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1.
Gazzi Shanker Chegonda K. Kumar Chandra Sekhara Rao Gonugunta B. Vijaya Kumar Prabhakar Reddy Veerareddy 《AAPS PharmSciTech》2009,10(2):530-539
The study aim was concerned with formulation and evaluation of bioadhesive buccal drug delivery of tizanidine hydrochloride
tablets, which is extensively metabolized by liver. The tablets were prepared by direct compression using bioadhesive polymers
such as hydroxylpropyl methylcellulose K4M, sodium carboxymethyl cellulose alone, and a combination of these two polymers.
In order to improve the permeation of drug, different permeation enhancers like beta-cyclodextrin (β-CD), hydroxylpropyl beta-cyclodextrin
(HP-β-CD), and sodium deoxycholate (SDC) were added to the formulations. The β-CD and HP-β-CD were taken in 1:1 molar ratio
to drug in formulations. Bioadhesion strength, ex vivo residence time, swelling, and in vitro dissolution studies and ex vivo permeation studies were performed. In vitro release of optimized bioadhesive buccal tablet was found to be non-Fickian. SDC was taken in 1%, 2%, and 3% w/w of the total tablet weight. Stability studies in natural saliva indicated that optimized formulation has good stability in
human saliva. In vivo mucoadhesive behavior of optimized formulation was performed in five healthy male human volunteers and subjective parameters
were evaluated. 相似文献
2.
The present research work focused on the comparative assessment of porous versus nonporous films in order to develop a suitable buccoadhesive device for the delivery of glibenclamide. Both films were prepared by solvent casting technique using the 32 full factorial design, developing nine formulations (F1–F9). The films were evaluated for ex vivo mucoadhesive force, ex vivo mucoadhesion time, in vitro drug release (using a modified flow-through drug release apparatus), and ex vivo drug permeation. The mucoadhesive force, mucoadhesion time, swelling index, and tensile strength were observed to be directly proportional to the content of HPMC K4M. The optimized porous film (F4) showed an in vitro drug release of 84.47 ± 0.98%, ex vivo mucoadhesive force of 0.24 ± 0.04 N, and ex vivo mucoadhesion time of 539.11 ± 3.05 min, while the nonporous film (NF4) with the same polymer composition showed a release of 62.66 ± 0.87%, mucoadhesive force of 0.20 ± 0.05 N, and mucoadhesive time of 510 ± 2.00 min. The porous film showed significant differences for drug release and mucoadhesion time (p < 0.05) versus the nonporous film. The mechanism of drug release was observed to follow non-Fickian diffusion (0.1 < n < 0.5) for both porous and nonporous films. Ex vivo permeation studies through chicken buccal mucosa indicated improved drug permeation in porous films versus nonporous films. The present investigation established porous films to be a cost-effective buccoadhesive delivery system of glibenclamide.KEY WORDS: buccoadhesive drug delivery, glibenclamide, in vitro release and ex vivo permeation, porous film 相似文献
3.
The aim of the present study was to develop and evaluate a buccal adhesive tablet containing ondansetron hydrochloride (OH).
Special punches and dies were fabricated and used while preparing buccal adhesive tablets. The tablets were prepared using
carbopol (CP 934), sodium alginate, sodium carboxymethylcellulose low viscosity (SCMC LV), and hydroxypropylmethylcellulose
(HPMC 15cps) as mucoadhsive polymers to impart mucoadhesion and ethyl cellulose to act as an impermeable backing layer. The
formulations were prepared by direct compression and characterized by different parameters such as weight uniformity, content
uniformity, thickness, hardness, swelling index, in vitro drug release studies, mucoadhesive strength, and ex vivo permeation study. As compared with the optimized formulation composed of OH—5 mg, CP 934—30 mg, SCMC LV—165 mg, PEG 6000—40 mg,
lactose—5 mg, magnesium stearate—1.5 mg, and aspartame—2 mg, which gave the maximum release (88.15%), non-bitter (OH) that
form namely ondansetron base and complexed ondansetron was used in order to make the selected formulation acceptable to human.
