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(11) EP 2 382 973 A1

(12) EUROPEAN PATENT APPLICATION

(43) Date of publication: (51) Int Cl.: 02.11.2011 Bulletin 2011/44 A61K 31/355 (2006.01) A61K 31/728 (2006.01) A61K 36/23 (2006.01) A61K 36/28 (2006.01) (2006.01) (2006.01) (21) Application number: 11003423.8 A61K 36/61 A61K 36/324 A61K 36/42 (2006.01) A61K 9/00 (2006.01) (2006.01) (22) Date of filing: 26.04.2011 A61P 15/00

(84) Designated Contracting States: (71) Applicant: VI.RUS SRL AL AT BE BG CH CY CZ DE DK EE ES FI FR GB 70121 Bari (IT) GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR (72) Inventor: Russo, Vincenzo Designated Extension States: 40126 Bologna (IT) BA ME

(30) Priority: 29.04.2010 IT BO20100264

(54) Composition of rectal suppositories based on n atural extracts for the soot hing and emollient treatment of the anorectal canal.

(57) THE PRESENT INVENTION CONCERNS A PRESENT INVENTION CAN BE USED IN THE SOOTH- PREPARATION FOR TOPICAL RECTAL USE AND ITS ING AND EMOLLIENT TREATMENT OF THE COMPOSITION. ANORECTAL CANAL IN THE PRESENCE OF CON- THE PREPARATION OF THE PRESENT INVEN- GESTIVE CONDITIONS ALSO DUE TO ACUTE AND TION CONTAINS SEED EXTRACT IN CHRONIC PROSTATITIS AND BENIGN PROSTATIC ASSOCIATION WITH OTHER NATURAL SUBSTANC- HYPERTHROPHY FOR EXAMPLE, BUT NOT ONLY, ES SUCH AS FOR EXAMPLE, BUT NOT ONLY, CEN- IN THE FORM OF A SUPPOSITORY. TELLA, HELICHRYSUM AND BOSWELLIA. IN PARTICULAR, THE PREPARATION OF THE EP 2 382 973 A1

