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Abstract
The solubility, absorption and distribution of a drug are involved in the basic aspects of oral bioavailability Solubility is an essential characteristic and influences the efficiency of the drug. Over the last ten years, the number of poorly soluble drugs has steadily increased. One of the progressive ways for increasing oral bioavaibility is the technique of nanoparticle preparation, which allows many drugs to thus reach the intended site of action. Candesartan cilexetil and atorvastatin, belonging to class II of the biopharmaceutical classification system, were chosen as model active pharmaceutical ingredients in this study. Forty samples were prepared either by antisolvent precipitation/solvent evaporation method or by the emulsion/solvent evaporation technique with various commonly used surface-active excipients as nanoparticle stabilizers. All samples were analyzed by means of dynamic light scattering. The particle size of the determined 36 nanoparticle samples was to 574 nm, whereas 32 samples contained nanoparticles of less than 200 nm. Relationships between solvents and excipients used and their amount are discussed. Based on the results the investigated solvent evaporation methods can be used as an effective and an affordable technique for the preparation of nanoparticles.
Highlights
For ensure the pharmacological activity of an active pharmaceutical ingredient (API), the solubility of the API in physiological liquids is required, so that the API can be available at the place of absorption
Both model APIs I and II dissolved in dichloromethane and acetone (2% concentration) were added to aqueous solutions (5%, 10% concentration) of excipients, i.e., eight samples were prepared with each excipient
The systems were stirred for 10 min at 35 °C; afterwards the mixtures were transferred to an ultrasonic bath, where they were mixed again for 40 min, and simultaneously the organic solvent was evaporated
Summary
For ensure the pharmacological activity of an active pharmaceutical ingredient (API), the solubility of the API in physiological liquids is required, so that the API can be available at the place of absorption. When API is dissolved in AC and mixed with water containing a stabilizer, nanoparticles are formed spontaneously and immediately upon mixing This method can be called antisolvent precipitation/solvent evaporation, and the procedure is in principle similar to the evaporative precipitation into aqueous solution [27,28] or the liquid antisolvent precipitation [25]. 12%) of atorvastatin is especially caused by an extensive first-pass metabolism in the liver, the overall solubility of atorvastatin is strictly pH-dependent (many atorvastatin solid dosage forms are buffered, e.g., by carbonates), and administration with food produces a 25% reduction of atorvastatin absorption [33,34] As mentioned, both APIs are BCS class II drugs, their oral bioavailability is solubility rate limited [30,31,32,35,36,37]. If the concentration is too high bubbles appear [46]
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