Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation

Tan, David Cheng Thiam; Chin, William W.; Tan, En Hui; Hong, Shiqi; Gu, Wei Wei; Gokhale, Rajeev

doi:10.1016/j.ijpharm.2013.12.053

Cited by 22 publications

(5 citation statements)

References 27 publications

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“…Twin-screw granulation is a continuous process that is cost effective and reduces the processing time compared to the conventional granulation process. Furthermore, optimization of process parameters and screw configuration enables granules to be produced with desired strength and compressibility (Tan et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Kallakunta

Tiwari

Sarabu

et al. 2018

European Journal of Pharmaceutical Sciences

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The current study's aim is to prepare lipid based sustained release tablets via a twin-screw granulation technique and compare those dosage forms with conventional techniques, namely wet granulation and direct compression. The granules were successfully manufactured in a single-step, continuous twin-screw granulation process with a low proportion of binder (Klucel™ EF, HPC SSL) using Compritol® 888 ATO, Precirol® ATO 5 and Geleol™ as sustained release agents. The granules prepared showed good flow characteristics and compaction properties. DSC and XRD studies were conducted to characterize the granules prepared via a twin-screw granulation method and the results demonstrated the crystalline nature of lipids within the granules. FTIR data indicated that there were no interactions with the formulation components investigated. The formulations developed by all three methods were compressed into tablets with a mechanical strength of 14-16 KP. The tablets formulated were characterized for physicochemical properties, in vitro drug release studies, water uptake and erosion studies. These results showed that the drug was not completely released after 24 h for tablets developed by the wet granulation process using all three lipids. The tablets prepared by the direct compression method demonstrated a burst release within 8 to 10 h from Precirol ATO 5® and Geleol™ formulations compared to Compritol® 888 ATO. However, tablets prepared using twin-screw granulation exhibited sustained release of the drug over 24 h and the water uptake and erosion results were in accordance with dissolution data. Stability data for 45 days at accelerated conditions (40 °C/75% RH) showed similar release profiles with ƒ2 values above 50 for all of the twin screw granulation formulations, indicating the suitability of the process for formulating sustained release tablets. These findings of a single-step, continuous twin-screw granulation process are novel and demonstrate new opportunities for development of sustained release tablets.

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Section: Introductionmentioning

confidence: 99%

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Kallakunta

Tiwari

Sarabu

et al. 2018

European Journal of Pharmaceutical Sciences

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“…Tan et al evaluated the combination of hydrophilic binder and hydrophobic binder on the dissolution profile of the verapamil high dose tablet produced by direct-molding melt granulation process with the twin-screw extruder design of experiment (DOE) approach. The hydrophilic binder had a significant impact on the release profile of verapamil [27] .…”

Section: Introductionmentioning

confidence: 99%

The importance of binder moisture content in Metformin HCL high-dose formulations prepared by moist aqueous granulation (MAG)

Takasaki

Yonemochi

Ito

et al. 2015

Results in Pharma Sciences

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The aim of this study was to evaluate binders to improve the flowability of granulates and compactibility of Metformin HCL (Met) using the moist aqueous granulation (MAG) process. The effect of the binder moisture content on granulate and tablet quality was also evaluated. Vinylpyrrolidone–vinyl acetate copolymer (Kollidon VA64 fine: VA64), polyvidone (Povidone K12: PVP), hydroxypropyl cellulose (HPC SSL SF: HPC) and hydroxypropyl methylcellulose (Methocel E5 LV: HPMC) were evaluated as binders. These granulates, except for HPMC, had a lower yield pressure than Met active pharmaceutical ingredient (API). HPMC Met was not sufficiently granulated with low water volume. No problems were observed with the VA64 Met granulates during the tableting process. However, HPC Met granulates had a bowl-forming tendency, and PVP Met granulates had the tendency to stick during the tableting process. These bowl-forming and sticking tendencies may have been due to the low moisture absorbency of HPC and the high volume of bound water of PVP, respectively. VA64 Met granulates had the highest ambient moisture content (bulk water, bound water) and moisture absorbency. It was concluded that the type of binder used for the Met MAG process has an impact on granulate flow and compactibility, as well as moisture absorbency and maintenance of moisture balance.

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“…Selection of binder and drug loading: Binder type has a significant effect on drug release profile from a pharmaceutical dosage form [22]. In the present study, we evaluated the effect of two different binders i.e., Hypromellose E 5LV and polyvinyl pyrrolidone K-30 for their binding efficiency (Table 3).…”

Section: Selection Of Inert Carrier (Sugar Spheres)mentioning

confidence: 99%

Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride

BOYAPATI¹,

Awasthi²,

Kulkarni³

2022

jrp

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Multiple unit particulate system (MUPS) is more recent, challenging, effective and attractive option for the pharmaceutical industries that gives an efficient way to deliver drugs in modified pattern. This study aimed to improve the release profile of venlafaxine hydrochloride by developing modified release MUPS using polyvinyl pyrrolidone K-30, ethyl cellulose 20 cps and Hypromellose E 5LV. Preliminary trials were carried out to select the inert carrier, binder, and viscosity grade of rate controlling polymers. Further, optimization of binder concentration and extended-release coating was carried out. The formulation development of MUPS was divided into two categories as (i) drug layering on inert carrier, i.e., sugar spheres and (ii) extended-release coating. Comparative multimedia dissolution study of venlafaxine hydrochloride extended-release capsules was carried out and compared with the marketed formulation to ascertain the in vitro drug release behavior. XRD study indicated conversion of monohydrate form of venlafaxine hydrochloride and remained unaffected during storage. SEM images confirmed smooth surface of MUPS without any pores. The coated spheres had more dense surface compared to the uncoated pellets. Hypromellose E 5 LV showed better binding properties. Ethyl cellulose (20 cps) showed sustained release profile. The blend containing ER -I spheres (10% coating) and ER -II spheres (11% coating) at 60: 40 ratio showed dissolution profile similar to that of the innovator product. The formulated venlafaxine hydrochloride loaded MUPS filled in hard gelatin capsule can open a new avenue for the delivery of therapeutics with improved potential.

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Effect of binders on the release rates of direct molded verapamil tablets using twin-screw extruder in melt granulation

Cited by 22 publications

References 27 publications

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

The importance of binder moisture content in Metformin HCL high-dose formulations prepared by moist aqueous granulation (MAG)

Formulation, characterization, and in vitro release studies of modified release multiple unit particulate system (MUPS) of venlafaxine hydrochloride

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