PMID- 17891586
OWN - NLM
STAT- MEDLINE
DCOM- 20080110
LR  - 20190923
IS  - 0363-9045 (Print)
IS  - 0363-9045 (Linking)
VI  - 33
IP  - 9
DP  - 2007 Sep
TI  - Investigations of a novel self-emulsifying osmotic pump tablet containing 
      carvedilol.
PG  - 990-8
AB  - Carvedilol has been made into a novel osmotic pump tablet which includes Gelucire 
      44/14, Lutrol F68, Transcutol P, silicon dioxide, mannitol, citric acid, and 
      sodium hydrogen carbonate. The Self-emulsifying osmotic pump tablet (SEOPT) has 
      two outstanding features. It could improve the bioavailability of carvedilol by 
      self-emulsifying drug delivery system (SEDDS), control the release rate and make 
      the plasma concentrations more stable by elementary osmotic pump tablet. The 
      results of transmission electron microscope (TEM) and particle size assessment 
      showed that the shape of the resultant emulsion was round and regular, the 
      average diameter of the particles was 246 nm. Since the solubility of carvedilol 
      was improved by the emulsion, the elementary SEOPT could guarantee a complete 
      release of carvedilol under the osmotic pressure of mannitol. The cumulative 
      release at 12 hr was 85.18%. Therefore the disadvantage that lipophilic drugs can 
      not be released completely when prepared into elementary osmotic pump tablet was 
      resolved. The results of Differential scanning calorimetry (DSC), Infrared 
      spectroscopy (IR) and X-ray diffraction diffraction (XRD) proved that carvedilol 
      was amorphous in the preparation. The relative bioavailability of carvedilol in 
      beagle dogs was 156.78%. The plasma concentrations were more stable compared with 
      that of commercially available tablet (Luode). And the in vitro and in vivo 
      correlation was good (r = 0.9725). Therefore, the elementary SEOPT developed in 
      this paper might provide a new idea for preparing lipophilic drugs into osmotic 
      pump tablet conveniently.
FAU - Wei, Lanlan
AU  - Wei L
AD  - Department of Pharmaceutics, Shen Yang Pharmaceutical University, Shen Yang, PR 
      China.
FAU - Li, Jie
AU  - Li J
FAU - Guo, Liangran
AU  - Guo L
FAU - Nie, Shufang
AU  - Nie S
FAU - Pan, Weisan
AU  - Pan W
FAU - Sun, Peinan
AU  - Sun P
FAU - Liu, Hui
AU  - Liu H
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - England
TA  - Drug Dev Ind Pharm
JT  - Drug development and industrial pharmacy
JID - 7802620
RN  - 0 (Antihypertensive Agents)
RN  - 0 (Carbazoles)
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Emulsions)
RN  - 0 (Excipients)
RN  - 0 (Propanolamines)
RN  - 0 (Tablets)
RN  - 0K47UL67F2 (Carvedilol)
RN  - 3OWL53L36A (Mannitol)
SB  - IM
MH  - Animals
MH  - Antihypertensive Agents/administration & dosage/chemistry/*pharmacokinetics
MH  - Biological Availability
MH  - Carbazoles/administration & dosage/chemistry/*pharmacokinetics
MH  - Carvedilol
MH  - *Chemistry, Pharmaceutical
MH  - Cross-Over Studies
MH  - Delayed-Action Preparations
MH  - Dogs
MH  - Emulsions
MH  - Excipients/*chemistry
MH  - Mannitol/chemistry
MH  - Microscopy, Electron, Transmission
MH  - Osmosis
MH  - Osmotic Pressure
MH  - Particle Size
MH  - Propanolamines/administration & dosage/chemistry/*pharmacokinetics
MH  - Random Allocation
MH  - Solubility
MH  - Tablets
EDAT- 2007/09/25 09:00
MHDA- 2008/01/11 09:00
CRDT- 2007/09/25 09:00
PHST- 2007/09/25 09:00 [pubmed]
PHST- 2008/01/11 09:00 [medline]
PHST- 2007/09/25 09:00 [entrez]
AID - 782316342 [pii]
AID - 10.1080/03639040601150328 [doi]
PST - ppublish
SO  - Drug Dev Ind Pharm. 2007 Sep;33(9):990-8. doi: 10.1080/03639040601150328.