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1.
Siahi MR Barzegar-Jalali M Monajjemzadeh F Ghaffari F Azarmi S 《AAPS PharmSciTech》2005,6(4):E626-E632
The present study was performed to design oral controlled delivery systems for the water-soluble drug, verapamil hydrochloride,
using natural and semisynthetic polymers as carriers in the forms of 1- and 3-layer matrix tablets. Verapamil hydrochloride
1-layer matrix tablets containing hydroxypropylmethylcellulose, tragacanth, and acacia either alone or mixed were prepared
by direct compression technique. 3-layer matrix tablets were prepared by compressing the polymers as release retardant layers
on both sides of the core containing the drug. The prepared tablets were subjected to in vitro drug release studies. Tragacanth
when used as the carrier in the formulation of 1- and 3-layer matrices produced satisfactory release prolongation either alone
or in combination with the other 2 polymers. On the other hand, acacia did not show enough prolonging efficiency in 1- and
3-layer matrix tablets. The results also showed that the location of the polymers in the 3-layer tablets has a pronounced
effect on the drug release. Kinetic analysis of drug release from matrices exhibiting sustained release indicated that release
was predominantly attributable to the contribution made by Fickian diffusion, while the erosion/relaxation mechanisms had
a minor role in the release.
Published: December 7, 2005 相似文献
2.
Novel polyelectrolyte hydrogels (coded as GA) based on cationic guar gum (CGG) and acrylic acid monomer by photoinitiated free-radical polymerization were synthesized with various feed compositions. Fourier transform infrared spectra (FTIR), scanning electron microscopy (SEM), and differential scanning calorimetry (DSC) confirmed that the formation of the polyelectrolyte hydrogels was attributed to the strong electrostatic interaction between cationic groups in CGG and anionic groups in poly (acrylic acid) (PAA). Swelling experiments provided important information on drug diffusion properties, which indicated the GA hydrogels were highly sensitive to pH environments. Potential applications of the hydrogels matrices in controlled drug delivery were also examined. The ketoprofen-loaded CGG/PAA matrices were prepared by hydrogels and directly compressed tablets, respectively. Release behavior of ketoprofen relied on the preparative methods of matrices, ratios of CGG/AA and pH environments. The release mechanism was studied by fitting experimental data to a model equation and calculating the corresponding parameters. The result showed that the kinetics of drug release from the hydrogels in pH 7.4 buffer solution was mainly non-Fickian diffusion. However, for tablets, the drug release in pH 7.4 buffer solution was mainly affected by polymer erosion. The pH of the dissolution medium appeared to have a strong effect on the drug transport mechanism. At more basic pH values, Case II transport was observed, indicating a drug release mechanism highly influenced by macromolecular chain relaxation. The ketoprofen release is also tested in the conditions chosen to simulate gastrointestinal tract conditions. The results implied that the GA hydrogels can be exploited as potential carriers for colon-specific drug delivery. 相似文献
3.
Phaechamud T 《AAPS PharmSciTech》2008,9(2):668-674
The purpose of this study was to prepare and evaluate layered matrix tablets of propranolol HCl containing HPMC and phytowax
as matrix component using direct compression technique. Layering with this polymeric matrix could prolong the release of drug
and shift the release pattern approach to zero order as described from the least square curve fitting. Increasing the amount
of coating layer could apparently prolong the drug release. The longer lag time of drug release from one planar apparently
when the amount of coating layer was increased. HPMC concentration and compression force did not affect the drug release from
this three-layer tablet. The drug release from this three-layer tablet was influenced by hydrodynamic force. An increase in
stirring rate was a corresponding increasing in the release rate. From photoimage and SEM, gel mass of HPMC was increased
with time during dissolution and covered the core surface, therefore dissolved drug molecules were allowed to diffuse out
from the core through the polymer network of gel layer containing the porous structure. This suggested that HPMC and phytowax
could be fabricated into the layered matrix tablet exhibiting sustained drug release. 相似文献
4.
The purpose of this research was to design oral controlled release (CR) matrix tablets of zidovudine (AZT) using hydroxypropyl
methylcellulose (HPMC), ethyl cellulose (EC) and carbopol-971P (CP) and to study the effect of various formulation factors
on in vitro drug release. Release studies were carried out using USP type 1 apparatus in 900 ml of dissolution media. Release kinetics
were analyzed using zero-order, Higuchi’s square root and Ritger–Peppas’ empirical equations. Release rate decreased with
increase in polymer proportion and compression force. The release rate was lesser in formulations prepared using CP (20%)
as compared to HPMC (20%) as compared to EC (20%). No significant difference was observed in the effect of pH of dissolution
media on drug release from formulations prepared using HPMC or EC, but significant difference was observed in CP based formulations.
