Combination Topical Analgesia Post Haemorrhoidectomy: a Study on Metronidazole, Diltiazem and Lignocaine

Abstract Amitriptyline, administered orally, is currently one of the treatment options for the management of neuropathic pain and migraine. Because of the physicochemical properties of the molecule, amitriptyline is also a promising candidate for delivery as a topical analgesic. Here we report the dermal delivery of amitriptyline from a range of simple formulations. The first stage of the work required the conversion of amitriptyline hydrochloride to the free base form as confirmed by nuclear magnetic resonance (NMR). Distribution coefficient values were measured at pH 6, 6.5, 7, and 7.4. Solubility and stability of amitriptyline were assessed prior to conducting in vitro permeation and mass balance studies. The compound demonstrated instability in phosphate-buffered saline (PBS) dependent on pH. Volatile formulations comprising of isopropyl alcohol (IPA) and isopropyl myristate (IPM) or propylene glycol (PG) were evaluated in porcine skin under finite dose conditions. Compared with neat IPM, the IPM:IPA vehicles promoted 8-fold and 5-fold increases in the amount of amitriptyline that permeated at 24 h. Formulations containing PG also appear to be promising vehicles for dermal delivery of amitriptyline, typically delivering higher amounts of amitriptyline than the IPM:IPA vehicles. The results reported here suggest that further optimization of topical amitriptyline formulations should be pursued towards development of a product for clinical investigational studies. Graphical abstract

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Postoperative topical analgesia of hemorrhoidectomy with policresulen and cinchocaine: a prospective and controlled study

Revista do Colégio Brasileiro de Cirurgiões ◽

10.1590/s0100-69912014000200004 ◽

2014 ◽

Vol 41 (2) ◽

pp. 92-98 ◽

Cited By ~ 6

Author(s):

Ilario Froehner Junior ◽

Paulo Gustavo Kotze ◽

Juliana Gonçalves Rocha ◽

Eron Fábio Miranda ◽

Maria Cristina Sartor ◽

...

Keyword(s):

Pain Intensity ◽

Bowel Movement ◽

Controlled Study ◽

Control Group ◽

Oral Medications ◽

Average Pain Intensity ◽

Average Pain ◽

The Mean ◽

Double Blinded ◽

Topical Analgesia

OBJECTIVE: To evaluate the effects of topical policresulen and cinchocaine in the postoperative pain behavior of open hemorrhoidectomy.METHODS: We conducted a prospective, double-blinded, controlled study. The control group received the usual guidelines with oral medications. The topical treatment group received, in addition, the application of the ointment and was comprised of two subgroups (policresulen + cinchocaine, and placebo). Pain intensity was recorded with the visual analogue scale.RESULTS: 43 patients were operated on: control group - n = 13, one excluded; placebo - n = 15; and policresulen + cinchocaine - n = 15. The mean age was 45.98 years and 37.2% were men. The average pain intensity was 4.09 (immediate postoperative), 3.22 (hospital discharge), 5.73 (day 1) , 5.77 (day 2), 5.74 (day 3), 5.65 (day 7), 5.11 (day 10), 2.75 (day 15) and 7.70 (first bowel movement), with no difference between groups in all periods.CONCLUSION: This study showed no reduction in pain after hemorrhoidectomy with the use of topical policresulen and cinchocaine.

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