CS, 4                                                              48       81

70F        200              CS, 4                                                              52       84

Patients with (n=2) and patients without (n=2) a colon

               45-180            CS,6                           35        52                    37       52                 2.0      2.2                   72

                                       CS,12                         35        55                    37       55                 2.0      2.3