The result of the in vitro release studies and permeation studies through bovine buccal mucosa revealed that complexed ondansetron gave the maximum
release and permeation. The stability of drug in the optimized adhesive tablet was tested for 6 h in natural human saliva;
both the drug and device were found to be stable in natural human saliva. Thus, buccal adhesive tablet of ondansetron could
be an alternative route to bypass the hepatic first-pass metabolism and to improve the bioavailability of (OH). 相似文献
4.
Surya N. Ratha Adhikari Bhabani S. Nayak Amit K. Nayak Biswaranjan Mohanty 《AAPS PharmSciTech》2010,11(3):1038-1044
Buccal patches for the delivery of atenolol using sodium alginate with various hydrophilic polymers like carbopol 934 P, sodium
carboxymethyl cellulose, and hydroxypropyl methylcellulose in various proportions and combinations were fabricated by solvent
casting technique. Various physicomechanical parameters like weight variation, thickness, folding endurance, drug content,
moisture content, moisture absorption, and various ex vivo mucoadhesion parameters like mucoadhesive strength, force of adhesion, and bond strength were evaluated. An in vitro drug release study was designed, and it was carried out using commercial semipermeable membrane. All these fabricated patches
were sustained for 24 h and obeyed first-order release kinetics. Ex vivo drug permeation study was also performed using porcine buccal mucosa, and various drug permeation parameters like flux and
lag time were determined. 相似文献
5.
The purpose of this research work was to establish mucoadhesive buccal devices of propranolol hydrochloride (PRH) in the forms
of bilayered and multilayered tablets. The tablets were prepared using sodium carboxymethylcellulose (SCMC) and Carbopol-934
(CP) as bioadhesive polymers to impart mucoadhesion and ethyl cellulose (EC) to act as an impermeable backing layer. Buccal
devices were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, surface
pH, swelling index, ex vivo mucoadhesive strength, ex vivo mucoadhesion time, in vitro drug release, and in vitro drug permeation.
As compared with bilayered tablets, multilayered tablets showed slow release rate of drug with improved ex vivo bioadhesive
strength and enhanced ex vivo mucoadhesion time. The mechanism of drug release was found to be non-Fickian diffusion (value
of n between 0.5 and 1.0) for both the buccal devices. The stability of drug in both the optimized buccal devices was tested
for 6 hours in natural human saliva; both the buccal devices were found to be stable in natural human saliva. The present
study concludes that mucoadhesive buccal devices of PRH can be a good way to bypass the extensive hepatic first-pass metabolism
and to improve the bioavailability of PRH.
Published: March 16, 2007 相似文献
6.
In this study an attempt was made to prepare mucoadhesive microcapsules of gliclazide using various mucoadhesive polymers
designed for oral controlled release. Gliclazide microcapsules were prepared using sodium alginate and mucoadhesive polymer
such as sodium carboxymethyl cellulose (sodium CMC), carbopol 934P or hydroxy propylmethyl cellulose (HPMC) by orifice-ionic
gelation method. The microcapsules were evaluated for surface morphology and particle shape by scanning electron microscope.
Microcapsules were also evaluated for their microencapsulation efficiency, in vitro wash-off mucoadhesion test, in vitro drug release and in vivo study. The microcapsules were discrete, spherical and free flowing. The microencapsulation efficiency was in the range of
65–80% and microcapsules exhibited good mucoadhesive property in the in vitro wash off test. The percentage of microcapsules adhering to tissue at pH 7.4 after 6 h varied from 12–32%, whereas the percentage
of microcapsules adhering to tissue at pH 1.2 after 6 h varied from 35–68%. The drug release was also found to be slow and
extended for more than 16 h. In vivo testing of the mucoadhesive microcapsules in diabetic albino rats demonstrated significant antidiabetic effect of gliclazide.
The hypoglycemic effect obtained by mucoadhesive microcapsules was for more than 16 h whereas gliclazide produced an antidiabetic
effect for only 10 h suggesting that mucoadhesive microcapsules are a valuable system for the long term delivery of gliclazide. 相似文献
7.