Printed by Jouve, 75001 PARIS (FR) 1 EP 2 382 973 A1 2

Description active metabolite, the dihydrotestosterone, which stimu- lates the growth of the prostate. Reducing the levels of FIELD OF THE INVENTION dihydrotestosterone reduces the prostate enlargement. [0006] One purpose of the present invention is to make [0001] The present invention concerns a preparation 5 a preparation which contains natural and not synthetic for topical rectal use and its composition. In particular, substances having the therapeutic effects as described the preparation of the present invention can be used in above in a single product for topical rectal use for the the soothing and emollient treatment of the anorectal ca- prostatic pathologies. nal in the presence of congestive conditions also due to acute and chronic prostatitis and benign prostatic hyper- 10 SUMMARY OF THE INVENTION trophy for example, but not only, in the form of a suppos- itory. [0007] The present invention is set forth and charac- terized in the independent claims. The dependent claims STATE OF THE ART describe other characteristics of the present invention or 15 variants to the main inventive idea. [0002] The main treatments currently available for the [0008] In accordance with the above purpose, a prep- prostatic pathologies are oral drugs and food supple- aration for rectal use according to the present invention ments and they are listed below: comprises the pumpkin extract (1). [0009] It is known from scientific bibliography that the ANTIBIOTICS: Antibiotic therapy is indicated for20 extracted from pumpkin seeds selectively inhibit the acute bacterial prostatitis and chronic bacterial pros- 5-alpha reductase thus blocking the conversion of testo- tatitis. In the acute forms, a therapy including broad- sterone into dihydrotestosterone (2). Because of its an- spectrum penicillins, as well as third generation ce- tiandrogen action, the inhibition of DHT is the main aim phalosporins and aminoglycosides for 10-14 days in the control of benign prostatic hypertrophy. In addition, until disappearance of fever and other systemic25 the β-sitosterol, which is present in the oils extracted from symptoms is sufficient. In the chronic forms, longer pumpkin seeds, is a potent inhibitor of the biosynthesis cycles of 4-8 weeks are necessary. Depending on of prostaglandin (PGE2), a mediator of inflammation that the sensitivity of the infecting microorganism, the causes hyperemia and vascular congestion (3). combination therapy consists of a broad-spectrum [0010] In accordance with some forms of embodiment fluoroquinolone (usually ciprofloxacin) as basic an- 30 of the present invention, the oil extract is tibacterial, which is associated with a macrolide (usu- incorporated in a lipophilic excipient. The lipophilic ex- ally azithromycin). cipient is advantageous in determining the structure of the preparation of the present invention, for example in [0003] ANTI-INFLAMMATORIES: The use of anti-in- the form of suppositories. flammatory drugs is indicated in case of chronic prosta- 35 [0011] In some forms of embodiment, the pumpkin titis; since the therapy consists of a prolonged period of seed oil extract can be combined, in the preparation ac- administration (4-6 weeks, with the possibility of repeat- cording to the present invention, with one or more other ing a second cycle of treatment) it is preferred to use active substances selected from a group containing Cen- drugs that, if administered for long periods, do not cause tella, Helichrysum, Boswellia, Tea Tree oil, Vitamin E ac- any side effects in the stomach. It is preferred the use of 40 etate and hyaluronic acid. As a whole the preparation cortisone anti-inflammatories (corticosteroids and gluco- has a beneficial and salutary effect on the rectal mucosa. corticosteroids. Centella has an antiedemigene action (4), Helichrysum [0004] ALPHA-LYTICS: Alpha-adrenergic receptor and Boswellia (5) give the preparation anti-inflammatory blockers drugs also called alpha-blockers or alpha-lyth- properties and the Teat Tree oil has a mild antibacterial ics such as alfuzosin, tamsulosin, terazosin are admin- 45 action (6). In addition, hyaluronic acid and Vitamin E ac- istered in combination with antibiotic therapy in both etate have soothing and emollient properties (7, 8). acute and chronic prostatitis. Alpha-lythic therapy is [0012] In some forms of embodiment, the active sub- based on the assumption that prostatitis and prostatic stances of the present invention, in particular the pump- congestion are associated with and resulting from the kin seed oil extract, are incorporated into a suppository difficulty in the passage of urine and semen through the 50 provided for the purpose and made to a large extent urethra and in particular through the prostatic urethra due based on said lipophilic excipient. to the hypertonicity of its smooth muscles. Alpha-lytics [0013] The chosen lipophilic excipient has the property act by relaxing the muscles of the bladder neck, prostatic that it melts quickly so that it can be easily eliminated urethra and of the same prostate, thus facilitating the from the body. A lipophilic excipient which is commonly passage of urine into the urethra. 55 used is semi-synthetic glycerides which have these ad- [0005] ANTI-PROSTATICS: Anti-prostatics (such as vantageous properties. Semi-synthetic glycerides are a finasteride and dutasteride) inhibit the activity of 5-alpha mass of triglycerides of hydrogenated fatty acids deriving reductase, the enzyme that converts testosterone to its from and palm heart oil, with the shape and color

