CA2165446C - Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade - Google Patents

Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade Download PDF

Info

Publication number
CA2165446C
CA2165446C CA002165446A CA2165446A CA2165446C CA 2165446 C CA2165446 C CA 2165446C CA 002165446 A CA002165446 A CA 002165446A CA 2165446 A CA2165446 A CA 2165446A CA 2165446 C CA2165446 C CA 2165446C
Authority
CA
Canada
Prior art keywords
ropivacaine
weight
concentration
pain relief
manufacture
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA002165446A
Other languages
French (fr)
Other versions
CA2165446A1 (en
Inventor
Arne Torsten Eek
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
AstraZeneca AB
Original Assignee
Astra AB
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=20390432&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2165446(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astra AB filed Critical Astra AB
Publication of CA2165446A1 publication Critical patent/CA2165446A1/en
Application granted granted Critical
Publication of CA2165446C publication Critical patent/CA2165446C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • A61P23/02Local anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Insulation, Fastening Of Motor, Generator Windings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Particle Accelerators (AREA)
  • Air Conditioning Control Device (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Electromechanical Clocks (AREA)

Abstract

Use of a pharmaceutically acceptable salt of ropivacaine for the manufacture of a pharmaceutical preparation with sensoric block and minimal motor blockade.

Description

21 b5~46 Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade Field of the invention The present invention is related to the use of a low concentration of a pharmaceutically acceptable salt of ropivacaine in the manufacture of pharmaceutical preparations for pain relief post operatively and in labour.
Background of the invention Post operative pain relief is still a problem within modern surgery. According to a newly published study about 70% of all patients treated surgically felt moderate to severe pain after the surgical treatment.
The need for qualified pain relief is greatest during the first 24 hours after the surgical treatment. The traditional method to treat the patients is to give narcotics intramuscularly or intravenously. Such treatment is often insufficient as narcotic analgetics have many negative effects. One disadvantage is depression of the breathing, which may occur even after treatment. This means that the patient must be intensively looked after by specialists.
A patient, who has been treated with morfine is tired, apathetic and is often feeling sick. The patient thus has no interest in things around him. It is thus difficult to take care of the patient and make him participate in respitatory exercises and prophylaxis for thromboses.
One method is administration epidurally, by infusion or ~'~~46 2~
intermittent injections of local anaesthetics. Such treatments can only be carried out on patients with epidural catheters being taken care of at an intensive care or post surgical unit by specially trained persons.
There has been a long felt need at ward leval to be able to give a greater group of patients qualified pain relief by epidural infusion of e.g. local anaesthetics instead of opiates. -Normally, with local anaesthetics a good blockade of the pain is obtained. The draw back is the motor blockade in the legs, which is disturbing to the patients, who wants to give up the pain relief treatment in advance. Among other effects the motor blockade means that the patient cannot leave his bed without assistance as the legs will not bear.
Outline of the invention According to the present invention it has surprisingly been found that the local anaesthetic agent ropivacaine, described e.g. in WO/85/00599, in form of its hydrochloride can be given to the patient in a dosage which gives pain relief with minimal effect on motor function. This is at a dosage of lower than 0.5% by weight, especially from 0.01% to 0.45% by weight. Such low dosages are normally considered to be ineffective.
The normal dosage is from 0.5-2% by weight.
The local anaesthetic compound used according to the invention is in the form of its pharmaceutically acceptable salts. It is especially preferred to use ropivacaine hydrochloride.
The local anaesthetic is incorporated into a solution.
The local anaesthetic composition contains less than 0.5% by weight of the local anaesthetic compound, preferably from 0.01 up to 0.45% by weight, especially preferred 0.1-0.3% by weight.
In a use aspect, the invention provides use of a pharmaceutically acceptable salt of ropivacaine for the manufacture of a medicament with sensoric block and with minimal motor blockade, for pain relief post operatively and in labour wherein the concentration of ropivacaine is lower than 0.5% by weight.
In a further use aspect, the invention provides use of a pharmaceutically acceptable salt of ropivacaine in a concentration lower than 0.5% by weight for pain relief post operatively and in labour with minimal motor blockade.
The invention also provides a pharmaceutical preparation for use in pain relief post operatively and in labour with minimal motor blockade, wherein the active ingredient is a pharmaceutically acceptable salt of ropivacaine in a concentration lower than 0.5% by weight.
The invention also provides a commercial package, comprising a pharmaceutical preparation according to the invention and associated therewith instructions for use thereof for pain relief post operatively and in labour.

