Development and evaluation of sustained release gastroretentive minimatrices for effective treatment of H. pylori infection.
In the present work, sustained release gastroretentive minimatrices of amoxicillin have been designed and optimized using central composite design. Effect of amount of xanthan gum, rate controlling polymers (HPMC K100M CR/PEO coagulant (1:1)), carbopol 974P, and gas generating couple (sodium bicarbonate/citric acid (3:1)) was studied on dependent (response) variables, i.e., buoyancy lag time, drug release at 1 h, time required for 95% drug release, swelling index, and bioadhesive strength. Minimatrices were prepared by non aqueous granulation method using solution of PVP K30 in isopropyl alcohol. All the formulations were found to contain 99.2% to 100.9% of amoxicillin per minimatrix. Optimum formulation (Formulation number AGT09) containing high level of the independent variables was having buoyancy lag time of 7 min and drug release at 1 h was 32.5%. It required 9.39 h for 95% drug release while swelling index and bioadhesive strength were 341 and 17.9 dyn/cm(2), respectively. This formulation was said to be optimum because it has minimum buoyancy lag time, requires maximum time for 95% drug release, and has higher bioadhesive capabilities. In vitro results of an optimized formulation indicate its sustained drug release and gastric retention capability, which may be very useful for effective treatment of H. pylori infection.
Badhan
Atul C
AC
Centre of Relevance and Excellence in Novel Drug Delivery systems, Pharmacy Department, The M.S. University of Baroda, Fatehgunj, Baroda, 390002, India. atulbadhan@rediffmail.com
Mashru
Rajashree C
RC
Shah
Punit P
PP
Thakkar
Arti R
AR
Dobaria
Nitin B
NB
D000658:Amoxicillin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D003692:Delayed-Action Preparations; D005753:Gastric Mucosa / Q000378:metabolism*; D006041:Goats; D016481:Helicobacter Infections / Q000188:drug therapy*; D016480:Helicobacter pylori; D011135:Polysaccharides, Bacterial / Q000008:administration & dosage; D012995:Solubility
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D011135:Polysaccharides, Bacterial; D000658:Amoxicillin; C002563:xanthan gum