摘要:
A method and an apparatus useful for the production of microparticles and nanoparticles are disclosed in which a compressed fluid and a solution including a solvent and a solute are introduced into a nozzle to produce a mixture. The mixture is then passed out of the nozzle to produce a spray of atomized droplets. The atomized droplets are contacted with a supercritical antisolvent to cause depletion of the solvent in the droplets so that particles are produced from the solute. Preferably, these particles have an average diameter of 0.6 .mu.m or less. The invention can be used in the pharmaceutical, food, chemical, electronics, catalyst, polymer, pesticide, explosives, and coating industries, all of which have a need for small-diameter particles.
摘要:
Improved methods and apparatus for particle precipitation and coating using near- or supercritical fluid conditions are described. A fluid dispersion having a continuous phase dispersant and at least one precipitatable substance therein is contacted with a supercritical fluid (SCF) antisolvent so as to generate focused high frequency antisolvent sonic waves, breaking up the dispersion into extremely small droplets; the enhanced mass transfer rates between the droplets and the antisolvent causes precipitation of very small particles on the order of 0.1-10 .mu.m. In coating processes, a turbulent fluidized flow of core particles is created using an SCF antisolvent in an enclosed zone. The core particles are contacted therein at near- or supercritical conditions by a fluid dispersion containing a dispersant together with a precipitatable substance. The antisolvent depletes the dispersant and the substance is precipitated onto the fluidized core particles. In another aspect of the invention, a process for preparing and administering a medicament using only a single container is provided. In such method, a fluid dispersion having a dispersant with the medicament therein is contacted with an antisolvent at near- or supercritical conditions within a use container, so as to directly precipitate small particles of the medicament in the container. The antisolvent is then removed and the use container is sealed with the medicament particles therein. Thereafter, dose(s) of the medicament can be withdrawn from the use container and administered to a patient.
摘要:
Sulfoalkyl ether-cyclodextrin (SAE-CD) based pharmaceutical formulations are provided by the present invention. These formulations comprise SAE-CD derivatives and a therapeutic agent, a major portion of which is not complexed to the SAE-CD. The present formulations are advantageously easier to prepare than other SAE-CD based formulations in the art yet provide similar or improved effectiveness. The SAE-CD derivative can be used to modify the bioavailability and/or rate of bioabsorption of therapeutic agents.
摘要:
Therapeutic compositions comprising the new derivatives of aminooxodihydroisoindolo-quinazoline of the formula ##STR1## are useful in inhibiting the growth of colon and rectal tumors.
摘要:
A sulfoalkyl ether-alkyl ether cyclodextrin (SAE-AE-CD) derivative is provided. The SAE-AE-CD possesses advantages over known SAE-CD and AE-CD derivatives as well as over the parent cyclodextrin by being more water soluble and less membrane disturbing. The SAE-AE-CD includes at least one sulfoalkyl ether group and at least one alkyl ether group even though the degree of substitution for the functional groups can be different. The SAE functional group can be present in molar excess over the AE functional group and vice versa. The total degree of substitution of the cyclodextrin, with respect to both functional groups, can be varied such that a minority or a majority of the hydroxyl moieties of the CD are derivatized. The SAE-AE-CD derivative can be used to solubilize compounds with insufficient water solubility. In some cases, they also stabilize compounds in solution against degradation or to solubilize degradation products formed during degradation. In addition, SAE-AE-CD can also be used for other purposes such as osmotic agents, agents used to mask the taste of problematic drugs. Surprisingly, while AE-CDs are known to be toxic by being membrane disturbing, SAE-AE-CDs are less membrane disturbing and therefore have greater safety.
摘要:
The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water soluble derivatives of aliphatic and aromatic secondary and tertiary amine containing drugs.
摘要:
Sulfoalkyl ether cyclodextrin derivatives and their use as solubilizing agents for water insoluble drugs for oral, intranasal, or parenteral administration are disclosed.