Journal
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 47, Issue 3, Pages 394-402Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/03639045.2021.1890110
Keywords
Clonidine hydrochloride; ion-exchange resin; fluidized bed; sustained-release; suspension
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The study aimed to prepare a clonidine hydrochloride sustained-release suspension. The results showed that the suspension had a delayed Tmax, reduced Cmax, and a gentler concentration-time curve compared to ordinary tablets. The relative bioavailability of the suspension was 111.65% compared to the tablets.
Objective The purpose of the present study was to prepare a clonidine hydrochloride (CH) sustained-release suspension. Methods The processes involved in the drug formulation included drug loading, impregnating, and suspension preparation. Clonidine hydrochloride drug-resin complexes (CH-DRC) were prepared using the bath method and the CH-DRC impregnated before the microencapsulation process. Based on the bottom spray fluidized bed coating method, the CH microencapsulated drug-resin complexes (CH-MC) were also prepared using Surelease(R) (the suspension of ethyl cellulose aqueous dispersion) as the coating material. The effects of coating (process/formulation) on the in vitro release of coating microcapsule were evaluated via single factor investigation and orthogonal design optimization. The CH-MC with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. Rats were given commercial CH ordinary tablets and the CH sustained-release suspension via intragastric administration. The plasma concentration-time curve and related pharmacokinetic parameters were investigated using the non-compartment model. Results The T (max) of the CH sustained-release suspension was delayed from 2 h to 5 h compared with the CH ordinary tablets. Similarly, the C (max) was reduced from 32.138 mu g.mL(-1) to 18.150 mu g.mL(-1) with the concentration-time curve being more gentle compared with the commercially CH ordinary tablets. After oral administration, the relative bioavailability of CH sustained-release suspension (AUC(0-24) of 137.703 mu g.h.mL(-1)) to its CH ordinary tablets (AUC(0-24) of 123.337 mu g.h.mL(-1)) was 111.65%. Conclusions The findings showed that the CH sustained-release suspension for oral administration was successfully formulated.
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