Reaction mass of 2-(3-{6-[3-(2-Hydroxyethyl)-3-methylureido]hexyl}-1-methylureido)ethanol and 6-[3-(2-Hydroxyethyl)-3-methylureido]hexylamino 3-(methylamino)propionate

Stability in organic solvents and identity of relevant degradation products

Link to relevant study record(s)

Reference

Reference 1

Endpoint:

stability in organic solvents and identity of relevant degradation products

Type of information:

experimental study

Adequacy of study:

other information

Reliability:

2 (reliable with restrictions)

Rationale for reliability incl. deficiencies:

study well documented, meets generally accepted scientific principles, acceptable for assessment

Qualifier:

according to guideline

Guideline:

other: SOP 00191

Version / remarks:

Version 2

Deviations:

no

Principles of method if other than guideline:

Formulations preparation: The test item was heated at 110 °C.
10 mg/ml: approx. 100 mg of the test item were dissolved and homogenized in 10 ml with DMF by manual shaking and ultrasonic bath (approx. 3 min.).
500 mg/ml: approx. 5 g of the test item were dissolved and homogenized in 10 ml with DMF by stirring with a mechanical stirrer at 2500 rev/min. (approx. 20 min.).
Analytical Method: Quantification by HPLC

GLP compliance:

no

Specific details on test material used for the study:

Expiry Date: 2015-07-12

Test substance stable:

yes

Transformation products:

no

The stability of the test item was determined based on the monitoring of the two main peaks present in the HPLC-UV chromatogram of the test item.

Nominal value mg/ml	Theoretical value mg/ml	Content Test Item mg/ml		Recovery as % of theoretical value
		Start	After 2 hours	Start	After 2 hours
10	10.18	10.36	10.36	102	102
500	503.6	483.3	474.0	96	94

Conclusions:

The 10 mg/ml and 500 mg/ml formulations of the test item EGGE 2806-1 in DMF are stable for at least 2 hours at room temperature.

Executive summary:

According to SOP 00191 Version 2, the 10 mg/ml (1% w/v) and 500 mg/ml (50% w/v) formulations of the test item EGGE 2806-1 in DMF are stable for at least 2 hours at room temperature.

Reference 2

Endpoint:

stability in organic solvents and identity of relevant degradation products

Type of information:

experimental study

Adequacy of study:

other information

Reliability:

2 (reliable with restrictions)

Rationale for reliability incl. deficiencies:

study well documented, meets generally accepted scientific principles, acceptable for assessment

Qualifier:

according to guideline

Guideline:

other: SOP 00191

Version / remarks:

Version 2

Deviations:

no

Principles of method if other than guideline:

Formulations preparation: The test item was heated at 110 °C.
0.5 mg/mL: approx. 250 mg of the test item were dissolved and homogenized in 50 ml with Kolliphor HS15/Ethanol/Tap water (40/10/50; v/v/v) by magnetic stirring at ca. 100 °C and by manual shaking. The air bubbles were eliminated by ultrsonic bath (approx. 3 min.) 2 mL of the solution was diluted immediately to 20 mL with the same solvent.
200 mg/mL: approx. 3 g of the test item were dissolved and homogenized in 15 ml with Kolliphor HS15/Ethanol/Tap water (40/10/50) by shaking with a mechanical shaker at 2500 rev. min (approx. 5 min.), by ultrasonic bath (5 min.) and by stirring with a magnetic stirrer at approx. 100 °C (approx. 20 min.). The air bubbles were eliminated by ultrasonic bath (approx. 3 min.). This formulation was placed in a cabinet at 40 °C for 15 min. before the sample was taken for analysis after 48 hours and 7 days.

GLP compliance:

not specified

Specific details on test material used for the study:

Expiry Date: 2015-07-12

Test substance stable:

yes

Transformation products:

no

The stability of the test item was determined based on the monitoring of the two main peaks present in the HPLC-UV chromatogram of the test item.

Nominal value	Theoretical value	Content Test Item [mg/mL]			Recovery as % of theoretical value [mg/mL]
mg/mL	mg/mL	Start	After 48 hours	After 7 days	Start	After 48 hours	After 7 days
0.5	0.505	0.476	0.479	0.479	94	95	95
200	119.3	198.5	197.4	198.5	100	99	100

Conclusions:

The 0.5 mg/ml and 200 mg/ml formulations of the test item EGGE 2806-1 in Kolliphor HS15/Ethanol/Tap water (40/10/50; v/v/v) are stable for at least 7 days at room temperature.

Executive summary:

According to SOP 00191 Version 2, the 0.5 mg/ml and 200 mg/ml formulations of the test item EGGE 2806-1 in Kolliphor HS15/Ethanol/Tap water (40/10/50; v/v/v) are homogeneous and stable for at least 7 days at room temperature.

Description of key information

According to SOP 00191 Version 2, the 10 mg/ml (1% w/v) and 500 mg/ml (50% w/v) formulations of the test item EGGE 2806-1 in DMF are stable for at least 2 hours at room temperature.

According to SOP 00191 Version 2, the 0.5 mg/ml and 200 mg/ml formulations of the test item EGGE 2806-1 in Kolliphor HS15/Ethanol/Tap water (40/10/50; v/v/v) are homogeneous and stable for at least 7 days at room temperature.