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Solid support for self- emulsifying drug delivery system of micro-

Author: HuanZuo
Tutor: YiTao
School: Southwestern University
Course: Pharmaceutical Analysis
Keywords: Since the micro- emulsifying drug delivery system Water- insoluble drugs Solid carrier Lipolysis Indomethacin Hydroxypropylmethylcellulose Silica powder β- cyclodextrin Absorb
CLC: R943
Type: Master's thesis
Year: 2011
Downloads: 111
Quote: 1
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Abstract

Since the micro-emulsifying drug delivery system (self-microemulsifying drug delivery system, SMEDDS) can significantly improve the water-insoluble drugs for oral bioavailability. However, the traditional forms SMEDDS more liquid, there is a complex production process taking inconvenience, a single dosage form, the capsule shell formulation ingredients compatibility and long-term storage leaks and other problems may occur capsule; other SMEDDS may be gastric juice after oral administration diluted dispersion, because intestinal lipolysis lipase digestion led to some precipitation of the drug from the system, is not conducive to drug absorption. To overcome the shortcomings of SMEDDS, solid self-micro-emulsifying drug delivery system (solid self-microemulsifying drug delivery system, S-SMEDDS) began to be studied. S-SMEDDS SMEDDS and solid formulations combining the dual advantages: on the one hand by adding a variety of solid materials SMEDDS the traditional solid preparation, coating technology can also be prepared using the controlled release formulations, rich SMEDDS formulations; another , the choice of suitable solid materials will help suppress SMEDDS curable water-insoluble drugs in the gastrointestinal tract crystalline precipitate. Solid carrier selection is S-SMEDDS ability to maintain existing conventional liquid SMEDDS vivo advantage of the important factors, including drug loading capacity SMEDDS digestive and gastrointestinal effects. To solve these problems, this paper indomethacin as a model drug preparation liquid SMEDDS, studied three different solid support structure that hydroxypropyl methylcellulose (hydroxypropylmethylcellulose, HPMC), silica powder and β-cyclodextrin SMEDDS of The main impact of research are: (1) HPMC is widely used in oral formulations of hydrophilic materials, molecular structure having a hydrophilic lipophilic group, with the promotion of emulsification and surface active role. With indomethacin as a model drug preparation SMEDDS, using simulated gastric dispersion test and measurement models in vitro lipolysis in three sizes HPMC (K4M, K15M, K100M) and different concentrations of HPMC K100M right SMEDDS gastrointestinal behavior. The results showed that all three sizes of HPMC SMEDDS inhibit the dispersion in the precipitation of the gastrointestinal tract, with the HPMC viscosity increases, the ability to inhibit the precipitation did not change significantly, drug loading capacity enhancement; HPMC viscosity, and with the increasing of the concentration of 0-5min lipolytic increase the rate of lipolysis and the aqueous phase after the drug distribution. Prepared by spray drying using the S-SMEDDS, in vitro release results show that with the increase in viscosity HPMC, in vitro release rate slows down to a low viscosity HPMC as the carrier S-SMEDDS release mechanism of diffusion and erosion of the mixing mechanism of the skeleton; with high viscosity HPMC as the carrier of S-SMEDDS release mechanism for the skeleton dissolution. (2) silica powder has good biocompatibility, stability, and hydrophilicity. With indomethacin as a model drug preparation SMEDDS, with silica powder prepared from the solid support as the main micro-emulsifying pellets (self-microemulsifying pellets, SMEP), examine the small intestine aerosil right SMEDDS vitro lipolysis and SMEP two effects , and then using the new in vitro lipolysis - absorption model aerosil right SMEP intestinal absorption. The results showed that silica powder can raise the rate of lipolysis, increased lipolysis after the aqueous dispersion of colloidal drug distribution, promotion of drug absorption; would delay the S-SMEDDS vitro, affect drug absorption rate; resulting off-on S-SMEDDS small intestinal absorption is not significantly affected. (3) p-cyclodextrin having a hole structure can be improved by the inclusion of a guest molecule bioavailability. With indomethacin as a model drug preparation SMEDDS, study β-cyclodextrin SMEDDS intestinal lipolysis effect. The results showed that, β-cyclodextrin increase lipolysis distribution into the aqueous phase after concentration of the drug. Prepared by spray drying using S-SMEDDS, in vitro release test showed β-cyclodextrin S-SMEDDS in vitro release was significantly faster than the commercially available tablets; vitro intestinal absorption measurement results revealed that β-cyclodextrin as a solid vector S-SMEDDS and SMEDDS vitro intestinal absorption was significantly better than the commercially available tablets, with time, S-SMEDDS in vitro intestinal absorption edge starting to show. In this paper, different in vitro model to study three kinds of solid support for SMEDDS impact study has yielded good results, the next step method can be used in vivo pharmacokinetic studies in vivo absorption of S-SMEDDS in order to better evaluate the solid support on the oral bioavailability of SMEDDS effects to reveal the influence of the solid support on the absorption law for S-SMEDDS prescription screening and provide a basis for evaluation in vivo.

Solid support for self- emulsifying drug delivery system of micro-

Abstract

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