Die Arzneimittelversorgung in der Onkologie zeichnet sich durch einige Besonderheiten wie die Verordnung von Rezepturarzneimitteln aus. Neu zugelassene Medikamente beinhalten Biopharmazeutika sowie ...Proteinkinasehemmer. Die klassischen Rabattverträge für Generika erbringen keine weiteren Einsparungen. Die Möglichkeit, nach AMNOG für patentgeschützte Arzneimittel einen Erstattungsbeitrag zu verhandeln, wird kontinuierlich genutzt. Die Ausschreibung der Zubereitung ist durch das AMVSG wieder entfallen.
The purpose of the study was to develop and evaluate different lipid-based formulations for parenteral administration, as potential novel carrier systems for lipophilic drugs, and to turn an unstable ...drug such as chlorambucil into a useful one.
A two-stage, high-pressure homogenizer was used to yield a very fine monodispersed lipid nanosphere. The strategy of combining egg yolk phospholipid and nonionic emulsifier (Lutrol F 68 and Tween 80) as an emulsifier mixture was adopted to increase safety and tolerance. The final lipid nanospheres, in a lipophilic mixture consisting of three components, monostearin, medium-chain triglycerides and soya oil, were evaluated for physicochemical properties, such as particle size, surface morphology, drug-entrapment efficiency, drug-loading capacity, lyophilization and in vivo drug-release behavior.
A monodispersed lipid nanosphere with a mean particle size ranging from 90 to 150 nm was achieved. The optimized injectable cryoprotectants for lipid nanosphere were sucrose (7.5%) and mannitol (7.5%), which can stabilize the particle size (LD50) at approximately 129 nm after reconstitution. The results show that the formulation can effectively administer anticancer drugs and thus improve patient quality of life.
The novel lipid nanosphere complex developed is a useful anticancer drug delivery vehicle for parenteral administration. The formulation strategy has the potential for the development of further methods of drug delivery for a wide variety of anticancer drugs.
A novel parenteral formulation for tetrazepam (10 mg/ml) was developed using lipid emulsions. This formulation utilized a new lipid emulsion formulation, which was developed by changing the polarity ...of the oil phase. It was found that increasing the polarity of the oil phase resulted in enhanced solubility of tetrazepam. Tetrazepam showed higher solubility in a mixture of castor oil and middle-chain triglycerides (MCTs) (1:1) than in any other oil investigated. This mixture resulted in low interfacial tension and moderate viscosity, which seemed to be the optimum oil phase. In addition, to increase the concentration of tetrazepam, an emulsion formulation containing 30% oil phase was produced and optimized. The drug-free emulsion formulation showed fine particle sizes with an imperceptible change in physicochemical properties after more than 2 years on the shelf. As a result, it was possible to produce a parenteral emulsion formulation containing 10 mg/ml tetrazepam. No change in the physicochemical properties of the emulsion was observed after the addition of tetrazepam. The tetrazepam emulsion showed stable behavior during the autoclaving process and good shelf stability for at least 10 months as well. Tetrazepam itself also displayed good stability during the autoclaving process and also showed good shelf stability in this emulsion formulation.
Cyclodextrins are able to form inclusion complexes with a number of drugs if their molecular dimensions correspond to those of the cyclodextrin cavity which leads to change of physicochemical and ...biopharmaceutical properties of drugs. 2-Hydroxypropyl beta cyclodextrin (HP beta CD) is suitable for parenteral application because of its considerable solubility in water and low hemolytic activity. Digoxin is insoluble in water, sensitive to light and is a subject of acidic hydrolysis, it is a challenge to the technologists of parenteral dosage forms. Dexamethasone (Dex) has a very small solubility in water (0.1 mg/ml), which caused troubles by preparing liquid medicine forms. The inclusion of hydroxy acids in CD-complexes in the necessary molar proportions leads to considerable increase in the solubility of a medicine and to several times decrease of the amount of CD used. Inclusion complexation was confirmed by the results from the studies of Differential Scanning Calorimetry. The present investigation demonstrated that Digoxin/CD complex shows stability in water medium and the optimum molar ratio Digoxin/HP beta CD is 1:6. The same results can be achieved through HP beta CD, by including Dex in a multicomponent composition containing HP beta CD and citric acid in a molar ratio of 1:4:1.
► Introduce nanocrystals as commercially viable pharmaceutical products. ► Review different methods of producing nanocrystals. ► Review parenteral applications of nanocrystals. ► Discuss remaining ...challenges in the development of nanocrystal products.
Nanocrystals have drawn increasing interest in pharmaceutical industry because of the ability to improve dissolution of poorly water-soluble drugs. Nanocrystals can be produced by top-down and bottom-up technologies and have been explored for a variety of therapeutic applications. Here we review the methods of nanocrystal production and parenteral applications of nanocrystals. We also discuss remaining challenges in the development of nanocrystal products.
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