Decrease in agitation speed from 100 to 50 rpm decreased release rate from HPMC and CP formulations but no significant difference
was observed in EC formulations. Mechanism of release was found to be dependent predominantly on diffusion of drug through
the matrix than polymer relaxation incase of HPMC and EC formulations, while polymer relaxation had a dominating influence
on drug release than diffusion incase of CP formulations. Designed CR tablets with pH independent drug release characteristics
and an initial release of 17–25% in first hour and extending the release up to 16–20 h, can overcome the disadvantages associated
with conventional tablets of AZT. 相似文献
5.
This study compared the release behavior of single-unit (tablets, capsules) and multiple-unit (minitablets in capsules) controlled-release
systems of furosemide. The swelling and erosion behaviors of these systems, which contained the swellable hydrophilic polymers
sodium alginate (high viscosity) and Carbopol 974P, were compared. Swelling and erosion experiments showed a high degree of
swelling and limited erosion for the Carbopol preparations, whereas less swelling but greater erosion was observed for the
sodium alginate preparations. The sodium alginate preparations were eroded in 6 hours, while Carbopol preparations exhibited
limited erosion within this period of time. These results appear to be attributed to the physicochemical characteristics of
the polymers used in this study. Polymer characteristics greatly influenced the release of furosemide (model drug) from the
formulations prepared and tested. Sodium alginate had a less pronounced sustained release effect compared with Carbopol (ie,
in 8 hours all 3 sodium alginate dosage forms displayed complete release of furosemide, while only 30% of the drug was released
from Carbopol dosage forms). Finally, all 3 Carbopol dosage forms (single- and multiple-unit) displayed similar release behavior
while sodium alginate dosage forms displayed a different and more distinctive behavior. Minitablets and tablets showed a greater
sustained release effect compared with capsules. Evaluation of the release data indicates that the release mechanism for sodium
alginate formulations may be attributed to erosion/dissolution, while for Carbopol it may be attributed mainly to polymer
relaxation and diffusion of the drug from the polymer surface. 相似文献
6.
Sirpa Vuorinen Jyrki Heinämäki Osmo Antikainen Mohammed Lahcini Timo Repo Jouko Yliruusi 《AAPS PharmSciTech》2009,10(2):566-573
Sugar end-capped poly-d,l-lactide (SPDLA) polymers were investigated as a potential release controlling excipient in oral sustained release matrix
tablets. The SPDLA polymers were obtained by a catalytic ring-opening polymerization technique using methyl α-d-gluco-pyranoside as a multifunctional initiator in the polymerization. Polymers of different molecular weights were synthesized
by varying molar ratios of monomer/catalyst. The matrix tablets were prepared by direct compression technique from the binary
mixtures of SPDLA and microcrystalline cellulose, and theophylline was used as a model drug. The tablet matrices showed in vitro reproducible drug release profiles with a zero-order or diffusion-based kinetic depending on the SPDLA polymer grade used.
Further release from the tablet matrices was dependent on the molecular weight of the SPDLA polymer applied. The drug release
was the fastest with the lowest molecular weight SPDLA grade, and the drug release followed zero-order rate. With the higher
molecular weight SPDLAs, more prolonged dissolution profiles for the matrix tablets (up to 8–10 h) were obtained. Furthermore,
the prolonged drug release was independent of the pH of the dissolution media. In conclusion, SPDLAs are a novel type of drug
carrier polymers applicable in oral controlled drug delivery systems. 相似文献
7.
The aim of the present investigation was to develop oral controlled release matrix tablet formulations of isoniazid using
hydroxypropyl methylcellulose (HPMC) as a hydrophilic release retardant polymer and to study the influence of various formulation
factors like proportion of the polymer, polymer viscosity grade, compression force, and release media on the in vitro release characteristics of the drug. The formulations were developed using wet granulation technology. The in vitro release studies were performed using US Pharmacopoeia type 1 apparatus (basket method) in 900 ml of pH 7.4 phosphate buffer
at 100 rpm. The release kinetics was analyzed using Korsmeyer–Peppas model. The release profiles were also analyzed using
statistical method (one-way analysis of variance) and f
2 metric values. The release profiles found to follow Higuchi’s square root kinetics model irrespective of the polymer ratio
and the viscosity grade used. The results in the present investigation confirm that the release rate of the drug from the
HPMC matrices is highly influenced by the drug/HPMC ratio and viscosity grade of the HPMC. Also, the effect of compression
force and release media was found to be significant on the release profiles of isoniazid from HPMC matrix tablets. The release
mechanism was found to be anomalous non-Fickian diffusion in all the cases. In the present investigation, a series of controlled
release formulations of isoniazid were developed with different release rates and duration so that these formulations could
further be assessed from the in vivo bioavailability studies. The formulations were found to be stable and reproducible. 相似文献
8.