Sanjay Bansal Sarwar Beg Babita Garg Abhay Asthana Gyati S. Asthana Bhupinder Singh 《AAPS PharmSciTech》2016,17(5):1086-1099
The objective of the present studies was systematic development of floating-bioadhesive gastroretentive tablets of cefuroxime axetil employing rational blend of hydrophilic polymers for attaining controlled release drug delivery. As per the QbD-based approach, the patient-centric target product profile and quality attributes of tablet were earmarked, and preliminary studies were conducted for screening the suitability of type of polymers, polymer ratio, granulation technique, and granulation time for formulation of tablets. A face-centered cubic design (FCCD) was employed for optimization of the critical material attributes, i.e., concentration of release controlling polymers, PEO 303 and HPMC K100 LV CR, and evaluating in vitro buoyancy, drug release, and ex vivo mucoadhesion strength. The optimized formulation was embarked upon through numerical optimization, which yield excellent floatation characteristic with drug release control (i.e., T 60%?>?6 h) and bioadhesion strength. Drug-excipient compatibility studies through FTIR and P-XRD revealed the absence of any interaction between the drug and polymers. In vivo evaluation of the gastroretentive characteristics through X-ray imaging and in vivo pharmacokinetic studies in rabbits revealed significant extension in the rate of drug absorption (i.e., T max, K a, and MRT) from the optimized tablet formulation as compared to the marketed formulation. Successful establishment of various levels of in vitro/in vivo correlations (IVIVC) substantiated high degree of prognostic ability of in vitro dissolution conditions in predicting the in vivo performance. In a nutshell, the studies demonstrate successful development of the once-a-day gastroretentive formulations of cefuroxime axetil with controlled drug release profile and improved compliance. 相似文献
8.
The purpose of this research was to develop and evaluate buccal mucoadhesive controlled release tablets of lercanidipine hydrochloride
using polyethylene oxide and different viscosity grades of hydroxypropyl methylcellulose individually and in combination.
Effect of polymer type, proportion and combination was studied on the drug release rate, release mechanism and mucoadhesive
strength of the prepared formulations. Buccal mucoadhesive tablets were made by direct compression and were characterized
for content uniformity, weight variation, friability, surface pH, thickness and mechanism of release. In order to estimate
the relative enhancement in bioavailability one optimized formulation was evaluated in rabbits. Further, placebo tablets were
also evaluated for acceptability in human subjects. Results indicated acceptable physical characteristics of designed tablets
with good content uniformity and minimum weight variation. Drug release and mucoadhesive strength were found to depend upon
polymer type, proportion and viscosity. The formulations prepared using poly ethylene oxide gave maximum mucoadhesion. The
release mechanism of most formulations was found to be of anomalous non-Fickian type. In vivo studies of selected formulation in rabbits demonstrated significant enhancement in bioavailability of lercanidipine hydrochloride
relative to orally administered drug. Moreover, in human acceptability studies of placebo formulations, the designed tablets
adhered well to the buccal mucosa for more than 4 h without causing any discomfort. It may be concluded that the designed
buccoadhesive controlled release tablets have the potential to overcome the disadvantage of poor and erratic oral bioavailability
associated with the presently marketed formulations of lercanidipine hydrochloride. 相似文献
9.
Two groups of fluconazole mucoadhesive buccal discs were prepared: (a) Fluconazole buccal discs prepared by direct compression
containing bioadhesive polymers, namely, Carbopol 974p (Cp), sodium carboxymethyl cellulose (SCMC), or sodium alginate (SALG)
in combination with hydroxypropyl methylcellulose (HPMC) or hydroxyethyl cellulose (HEC). (b) Fluconazole buccal discs prepared
by freeze drying containing different polymer combinations (SCMC/HPMC, Cp/HPMC, SALG/HPMC, and chitosan/SALG). The prepared
discs were evaluated by investigating their release pattern, swelling capacity, mucoadhesion properties, and in vitro adhesion time. In vivo evaluation of the buccal disc and in vivo residence times were also performed. Fluconazole salivary concentration after application of fluconazole buccal systems to
four healthy volunteers was determined using microbiological assay and high-performance liquid chromatography. SCMC/HPMC buccal
disc prepared by direct compression could be considered comparatively superior mucoadhesive disc regarding its in vitro adhesion time, in vivo residence time, and in vitro/in vivo release rates of the drug. Determination of the amount of drug released in saliva after application of the selected fluconazole
disc confirmed the ability of the disc to deliver the drug over a period of approximately 5 h and to reduce side effects and
possibility of drug interaction encountered during systemic therapy of fluconazole, which would be beneficial in the case
of oral candidiasis. 相似文献
10.