3a Pharmaceutical preparations Examples 1-3 Solution 5 mg/ml, 3 mg/ml, 2 mg/ml Examples Ropivacaine hydrochloride monohydrate 0.53 kg 0.32 kg 0.21 kg sodium hydroxide 2M to pH 5.0-6.0 _ Purified water qs ad 100 kg 100 kg 100 kg Ropivacaine is dissolved in the water. Sodium hydroxide is added to pH 5.0-6Ø The resulting solution is autoclaved.
The best mode of carrying out the invention known at present is to use the preparations according to Example 3.
Biological test A~double blind study_of sensory and motor blockade with 0.1%, 0.2%; 0.3% ropivacaine and 0.25% bupivacaine during continous epidural infusion in healthy male volunteers.

'/
Background The aim of the study was to find a low concentration of ropivacaine giving a sufficient sensory block but as little or no motor block at all during continous epidural infusion. This study is a first step towards finding a low concentration of ropivacaine which later will be used for treatment of post operative pain in patients. 37 volunteers participated in the study. They were divided into 5 treatment groups, receiving either 0.1%, 0.2% or 0.3% ropivacaine or 0.25% bupivacaine. There was also a control group receiving 0.9% saline. All solutions were first given as a bolus dose of 10 ml, followed by a continous epidural infusion at a rate of 10 ml/hour for 21 hours. During the infusion both motor and sensory blockade was tested using different methods. The postural stability of the volunteers was also evaluated.
Preliminary results Group 1. No motor and sensory block was acheived in the volunteers receiving saline.
Group 2. Bupivacaine 0.25% gave a good segmental spread (from the lower part of the abdomen to the lower part of the extremities) of sensoric block during the infusion.
All of the volunteers had a high degree of motor block and 75% (6/8) could not stand up at any occasion during the infusion.
Group 3. Ropivacaine 0.3% gave an equal duration of sensory blockade compared to bupivaciane 0.25%. The upper segmental spread of sensoric block was somewhat higher than for bupivacaine. The lower segmental spread of sensoric block was, after 10 hours of continous infusion, WO 95/00148 a ~ ~ J ~~~ PCT/SE94100496 shifted up to just below the knees compared to bupivacaine and at the end of infusion was found above = the knees. The motorblock was somewhat less profound compared to bupivacaine. 5 out of 7 volunteers could not 5 stand at any occasion during the infusion to perform the postural stability tests.
Group 4. Ropivacaine 0.2% gave an equal sensory block compared to bupivacaine 0.25% in the lower part of the abdomen, but showed a less sensory block around the ancles. After 10 hours of continous infusion the sensory block was less than for both ropivacaine 0.3% and bupivacaine. The motor block was less profound compared to the 0.3% ropivacaine as well as to the 0.25%
bupivacaine solution. 25% (2/8) of the volunteers could not at any occasion stand up whereas the rest of the volunteers (6/8) could at some point during the infusion make some of the postural tests.
Group 5. Ropivacaine 0.1% gave, during the first 5 hours of the infusion, a more narrow spread of the sensory block compared to the 0.2% ropivacaine solution. Normal sensation returned after 8 hours of the epidural infusion.
No serious or unexpected adverse events could be noted in any of the test groups.
It was found that bupivacaine gives 75% higher motor blockade than ropivacaine, which only gives 25% at comparable dosage levels.
At the dosages 0.3% and 0.2% ropivacaine gives about the same motor blockade. At the dosage 0.1% it is less.

conclusion From the unique effect of ropivacaine the conclusion can be drawn that said compound is especially useful for administering at low dosage to patients in the need of post surgical and labour pain treatment, with good balance between sufficient sensoric block and a desirable minimal degree of motor block.

