摘要:
An aerosol solution composition for use in an aerosol inhaler comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler.The composition is stabilized by using a small amount of mineral acid and a suitable can having part or all of its internal metallic surfaces made of stainless steel, anodized aluminium or lined with an inert organic coating.
摘要:
The device comprises conventionally a plug (2) for the electrical supply of a heater element (14) to bring about the heating and evaporation, by way of a flat wick (10), of an active substance contained in a main receptacle (5). The novelty lies in the fact that said container (5) is heat-formed and defines a triangular configuration reservoir (6) with a flat extension (7) that accommodates the flat “Y”-shaped wick (10) in which the ends of its divergent arms (11) are engaged in recesses (9) in the mouth of the active substance reservoir (6), said wick (10) being pressed by an impermeable strip (12) which is heat-sealed to the body of the reservoir (6), so that the heater element (14) positioned facing the front end of the extension (7) brings about the warming of the wick (10) and the corresponding evaporation of the active substance, which will issue by way of a hole (16) in the impermeable strip (12) to be diffused in the environment. In the plug-in position the device remains with the container (5) of the wick (10) in the vertical position, and in direct contact of this with the active substance contained in the reservoir (6).
摘要:
The invention concerns a storage stable pharmaceutical formulation comprising preferably two active compounds in a non-swellable diffusion matrix, whereby the compounds are released from the matrix in a sustained, invariant and, if several compounds are present, independent manner and the matrix is determined with respect to its substantial release characteristics by ethylcellulose and at least one fatty alcohol. The invention also concerns methods for producing such pharmaceutical formulations.
摘要:
The invention relates to a method of producing hollow, microporous particles which are intended, in particular, to be inhaled or for any other application. The inventive method consists in: providing a composition, in a given form, comprising at least one active principle and at least one blowing agent; cooling the aforementioned composition to below the solidification point of said at least one blowing agent so as to increase the volume of the given form and to create ruptures in the surface and/or in all of said given form, thereby enabling the structure of the hollow, microporous particle to be obtained; and removing all or part of said at least one blowing agent.
摘要:
The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain; B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.
摘要:
Inhalable pharmaceutical compositions are provided, for use in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD). These compositions have high storage stability, and include formoterol and a corticosteroid.
摘要:
Improved aerodynamically light particles for drug delivery to the pulmonary system, and methods for their synthesis and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of biodegradable material and have a tap density of less than 0.4 g/cm3 and a mass mean diameter between 5 μm and 30 μm. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear α-hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 μm, can be used for enhanced delivery of a therapeutic agent to the alveolar region of the lung. The aerodynamically light particles incorporating a therapeutic agent may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide variety of therapeutic agents.
摘要翻译:提供用于向肺系统输送药物的空气动力学轻微颗粒,以及用于其合成和给药的方法。 在优选的实施方案中,空气动力学轻微颗粒由可生物降解的材料制成,并且具有小于0.4g / cm 3的振实密度和5μm和30μm之间的质量平均直径。 颗粒可以由可生物降解的材料如可生物降解的聚合物形成。 例如,颗粒可以由官能化的聚酯接枝共聚物形成,所述聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚(氨基酸)侧链组成 集团在聚酯骨干。 在一个实施方案中,具有大平均直径(例如大于5μm)的空气动力学轻微颗粒可用于增强治疗剂递送至肺的肺泡区域。 掺入治疗剂的空气动力学轻微颗粒可以被有效地雾化,用于给予呼吸道以允许全身或局部递送多种治疗剂。
摘要:
The present invention provides active, hydrophilic polymer-modified derivatives of insulin. The insulin derivatives of the invention are, in one aspect, suitable for delivery to the lung and exhibit pharmakokinetic and/or pharmacodynamic properties that are significantly improved over native insulin.