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Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads.
Drug Dev Ind Pharm. 1998 Jul; 24(7):661-6.DD

Abstract

Diclofenac sodium enteric-coated beads were prepared using the conventional pan coating technique. Eudragit L100 was used as a pH-dependent release-controlling polymer. The beads were evaluated for their particle size distribution, drug loading efficiency, flowability, in vitro release in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8), and bioavailability in beagle dogs relative to the commercial enteric-coated tablets Voltaren. The beads showed a narrow particle size distribution in which 83% of the beads were in the range of 1-2 mm. The actual yield of the beads was 90.5% and their drug loading was 92%. The beads released about 8% of the drug during 2 hr of dissolution in 0.1 N HCl, and the commercial tablets released no drug. In phosphate buffer (pH 6.8) both formulations released their drug content in 1 hr. Both formulations are, therefore, in compliance with the USP requirements for release from enteric-coated dosage forms. The in vivo availability study in six beagle dogs revealed that the formulated enteric-coated beads filled in hard gelatin capsules had a 197.54% bioavailability relative to that of the commercial Voltaren tablets. The tablets showed a significantly lower (p < 0.05) area under curve for 0-8 hr (AUC0-8 hr) of 13.44 +/- 15.02 micrograms hr/ml compared to 26.55 +/- 5.19 micrograms hr/ml for the capsules. The capsules showed a nonsignificantly (p > 0.05) higher peak plasma concentration (Cmax) of 6.77 +/- 0.67 micrograms/ml compared to 5.88 +/- 7.38 micrograms/ml for the tablets. The time to reach peak (Tmax) values were 2 +/- 1.48 and 2.25 +/- 1.08 hr for the capsules and tablets, respectively. The capsules showed less interdog variability with respect to Cmax (CV% 34.6) and AUC (CV% 19.55) compared to CV% 79.9 and 111.76, respectively, for the commercial tablets.

Authors+Show Affiliations

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

9876511

Citation

Hosny, E A., et al. "Formulation and in Vitro and in Vivo Availability of Diclofenac Sodium Enteric-coated Beads." Drug Development and Industrial Pharmacy, vol. 24, no. 7, 1998, pp. 661-6.
Hosny EA, el-Mahrouk GM, Gouda MW. Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads. Drug Dev Ind Pharm. 1998;24(7):661-6.
Hosny, E. A., el-Mahrouk, G. M., & Gouda, M. W. (1998). Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads. Drug Development and Industrial Pharmacy, 24(7), 661-6.
Hosny EA, el-Mahrouk GM, Gouda MW. Formulation and in Vitro and in Vivo Availability of Diclofenac Sodium Enteric-coated Beads. Drug Dev Ind Pharm. 1998;24(7):661-6. PubMed PMID: 9876511.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and in vitro and in vivo availability of diclofenac sodium enteric-coated beads. AU - Hosny,E A, AU - el-Mahrouk,G M, AU - Gouda,M W, PY - 1999/1/7/pubmed PY - 1999/1/7/medline PY - 1999/1/7/entrez SP - 661 EP - 6 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 24 IS - 7 N2 - Diclofenac sodium enteric-coated beads were prepared using the conventional pan coating technique. Eudragit L100 was used as a pH-dependent release-controlling polymer. The beads were evaluated for their particle size distribution, drug loading efficiency, flowability, in vitro release in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8), and bioavailability in beagle dogs relative to the commercial enteric-coated tablets Voltaren. The beads showed a narrow particle size distribution in which 83% of the beads were in the range of 1-2 mm. The actual yield of the beads was 90.5% and their drug loading was 92%. The beads released about 8% of the drug during 2 hr of dissolution in 0.1 N HCl, and the commercial tablets released no drug. In phosphate buffer (pH 6.8) both formulations released their drug content in 1 hr. Both formulations are, therefore, in compliance with the USP requirements for release from enteric-coated dosage forms. The in vivo availability study in six beagle dogs revealed that the formulated enteric-coated beads filled in hard gelatin capsules had a 197.54% bioavailability relative to that of the commercial Voltaren tablets. The tablets showed a significantly lower (p < 0.05) area under curve for 0-8 hr (AUC0-8 hr) of 13.44 +/- 15.02 micrograms hr/ml compared to 26.55 +/- 5.19 micrograms hr/ml for the capsules. The capsules showed a nonsignificantly (p > 0.05) higher peak plasma concentration (Cmax) of 6.77 +/- 0.67 micrograms/ml compared to 5.88 +/- 7.38 micrograms/ml for the tablets. The time to reach peak (Tmax) values were 2 +/- 1.48 and 2.25 +/- 1.08 hr for the capsules and tablets, respectively. The capsules showed less interdog variability with respect to Cmax (CV% 34.6) and AUC (CV% 19.55) compared to CV% 79.9 and 111.76, respectively, for the commercial tablets. SN - 0363-9045 UR - https://www.unboundmedicine.com/medline/citation/9876511/Formulation_and_in_vitro_and_in_vivo_availability_of_diclofenac_sodium_enteric_coated_beads_ DB - PRIME DP - Unbound Medicine ER -