Hemorrhoid and anorectal disease treatment method

A method of treating hemorrhoids and diseases of the anorectum by applying to hemorrhoidal or to inflamed or irritated anorectal tissues a treatment composition including by weight carbamide peroxide or benzoyl peroxide in an amount of between about 2% and 40%, an anesthetic in an amount of between about 0.5% and 25%, polyvinylpyrrolidone in an amount of between about 5% and 70% dissolved in glycerine in an amount of between about 10% and 90%, and appropriate surfactants, suspending agents, emollients, humectants and preservatives in an amount of between about 0.1% and 25%.

BACKGROUND OF THE INVENTION 
The present invention relates to an improved method for treating 
hemorrhoids and anorectal diseases by use of a preparation having 
cleansing, healing, antiseptic, re-epithelization, debriding, keratolytic 
properties. 
By way of background, there are numerous preparations for treatment of 
hemorrhoids and anorectal diseases disclosed in the literature which 
include compounds for soothing and healing inflamed hemorrhoidal and 
anorectal tissues. U.S. Pat. No. 2,436,673 discloses the use of 
suppositories containing zinc peroxide for treatment of hemorrhoids. 
However, urea hydrogen peroxide, which is also known as carbamide peroxide 
and hydrogen peroxide carbamide, is not disclosed in the literature for 
treatment of hemorrhoids and other anorectal diseases including fissures, 
fistulas, etc. 
In the past, urea hydrogen peroxide has been disclosed for use in oral and 
otic pharmaceutical preparations (U.S. Pat. Nos. 2,120,430, 3,657,413 and 
4,302,441); for use as an antiseptic (U.S. Pat. No. 2,542,898); and for 
use as an antiseptic when used in combination with glycerol for promoting 
the healing of damaged tissues (U.S. Pat. No. 2,430,450). Urea, by itself 
has been mentioned for use in suppositories, but not as the chemical 
peroxide, urea hydrogen peroxide compound (U.S. Pat. Nos. 1,661,588 and 
4,291,062). Also, benzoyl peroxide has been described for use as a skin 
treatment for such ailments as acne and seborrhea (U.S. Pat. Nos. 
3,535,422, 4,056,611, 4,075,353, 4,163,800 and 4,228,163). U.S. Pat. No. 
4,320,116 discloses a foodstuff and animal feed stuff containing an 
antibacterial system and teaches the use of carbamide peroxide for the 
foregoing purpose. However, none of the foregoing patents or other prior 
art known to applicant has ever used urea hydrogen peroxide or benzoyl 
peroxide in a formulation for treatment of hemorrhoids and other anorectal 
diseases. 
SUMMARY OF THE INVENTION 
It is accordingly one important object of the present invention to provide 
an improved method of treating hemorrhoids and other diseases of the 
anorectum including but not limited to fissures and fistulas, by using a 
preparation containing urea hydrogen peroxide or benzoyl peroxide for 
producing a healing, cleansing, debriding, keratolytic, antiseptic, and 
re-epithelization action on hemorrhoids and anorectal tissues. 
It is a related object of the present invention to provide an improved 
method of treating hemorrhoids and anorectal diseases by the use of a 
composition having an urea hydrogen peroxide or benzoyl peroxide component 
and a vehicle having a sufficiently high molecular weight so that the 
vehicle is not adsorbed through the rectal membranes. Other objects and 
attendant advantages of the present invention will readily be perceived 
hereafter. 
The present invention relates to a method of treating hemorrhoids and other 
anorectal diseases by applying to hemorrhoidal or anorectal tissues a 
treatment preparation comprising a peroxide selected from the group of 
urea hydrogen peroxide and benzoyl peroxide in a pharmaceutically 
effective amount for treatment of hemorrhoidal and anorectal tissues, and 
a vehicle containing said peroxide. In its more specific aspects, the 
vehicle comprises a compound having a sufficiently high molecular weight 
so as not to be adsorbed by the rectal mucosa. Also, in its more specific 
aspects, the preparation contains an anesthetic. The various aspects of 
the present invention will be more fully understood upon a reading of the 
following portions of the specification. 
