Management of diabetic foot ulcers: a 25% lidocaine topical cream formulation design, physicochemical and microbiological assessments.
Administration, Cutaneous
Anesthetics, Local
/ administration & dosage
Chemistry, Pharmaceutical
/ methods
Diabetic Foot
/ drug therapy
Drug Compounding
/ methods
Drug Stability
Drug Storage
Humans
Hydrogen-Ion Concentration
Lidocaine
/ administration & dosage
Pain
/ drug therapy
Skin Cream
Temperature
diabetes
drug analysis
drug stability
pain management
validation analytical procedure
Journal
European journal of hospital pharmacy : science and practice
ISSN: 2047-9956
Titre abrégé: Eur J Hosp Pharm
Pays: England
ID NLM: 101578294
Informations de publication
Date de publication:
05 2020
05 2020
Historique:
received:
15
07
2018
revised:
03
10
2018
accepted:
09
10
2018
entrez:
19
5
2020
pubmed:
19
5
2020
medline:
1
7
2021
Statut:
ppublish
Résumé
Given the importance of surgical debridement in healing of diabetic foot ulcers, effective local anaesthesia is required to manage the related extreme pain. The pharmaceutical proprietary products currently available have low concentrations and do not exceed 5% w/w local anaesthetic. Formulation design of a lidocaine cream of 25% and assessment of the intrinsic stability. A cream pharmaceutical form was chosen for its ability to cross the skin barrier and effectively anaesthetise the skin. The choice of cream formula is based on changes in the size of the emulsions and resistance to physical stress. Stability tests were assessed over a 6-month period in terms of physical (evaluation of oil droplets), microbiological (germ count and identification, and preservative antimicrobial efficacy) and chemical parameters (content and pH). Under the study conditions, the drug product displayed good physicochemical and microbiological stability for 6 months at 20°C and 40°C, and no degradation product was detected. Due to the systemic adverse effects of lidocaine, the pH stability guarantee the drug product tolerance along with very weak systemic passage. Given the good physicochemical and microbiological stability of the drug product over 6-month period, it has been made available to the clinical unit. An average of 250 patients per year benefit from the treatment with an excellent efficacy/tolerability ratio.
Sections du résumé
Background
Given the importance of surgical debridement in healing of diabetic foot ulcers, effective local anaesthesia is required to manage the related extreme pain. The pharmaceutical proprietary products currently available have low concentrations and do not exceed 5% w/w local anaesthetic.
Objective
Formulation design of a lidocaine cream of 25% and assessment of the intrinsic stability.
Methods
A cream pharmaceutical form was chosen for its ability to cross the skin barrier and effectively anaesthetise the skin. The choice of cream formula is based on changes in the size of the emulsions and resistance to physical stress. Stability tests were assessed over a 6-month period in terms of physical (evaluation of oil droplets), microbiological (germ count and identification, and preservative antimicrobial efficacy) and chemical parameters (content and pH).
Results
Under the study conditions, the drug product displayed good physicochemical and microbiological stability for 6 months at 20°C and 40°C, and no degradation product was detected. Due to the systemic adverse effects of lidocaine, the pH stability guarantee the drug product tolerance along with very weak systemic passage.
Conclusions
Given the good physicochemical and microbiological stability of the drug product over 6-month period, it has been made available to the clinical unit. An average of 250 patients per year benefit from the treatment with an excellent efficacy/tolerability ratio.
Identifiants
pubmed: 32419937
doi: 10.1136/ejhpharm-2018-001680
pii: ejhpharm-2018-001680
pmc: PMC7223286
doi:
Substances chimiques
Anesthetics, Local
0
Lidocaine
98PI200987
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
162-167Informations de copyright
© European Association of Hospital Pharmacists 2020. No commercial re-use. See rights and permissions. Published by BMJ.
Déclaration de conflit d'intérêts
Competing interests: None declared.
Références
Curr Microbiol. 2000 Mar;40(3):145-8
pubmed: 10679044
Clin Biomech (Bristol, Avon). 2016 Aug;37:98-107
pubmed: 27389946
Diabetes Metab. 2002 Nov;28(5):356-61
pubmed: 12461472
J Microencapsul. 2015;32(5):419-31
pubmed: 26066775
J Chromatogr B Biomed Sci Appl. 1997 Aug 29;696(2):303-6
pubmed: 9323552
Toxicology. 2017 Feb 1;376:102-112
pubmed: 27142991
Insect Biochem Mol Biol. 2011 Jan;41(1):36-41
pubmed: 20888415
Diabetes Care. 2003 Jan;26 Suppl 1:S78-9
pubmed: 12502623
J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Apr 1;877(10):1005-10
pubmed: 19269905
J Gen Physiol. 2012 Jun;139(6):507-16
pubmed: 22641643
Arch Dermatol Res. 1987;279(6):398-401
pubmed: 3674963
Sichuan Da Xue Xue Bao Yi Xue Ban. 2010 Jul;41(4):696-9
pubmed: 20848799
Skin Pharmacol Physiol. 2009;22(4):190-9
pubmed: 19648780
Clin Pharmacokinet. 1984 Jan;9 Suppl 1:27-31
pubmed: 6705424
J Struct Biol. 2010 Sep;171(3):353-60
pubmed: 20347991
Clin Pharmacol Ther. 2006 Dec;80(6):597-606
pubmed: 17178261
Arch Dermatol. 2006 Aug;142(8):1024-6
pubmed: 16924052