Welcome to ActiveryActivery is a drug delivery specialized in the research, development and production of new drug delivery systems and novel crystal forms. Activery as a young and open minded company would like to respond to the following major challanges in the pharmaceutical industry: - Out of patent of important drugs or blockbusters (products with sales exceeding 1 billion $)
- Insoluble or very poor soluble drugs are the majority of current API (Activer Pharmaceutical Ingredients) and new chemical entities(NCE)
- Enable new routes of administration to big molecules in order to create more convenient ways of treating the pacients.
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Background Nowadays combinatorial chemistry is routinely used as method of choice for the discovery of new drugs. Despite its successes the technique frequently optimizes lead molecules which are poorly or completely insoluble in aqueous media. This insolubility causes low total bioavailability and poses a significant challenge to formulators. Overcoming the solubility challenge has opened possibilities for new solid-state forms with enhanced solubility. Thermodynamically, the amorphous state shows the greatest solubility advantage [1], however it has also the largest propensity to revert to other, less soluble solid-state forms on storage. Further, the lack of a crystal lattice can cause increased degradation or even expose new parts of a molecule to chemical attack leading to additional stability storage problems. The Challenge Preventing the transition into thermodynamically more stable forms is still a major challenge. Amorphous forms of pure drugs are often unstable and recrystallize easily. |
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Background An estimated 80 % of all drugs are delivered orally, with only a small percentage administered via the lung. Historically, these have been medicaments targeted to relieve pulmonary related diseases like asthma. However, efforts to deliver non-pulmonary drugs to overcome first pass metabolism and to discover new routes of administration drugs are increasingly targeted. The key to efficient pulmonary delivery are the right particle size and particle size distribution of the particles. Currently, the desired particle size is often achieved using micronization techniques. These techniques are often classified as ‘top-down’ methods as they involve the comminution of larger particles into smaller ones. Historically, jet-milling has been used extensively in the pharmaceutical industry to provide acceptable particles for different inhaler types. Despite the wealth of knowledge and numerous applications of ‘top-down’ techniques, several important issues, such as crystallinity, solid-state and batch-to-batch consistency regarding particle size and distribution are still a major concern. The Challenge Providing suitable particles with the right particle size and distribution is still a major challenge. Jet-milling frequently generates a substantial amount of fines in the powder, while simultaneously a fraction of the powder is only incompletely milled, leading to lower fine particle fractions (FPF) making larger doses necessary. Further, milling often introduces static electricity onto the powder making them cohesive leading to handling problems and potentially to lower emitted doses (ED) from the device. |
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