PMID- 22266529
OWN - NLM
STAT- MEDLINE
DCOM- 20120622
LR  - 20180314
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 426
IP  - 1-2
DP  - 2012 Apr 15
TI  - Preparation and in vitro/in vivo evaluation of sustained-release venlafaxine 
      hydrochloride pellets.
PG  - 21-28
LID - S0378-5173(11)01183-5 [pii]
LID - 10.1016/j.ijpharm.2011.12.053 [doi]
AB  - The objective of this study was to prepare different venlafaxine hydrochloride 
      sustained-release products and to elucidate the influence of composition of the 
      coating film on the in vitro drug release profiles and in vivo pharmacokinetics. 
      Pellets were prepared by a standardized process of extrusion/spheronization. A 
      selected fraction size (0.8-1.0 mm diameter) of pellets of each formulation was 
      coated with Eudragit NE30D or ethylcellulose (10 cps). Many efforts have been 
      made to tailor drug release rate by choosing different coating materials, 
      different percent of pore forming components and coating weight variation to 
      achieve a desired sustained-release effect. The dissolution studies were 
      performed and data were analyzed in terms of cumulative release as a function of 
      time. The influence on the release of venlafaxine from sustained-release capsules 
      was observed in dissolution media of different pH and gradient pH. Scanning 
      electron microscope (SEM) micrographs revealed morphological changes of the 
      pellet coating surface which were related to in vitro drug release profiles. The 
      relative bioavailability for Formulation 1 and Formulation 2 was evaluated in six 
      healthy beagle dogs after oral administration in a fast state using 
      sustained-release capsules (Effexor XR) as a reference. The results suggested 
      that Formulation 1 and Formulation 2 both had better bioavailability compared 
      with Effexor XR. It could be found that there existed quite difference in the in 
      vivo release and oral absorption performances, despite the similar in vitro drug 
      release behavior for the two formulations. It might be attributable to complex in 
      vivo environment and then variation in the release behavior. Thus differences in 
      the film micro-structure and surface roughness caused by aqueous dispersion and 
      organic solvent coating techniques strongly influence the in vivo release and 
      oral absorption performances.
CI  - Copyright (c) 2011 Elsevier B.V. All rights reserved.
FAU - Liu, Yang
AU  - Liu Y
AD  - Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical 
      University, No. 103 Wenhua Road, Shenyang 110016, China.
FAU - Sun, Yinghua
AU  - Sun Y
AD  - Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical 
      University, No. 103 Wenhua Road, Shenyang 110016, China.
FAU - Sun, Jin
AU  - Sun J
AD  - Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical 
      University, No. 103 Wenhua Road, Shenyang 110016, China. Electronic address: 
      sunjin66@21cn.com.
FAU - Zhao, Nana
AU  - Zhao N
AD  - Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical 
      University, No. 103 Wenhua Road, Shenyang 110016, China.
FAU - Sun, Mingyu
AU  - Sun M
AD  - Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical 
      University, No. 103 Wenhua Road, Shenyang 110016, China.
FAU - He, Zhonggui
AU  - He Z
AD  - Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical 
      University, No. 103 Wenhua Road, Shenyang 110016, China. Electronic address: 
      hezhonggui@gmail.com.
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20120114
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Antidepressive Agents, Second-Generation)
RN  - 0 (Capsules)
RN  - 0 (Cyclohexanols)
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Eudragit NE 30-D)
RN  - 0 (Excipients)
RN  - 0 (Methacrylates)
RN  - 0 (Polymers)
RN  - 7D7RX5A8MO (Venlafaxine Hydrochloride)
RN  - 7Z8S9VYZ4B (ethyl cellulose)
RN  - 9004-34-6 (Cellulose)
SB  - IM
MH  - Administration, Oral
MH  - Animals
MH  - Antidepressive Agents, Second-Generation/administration & 
      dosage/blood/chemistry/*pharmacokinetics
MH  - Biological Availability
MH  - Calorimetry, Differential Scanning
MH  - Capsules
MH  - Cellulose/analogs & derivatives/chemistry
MH  - Chemistry, Pharmaceutical
MH  - Cyclohexanols/administration & dosage/blood/chemistry/*pharmacokinetics
MH  - Delayed-Action Preparations
MH  - Dogs
MH  - Drug Compounding
MH  - Excipients/chemistry
MH  - Hydrogen-Ion Concentration
MH  - Intestinal Absorption
MH  - Male
MH  - Methacrylates/chemistry
MH  - Microscopy, Electron, Scanning
MH  - Particle Size
MH  - Polymers/chemistry
MH  - Solubility
MH  - Surface Properties
MH  - Technology, Pharmaceutical/methods
MH  - Venlafaxine Hydrochloride
EDAT- 2012/01/24 06:00
MHDA- 2012/06/23 06:00
CRDT- 2012/01/24 06:00
PHST- 2011/07/03 00:00 [received]
PHST- 2011/12/06 00:00 [revised]
PHST- 2011/12/25 00:00 [accepted]
PHST- 2012/01/24 06:00 [entrez]
PHST- 2012/01/24 06:00 [pubmed]
PHST- 2012/06/23 06:00 [medline]
AID - S0378-5173(11)01183-5 [pii]
AID - 10.1016/j.ijpharm.2011.12.053 [doi]
PST - ppublish
SO  - Int J Pharm. 2012 Apr 15;426(1-2):21-28. doi: 10.1016/j.ijpharm.2011.12.053. Epub 
      2012 Jan 14.