Progress on solid self-microemulsifying drug delivery system for oral administration / 药学实践杂志

Objective To review the newly developed solid self-microemulsifying drug delivery system (S-SMEDDS).Meth-ods Relevant literatures at home and abroad in recent years were consulted and summarized .Results Solid self-microemulsions car-rier, solidification technology and controlled release formulations were discussed , in order to provide relevant references for improving the bioavailability of water-insoluble drugs and the SMEDDS technology for drug release characteristics .Conclusion The utilization of the solid self-emulsifying drug delivery system could significantly enhance the oral bioavailability of water -insoluble drugs .As a new formulation, S-SMEDDS presented huge potential .

Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier.

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 μm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.

Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier.

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 μm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitant-ly bioavailability.

Pharmacokinetics of supersaturable self microemulsion drug delivery system of silybin in rats / 中草药

Objective: To study in vivo pharmacokinetic characteristic of supersaturable self microemulsion drug delivery system (S-SMEDDS) of silybin in rats. Methods: According to the random design, 12 male rats were divided into one control group and one experimental group by six each. SMEDDS of silybin was given to the control group and S-SMEDDS of silybin to the experimental group by both ig administration at dosage of 533 mg/kg, respectively. Blood sampling was conducted by means of an automated blood sampling device (Accusampler) at different time points. After ig administration of S-SMEDDS of silybin to rats, the silybin concentrations in plasma were determined by HPLC and the pharmacokinetic parameters were calculated by non-compartment model of statistical moment analysis. Results: The main pharmacokinetic parameters of the control and experimental groups were as follows: tmax is (1.00 ± 0.40) and (1.50 ± 0.84) h, Cmax is (5.68 ± 0.52) and (16.10 ± 4.06) μg/mL, AUC0→1 is (27.30 ± 3.29) and (82.64 ± 12.36) μg·h·mL-1, respectively. Conclusion: This assessment demonstrates that the oral absorption bioavailability could be substantially improved via the approach: by S-SMEDDS of silybin.