2 3 EP 2 382 973 A1 4 of a waxy white pellet and a melting point of between 1 mg and about 8 mg is used. about 34°C and 36°C. When the lipophilic excipient melts [0026] In some forms of embodiment, for the produc- and is eliminated, the active substances, in particular the tion of the preparation according to the present invention pumpkin seed oil extract, stay in situ to interact with the a quantity of Hyaluronic acid is used with a percentage mucosa. 5 in weight comprised between about 0.05% and about [0014] In some forms of embodiment, for the produc- 0.3% with respect to the overall preparation. tion of the preparation according to the present invention [0027] In forms of embodiment of a suppository with a a quantity of pumpkin seed oil extract is used with a per- weight comprised between about 2 g and about 5 g, a centage in weight comprised between about 1.5% and quantity of Hyaluronic acid comprised between about 1 about 12% with respect to the overall preparation. 10 mg and about 6 mg is used. [0015] In forms of embodiment of a suppository with a [0028] The form of embodiment and application by weight comprised between about 2 g and about 5 g, a means of suppositories is particularly advantageous be- quantity of pumpkin seed oil extract comprised between cause it allows the active substances, in particular the about 30 mg and about 240 mg is used. pumpkin seed oil extract, to be kept in the anorectal canal [0016] In some forms of embodiment, for the produc- 15 for a long period and released gradually. tion of the preparation according to the present invention [0029] The above mentioned lipophilic excipients are a quantity of Centella is used with a percentage in weight useful because they give to the suppository, the right comprised between about 1% and about 5% with respect consistency and influence positively the release of the to the overall preparation. active substances, in particular the pumpkin seed oil ex- [0017] In forms of embodiment of a suppository with a 20 tract. weight comprised between about 2 g and about 5 g, a [0030] A preparation as described above also comes quantity of Centella comprised between about 20 mg and within the scope of the present invention, for use in the about 100 mg is used. soothing and emollient treatment of the anorectal canal [0018] In some forms of embodiment, for the produc- inthe presenceof congestive conditions alsodue to acute tion of the preparation according to the present invention 25 and chronic prostatitis and benign prostatic hypertrophy a quantity of Helichrysum is used with a percentage in for example, but not only, in the form of a suppository. weight comprised between about 1% and about 5% with respect to the overall preparation. DESCRIPTIONOF SOME PREFERENTIAL FORMS OF [0019] In forms of embodiment of a suppository with a EMBODIMENT weight comprised between about 2 g and about 5 g, a 30 quantity of Helichrysum comprised between about 20 mg [0031] For suppositories with a weight between about and about 100 mg is used. 2 g and about 5 g, formed for the most part by a lipophilic [0020] In some forms of embodiment, for the produc- excipient, for example semi-synthetic glycerides, signif- tion of the preparation according to the present invention icant results can be achieved in the treatment of anorectal a quantity of Boswellia is used with a percentage in weight 35 mucosa, using the following quantities of active sub- comprised between about 1% and about 5% with respect stances added to the lipophilic excipient: to the overall preparation. [0021] In forms of embodiment of a suppository with a - pumpkin seed oil extract: from about 30 mg to about weight comprised between about 2 g and about 5 g, a 240 mg; quantity of Boswellia comprised between about 20 mg 40 - Centella: from about 20 mg to about 100 mg; and about 100 mg is used. - Helichrysum: from about 20 mg to about 100 mg; [0022] In some forms of embodiment, for the produc- - Boswellia: from about 20 mg to about 100 mg; tion of the preparation according to the present invention - Tea Tree oil: from about 1 mg to about 6 mg; a quantity of Teat Tree oil is used with a percentage in - Vitamin E acetate: from about 1 mg to about 8 mg; weight comprised between about 0.05% and about 0.3% 45 - hyaluronic acid: from about 1 mg to about 6 mg. with respect to the overall preparation. [0023] In forms of embodiment of a suppository with a [0032] One form of embodiment particularly preferred weight comprised between about 2 g and about 5 g, a in the present invention provides to make a suppository quantity of Teat Tree oil comprised between about 1 mg which weighs about 2 g and which uses, as active ingre- and about 6 mg is used. 50 dients, a mixture which contains the following quantities [0024] In some forms of embodiment, for the produc- of substances: tion of the preparation according to the present invention a quantity of Vitamin E acetate is used with a percentage - pumpkin seed oil extract: about 120 mg; in weight comprised between about 0.05% and about - Centella: about 40 mg; 0.4% with respect to the overall preparation. 55 - Helichrysum: about 40 mg; [0025] In forms of embodiment of a suppository with a - Boswellia: about 40 mg; weight comprised between about 2 g and about 5 g, a - Tea Tree oil: about 2 mg; quantity of Vitamin E acetate comprised between about - Vitamin E acetate:about 4 mg;

