The bioavailability of violent

A randomized, open, crossover trial comparing Sandoz of cyclosporine A ( cyclosprine, CsA ) solution and soft capsules, the results showed: CsA soft capsules peak and total absorption are larger than the solution, respectively38%,11%, but the peak and trough concentrations are similar. MinDI study of the renal allograft transplantation in a patient with oral soft capsule and solution of bioequivalence, patient compliance. Blood samples with HPLC and fluorescence polarization immunoassay ( FPIA ) determination of peak, peak concentration and area under the curve, and using a paired t test was used to compare, patient compliance using a questionnaire form. The results showed: PFIA, HPLC determination of bioavailability of no significant difference (P > 0.01), CsA capsule and solution of biological equivalent, but most patients are more like the soft capsule.

In 24 healthy men with oral cyclosporine microemulsion solution and emulsion type soft capsule, with a single oral dose of180 mg CsA soft capsule as a reference preparation, in fasting conditions oral solution, orange juice solution, using a specific monoclonal radioimmunoassay in hours. Three serum concentration in13 hours after administration of the peak, the peak concentration of about 1100 ng / ml, the mean area under the curve of 4700 ng / ml / hour, from the degree of absorption and the speed can be judged three of bioequivalence. Therefore, these two kinds of micro emulsion oral preparations in a daily dose of medication, can replace each other without the need for dose adjustment. In addition, with orange juice against the clothing solution does not affect the absorption rate and extent.

SadlerBM study of the HIV1protein inhibitor amprenavir ( amprenavir ) soft, hard capsules pharmacokinetic constants, found two AUC0similar for Cmax differ 1.25 times, if given a high-fat breakfast, soft capsule for AUC0will reduce14%. In 16 healthy male oral hypoglycemic drug gliclazide ( GLI / cazide ) soft capsule and tablet ( Diamicron ), PH7.2, two in vitro dissolution is consistent. In vivo bioavailability parameter study shows: soft capsule and tablet of total absorption ( such as: AUC024, Cmax ) no statistical significance of the differences, but the peak time of soft capsule is much shorter than the tablet. And in the acidic conditions, increase the drug in vitro dissolution can improve gliclazide ( GLI / cazide ) plasma concentration.

The dissolution to effectively release

In solid dosage forms of drug bioavailability and dissolution of closely related, can be a simple in vitro experiments instead of in vivo bioavailability studies. For different drugs and preparations, selective dissolution test method is different, its relevance to the study of inconsistent results.

Japanese scholars using the rotating dialysis cell method ( therotatingdialysiscell, RDC ) and slurry method (thePaddle, PD ) evaluation of ibuprofen ( ibuprofen, IB ) of the dissolution rate in vitro. In vivo beagles dog on the plasma concentrations of IB were determined by RDC method, that can be observed in higher in vivo, in vitro correlation. The researchers also studied the effects of nifedipine ( nifedipine ) soft capsule dissolution tests, found RDC method with N octanol buffer as the dissolution medium, the in vitro dissolution test can better simulate the in vivo release, RDC method in soft capsule dissolution test is effective.

The preparation process to improve the stability of

In order to accelerate the drug from soft capsule dissolution or enhance the stability of the preparation, some polymers have been used and joined to a soft capsule filled with liquid. Research shows that, the addition of specific polymer, surfactant can achieve faster drug release, improve the stability of.

In order to prevent the soft capsule solvent system sol transition,1%,2%,3% PEG6000 or PVP30partially replaces the original matrix in PEG400. When the 2% or3%PEG400PEG 6000replacement, the temperature dependence of the colloid degeneration in40 DEG C is blocked, the solvent system in 4~ 40 C storage8 weeks is stable, the particle size distribution is not changed, and the 1%PEG6000 and PVP 30failed to achieve this goal.

The composition of PEG400, a hydrophobic phase, surfactant systems were screened BC20TX ( Polyoxyethylene20cetylether ) as a" model" surface active agent, can obtain homogeneous, sticky white glue, room temperature with thixotropy, the phase transition temperature of37 DEG C, exactly in line with the needs of filling soft capsule.

Similar reports are: gliclazide ( glicazide ) suspension with PEG400filled capsules, can promote the body's absorption of oral vitamin E; self emulsifying preparation can raise the biological utilization degree.

The soft capsule shells new Diechu

British bioprogress industrial company researchers have found a new rubber, its processing performance and gelatin similar and no animal ingredients, non-toxic, no allergic, is a water soluble biodegradable hydroxymethyl cellulose, is named "X glue". The first batch of production of soft capsule preparation --" bath oil soft capsule", into the tub in a few minutes dissolved. If the X glue can be approved as pharmaceutical excipients and substitution was followed 60 years of gelatin, will have infinite and wide commercial prospect.