《纳米混悬剂（nano suspension）》由会员分享，可在线阅读，更多相关《纳米混悬剂（nano suspension）（14页珍藏版）》请在金锄头文库上搜索。
1、纳米混悬剂（Nano suspension）Research progress of nano suspensionAuthor: Wangyu scientific research sources: literature data, click: 531, update time: 2007-4-3keyword: nanosuspension, sirolimus, aprepitant, insulinHealth net:At present, more than 40% of the drugs in the study have poor water solubility pro
2、blems, which makes the potential good varieties can not be listed or can not give full play to the curative effect. Therefore, it is urgent to solve the problem of low bioavailability of poorly soluble drugs. The commonly used solvent solubilization, cyclodextrin and emulsion technology has some lim
3、itations, such as the co solvent of organic solvents in toxicity, and drug release; the inclusion of the size of the drug molecules with special requirements; requires high drug solubility emulsion in oil phase.In 1994, Muller and other research and development of nano suspension (nanosuspensions) c
4、an better solve the above problems. The nanoparticles are dispersed in water by the stabilization of the surfactant, and stable colloidal dispersions are formed by crushing or controlling the crystallization technique. Whether it is water insoluble drugs or drugs that are difficult to dissolve in wa
5、ter and are difficult to dissolve in oil, the corresponding nano suspension can be prepared by this method. As an intermediate dosage form, the nano suspension can be further prepared as a pharmaceutical dosage form suitable for oral administration, injection or other route of administration, thereb
6、y improving the absorption and bioavailability of the drug. Moreover, nano suspension can improve the content of the drug in the preparation, and is especially suitable for oral administration and injection of large dosage and difficult soluble medicine. In addition, because the formulation does not
7、 contain the carrier and the co solvent, the injection has the poisonous side effect to be very low.Preparation characteristicsNano suspension is the colloidal dispersion system of pure drug nanoparticles. Different from the matrix type nano system in the traditional sense, nanosuspension without ca
8、rrier material, it is through the stabilizing effect of the surfactant, the drug particles of nano scale dispersion system formed in water.Because of the characteristics of nanosuspension, which reflects the unique advantages in various administration (Table 1): such as simple prescription and prepa
9、ration, is conducive to the rapid screening of active compounds to reduce the cost and improve the drug dissolution and bioavailability, without additional ingredients caused by irritating and toxic effect and low dose volume etc.Table 1 Characteristics of pharmaceutical suspensions- - - - - - - - -
10、 - - - - - - - - - - - - - - - - - - - - - -Route of administration, dosage forms, characteristics- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -The oral administration has the advantages of small particle size, increased drug absorption rate and absorption rate, and improved bioavaila
11、bilityHigh drug content, increased mucosal adhesion, prolonged gastrointestinal retention time, and reduced individual differences in absorptionFirst pass metabolism is avoided and targeted therapy can be used to treat lymphatic system diseasesInjection without carrier or cosolvent, reduced toxicity
12、, reduced dosage (especially intramuscular, subcutaneous, and intradermal)High drug content, phagocytosis by monocytes, reduced toxicity, and increased effectivenessTwain -80 was used to deposit apo E on nanoparticlesReceptors on brain endothelial cells promote brain absorptionInhaled drugs were sma
13、ll in size, targeting alveolar macrophages, increasing respiratory tract drug absorption, and reducing systemic absorption- - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -PreparationThere are mainly two aspects of preparation of nano suspension, namely prescription screening and process
14、optimization. The prescription is mainly the choice of type and amount of surfactant, in order to improve the long-term stability of the product; process optimization by adjusting the production process such as pressure and cycle number and other parameters of the high pressure homogenizer, the idea
15、l particle size distribution.Screening of surfactantsIn order to prepare stable nano suspension and avoid the aggregation and increase of nanoparticles, the appropriate surfactant must be screened. Ionic and nonionic surfactants are generally available, and ionic surfactants can cause electrostatic
16、repulsion between nanoparticles. Non ionic polymers cause steric repulsion between nanoparticles. Studies have shown that the combination of two types of surfactants can lead to better long-term stability.In the preparation of nano suspension by direct homogenization method, the type and amount of surfactant only affect the long term stability of the product, and the particle size of the
