PMID- 22809245
OWN - NLM
STAT- MEDLINE
DCOM- 20130425
LR  - 20181201
IS  - 1744-7593 (Electronic)
IS  - 1742-5247 (Linking)
VI  - 9
IP  - 9
DP  - 2012 Sep
TI  - Clinical development of a once-daily gastroretentive formulation of gabapentin 
      for treatment of postherpetic neuralgia: an overview.
PG  - 1147-60
LID - 10.1517/17425247.2012.709231 [doi]
AB  - INTRODUCTION: Gabapentin immediate-release formulations (G-IR) administered three 
      times a day is an efficacious treatment for postherpetic neuralgia (PHN), but its 
      potential benefits may not be fully realized due to tolerability issues as well 
      as its pharmacokinetic (PK) properties such as its short half-life, and regional 
      and saturable absorption in the proximal small intestine. The gastroretentive 
      once-daily formulation of gabapentin (G-GR) allows for less frequent dosing while 
      maintaining efficacy and may also reduce adverse events (AEs) associated with 
      high plasma concentration of gabapentin occurring during the waking hours. G-GR 
      slowly releases the drug from the tablet to the upper small intestine, where 
      gabapentin is best absorbed, over approximately 10 h. AREA COVERED: This report 
      reviews the development of the gastroretentive technology used in the once-daily 
      formulation of gabapentin (G-GR), and describes the clinical development of G-GR 
      from PK studies through the Phase III efficacy and safety studies, with 
      comparisons made with G-IR. EXPERT OPINION: The technology takes advantage of the 
      normal physiology of the stomach in the fed state to provide gastroretention, 
      which in turn allows for gradual release of the active ingredient over several 
      hours to the small intestine where gabapentin is best absorbed. The GR technology 
      used in G-GR resulted in a decreased dosing frequency from three times per day 
      for the IR product to once daily in the treatment of PHN, while maintaining the 
      same efficacy with an apparent reduced incidence of AEs common to G-IR therapy.
FAU - Argoff, Charles E
AU  - Argoff CE
AD  - Albany Medical College Neurology Group, 47 New Scotland Avenue, MC 70, Physicians 
      Pavilion, 1st Floor, Albany, NY 12208, USA. argoffc@mail.amc.edu
FAU - Chen, Cuiping
AU  - Chen C
FAU - Cowles, Verne E
AU  - Cowles VE
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20120718
PL  - England
TA  - Expert Opin Drug Deliv
JT  - Expert opinion on drug delivery
JID - 101228421
RN  - 0 (Amines)
RN  - 0 (Analgesics)
RN  - 0 (Cyclohexanecarboxylic Acids)
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Tablets)
RN  - 56-12-2 (gamma-Aminobutyric Acid)
RN  - 6CW7F3G59X (Gabapentin)
SB  - IM
MH  - Amines/*administration & dosage/chemistry/pharmacokinetics
MH  - Analgesics/*administration & dosage/chemistry/pharmacokinetics
MH  - Biological Availability
MH  - Chemistry, Pharmaceutical
MH  - Cyclohexanecarboxylic Acids/*administration & dosage/chemistry/pharmacokinetics
MH  - Delayed-Action Preparations
MH  - Gabapentin
MH  - Humans
MH  - Intestinal Absorption
MH  - Neuralgia, Postherpetic/*drug therapy
MH  - Tablets
MH  - gamma-Aminobutyric Acid/*administration & dosage/chemistry/pharmacokinetics
EDAT- 2012/07/20 06:00
MHDA- 2013/04/26 06:00
CRDT- 2012/07/20 06:00
PHST- 2012/07/20 06:00 [entrez]
PHST- 2012/07/20 06:00 [pubmed]
PHST- 2013/04/26 06:00 [medline]
AID - 10.1517/17425247.2012.709231 [doi]
PST - ppublish
SO  - Expert Opin Drug Deliv. 2012 Sep;9(9):1147-60. doi: 10.1517/17425247.2012.709231. 
      Epub 2012 Jul 18.