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Novel galenical system for active transport, method for preparation and useRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical FormNovel galenical system for active transport, method for preparation and use description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070116728, Novel galenical system for active transport, method for preparation and use. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This invention relates to a new galenic system for the protection of an active constituent, particularly a medicine, against degradation during transit in the stomach following oral absorption. [0002] The galenic system according to the invention also enables masking of the taste of an active constituent in the galenic system, if any, stabilisation of the said active constituent, modulation of the release properties of the said active constituent, masking or mucosal irritability effects and toxicity of some active constituents. [0003] The simplest and the most practical therapeutic administration path is oral. In France, this path is used for 75% of all medicines taken (Pharmacie galenique, A. Le Hir-Editions Masson). Galenic forms intended to be taken orally are essentially in two forms, liquid and dry. They have the enormous advantage that they do not require any medical treatment when taking medicine. [0004] The pH of the stomach is between 2 and 6. The acid nature of the stomach environment can cause degradation of active constituents contained in ingested compositions before they have reached the intestine, where theoretically they are absorbed through the intestinal mucous membrane to pass into the circulation. Such a deleterious stomach transit effect could be contradictory to the objective, namely absorption of the said active constituent by the organism in the most efficient form for the required effect. This disadvantage is particularly important for pharmaceutical compositions. [0005] Therefore there is a need for an excipient for active constituents ingested orally, capable of assuring stomach transit for the said active constituent without degrading the said active constituent. This is one of the purposes of this invention. [0006] Other problems are well known, with galenic forms intended to be taken orally, particularly galenic forms for medical purposes. A recurrent problem with these galenic forms is compliance. [0007] Compliance is a capital factor that directly depends on the efficiency of the therapeutic treatment. Compliance, or correct use of the medicine, is defined as being the action of following a medical treatment in accordance with the indications in the prescription; respecting the treatment duration, the number of times and the times during the day that the medicine is taken. A medicine may be inactive or not very efficient if is not taken at a sufficient dose or sufficiently frequently. For intermittent disorders, failure of correct compliance of the treatment can only delay the cure and lead to relapses, sometimes responsible for serious complications. Poor compliance in the case of chronic diseases can cause irreversible damages. [0008] The main difficulties encountered during oral administration vary depending on the presentation. [0009] The disadvantages for dry forms, tablets, capsules, gelatine capsules are deglutition and taste. Some populations such as the elderly, children and some persons with mental disorders must choose the liquid form. [0010] It is very easy to take medicine in liquid form, but this form always faces the unsolved problems of concealing the taste and instability of many active constituents in the aqueous phase. [0011] Another of the objectives of this invention is to propose a galenic system capable of efficiently concealing the taste. [0012] Finally, regardless of the form, irritability, mucosal toxicity and gastro-toxicity problems are also encountered when taking some active constituents, particularly medicines such as anti-inflammatory medicines. [0013] Another purpose of this invention is to propose a galenic system capable of a delayed release of an active constituent, particularly so that it is not released into stomach during ingestion. This property requires the use of a galenic system stable in an acid medium, in other words resistant to an acid pH. [0014] As mentioned in document PCT/US99/27981, page 2, line 4, methods used to minimise bad taste are varied, including the addition of sweeteners, aromas, effervescent formulation and coating technologies. Coating techniques provide the only means of concealing the taste, while other approaches attempt to make the nature of the preparation more appetising. These coating techniques were also selected to prevent the release of gastrotoxic active constituents into the stomach. [0015] Coating techniques consist of putting a layer of isolating compounds, polymers and mixes into place around the active constituent to isolate it from the external environment. Many natural and synthetic polymer compounds have been used to build up this external layer. They include mainly cellulose derivatives such as hydroxypropylmethylcellulose (HPCM), ethylcellulose, carboxymethylcelluloses, hydroxypropylmethylcellulose phthalate or mixes of these products. This technique has given interesting results for varying the release rate and for gastroprotection, but those skilled in the art know that the taste is not concealed satisfactorily and the formulation in water remains unstable in time, which is incompatible with the preparation of aqueous forms such as syrups and suspensions. [0016] Other polymers such as polyacrylate derivatives, amonio-methacrylate polymers or methacrylate proposed by the ROHM Company have been used, as described in document FR 2795962 and WO 98/47493. A lot of work has been carried out with starch and particularly polycarbophiles and Carbopol as described in patent WO 02/092106. [0017] These coating techniques are well known to those skilled in the art. A distinction can be made between physical coating processes based on sprinkling of the coating solution in a turbine or in a fluidised bed as described in patents WO 00/30617 and WO 02/092106 firstly, and secondly physicochemical coating based on coacervation or the separation of phases as described in patent U.S. Pat. No. 3,341,416. All these techniques lead to setting up one or several external polymeric layers covering a central particle composed of the pure active constituent or a mix in the form of granules of active constituents with other support materials as described in document EP 1194125 issued by the Prographarm Company. [0018] We have seen that it was impossible to conceal the taste and keep absorption properties of the initial molecule at the same time. [0019] Immediate release at the digestive tube depends on the use of a dependent pH polymer very sensitive to a pH greater than 7 in the mouth cavity or the stomach, which requires the addition of acid into the final formulation. [0020] These coating techniques have a number of disadvantages: [0021] gastroprotection is not complete [0022] the taste is not completely concealed and the taste of compounds that are very bitter is still too unpleasant [0023] release rates are modified [0024] coating particles have a size of a few hundred microns and are perceptible during absorption. In this case, rupture of the particles can cause a bad taste [0025] coating processes are complex, they include many steps and are expensive. [0026] These technologies are not compatible with preparation of syrups that are stable in the long term. [0027] Therefore these technologies are not fully satisfactory. [0028] The inventors have demonstrated that, surprisingly and unexpectedly, the addition of non-neutralised fatty acids to the compositions of solid lipidic particles prepared according to the process described in patent WO 99/65448 that can contain an active constituent, provides a means of obtaining stable hydrophobic particles in the stomach and that are released only in the digestive tube, thus providing gastroprotection and complete concealing of the taste without modifying the release properties of the active constituent. [0029] Thus, this invention proposes a new galenic system enabling: [0030] gastroprotection, [0031] concealing the taste, [0032] protection of the active constituent, particularly in an acid environment, [0033] the possibility of modulating release properties, [0034] concealing of mucosal irritability effects and toxicity of some active constituents, [0035] the preparation of aqueous forms with a concealed taste, stable and with independent pH. 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