DESCRIPTION OF THE PREFERRED EMBODIMENTS 
The improved hemorrhoidal and anorectal treatment composition used in the 
present method comprises urea hydrogen peroxide or benzoyl peroxide, an 
anesthetic and a vehicle, and is directed to the basic subject matter of 
copending application Ser. No. 475,342, which is an improvement over the 
subject matter of the present application. In addition, it may also 
contain such added items as aromatics and emulsifiers, such as menthol, 
Polysorbate 80, olive oil, lecithin, and an antifungal or preservative 
agent, as will appear more fully hereafter. The vehicle may be any one of 
numerous anhydrous innocuous watersoluble compounds which are commercially 
available. 
The urea hydrogen peroxide, which is also known as carbamide peroxide and 
hydrogen peroxide carbamide, and which has a formula 
CO(NH.sub.2).sub.2.H.sub.2 O.sub.2, provides a cleansing, healing, and 
oxygenating action on hemorrhoid tissues and on anorectal tissues, such as 
fissures and fistulas. It decomposes to provide epidermal irrigation and 
desquamation (keratolysis), and produces bacteriostatic activity by way of 
damaging bacterial proteins. It also inhibits triglyceride (lipid and 
sebum) hydrolysis, thereby reducing levels of free fatty acids. This tends 
to decrease inflamation of surrounding tissues or lesions. The production 
of oxygen also demonstrates a mild astringent activity on injured tissue 
and, as noted above, hydrogen peroxide exerts a cleansing and debriding 
action through effervescent activity. The urea aids in solubilizing 
organic debris. Oxygen (O.sub.2) stimulates re-epithelization of insured 
or denudated skin or tissue. The degradation byproducts of urea hydrogen 
peroxide are harmless and nontoxic if absorbed through the rectal mucosa. 
The urea hydrogen peroxide can be used in an amount of by weight of 
between about 2%-40%, and more preferably between about 5%-10%, and most 
preferably between about 7% and 10%. Benzoyl peroxide may be used in the 
foregoing amounts in place of carbamide peroxide as the oxygenating agent. 
The improved composition also includes an anesthetic. This compound may be 
Lidocaine, which has the formula C.sub.14 H.sub.22 N.sub.2 O. It is known 
for use epidurally, intravenously for cardiac arrythmia, topically on 
mucous membranes and for peripheral nerveblock. Furthermore, it is an 
accepted safe and effective composition for external rectal use. Being an 
amide and nonester type of anesthetic, adverse and allegeric reactions to 
it are rare. Alternate types of anesthetics which can be used are known as 
dibucaine, diperidon, benzocaine, tetracaine, pramoxine, or others. The 
anesthetics may be present in an amount by weight from between about 0.25% 
to 25%, and more preferably between about 1% and 10%, and most preferably 
between about 1.5% to 10%. 
The vehicle for the urea hydrogen peroxide or benzoyl peroxide and 
anesthetic is a viscous solution of polyvinylpyrrolidone dissolved in 
glycerine. Polyvinylpyrrolidone is also known as P.V.P. and Povidone and 
poly[1-(2-oxo-1-pyrrolidinyl)ethylene]. It is a white to creamy white 
odorless powder which is hygroscopic and is soluble in water, glycerol and 
alcohol. It has a molecular weight of 10,000 to 700,000. Its large 
molecular weight will prevent absorption through the rectal membranes. 
P.V.P. has been used as a plasma expander. It can be used in an amount by 
weight of between 5% and 70%, and more preferably between 20% and 50%, and 
most preferably between 30% and 50%. Glycerine (C.sub.3 H.sub.8 O.sub.3) 
which is an accepted emollient, humectant, lubricant and vehicle is safe 
for internal use. It can be used in an amount by weight of between 5% and 
90%, and more preferably between 7% and 70%, and most preferably between 
10% and 50%. 
The composition preferably also contains a suitable wetting, emulsifying, 
surfactant and suspending agent. One such agent is known as polysorbate 80 
(sorbitan monooleate polyoxethylene) or (TWEEN 80). This or equivalent 
agents can be used in an amount of by weight of between about 1% and 30%, 
and more preferably between about 2% and 15%, and most preferably between 
about 5% and 10%. 
