Effects of supercritical carbon dioxide processing on optical crystallinity and in vitro release of progesterone and Gelucire 44/14 solid and semi-solid dispersions

Blackcurrant juice (Ribes nigrum L.) was subjected to supercritical carbon dioxide (SCCD) at 10, 30 and 60 MPa for 10 min at 45°C as well as thermally treated at 45°C and 85°C for 10 min to determine the stability, antioxidant capacity (AC) and bioaccessibility (BAc) of vitamin C, total anthocyanins and their individual monomers. An in vitro gastrointestinal digestion model completed with dialysis was used to assess BAc. The use of SCCD at each of the pressures applied improved the stability of vitamin C, total anthocyanins, and AC before in vitro digestion. As a result of digestion, L-ascorbic acid was oxidized to L-dehydroascorbic acid, and finally, the total content of vitamin C, anthocyanins, and AC decreased. SCCD did not significantly improve the BAc of vitamin C and total anthocyanins. The highest BAc of vitamin C was noted in fresh juice (FJ) (40%) and after mild heat treatment at 45°C (T45) (46%). The highest BAc of total anthocyanins was also noted in the FJ (4.4%). The positive effect of the application of SCCD on the BAc of the delphinidin-3-O-glycosides was observed compared to T45 and thermal pasteurization at 85°C (T85). Moreover, cyanidins were generally more bioaccessible than delphinidins in all samples. AC after digestion was higher in SCCD samples compared to thermally treated measured using ABTS+• and DPPH• assays, whereas in dialysate similar trends were observed only for AC measured using the ABTS+• assay. This phenomenon was justified by the formation of individual metabolites detected by UPLC-PDA-MS / MS in the model experiment with delphinidin-3-O-rutinoside. The protocatechuic acid which is well known as a strong antioxidant was detected in the model experiment after digestion. Further research is needed to better understand the metabolic pathway of anthocyanins and the possible uses of SCCD to improve the health properties of fruit products.

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Assessment of “Sameness” and/or Differences between Marketed Creams Containing Miconazole Nitrate Using a Discriminatory in vitro Release Testing (IVRT) Method

Scientia Pharmaceutica ◽

10.3390/scipharm88010006 ◽

2020 ◽

Vol 88 (1) ◽

pp. 6

Author(s):

Potiwa Purazi ◽

Seeprarani Rath ◽

Ashmita Ramanah ◽

Isadore Kanfer

Keyword(s):

Drug Release ◽

In Vitro Release ◽

Vertical Diffusion ◽

Discriminatory Ability ◽

Miconazole Nitrate ◽

Performance Verification Test ◽

Semi Solid ◽

Vitro Release ◽

Release Testing

In vitro release testing (IVRT) provides an efficient method for the evaluation of drug release from semi-solid formulations. The aim of this research was to develop and validate a discriminatory IVRT system using vertical diffusion cells (VDCs) to assess generic topical products containing miconazole nitrate (MCZ). A comprehensive approach addressing all essential suitability criteria supporting the reliability of IVRT results was applied. These include mechanical validation of the VDCs, a performance verification test (PVT), validation of the analytical method (HPLC) used to quantify the drug release and validation of the IVRT method to confirm its precision, reproducibility, discriminatory ability, and robustness. Two marketed generic products were tested and assessed in accordance with the acceptance criteria for “sameness” in the FDA’s SUPAC-SS guidance which requires that the 90% confidence interval (CI) should fall within the limits of 75%–133.33%. One product was found to be in vitro equivalent to the reference product whereas the other was not. The results confirmed the suitability of the IVRT method to accurately measure the release of MCZ from topical cream products and, importantly, demonstrated the necessary discriminatory ability to assess “sameness”/differences of dermatological creams containing MCZ. Furthermore, the developed IVRT method was able to detect differences between formulations, which may be attributed to qualitative (Q1) and quantitative (Q2) properties and the microstructure and arrangement of matter (Q3).

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Inclusion Complex Formation of Water- Soluble Drug, Captopril, and Peracetylated-β-Cyclodextrin in Supercritical CO2 for Controlled Release Applications

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.342-343.489 ◽

2007 ◽

Vol 342-343 ◽

pp. 489-492 ◽

Cited By ~ 6

Author(s):

Hullathy Subban Ganapathy ◽

Min Hee Woo ◽

Yeong Soon Gal ◽

Kwon Taek Lim

Keyword(s):

Carbon Dioxide ◽

Inclusion Complex ◽

In Vitro Release ◽

Water Soluble ◽

Inclusion Complex Formation ◽

Hydrophobic Properties ◽

Water Soluble Drug ◽

Xrd Studies ◽

Vitro Release

The inclusion complex of CO2-soluble peracetylated-β-cyclodextrin (PAc-β- CD), heptakis(2,3,6-tri-O-acetyl)-β-cyclodextrin, and highly water-soluble drug captopril, was prepared by a chemical solvent-free method using supercritical carbon dioxide. The captopril-PAc-β-CD inclusion complex was further confirmed by DSC and XRD studies. In- vitro release of captopril from an oily suspension confirmed that the dissolution rate of captopril was much retarded from the inclusion complex as a result of the hydrophobic properties of PAc-β-CD.

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