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Biomedical subjects

P Piccerelle

Publications and source records attributed to P Piccerelle.

7 recordsLinked to original sources

In-vitro comparative study of buccal mucoadhesive performance of different polymeric films.

A comparison of the buccal mucoadhesive performance of different polymeric films was carried out using texture analyzer TA-XT2i. A large range of putative polymers differing in their chemical nature, molecular structure as well as hydration status was used. The used polymeric films were classified in rank order of buccal mucoadhesive performance, namely carbopol 971P>polycarbophil>Carrrageenan type lambda > Sodium carboxymethylcellulose. Swelling state as well as tensile strength of the used polymeric films was used as measuring parameters of mucoadhesive interaction. These two approaches gave two opposite orders of performance between CMC and Carrrageenan type lambda after a contact time of 15 min. However the measurement of the viscoelastic moduli of the hydrogels gave the same ranking order of mucoadhesive performance after the same contact time. In reference to the previous works, we noted the importance of the molecular weight, the density of charges, the composition of which the chains of molecules are capable to arrange themselves in a network like form, thus those which are characterized by a tan delta<1 (i.e network formation), are those which develop the best synergism with the mucus because of the reinforcement of an established link. The goal of this study is to assess the buccal mucoadhesive performance aiming to optimize the design of drug delivery via buccal mucoadhesive polymeric films

Adhesiveness↗

Stress relaxation studies of granules as a function of different lubricants.

Viscoelastic properties of granules may be studied using stress relaxation. The effect of viscoelastic properties of different lubricants, namely magnesium stearate (Mgst), talc and precirol, on granule compaction properties was examined using texture analyzer TA-XT2i at low pressure. Normalized compact curves of stress relaxation have been discussed in relation to some parameters (flowability, porosity, viscoelasticity as well as particle size). The literature shows that viscoelasticity is always present and it produces an accompanying plastic deformation.This study revealed that bonding in compacted granules lubricated with Mgst was higher than those in compacts lubricated with the other two lubricants being studied. When studying the partial porosity of granule beds, we see that this is the result of stored energy, like the tablet case and the problem of its capping. The small stress relaxation due to talc or precirol suggested that these materials deformed principally by energy storage. However, a qualitative characterization of Mgst as tablet lubricant would be that it avoids the accumulation of stress in the compact that causes the problem of capping due to the entrapped air and therefore facilitates the optimization of pharmaceutical manufacturing. It has been possible to normalize stress relaxation using the Wischert model, represented by the sum of several exponentials, according to the nature of the lubricant. The use of texture analyzer TA-XT2i was considered to be a good technique for the evaluation of the stress relaxation of solid particles in the compression process at low pressure. It permitted the observation that viscoelasticity is influenced by the lubricant used. The brittle fracture index, like Carr's index values, has been correlated with the viscoelastic characteristics of granules.

Diglycerides↗

Hot melt coating technology: influence of Compritol 888 Ato and granule size on chloroquine release.

The tangential spray technique was used to coat chloroquine granules with Compritol 888 Ato in a fluidized bed (Glatt GPCG-1,1). After validation of the assay method for chloroquine, dissolution tests were carried out on four size fractions obtained from the same batch of granules. The dissolution profiles obtained showed differences in the rate of release between one fraction and another, despite the fact that each of these fractions had been coated with the same quantity of wax. This suggests that the rate of release of the chloroquine may be adjusted by controlling the size of the granules. Furthermore these dissolution profiles were characterized by a rapid release phase followed by a slow release phase. Examination of the surfaces of the granules from the various size fractions under a scanning electron microscope revealed that Compritol did not form a continuous film but existed rather as a lipid environment around the granule. This lipid environment was made up of solidified droplets of the wax which had become piled up on the surface of the granule. Compression of the granules produced tablets which remained intact until chloroquine dissolution was complete. This undicated that the active substance diffused across the Compritol matrix generated during compression. Determination of the dissolution kinetics using the Higuchi model demonstrated the diffusion release mechanism.

Amebicides↗

Controlled-release behavior of diphenhydramine hydrochloride loaded neutral microgranules and coated using ethylcellulose water dispersion.

The development of a loading method of a water-soluble drug using aqueous binding solution to produce microgranules that were then coated with an aqueous ethylcellulose dispersion to sustain drug release is described. The results, in terms of drug used, showed that besides the fluidized bed parameters, the amount of drug dissolved in the binder solution plays an important role in obtaining a satisfying result during the spraying process. Thus, it seems necessary to determine the critical concentration above which the material started to adhere to the interior of the fluidization column, and the possibility of drug layering onto carrier material is aggravated. ANOVA of the time parameter for release of 63.2% of total drug (td) value showed significant influence of ethylcellulose (Aquacoat ECD-30) and dibutyl sebacate concentration on diphenhydramine hydrochloride (DPH) release. The dissolution rate decreased with an increase in polymer concentration. The diffusional exponent n of the Peppas equation indicated that the DPH release kinetic was non-Fickian but approached Fickian diffusion, particularly at higher coating levels.

Cellulose↗

Comparative tablet and rheological properties of new microcrystalline cellulose: direct compression and wet granulation methods.

The overall objective of this study was to compare the rheological properties and tablet characteristics of two new varieties of celluloses (Vivacel 101 and 102), recently produced and commercialized, with the classical varieties of celluloses (Avicel and Elcema). The results showed no significant differences in the rheological properties of Vivacel and Avicel, while significant differences were found between the two celluloses and Elcema. Furthermore, there were no statistically significant differences in the disintegration times and Td values of Vivacel and Avicel. In conclusion, it was found that these new celluloses offer all the known advantages of Avicel.

Cellulose↗

Evidence for a tissue-specific induction of cutaneous CYP2E1 by dexamethasone.

We studied in mouse the effect of topical application of dexamethasone or salicylic acid, on CYP2E1 and CYP3A expression (proteins and/or mRNA) in liver and skin. Dexamethasone was also administered by intraperitoneal injection. Topical application or intraperitoneal injection of dexamethasone increased cutaneous CYP2E1 (8 and 4-fold respectively) whereas the hepatic level of this isoform showed a slight decrease and hepatic CYP3A expression was increased (3-fold). Cutaneous CYP2E1 was increased (3-fold) after topical treatment by salicylic acid. This compound had no effect on hepatic CYP3A and CYP2E1 expression. Cutaneous CYP3A (protein and mRNA) was not detectable in all groups (control or treated animals). Dexamethasone and salicylic acid increased cutaneous CYP2E1 mRNA level (2.5 and 1.4-fold respectively). In conclusion, dexamethasone and salicylic acid induced cutaneous CYP2E1 protein and mRNA level. Cutaneous CYP2E1 induction by dexamethasone is a tissue-specific process.

Administration, Topical↗