Abstract:
The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form. More specifically, the invention relates to a solid oral drug form comprising anti-misuse means and at least one active ingredient, which is characterized in that: at least part of the active ingredient is contained in microparticles; and the anti-misuse means comprise anti-crushing means (a) which enable the microparticles of the active ingredient to resist crushing, such as to prevent the misuse thereof. According to the invention, the drug form can also comprise means (b) for preventing the misuse of the active ingredient following a possible liquid extraction process.
Abstract:
The invention relates to an osteogenic synergic composition comprising at least one osteogenic growth factor, and at least one growth factor having a chemoattractant and angiogenic capacity. It also relates to the method for the preparation thereof and to the use thereof for the preparation and production of pharmaceutical products for use in bone reconstruction and regeneration, in the form of topical compositions, for example implants, pastes or gels.
Abstract:
An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents. Said oral solid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.
Abstract:
The present invention is directed to a suspension of particles for delivering active principles, in particular proteins. Said particles are based on a diblock copolymer consisting of a neutral hydrophobic alpha hydroxy carboxylic acid polymer block and a hydrophilic linear polyaminoacid block with peptide alpha chaining, at least partly ionized. Said alpha hydroxy carboxylic acid polymer/linear polyaminoacid delivery particles spontaneously obtainable in the absence of surfactant can be stable. Said delivery particles are capable of being associated undissolved in colloidal suspension with at least an active principle and of delayed or prolonged release thereof. The invention is also directed to a powdery solid from which are derived the delivery particles and the preparation of said solid and said delivery particle suspension.
Abstract:
The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system consists of microcapsules (200 to 600 μm) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5. These microcapsules have a dissolution behavior in vitro such that, at a constant pH of 1.4, a latency phase of between 1 and 5 hours is observed, followed by a release of the AP, and such that the change from pH 1.4 to pH 6.8 results in a release of the AP without a latency period in vitro.
Abstract:
Novel organosilicon compounds having a second order hyperpolarizability coefficient .beta. greater than zero, well suited for use in the field of nonlinear optics, e.g., in telecommunication devices, have the general formula: ##STR1## which n is an integer ranging from 1 to 20; R.sub.1 is an electron donating group; R.sub.2 is an electron accepting group; R.sub.3 is an alkyl radical having from 1 to 8 carbon atoms, a hydrogen atom, an aryl radical, or an R.sub.1 or R.sub.2 radical; and R.sub.4 is an alkyl radical having from 1 to 8 carbon atoms, a hydrogen atom, an aryl radical, or an R.sub.1 radical when R.sub.3 is not an R.sub.2 radical or an R.sub.2 radical when R.sub.3 is not an R.sub.1 radical.
Abstract:
Hydrogenated silanes are facilely prepared by redistribution, by reacting (1) a silane having the formula H.sub.m SiX.sub.4-m in which X is halogen or an alkoxy group and m is an integer equal to 0, 1, 2 or 3, with (2) an alkyl or aryl hydrosilane having the formula R.sub.n H.sub.p SiX'.sub.4-(n+p) in which X' is halogen or an alkoxy group, R is an alkyl or aryl group and n and p, which may be identical or different, are integers equal to 1, 2 or 3, with the proviso that n+p.ltoreq.4, in the presence of (3) a catalytically effective amount of a catalyst comprising (i) a quaternary ammonium salt having the formula R'.sub.4 NY or a quaternary phosphonium salt having the formula R'.sub.4 PY, in which formulae R', which may be identical or different, are each a monovalent hydrocarbon radical and Y is halogen, (ii) a tertiary amine of the general formula NR'R"R"', in which R', R" and R"', which may be identical or different, are monovalent hydrocarbon radicals, or (iii) an ion exchange resin comprising tertiary amine or quaternary ammonium groups.
Abstract:
Novel polyoxaalkyl aminoalcohols, well adapted for the complexation/solubilization of a wide variety of cations, have the structural formula: ##STR1##
Abstract:
Polymeric, advantageously elastomeric, e.g., natural or synthetic rubber, matrices including a reinforcing amount of a filler therefor, e.g., inorganic particulates, further comprise, as an interfacing additive between the matrix and the reinforcing filler, the condensation product of at least one polyamine with at least one carboxylic acid.
Abstract:
Novel polyoxaalkyl aminoalcohols, well adapted for the complexation/solubilization of a wide variety of cations, have the structural formula: ##STR1##