The composition may also contain olive oil for use as an emulsifying and 
suspending agent, emollient and pharmaceutical vehicle. The olive oil may 
be present in an amount of by weight of between about 1% and 20%, and more 
preferably between about 2% and 15%, and most preferably between about 5% 
and 12%. Other acceptable oils may be used in lieu of olive oil. 
An emulsifier which is safe for internal use is also used. Lecithin is 
preferred. It may be used by weight in an amount of between about 1% and 
20%, and more preferably between about 1.5% and 15%, and most preferably 
between about 2% and 12%. 
The composition may also contain an antibacterial or antifungal agent, such 
as methyl p-hydroxybenzoate, benzoic acid and/or acetone sodium bisulfite. 
Substances of this type are included for preventing bacterial or fungal 
growth. Suitable compounds are known under the trade names of 
Methylparaben and Propylparaben. The preservative agent may be present by 
weight in an amount of between about 0.1% and 2%, and more preferably 
between about 0.1% and 1%, and most preferably between about 0.25% and 
0.75%.

Actual preparations have been formulated according to the following 
examples wherein the ingredients are listed in percentages by weight. 
EXAMPLE 1 
______________________________________ 
Zinc Oxide 5.00% 
Urea hydrogen peroxide 
5.00% 
Polyvinylpyrrolidone 
39.48% 
Lidocaine 3.80% 
Glycerine 30.24% 
Polysorbate 80 4.76% 
Olive oil 7.14% 
Methylparaben .50% 
Menthol .50% 
Resorcinol (1,3-benzenediol) 
.190% 
Oil of Eucalyptus .5% 
Lecithin 2.89% 
100.00% 
______________________________________ 
EXAMPLE 2 
______________________________________ 
Urea hydrogen peroxide 
5.00% 
Polyvinylpyrrolidone 
44.48% 
Lidocaine 3.80% 
Glycerine 30.24% 
Polysorbate 80 4.76% 
Olive oil 7.14% 
Methylparaben .50% 
Menthol .50% 
Resorcinol (1,3-benzenediol) 
.190% 
Oil of Eucalyptus .5% 
Lecithin 2.89% 
100.00% 
______________________________________ 
EXAMPLE 3 
______________________________________ 
Urea hydrogen peroxide 
10.00% 
Polyvinylpyrrolidone 
39.48% 
Lidocaine 3.80% 
Glycerine 30.24% 
Polysorbate 80 4.76% 
Olive oil 7.14% 
Methylparaben .50% 
Menthol .50% 
Resorcinol (1,3-benzenediol) 
.190% 
Oil of Eucalyptus .5% 
Lecithin 2.89% 
100.00% 
______________________________________ 
EXAMPLE 4 
______________________________________ 
Urea hydrogen peroxide 
10.00% 
Polyvinylpyrrolidone 
40.17% 
Lidocaine 3.80% 
Glycerine 30.24% 
Polysorbate 80 4.76% 
Olive oil 7.14% 
Methylparaben .50% 
Menthol .50% 
Lecithin 2.89% 
100.00% 
______________________________________ 
EXAMPLE 5 
______________________________________ 
Benzoyl peroxide 10.00% 
Polyvinylpyrrolidone 
40.17% 
Lidocaine 3.80% 
Glycerine 30.24% 
Polysorbate 80 4.76% 
Olive oil 7.14% 
Methylparaben .50% 
Menthol .50% 
Lecithin 2.89% 
100.00% 
______________________________________ 
All of the above formulations were tested on subjects having from moderate 
to severe hemorrhoidal problems and relief from hemorrhoid or anorectal 
disease symptoms was obtained along with actual healing of the tissues. 
As noted briefly above, the product can be formulated as a solid, gel, 
paste, cream, salve, ointment, liquid, and as a powder, depending on the 
ingredients and amounts used and depending on whether additional fats or 
solid greases are added. 
While preferred embodiments of the present invention have been disclosed, 
it will be appreciated that it is not limited thereto, but may be 
otherwise embodied within the scope of the following claims.