Casein hydrolysate as a rapid and/or enteric dissolving additive for oral drugs

Pharmaceutical Development and Technology
T ImaiM Otagiri

Abstract

Two types of casein hydrolysates, casein A (mean peptide length 3.3) and casein B (mean peptide length 17.4) were prepared by the enzymatic hydrolysis of casein, and their effects on in vitro dissolution rates and oral bioavailability of drugs were evaluated. The in vitro dissolution behavior of the kneaded mixture of three drugs (diclofenac acid, diazepam, and prednisolone) with caseins A and B were significantly improved compared to the drugs alone, even at 1:1 weight ratio of drug and casein hydrolysate, even though casein A and casein B did not interact with drug molecules in the kneaded mixture. Only diclofenac, an acidic drug, showed an increased dissolution rate with added casein hydrolysates, and a more rapid dissolution with casein A than with casein B was observed. When the dissolution of prednisolone from kneaded mixture was compared at pH 1.2 and 6.8, the dissolution rate of prednisolone from the casein A kneaded mixture was considerably higher than that of prednisolone powder at both pHs, and the rate from the casein B kneaded mixture was higher only at pH 6.8. The plasma concentration-time profile showed that prednisolone was completely and rapidly absorbed from the casein A kneaded mixture as well as the predniso...Continue Reading

References

Aug 1, 1976·Journal of Pharmaceutical Sciences·G Zografi, S S Tam
Feb 1, 1992·Journal of Pharmaceutical Sciences·S KimuraM Otagiri
Sep 1, 1991·The Journal of Pharmacy and Pharmacology·S ShiraishiM Otagiri
May 1, 1991·Journal of Pharmaceutical Sciences·T ImaiM Otagiri
Sep 1, 1990·The Journal of Pharmacy and Pharmacology·T ImaiM Otagiri
Jun 1, 1983·Chemical & Pharmaceutical Bulletin·Y SawayanagiT Nagai
Nov 1, 1981·Journal of Pharmacobio-dynamics·K YamaokaT Uno

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