Claims (13)

CLAIMS:
1. ~Use of a pharmaceutically acceptable salt of ropivacaine for the manufacture of a medicament with sensoric block and with minimal motor blockade, for pain relief post operatively and in labour wherein the concentration of ropivacaine is lower than 0.5% by weight.
2. ~Use according to claim 1, wherein ropivacaine is in the form of its hydrochloride.
3. ~Use according to claim 1 or 2, wherein the concentration of ropivacaine is from 0.01 up to 0.45% by weight.
4. ~Use according to claim 3, wherein the concentration of ropivacaine is 0.2% by weight.
5. ~Use of a pharmaceutically acceptable salt of ropivacaine in a concentration of lower than 0.5% by weight for pain relief post operatively and in labour with minimal motor blockade.
6. ~Use according to claim 5, wherein ropivacaine is in the form of its hydrochloride.
7. ~Use according to claim 5 or 6, wherein the concentration of ropivacaine is from 0.01 up to 0.45% by weight.
8. ~Use according to claim 7, wherein the concentration of ropivacaine is 0.2% by weight.
9. ~A pharmaceutical preparation for use in pain relief post operatively and in labour with minimal motor blockade, wherein the active ingredient is a pharmaceutically acceptable salt of ropivacaine in a concentration lower than 0.5% by weight.
10. ~A pharmaceutical preparation according to claim 9, wherein ropivacaine is in the form of its hydrochloride.
11. ~A pharmaceutical preparation according to claim 9 or 10, wherein the concentration of ropivacaine is from 0.01 up to 0.45% by weight.
12. ~A pharmaceutical preparation according to claim 11, wherein the concentration of ropivacaine is 0.2%
by weight.
13. A commercial package, comprising a pharmaceutical preparation according to any one of claims 9 to 12 and associated therewith instructions for use thereof for pain relief post operatively and in labour.
CA002165446A 1993-06-28 1994-05-26 Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade Expired - Fee Related CA2165446C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE19939302218A SE9302218D0 (en) 1993-06-28 1993-06-28 NEW USE
SE9302218-4 1993-06-28
PCT/SE1994/000496 WO1995000148A1 (en) 1993-06-28 1994-05-26 Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade

Publications (2)

Publication Number Publication Date
CA2165446A1 CA2165446A1 (en) 1995-01-05
CA2165446C true CA2165446C (en) 2005-07-05

Family

ID=20390432

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002165446A Expired - Fee Related CA2165446C (en) 1993-06-28 1994-05-26 Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade

Country Status (32)

Country Link
US (2) US5670524A (en)
EP (1) EP0706395B1 (en)
JP (1) JP3725541B2 (en)
CN (1) CN1074918C (en)
AT (1) ATE216237T1 (en)
BR (1) BR9406865A (en)
CA (1) CA2165446C (en)
CZ (1) CZ283300B6 (en)
DE (2) DE69430427T2 (en)
DK (1) DK0706395T3 (en)
EE (1) EE03205B1 (en)
ES (1) ES2099048T3 (en)
FI (1) FI956269L (en)
GR (1) GR970300013T1 (en)
HU (1) HU218949B (en)
IL (1) IL110006A (en)
IS (1) IS4174A (en)
LT (1) LT3449B (en)
LV (1) LV12918B (en)
MY (1) MY119360A (en)
NO (1) NO955313L (en)
NZ (1) NZ268110A (en)
PH (1) PH31258A (en)
PL (1) PL175518B1 (en)
PT (1) PT706395E (en)
RU (1) RU2152215C1 (en)
SA (1) SA94150010B1 (en)
SE (1) SE9302218D0 (en)
SG (1) SG49078A1 (en)
SK (1) SK280111B6 (en)
TW (1) TW285640B (en)
WO (1) WO1995000148A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9302218D0 (en) * 1993-06-28 1993-06-28 Ab Astra NEW USE
BR9802536A (en) * 1997-07-21 1999-07-20 Darwin Discovery Ltd Method for anesthetizing a human patient before surgery
US20060270708A1 (en) * 2005-05-25 2006-11-30 Navinta Llc Novel process for preparation of isotonic aqueous injection of ropivacaine
USRE46397E1 (en) 2007-11-07 2017-05-09 Svip5 Llc Slow release of organic salts of local anesthetics for pain relief
CA2873138A1 (en) * 2012-05-10 2013-11-14 Cellixbio Private Limited Compositions and methods for the treatment of local pain
WO2013168167A1 (en) * 2012-05-10 2013-11-14 Painreform Ltd. Depot formulations of a hydrophobic active ingredient and methods for preparation thereof
US8558008B2 (en) 2013-02-28 2013-10-15 Dermira, Inc. Crystalline glycopyrrolate tosylate
EP3842419B1 (en) 2013-02-28 2024-04-03 Journey Medical Corporation Method of making threo glycopyrrolate tosylate
US9006462B2 (en) 2013-02-28 2015-04-14 Dermira, Inc. Glycopyrrolate salts

