Methods of dosing propofol prodrugs for inducing mild to moderate levels of sedation

A mild, sedative technology, used in pharmaceutical formulations, drug combinations, medical preparations containing active ingredients, etc., can solve problems such as hindering development and poor bioavailability of propofol

Inactive Publication Date: 2008-08-20
EISAI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the poor bioavailability of propofol when administered by any non-intravenous route hinders the development of this treatment

Method used

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  • Methods of dosing propofol prodrugs for inducing mild to moderate levels of sedation
  • Methods of dosing propofol prodrugs for inducing mild to moderate levels of sedation
  • Methods of dosing propofol prodrugs for inducing mild to moderate levels of sedation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1A

[0053] In this example, 93 patients were administered the fentanyl and bolus propofol prodrug doses as summarized in Table 2 below.

[0054] Table 2

[0055] Propofol prodrug rapid injection dose group

[0056] 7.5 mg /

kilogram

10mg / thousand

gram

12.5 mg /

kilogram

Total

Fentanyl

Quantitative

medicine

0.5 μg / kg

4

13

10

27

1.0 μg / kg

9

14

11

34

1.5 μg / kg

11*

10

11

32

Total

24

37

32

93

[0057] *One patient received 1.5 μg / kg fentanyl + 8.5 μg / kg bolus dose of propofol prodrug

[0058] Demographics of patients in Example 1A summarized by original assignment to treatment groups (mg / kg) in Table 3.

[0059] Table 3 Demographic and other baseline characteristics of treatment groups (Example 1A)

[0060] Rapid Injection Do...

Embodiment 1B

[0070] In this example, the initial dosing regimen was divided into 2 individual reconstitutions, each with fixed fentanyl and propofol prodrug doses. Some initial patients weighed 75 to 80 kg and were dosed with 980 mg (28 mL). During this initial portion, subjects became increasingly sedated (MOAA / S75 to >80 kg. Table 5 summarizes the adjusted weight-based fixed dosing regimen.

[0071] Table 5 Weight-Based Fixed Dosing Regimen

[0072] patient weight

Pretreatment Fen

Dosage of tanyl

Initial propofol prodrug rapid

injection dose

Propofol Prodrug Supplement Dosage

18-70 years old

≤50kg

50 micrograms

630 mg (18 mL)

Up to 105 mg (3 mL)

>50kg to ≤65kg

60 micrograms

700mg (20ml)

Up to 140 mg (4 mL)

>65kg to ≤80kg

70 micrograms

805 mg (23 mL)

Up to 175 mg (5 mL)

>80kg

80 micrograms

910 mg (26 mL)

Up to 175 mg (5 mL)

Patients ≥70 ...

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Abstract

A dosage of a propofol prodrug needed for inducing mild to moderate sedation levels in a patient is calculated based on a patient's lean body mass. It has been discovered dosages based on gross body mass may result in overdosing, particularly for obese patients. In another aspect, a dosage suitable for inducing mild to moderate sedation levels in a patient who is at least 60 years of age is determined. A weight- appropriate dosage for the patient is determined and then adjusted by an age-based factor. For example, the dosage needed to produce a sedated state or other effect in a patient who is 60 years of age or older may be about 0.6 - 0.8 times the dosage needed to produce a corresponding effect in a younger patient of the same weight.

Description

[0001] This application claims priority to US Provisional Application Serial No. 60 / 698,404, filed July 12, 2005, which is hereby incorporated by reference. field of invention Background of the invention [0002] The outpatient setting is becoming more common for various types of medical procedures that require sedation. During outpatient colonoscopy, for example, benzodiazepines are widely used for sedation. The combination of midazolam hydrochloride with a narcotic analgesic is a very common drug regimen used to provide mild to moderate sedation and analgesia. Gastroenterologists have sought alternative treatments, which are used on an outpatient basis, to provide faster recovery times and accelerated "street-fitness" after patient sedation for outpatient surgery and diagnostic procedures. [0003] The use of injectable anesthetics, especially propofol, for the induction and maintenance of general anesthesia has gained general acceptance in anesthesia care over the past 1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445
CPCA61K31/661A61K31/445A61P1/08A61P17/04A61P21/02A61P25/06A61P25/08A61P25/10A61P25/12A61P25/20A61P25/28
Inventor E·吉比安斯基L·吉比安斯基
Owner EISAI INC
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