Pharmaceutical composition of a papillomavirus inhibitor
Inventors
Blumenfeld, Marta • Compere, Delphine • Francon, Patricia • Hutin, Michel
Assignees
Publication Number
US-9670159-B2
Publication Date
2017-06-06
Expiration Date
2033-05-07
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Abstract
The invention relates to a pharmaceutical composition including a compound of general formula (I) combined with a solvent and a viscosity-enhancing agent, as well as to the use thereof as a drug, in particular for treating and preventing infection with the papillomavirus, and to the method for preparing same.
Core Innovation
The invention relates to a pharmaceutical composition comprising a compound of general formula (I), combined with a solvent and a viscosity-enhancing agent. The compound of formula (I) includes specified chemical groups, such as an aryl, cycloalkyl, or heterocycle as A, and an aryl or heterocycle as B, with various substituent possibilities detailed in the description. The composition particularly features a viscosity-enhancing agent like hydroxypropylcellulose and a solvent such as propylene glycol, forming a gel suited for topical application.
The problem addressed by the invention is that while compounds useful for treating and preventing papillomavirus infections were disclosed in prior art (WO 2007/135106), there was no description of pharmaceutical formulations to effectively deliver these compounds, especially for topical use. Additionally, the composition aims to enable simple preparation and ensure rapid and high release of the active ingredient.
The invention provides a detailed method for preparing the pharmaceutical composition, which involves mixing the active compound in part of the solvent and combining it with the viscosity-enhancing agent dissolved in the remaining solvent. The resulting product is a gel with defined viscosity and concentrations of components, optimally enhancing the delivery and stability of the papillomavirus-inhibiting compound. The innovation covers specific salts, including a potassium salt of the active ingredient, which increases solubility and is especially suitable for formulating into pharmaceutical compositions for the prevention and treatment of papillomavirus infections.
Claims Coverage
The patent includes several independent claims covering distinct inventive features related to the pharmaceutical composition, its specific ingredients, preparation method, and medical use.
Pharmaceutical composition comprising a compound of general formula (I), solvent, and viscosity-enhancing agent
The composition includes: - A compound of general formula (I) or a pharmaceutically acceptable salt thereof, as defined by chemical structure and substituents in the description. - A solvent selected from propylene glycol, glycerol, polyethylene glycol, or mixtures thereof. - A viscosity-enhancing agent, including hydroxypropylcellulose, hydroxypropylmethylcellulose, a carbomer, or mixtures thereof.
Method of preparing the pharmaceutical composition
Steps involved: 1. Mixing the compound of formula (I) in a part of the solvent to form solution A. 2. Mixing the viscosity-enhancing agent in the remaining part of the solvent to form solution B. 3. Mixing solutions A and B to yield the pharmaceutical composition.
Method for treating papillomavirus infection using the pharmaceutical composition
This method comprises administering to a person in need thereof an effective amount of the pharmaceutical composition containing the compound of formula (I), solvent, and viscosity-enhancing agent. The composition is intended for the treatment of papillomavirus infections, specifically including HPV6 or HPV11.
Method for treating lesions or diseases associated with papillomavirus infections
This method includes administration of an effective amount of the pharmaceutical composition to treat lesions or diseases associated with papillomavirus infections. The conditions covered include anogenital warts (such as condyloma acuminata and condyloma lata), laryngeal, conjunctival or oral papillomas, recurrent respiratory papillomatosis, intraepithelial neoplasia, bowenoid papulosis, various types of warts, epidermodysplasia verruciformis, and carcinomas.
The inventive features protect a pharmaceutical composition of a specific papillomavirus-inhibiting compound with a particular formulation, a method of manufacture involving separate preparation steps for ingredients, and therapeutic methods for treating papillomavirus infections and related diseases.
Stated Advantages
The pharmaceutical composition is simple to prepare and enables rapid and high release of the active ingredient.
The potassium salt form of the active compound increases solubility and facilitates product formulation compared to the hydrochloride form.
The composition achieves a high local concentration of active ingredient in the skin with low systemic exposure after topical application.
Very good tolerance was demonstrated in preclinical and clinical studies, with no local reactions or adverse effects observed.
The composition is stable in appearance, viscosity, and active ingredient concentration under various storage conditions.
The presence of propylene glycol provides antimicrobial preservation, obviating the need for additional preservatives.
The formulation retains the biological activity of the active ingredient against papillomavirus in both formulated and non-formulated states.
Documented Applications
Prevention or treatment of papillomavirus infection, particularly HPV6 or HPV11.
Treatment of lesions or diseases associated with papillomavirus infections, including anogenital warts, condyloma acuminata and condyloma lata, laryngeal, conjunctival or oral papillomas, recurrent respiratory papillomatosis, intraepithelial neoplasia, bowenoid papulosis, common, plantar, myrmecia, superficial or flat warts, epidermodysplasia verruciformis, and carcinomas.
Topical application to the skin or mucous membranes, especially the anogenital region, as a gel formulation.
Local injection in or around a lesion or tumor.
Oral administration can also be envisaged.
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