Formulation and evaluation of novel coated floating tablets of bergenin and cetirizine dihydrochloride for gastric delivery.
A novel coated gastric floating drug-delivery system (GFDDS) of bergenin (BN) and cetirizine dihydrochloride (CET) was developed. First, the pharmacodynamic studies were performed and the results revealed that the new compounds of bergenin/cetirizine dihydrochloride had comparative efficacy as commercial products (bergenin/chlorphenamine maleate) but with fewer side effects on central nervous system (CNS). Subsequently, bergenin was formulated as an extended-release core tablet while cetirizine dihydrochloride was incorporated into the gastric coating film for immediate release. The formulation of GFDDS was optimized by CET content uniformity test, in vitro buoyancy and drug release. Herein, the effects of sodium bicarbonate (effervescent), hydroxypropyl methylcellulose (HPMC, matrix polymer) and coating weight gain were investigated respectively. The optimized GFDDS exhibited good floating properties (buoyancy lag time < 2 min; floating duration > 10 h) and satisfactory drug-release profiles (immediate release of CET in 10 min and sustained release of BN for 12 h). In vivo gamma scintigraphy proved that the optimized GFDDS could retain in the stomach with a prolonged gastric retention time (GRT) of 5 h, and the coating layer showed no side effect for gastric retention. The novel coated gastric floating drug-delivery system offers a new approach to enhance BN's absorption at its absorption site and the efficacy of both CET and BN.
Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University . No. 17, Block 3, Southern Renmin Road, Chengdu 610041, PR China.
Shuang
S
He
Feng
F
Li
Dan
D
Zhou
Junrong
J
Du
Yuan
Y
Huang
D000042:Absorption; D000818:Animals; D018927:Anti-Asthmatic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D000996:Antitussive Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D001578:Benzopyrans / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D017332:Cetirizine / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D020099:Coated Materials, Biocompatible / Q000008:administration & dosage / Q000737:chemistry*; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems / Q000379:methods; D005079:Excipients / Q000737:chemistry; D005100:Expectorants / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D005753:Gastric Mucosa / Q000378:metabolism; D006168:Guinea Pigs; D065347:Hypromellose Derivatives; D007700:Kinetics; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D011877:Radionuclide Imaging / Q000379:methods; D017693:Sodium Bicarbonate / Q000737:chemistry; D013607:Tablets / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology
D018927:Anti-Asthmatic Agents; D000996:Antitussive Agents; D001578:Benzopyrans; D020099:Coated Materials, Biocompatible; D003692:Delayed-Action Preparations; D005079:Excipients; D005100:Expectorants; D013607:Tablets; D065347:Hypromellose Derivatives; D017693:Sodium Bicarbonate; D008747:Methylcellulose; C006741:bergenin; D017332:Cetirizine