Sustained local anesthetic composition containing preferably a sugar ester such as saib

A technology of local anesthesia and local anesthetics, applied in the field of controlled release systems, which can solve problems such as difficult to overcome and unavoidable systemic initial burst release of anesthetics

Active Publication Date: 2007-09-12
DURECT CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these polymeric controlled-release systems can provide suitable controlled-release properties for anesthesia and further overcome the disadvantages associated with injecting pure anesthetics (e.g., spread from the target site, entry into the bloodstream, and systemic toxicity), it is difficult to Overcoming disadvantages associated with said polymer systems, such as the inability to avoid a systemic initial burst of anesthetic, or having to provide accelerators to overcome too little anesthetic released from the system

Method used

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  • Sustained local anesthetic composition containing preferably a sugar ester such as saib
  • Sustained local anesthetic composition containing preferably a sugar ester such as saib
  • Sustained local anesthetic composition containing preferably a sugar ester such as saib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0164] The non-polymeric liquid carrier system containing the anesthetic was fabricated as follows. Sucrose acetate isobutyrate (SAIB) was mixed with N-methylpyrrolidone (NMP), a solvent for the SAIB vehicle, to form a 70:30 mixture. To this mixture was added either 2.5% (w / v (weight / volume)) or 5% bupivacaine (free base) to provide two test compositions.

[0165] Male Sprague Dawley rats (275g-300g) were divided into two test groups of 8 animals each. The test formulation was injected into the quadruped using a needle and cannula at either 25 mg or 50 mg bupivacaine doses. The presence of local anesthesia was then determined using a skin contraction response test in which there was an instinctive contraction of the skin stimulated by needle sticks in 10 random areas within 1 cm of the injection site. The percentage of needle sensory inhibition was calculated by subtracting the test response from the baseline response and dividing by the baseline response and multiplying by ...

Embodiment 2

[0168] subject. Male Fisher 344 rats (Charles River Laboratories) (N=96) were used for the study. Animals were maintained on a reversed light-dark cycle (dark from 5:00 to 17:00) in a temperature-humidity-controlled vivarium. Rats were given ad libitum (except during the experimental period) access to food and water. All tests were performed during the dark phase of the light-dark cycle. All procedures were approved by the Institutional Animal Care and Use Committee of Wake Forest University Health Science Center.

[0169] surgical procedure. After induction of anesthesia with 5% isoflurane vapor in oxygen, the left lower abdominal region of the animals was shaved. Anesthesia was maintained during the operation using 2.0% to 2.5% isoflurane vapor in oxygen. A 3 cm incision was made at a position 0.5 cm below the lowermost rib on the left side and parallel to the rib, and the incision penetrated into the abdominal cavity. Viscera and musculature are strongly stimulated by...

Embodiment 3

[0216] The following dose escalation, safety and pharmacokinetic evaluations were performed in healthy human volunteer subjects to evaluate the safety / tolerance of controlled release bupivacaine compositions containing sucrose acetate isobutyrate non-polymeric carriers and preliminary pharmacokinetic properties.

[0217] Bupivacaine formulated in a sucrose acetate isobutyrate (SAIB) non-polymeric vehicle further comprising N-methyl-2-pyrrolidone (NMP) used as a solvent for the bupivacaine and SAIB vehicle was used The composition was prepared from the free base. The composition was prepared by combining the SAIB vehicle and NMP solvent (70:30 vehicle substance) with 5% by weight bupivacaine to provide an individual containing 137.5 mg bupivacaine in a 2.5 mL injection volume dose. The composition is provided as an injectable solution.

[0218]There were two groups in the study. Group 1 included 6 healthy male subjects, aged 22-38 years. For Group 1, all subjects received ...

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Abstract

The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.

Description

technical field [0001] The present invention relates generally to the field of controlled release systems, and more particularly to controlled release systems containing an active agent capable of providing local anesthesia, wherein said system is suitable for use in connection with surgical therapy and drug therapy, and as a postoperative recovery Medications used during the procedure. Background technique [0002] Biodegradable controlled release systems for active agents are well known in the art. Biodegradable carriers for drug release are useful because they do not require removal of the device after the drug is exhausted. [0003] The most common carrier materials used in controlled release systems are polymers. The field of biodegradable polymers has grown rapidly since Kulkarni et al. (1966, Arch. Surg. 93:839) reported the synthesis and biodegradability of polylactic acid. Examples of other polymers that have been reported to be useful as matrix materials for con...

Claims

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Application Information

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IPC IPC(8): A61K47/26A61K9/08A61K31/445
Inventor 阿德里安·尼尔·维里蒂
Owner DURECT CORP
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