The purpose of the study was to investigate the effect of drug solubility on polymer hydration and drug dissolution from modified release matrix tablets of polyethylene oxide (PEO). Different PEO matrix tablets were prepared using acetaminophen (ACE) and ibuprofen (IBU) as study compounds and Polyox WSR301 (PEO) as primary hydrophilic matrix polymer. Tablet dissolution was tested using the USP Apparatus II, and the hydration of PEO polymer during dissolution was recorded using a texture analyzer. Drug dissolution from the preparations was dependent upon drug solubility, hydrogel formation and polymer proportion in the preparation. Delayed drug release was attributed to the formation of hydrogel layer on the surface of the tablet and the penetration of water into matrix core through drug dissolution and diffusion. A multiple linear regression model could be used to describe the relationship among drug dissolution, polymer ratio, hydrogel formation and drug solubility; the mathematical correlation was also proven to be valid and adaptable to a series of study compounds. The developed methodology would be beneficial to formulation scientists in dosage form design and optimization. 相似文献
9.
Interpolyelectrolyte (IPE) complexation between carrageenan (CG) and Eudragit E (EE) was studied in 0.1 M HCl and was used
to develop floating matrix tablets aimed to prolong gastric-residence time and sustain delivery of the loaded drug. The optimum
EE/CG IPE complexation weight ratio (0.6) was determined in 0.1 M HCl using apparent viscosity measurements. The IPE complex
was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. Metronidazole matrix tablets
were prepared by direct compression using EE, CG, or hybrid EE/CG with ratio optimal for IPE complexation. Corresponding effervescent
tablets were prepared by including Na bicarbonate as an effervescent agent. Tablets were evaluated for in vitro buoyancy and drug release in 0.1 M HCl. Both CG and EE–CG effervescent matrices (1:2 drug to polymer weight ratio, 60 mg
Na bicarbonate) achieved fast and prolonged floating with floating lag times less than 30 s and floating duration of more
than 10 h. The corresponding EE effervescent matrices showed delayed floating and rapid drug release, and completely dissolved
after 3 h of dissolution. CG matrices showed an initial burst drug release (48.3 ± 5.0% at 1 h) followed by slow drug release
over 8 h. EE–CG matrices exhibited sustained drug release in almost zero-order manner for 10 h (68.2 ± 6.6%). The dissolution
data of these matrices were fitted to different dissolution models. It was found that drug release followed zero-order kinetics
and was controlled by the superposition of the diffusion and erosion. 相似文献
10.
The present study was undertaken to evaluate the gum exudates of Terminalia catappa Linn. (TC gum) as a release retarding excipient in oral controlled drug delivery system. The rheological properties of TC
gum were studied and different formulation techniques were used to evaluate the comparative drug release characteristics.
The viscosity was found to be dependent on concentration and pH. Temperature up to 60°C did not show significant effect on
viscosity. The rheological kinetics evaluated by power law, revealed the shear thinning behavior of the TC gum dispersion
in water. Matrix tablets of TC gum were prepared with the model drug dextromethorphan hydrobromide (DH) by direct compression,
wet granulation and solid dispersion techniques. The dissolution profiles of the matrix tablets were compared with the pure
drug containing capsules using the USP Basket apparatus with 500 ml phosphate buffer of pH 6.8 as a dissolution medium. The
drug release from the compressed tablets containing TC gum was comparatively sustained than pure drug containing capsules.
Even though all the formulation techniques showed reduction of dissolution rate, aqueous wet granulation showed the maximum
sustained release of more than 8 h. The release kinetics estimated by the power law revealed that the drug release mechanism
involved in the dextromethorphan matrix is anomalous transport as indicated by the release exponent n values. Thus the study confirmed that the TC gum might be used in the controlled drug delivery system as a release-retarding
polymer. 相似文献
11.
Saeed Shojaee Parastou Emami Ahmad Mahmood Yemisi Rowaiye Alusine Dukulay Waseem Kaialy Iain Cumming Ali Nokhodchi 《AAPS PharmSciTech》2015,16(6):1281-1289
Polyethylene oxide has been researched extensively as an alternative polymer to hydroxypropyl methylcellulose (HPMC) in controlled drug delivery due to its desirable swelling properties and its availability in a number of different viscosity grades. Previous studies on HPMC have pointed out the importance of particle size on drug release, but as of yet, no studies have investigated the effect of particle size of polyethylene oxide (polyox) on drug release. The present study explored the relationship between polymer level and particle size to sustain the drug release. Tablets produced contained theophylline as their active ingredient and consisted of different polyethylene oxide particle size fractions (20–45, 45–90, 90–180 and 180–425 μm). It was shown that matrices containing smaller particle sizes of polyox produced harder tablets than when larger polyox particles were used. The release studies showed that matrices consisting of large polyox particles showed a faster release rate than matrices made from smaller particles. Molecular weight (MW) of the polymer was a key determining step in attaining sustained release, with the high MW of polyox resulting in a delayed release profile. The results showed that the effect of particle size on drug release was more detrimental when a low concentration of polyox was used. This indicates that care must be taken when low levels of polyox with different particle size fractions are used. More robust formulations could be obtained when the concentration of polyox is high. Differential scanning calorimetry (DSC) traces showed that particle size had no major effect on the thermal behaviour of polyox particles.KEY WORDS: DSC traces, particle size, polyox, sustained release, theophylline 相似文献
12.
The aim of this work is to design pH-dependent swellable and erodable-buffered matrices and to study the effect of the microenvironment
pH on the release pattern of diclofenac sodium. Buffered matrix tablets containing diclofenac sodium, physically mixed with
hydrophilic polymer (hydroxypropyl methylcellulose [HPMC]) and pH-dependent solubility polymer (Eudragit L100-55) were prepared
with different microenvironment pHs. The release of diclofenac sodium from the buffer matrices was studied in phosphate buffer
solutions of pH 5.9 and 7.4. The swelling and erosion matrices containing only HPMC and Eudragit L100-55 were studied in phosphate
buffer solution of pH similar to the microenvironment pHs of the matrices. Drug release from matrices was found to be linear
as a function of time. Amount of drug released was found to be higher in the medium of pH 7.4 than that of pH 5.9. The rate
of drug release increased with the increase of the microenvironment pH of the matrices as determined from the slope. The pattern
of drug release did not change with the change of microenvironment pH. The swelling and erosion occurred simultaneously from
matrices made up of HPMC and Eudragit L100-55. Both extent of swelling and erosion increased with increase of the medium pH.
It was concluded from this study that changing the pH within the matrix influenced the rate of release of the drug without
affecting the release pattern.
Fax: Not Forwarded 相似文献
13.
Providing pH-independent oral release of weakly basic drugs with conventional matrix tablets can be challenging because of the pH-dependent solubility characteristics of the drugs and the changing pH environment along the gastrointestinal tract. The aim of the present study was to use a hydrophobic polymer to overcome the issue of pH-dependent release of weakly basic model drug verapamil hydrochloride from matrix tablets without the use of organic buffers in the matrix formulations. Silicone pressure-sensitive adhesive (PSA) polymer was evaluated because of its unique properties of low surface energy, hydrophobicity, low glass transition temperature, high electrical resistance, and barrier to hydrogen ion diffusion. Drug release, hydrogen ion diffusion, tablet contact angle, and internal tablet microenvironment pH with matrix tablets prepared using PSA were compared with those using water-insoluble ethyl cellulose (EC). Silicone PSA films showed higher resistance to hydrogen ion diffusion compared with EC films. Verapamil hydrochloride tablets prepared using silicone PSA showed higher hydrophobicity and lower water uptake than EC tablets. Silicone PSA tablets also showed pH-independent release of verapamil and decreased in dimensions during drug dissolution. By contrast, verapamil hydrochloride tablets prepared using EC did not achieve pH-independent release. 相似文献
14.
The exudates from the incised trunk of Terminalia randii has been evaluated as controlled release excipient in comparison with xanthan gum and hydroxypropylmethylcellulose (HPMC)
using carvedilol (water insoluble) and theophylline (water soluble) as model drugs. Matrix tablets were prepared by direct
compression and the effects of polymer concentration and excipients—spray dried lactose, microcrystalline cellulose and dicalcium
phosphate dihydrate on the mechanical (crushing strength (CS) friability (F) and crushing strength–friability ratio (CSFR))
and drug release properties of the matrix tablets were evaluated. The drug release data were fitted into different release
kinetics equations to determine the drug release mechanism(s) from the matrix tablets. The results showed that the CS and
CSFR increased with increase in polymer concentration while F decreased. The ranking of CS and CSFR was HPMC > terminalia
> xanthan while the ranking was reverse for F. The ranking for t
25 (i.e. time for 25% drug release) at a polymer concentration of 60% was xanthan > terminalia = HPMC. The dissolution time,
t
25, of theophylline matrices was significantly lower (p < 0.001) than those of carvedilol matrix tablets. Drug release from the matrices was by swelling, diffusion and erosion.
The mechanical and drug release properties of the tablets were significantly (p < 0.05) dependent on the type and concentration of polymer and excipients used with the release mechanisms varying from Fickian
to anomalous. Terminalia gum compared favourably with standard polymers when used in controlled release matrices and could
serve as a suitable alternative to the standard polymers in drug delivery. 相似文献
15.
The objective of the present study was to design and evaluate unilaminate transdermal adhesive matrix systems capable of diffusing
bupropion base at a constant rate over an extended period of time as an alternative route of administration. Unilaminate transdermal
adhesive matrices have been fabricated with different concentrations of Eudragit E as the adhesive and rate-controlling polymer.
The in vitro release and epidermal flux through human cadaver skin were studied. The release of drug from the matrices obeyed
zero order release kinetics (r
2=0.9810 to 0.9960). The delivery rate of bupropion ranged from 10.5 mg to 31.4 mg per day from a 3.14 cm2 area of matrix. The relation between concentration of bupropion base in matrix and epidermal flux, concentration of drug
in matrix, and epidermal adsorption of bupropion during diffusion follow hyperbolic fashion. Triethylcitrate (TEC) and dibutylphthalate
(DBP) have no influence on the diffusion of bupropion through human cadaver skin when used as plasticizers. Incorporation
of succinic acid in the adhesive matrix retarded diffusion due to the formation of rigid cross linking of the polymer, while
propylene glycol and myristic acid, alone or in combination, significantly enhanced the flux of bupropion through human cadaver
skin. 相似文献
16.
Tamara Gonçalves-Araújo Ali R. Rajabi-Siahboomi Isidoro Caraballo 《AAPS PharmSciTech》2010,11(2):558-562
The principles of the percolation theory were applied to further understand and design hydroxypropyl methylcellulose (HPMC)
extended release matrix tablets containing carbamazepine and verapamil HCl. This statistical theory studies disordered or
chaotic systems where the components are randomly distributed in a lattice. The application of this theory to study the hydration
and drug release of hydrophilic matrices allows describing the changes in hydration and drug release kinetics of swellable
matrices. The aim of this work was to study and develop extended release matrix formulations for carbamazepine and verapamil
HCl, containing hypromellose (HPMC, METHOCEL™ Premium K100M CR) as rate controlling polymer using the concepts of percolation
theory. The knowledge of the percolation threshold of the components of the matrix formulations contributes to improve their
design. First, reducing the time to market and second, avoiding to formulate in the nearby of the percolation threshold, which
will result in a lower variability. Therefore these formulations will be more robust when they are prepared at industrial
scale. The HPMC percolation threshold for drugs with very different water solubilities was determined and it was shown that
there was no significant influence of drug solubility on the HPMC critical concentration threshold (excipient percolation
threshold). This may be related to the versatility and broad functionality of the swelling hydrophilic matrices. 相似文献
17.
The purpose of the present research was to produce a quick/slow biphasic delivery system for ibuprofen. A dual-component tablet
made of a sustained release tableted core and an immediate release tableted coat was prepared by direct compression. Both
the core and the coat contained a model drug (ibuprofen). The sustained release effect was achieved with a polymer (hydroxypropyl
methylcellulose [HPMC] or ethylcellulose) to modulate the release of the drug. The in vitro drug release profile from these
tablets showed the desired biphasic release behavior: the ibuprofen contained in the fast releasing component was dissolved
within 2 minutes, whereas the drug in the core tablet was released at different times (⊂16 or >24 hours), depending on the
composition of the matrix tablet. Based on the release kinetic parameters calculated, it can be concluded that the HPMC core
was suitable for providing a constant and controlled release (zero order) for a long period of time.
Published: September 21, 2007 相似文献
18.
Zolpidem tartrate is a non-benzodiazepine analogue of imidazopyridine of sedative and hypnotic category. It has a short half-life with usual dosage regimen being 5 mg, two times a day, or 10 mg, once daily. The duration of action is considered too short in certain circumstances. Thus, it is desirable to lengthen the duration of action. The formulation design was implemented by preparing extended-release tablets of zolpidem tartrate using the biphasic delivery system technology, where sodium starch glycolate acts as a superdisintegrant in immediate-release part and hydroxypropyl methyl cellulose as a release retarding agent in extended-release core. Tablets were prepared by direct compression. Both the core and the coat contained the drug. The pre-compression blends were evaluated for angle of repose, bulk density, and compressibility index. The tablets were evaluated for thickness, hardness, weight variation test, friability, and in vitro release studies. No interaction was observed between zolpidem tartrate and excipients from the Fourier transform infrared spectroscopy and differential scanning calorimetry analysis. The results of all the formulations prepared were compared with reference product Stilnoct®. Optimized formulations showed release patterns that match the United States Pharmacopeia (USP) guidelines for zolpidem tartrate extended-release tablets. The mechanism of drug release was studied using different mathematical models, and the optimized formulation has shown Fickian diffusion. Accelerated stability studies were performed on the optimized formulation.KEY WORDS: biphasic delivery system technology, hydroxypropyl methyl cellulose, modified release, sodium starch glycolate, zolpidem tartrate 相似文献
19.
The goal of the present study was to develop and evaluate microsponge-based topical delivery system of mupirocin for sustained
release and enhanced drug deposition in the skin. Microsponges containing mupirocin were prepared by an emulsion solvent diffusion
method. The effect of formulation and process variables such as internal phase volume and stirring speed on the physical characteristics
of microsponges were examined on optimized drug/polymer ratio by 32 factorial design. The optimized microsponges were incorporated into an emulgel base. In vitro drug release, ex vivo drug deposition, and in vivo antibacterial activity of mupirocin-loaded formulations were studied. Developed microsponges were spherical and porous, and
there was no interaction between drug and polymer molecules. Emulgels containing microsponges showed desired physical properties.
Drug release through cellulose dialysis membrane showed diffusion-controlled release pattern and drug deposition studies using
rat abdominal skin exhibited significant retention of active in skin from microsponge-based formulations by 24 h. The optimized
formulations were stable and nonirritant to skin as demonstrated by Draize patch test. Microsponges-based emulgel formulations
showed prolonged efficacy in mouse surgical wound model infected with S. aureus. Mupirocin was stable in topical emulgel formulations and showed enhanced retention in the skin indicating better potential
of the delivery system for treatment of primary and secondary skin infections, such as impetigo, eczema, and atopic dermatitis. 相似文献
20.
Famida G. Hoosain Yahya E. Choonara Pradeep Kumar Lomas K. Tomar Charu Tyagi Lisa C. du Toit Viness Pillay 《AAPS PharmSciTech》2014,15(5):1292-1306
The current study involved the development of a novel sustained release crosslinked semi-IPN xerogel matrix tablet prepared by chemical crosslinking of poly(ethylene) oxide (PEO) and gellan gum (GG) employing epichlorohydrin (EPI) as crosslinker. A Box–Behnken design was employed for the statistical optimization of the matrix system to ascertain the ideal combination of native polymeric and crosslinking agents. Characterization studies were performed by employing standard polymer characterization techniques such as Fourier transform infrared spectrometry, differential scanning calorimetry, and scanning electron microscopy. Formulated matrix tablets displayed zero-order release kinetics, extending over 24 h. The mechanism of drug release was primarily by swelling and surface erosion. Crosslinked semi-IPN xerogel matrix tablets were compared to non-crosslinked polymer blends; results from the study conducted showed that the physiochemical properties of the PEO and GG were sufficiently modified to allow for sustained release of sulpiride with a 100% drug release at 24 h in a controlled manner as compared to non-crosslinked formulations which displayed further release beyond the test period. Crosslinked formulations displayed water uptake between 450 and 500% indicating a controlled rate of swelling and erosion allowing for sustained release. Surface morphology of the crosslinked system depicted a porous structure formed by interpenetrating networks of polymers, allowing for a greater degree of controlled penetration into the system affording it the ability to sustain drug release. Therefore, conclusively, based on the study performed, crosslinked PEO-GG allows for the sustained release of sulpiride from a hydrophilic semi-IPN xerogel matrix system.KEY WORDS: epichlorohydrin, matrix tablet, semi-interpenetrating polymer network, sustained release, sulpiride 相似文献