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- hyaluronic acid: about 2 mg. percentage in weight with respect to the overall prep- aration comprised between about 1.5% and about [0033] In this form of embodiment, to obtain a suppos- 12%. itory of about 2 g, a quantity of about 1752 mg of semi- synthetic glycerides is used as lipophilic excipient. 5 6. Preparation as in any one of the preceding claims, characterized in that it further comprises one or BIBLIOGRAPHY more other active substances selected from a group comprising Centella, Helichrysum, Boswellia, Tea [0034] Tree oil, Vitamin E acetate and hyaluronic acid. 10 1. Pepo. L. Bombardelli E., Morazzoni P. 7. Preparation as in claim 6, characterized in that for Fitoterapia Vo. LXVIII, No 4, 1997 the production thereof a quantity of Centella is used 2. Inhibition of testosterone-induced hyperplasia of with a percentage in weight with respect to the overall the prostate of sprague- dawleyrats by pumpkin seed preparation comprised between about 1% and about oil. Gossell-Williams M, Davis A, O’Connor N. J Med 15 5%. Food. 2006 Summer; 9(2):284-6 3. Treatment of benign prostatic hyperplasia with 8. Preparation as in claims 6 or 7,characterized in phytosterols. Carbin BE, Larsson B, Lindahl O. Br J that for the production thereof a quantity of Heli- Urol. 1990 Dec; 66(6):639-41 chrysum is used with a percentage in weight with 4. Phytotherapeutics: an evaluation of the potential 20 respect to the overall preparation comprised be- of 1000 plants. Cravotto G, Boffa L, Genzini L, Garel- tween about 1% and about 5%. la D. J Clin Pharm Ther. 2010 Feb;35(1):11-48 5. Boswellic acids -components of frankincense- as 9. Preparation as in claims 6, 7 or 8, characterized in the active principle in treatment of chronic inflamma- that for the production thereof a quantity of Boswellia tory diseases. Ammon HP. Wien Med Wochenschr. 25 is used with a percentage in weight with respect to 2002; 152(15-16):373-8 the overall preparation comprised between about 6. Melaleuca alternifolia -Tea Tre- Oil: a Review of 1% and about 5%. Antimicrobial and Other Medicinal Properties. C.F. Carson, K.A. Hammer, and T.V. Riley. Clinical Micro- 10. Preparation as in claims 6, 7, 8 or 9, characterized biology Reviews, Jan. 2006, p. 50-62 Vol. 19, No. 1 30 in that for the production thereof a quantity of Tea 7. Topical vitamins. Burgess C. J Drugs Dermatol. Tree oil is used with a percentage in weight with re- 2008 Jul; 7(Suppl):s2-6 spect to the overall preparation comprised between 8. Beneficial actions of exogenous hyaluronic acid about 0.05% and about 0.3%. on wound healing. King SR. Hickerson WL, Proctor KG. Surgery 1991 Jan; 109(1):76-84 35 11. Preparation as in claims 6, 7, 8, 9 or 10, character- ized in that for the production thereof a quantity of Vitamin E acetate is used with a percentage in weight Claims with respect to the overall preparation comprised be- tween about 0.05% and about 0.4%. 1. Preparation for topical rectal use comprising pump- 40 kin seed oil extract. 12. Preparation as in any one of claims from 6 to 11, characterized in that for the production thereof a 2. Preparation as in claim 1, characterized in that the quantity Hyaluronic acid is used with a percentage pumpkin seed oil extractis incorporatedin a lipophilic in weight with respect to the overall preparation com- excipient. 45 prised between about 0.05% and about 0.3%.

3. Preparation as in claim 2, characterized in that said 13. Preparation as in any one of the preceding claims lipophilic excipient comprises semi- synthetic glycer- for use in the soothing and emollient treatment of the ides. anorectal canal in the presence of congestive con- 50 ditions also due to acute and chronic prostatitis and 4. Preparation as in claim 2 or 3, characterized in that benign prostatic hypertrophy. the preparation is in the form of a rectal suppository formed by said lipophilic excipient, suitable to be in- troduced into the rectal canal. 55 5. Preparation as in any one of the preceding claims, characterized in that for the production thereof a quantity of pumpkin seed oil extract is used with a

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REFERENCES CITED IN THE DESCRIPTION

This list of references cited by the applicant is for the reader’s convenience only. It does not form part of the European patent document. Even though great care has been taken in compiling the references, errors or omissions cannot be excluded and the EPO disclaims all liability in this regard.

Non-patent literature cited in the description

• GOSSELL-WILLIAMS M ; DAVIS A ; O’CONNOR • C.F. CARSON ; K.A. HAMMER ; T.V. RILEY. Mela- N. J Med Food., 2006, vol. 9 (2), 284-6 [0034] leuca alternifolia -Tea Tre- Oil: a Review of Antimi- • CARBIN BE ; LARSSON B ; LINDAHL O. Br J Urol, crobial and Other Medicinal Properties.Clinical December 1990, vol. 66 (6), 639-41 [0034] Microbiology Reviews, January 2006, vol. 19 (1), • CRAVOTTO G ; BOFFA L ; GENZINI L ; GARELLA 50-62 [0034] D. J Clin Pharm Ther., February 2010, vol. 35 (1), • BURGESS C. Topical vitamins. J Drugs Dermatol., 11-48 [0034] July 2008, vol. 7, 2-6 [0034] •AMMONHP. Wien Med Wochenschr, 2002, vol. 152 •KINGSR; HICKERSON WL ; PROCTOR KG. Ben- (15-16), 373-8 [0034] eficial actions of exogenous hyaluronic acid on wound healing. Surgery, January 1991, vol. 109 (1), 76-84 [0034]

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