Preparation and in vitro/in vivo evaluation of a clonidine hydrochloride drug-resin suspension as a sustained-release formulation
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® (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 Tmax of the CH sustained-release suspension was delayed from 2 h to 5 h compared with the CH ordinary tablets. Similarly, the Cmax was reduced from 32.138 µg·mL-1 to 18.150 µg·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 (AUC0-24 of 137.703 µg·h·mL-1) to its CH ordinary tablets (AUC0-24 of 123.337 µg·h·mL-1) was 111.65%.
CONCLUSIONS: The findings showed that the CH sustained-release suspension for oral administration was successfully formulated.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:47 |
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| Enthalten in: |
Drug development and industrial pharmacy - 47(2021), 3 vom: 19. März, Seite 394-402 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Liu, Hongfei [VerfasserIn] |
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| Links: |
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| Themen: |
Clonidine |
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| Anmerkungen: |
Date Completed 27.04.2021 Date Revised 21.04.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1080/03639045.2021.1890110 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM321744969 |
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| 100 | 1 | |a Liu, Hongfei |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Preparation and in vitro/in vivo evaluation of a clonidine hydrochloride drug-resin suspension as a sustained-release formulation |
| 264 | 1 | |c 2021 | |
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| 500 | |a Date Completed 27.04.2021 | ||
| 500 | |a Date Revised 21.04.2022 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a OBJECTIVE: The purpose of the present study was to prepare a clonidine hydrochloride (CH) sustained-release suspension | ||
| 520 | |a 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® (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 | ||
| 520 | |a RESULTS: The Tmax of the CH sustained-release suspension was delayed from 2 h to 5 h compared with the CH ordinary tablets. Similarly, the Cmax was reduced from 32.138 µg·mL-1 to 18.150 µg·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 (AUC0-24 of 137.703 µg·h·mL-1) to its CH ordinary tablets (AUC0-24 of 123.337 µg·h·mL-1) was 111.65% | ||
| 520 | |a CONCLUSIONS: The findings showed that the CH sustained-release suspension for oral administration was successfully formulated | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Clonidine hydrochloride | |
| 650 | 4 | |a fluidized bed | |
| 650 | 4 | |a ion-exchange resin | |
| 650 | 4 | |a suspension | |
| 650 | 4 | |a sustained-release | |
| 650 | 7 | |a Delayed-Action Preparations |2 NLM | |
| 650 | 7 | |a Suspensions |2 NLM | |
| 650 | 7 | |a Tablets |2 NLM | |
| 650 | 7 | |a Clonidine |2 NLM | |
| 650 | 7 | |a MN3L5RMN02 |2 NLM | |
| 700 | 1 | |a Xie, Xiaoya |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Chao |e verfasserin |4 aut | |
| 700 | 1 | |a Firempong, Caleb Kesse |e verfasserin |4 aut | |
| 700 | 1 | |a Feng, Yingshu |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Limin |e verfasserin |4 aut | |
| 700 | 1 | |a Yin, Xuezhi |e verfasserin |4 aut | |
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