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE40994T1 (en) * 1983-08-01 1989-03-15 Astra Laekemedel Ab L-N-N-PROPYLPIPECOLIC-2,6-XYLIDIDE AND ITS PRODUCTION.
SE9302218D0 (en) * 1993-06-28 1993-06-28 Ab Astra NEW USE

Also Published As

Publication number Publication date
HU218949B (en) 2001-01-29
FI956269A0 (en) 1995-12-27
IS4174A (en) 1994-12-29
DE69430427D1 (en) 2002-05-23
IL110006A (en) 1999-01-26
ATE216237T1 (en) 2002-05-15
BR9406865A (en) 1996-03-26
PT706395E (en) 2002-09-30
CN1126435A (en) 1996-07-10
LTIP1958A (en) 1995-01-31
NO955313D0 (en) 1995-12-27
SK164695A3 (en) 1996-07-03
SK280111B6 (en) 1999-08-06
AU692161B2 (en) 1998-06-04
DE69430427T2 (en) 2002-11-14
JP3725541B2 (en) 2005-12-14
NZ268110A (en) 1999-06-29
SA94150010B1 (en) 2006-04-04
SG49078A1 (en) 1998-05-18
JPH09500620A (en) 1997-01-21
LT3449B (en) 1995-10-25
IL110006A0 (en) 1994-11-11
CZ336495A3 (en) 1996-06-12
FI956269A7 (en) 1995-12-27
EE03205B1 (en) 1999-08-16
PH31258A (en) 1998-06-18
HUT75115A (en) 1997-04-28
MY119360A (en) 2005-05-31
GR970300013T1 (en) 1997-05-31
NO955313L (en) 1995-12-27
CA2165446A1 (en) 1995-01-05
WO1995000148A1 (en) 1995-01-05
AU7086694A (en) 1995-01-17
EP0706395A1 (en) 1996-04-17
CZ283300B6 (en) 1998-02-18
CN1074918C (en) 2001-11-21
RU2152215C1 (en) 2000-07-10
PL175518B1 (en) 1999-01-29
US5670524A (en) 1997-09-23
US5834489A (en) 1998-11-10
EP0706395B1 (en) 2002-04-17
DK0706395T3 (en) 2002-07-22
TW285640B (en) 1996-09-11
LV12918B (en) 2003-03-20
DE706395T1 (en) 1997-09-04
ES2099048T3 (en) 2002-11-16
HK1010344A1 (en) 1999-06-17
PL312198A1 (en) 1996-04-01
ES2099048T1 (en) 1997-05-16
FI956269L (en) 1995-12-27
HU9503692D0 (en) 1996-02-28
SE9302218D0 (en) 1993-06-28

Similar Documents

Publication Publication Date Title
Stenseth et al. Epidural morphine for postoperative pain: experience with 1085 patients
Lehmann Tramadol for the management of acute pain
JP2002532392A (en) Exo-S-mecamylamine formulations and their use in therapy
JPH09503777A (en) Levobupivacaine useful for the treatment of chronic pain
EP0727210A2 (en) Analgesic agent and its use
KR20000075894A (en) The use of levobupivacaine in paediatric surgery
CA2165446C (en) Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade
JP2620642B2 (en) Drugs to antagonize the decrease in mean blood pressure observed after parenteral administration of a combination of a narcotic analgesic and a benzodiazepine
AU692161C (en) Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade
US6114370A (en) Amnesic sedation composition and method of administering same
Milligan et al. The characteristics of analgesic requirements following subarachnoid diamorphine in patients undergoing total hip replacement
Stanton-Hicks et al. High thoracic epidural with sufentanil for post-thoracotomy pain
HK1010344B (en) Use of ropivacaine in the manufacture of a pharmaceutical with analgetic effect with minimal motor blockade
RU2016586C1 (en) Method of general anesthesia
Atallah et al. Presurgical analgesia in children subjected to hypospadias repair
SWARTZ Narcan (Naloxone HCI)
AU7231291A (en) Use of local anaesthetic agents in the manufacture of pharmaceutical preparations for iontophoresis
Corssen Proper Use of Ketamine and Innovar
MXPA99008057A (en) The use of levobupivacaine in paediatric surgery
IE911793A1 (en) Use of local anaesthetic agents in the manufacture of¹pharmaceutical preparations for iontophoresis
HK1022649B (en) The use of levobupivacaine in paediatric surgery
JPS62111925A (en) Analgesic and sedative in emergence recovery from anesthesia

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed