Compartmental Absorption Modeling and Site of Absorption Studies to Determine Feasibility of an Extended-Release Formulation of an HIV-1 Attachment Inhibitor Phosphate Ester Prodrug

2013 ◽  
Vol 102 (6) ◽  
pp. 1742-1751 ◽  
Author(s):  
Jonathan Brown ◽  
Caly Chien ◽  
Peter Timmins ◽  
Andrew Dennis ◽  
Walter Doll ◽  
...  
Keyword(s):  
Extended Release ◽  
Phosphate Ester ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
Absorption Studies ◽  
Absorption Modeling ◽  
Ester Prodrug ◽  
Site Of Absorption ◽  
Hiv 1

scholarly journals Nevirapine Extended-Release Formulation Tablets in HIV-1–Infected Children—Long-term Follow-up: Table 1.

2015 ◽  
Vol 61 (3) ◽  
pp. 476-479 ◽  
Author(s):  
Gabriel Anabwani ◽  
Christoph Königs ◽  
Carlos Giaquinto ◽  
Stella Aslanyan ◽  
John P. Sabo ◽  
...  
Keyword(s):  
Extended Release ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
Long Term Follow Up ◽  
Hiv 1

Extended-release Formulation Attenuates the Impacts of Fluvastatin on Serum PCSK9 Levels in Humans

2017 ◽  
Vol 14 (7) ◽  
Author(s):  
Yuan-Lin Guo ◽  
Wei Zhang ◽  
Qian Dong ◽  
Geng Liu ◽  
Cheng-Gang Zhu ◽  
...  
Keyword(s):  
Extended Release ◽  
Release Formulation ◽  
Extended Release Formulation

scholarly journals Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technology

2009 ◽  
Vol 59 (1) ◽  
pp. 15-30 ◽  
Author(s):  
Pramod Kumar ◽  
Sanjay Singh ◽  
Brahmeshwar Mishra
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Relative Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Healthy Human ◽  
Tramadol Hydrochloride ◽  
Release Formulation ◽  
Extended Release Formulation

Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technologyExtended release formulation of tramadol hydrochloride (TRH) based on osmotic technology was developed and evaluated. Target release profile was selected and different variables were optimized to achieve it. Formulation variables such as the level of swellable polymer, plasticizer and the coat thickness of semipermeable membrane (SPM) were found to markedly affect drug release. TRH release was directly proportional to the levels of plasticizer but inversely proportional to the levels of swellable polymer and coat thickness of SPM. Drug release from developed formulations was independent of pH and agitation intensity but dependent on osmotic pressure of the release media.In vivostudy was also performed on six healthy human volunteers and various pharmacokinetic parameters (cmax,tmax,AUC0-24,MRT) and relative bioavailability were calculated. Thein vitroandin vivoresults were compared with the performance of two commercial TRH tablets. The developed formulation provided more prolonged and controlled TRH release compared to the marketed formulation.In vitro-in vivocorrelation (IVIVC) was analyzed according to the Wagner-Nelson method. The optimized formulation (batch IVB) exhibited good IVIV correlation (R= 0.9750). The manufacturing procedure was found to be reproducible and formulations were stable over 6 months of accelerated stability testing.

Brompheniramine Maleate: A Double-Blind, Placebo-Controlled Comparison with Terfenadine for Symptoms of Allergic Rhinitis

1998 ◽  
Vol 12 (4) ◽  
pp. 293-300 ◽  
Author(s):  
William R. Thoden ◽  
Howard M. Druce ◽  
Sandy A. Furey ◽  
Earle A. Lockhart ◽  
Paul Ratner ◽  
...  
Keyword(s):  
Allergic Rhinitis ◽  
Symptom Severity ◽  
Extended Release ◽  
Nasal Symptom ◽  
Double Blind ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
Adverse Experiences ◽  
Severity Scores ◽  
Brompheniramine Maleate

This was a double-blind, randomized, placebo-controlled, multicenter, parallel study comparing the effectiveness, at recommended doses, of an extended-release formulation of brompheniramine maleate and terfenadine in the treatment of allergic rhinitis. Subjects with symptoms of seasonal and/or perennial allergic rhinitis received brompheniramine 12 mg (n = 106), 8 mg (n = 105), terfenadine 60 mg (n = 106), or placebo (n = 53) twice daily for 14 days. On treatment days 3, 7, and 14, symptom severity ratings (i.e., rhinorrhea, sneezing, nasal congestion, itchy nose, eyes or throat, excessive tearing, postnasal drip) were completed by the physician; subjects and physicians each completed a global efficacy evaluation. Brompheniramine 12 mg and 8 mg and terfenadine were more effective than placebo (p ≤ 0.05) on the physicians’ global; brompheniramine 12 mg was more effective than terfenadine (p ≤ 0.05) on days 7 and 14 and brompheniramine 8 mg on day 3. On the subjects’ global evaluation, brompheniramine 12 mg and 8 mg and terfenadine were more effective than placebo (p ≤ 0.05); brompheniramine 12 mg was more effective than terfenadine (p ≤ 0.05) on days 7 and 14 and brompheniramine 8 mg on day 3. In general, brompheniramine 8 mg was comparable to terfenadine. On days 3 and 7, the total symptom and total nasal symptom severity scores for subjects receiving brompheniramine 12 mg were significantly more improved than for placebo (p < 0.05); terfenadine was not different from placebo; brompheniramine 12 mg was significantly better than terfenadine on day 7 (p < 0.05) for reducing total symptom severity and on days 3, 7, and 14 for reducing total nasal symptom severity. Adverse experiences were reported by 155 (41.9%) of the 370 subjects enrolled in the study. The overall rate of adverse experiences in the brompheniramine 12 mg treatment group (57.5%) was significantly greater (p < 0.05) than for brompheniramine 8 mg (38.1%), terfenadine (31.1%), and placebo (39.6%). In conclusion, an extended-release formulation of brompheniramine 12 mg or 8 mg bid alleviates allergic rhinitis symptoms and brompheniramine 12 mg provides significantly better relief of these symptoms than terfenadine 60 mg bid.

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