The objective of this work was to design a mucoadhesive tablet with a potential use in the treatment of oral candidosis. A 2-layered tablet containing nystain was formulated. Lactose CD (direct compression), carbomer (CB), and hydroxypropylmethylcellulose (HPMC) were used as excipients. Tablets were obtained through direct compression. Properties such as in vitro mucoadhesion, water uptake, front movements, and drug release were evaluated. The immediate release layer was made of lactose CD (100 mg) and nystatin (30 mg). The CB:HPMC 9∶1 mixture showed the best mucoadhesion properties and was selected as excipient for the mucoadhesive polymeric layer (200 mg). The incorporation of nystatin (33.3 mg) in this layer affected the water uptake, which, in turn, modified the erosion front behavior. Nystatin showed a first-order release. The polymeric layer presented an anomalous kinetic (n=0.82) when this layer layer was individually evaluated. The mucoadhesive tablet formulated in this work releases nystatin quickly from the lactose layer and then in a sustained way, during approximately 6 hours. from the polymeric layer. The mixture CB:HPMC 9∶1 showed good in vitro mucoadhesion. A swelling-diffusion process modulates the release of nystatin from this layer. A non-Fickian (anomalous) kinetic was observed. 相似文献
11.
This work aims to prepare sustained release buccal mucoadhesive lyophilized chitosan sponges of buspirone hydrochloride (BH) to improve its systemic bioavailability. Chitosan sponges were prepared using simple casting/freeze-drying technique according to 32 factorial design where chitosan grade was set at three levels (low, medium, and high molecular weight), and concentration of chitosan solution at three levels (0.5, 1, and 2%). Mucoadhesion force, ex vivo mucoadhesion time, percent BH released after 8 h (Q8h), and time for release of 50% BH (T50%) were chosen as dependent variables. Additional BH cup and core buccal chitosan sponge were prepared to achieve uni-directional BH release toward the buccal mucosa. Sponges were evaluated in terms of drug content, surface pH, scanning electron microscopy, swelling index, mucoadhesion strength, ex vivo mucoadhesion time, and in vitro drug release. Cup and core sponge (HCH 0.5E) were able to adhere to the buccal mucosa for 8 h. It showed Q8h of 68.89% and exhibited a uni-directional drug release profile following Higuchi diffusion model.KEY WORDS: buspirone HCL, casting/freeze-drying technique, chitosan, cup and core sponge, mucoadhesive buccal sponges 相似文献
12.
This work combines several methods in an integrated strategy to develop a matrix for buccal administration. For this purpose,
tablets containing selected mucoadhesive polymers loaded with a model drug (omeprazole), free or in a complexed form with
cyclodextrins, and in the absence and presence of alkali agents were subjected to a battery of tests. Mucoadhesion studies,
including simple factorial analysis, in vitro release studies with both model-dependent and model-independent analysis, and permeation studies were performed. Mucoadhesive
profiles indicated that the presence of the drug decreases the mucoadhesion profile, probably due its hydrophobic character.
In tablets loaded with the drug complexed with β-cyclodextrin or methyl-β-cyclodextrin, better results were obtained with
the methylated derivative. This effect was attributed to the fact that in the case of β-cyclodextrin, more hydroxyl groups
are available to interact with the mucoadhesive polymers, thus decreasing the mucoadhesion performance. The same result was
observed in presence of the alkali agent (l-arginine), in this case due to the excessive hydrophilic character of l-arginine. Drug release from tablets was also evaluated, and results suggested that the dissolution profile with best characteristics
was observed in the matrix loaded with omeprazole complexed with methyl-β-cyclodextrin in the presence of l-arginine. Several mathematical models were applied to the dissolution curves, indicating that the release of the drug, in
free or in complexed state, from the mucoadhesive matrices followed a super case II transport, as established on the basis
of the Korsmeyer–Peppas function. The feasibility of drug buccal administration was assessed by permeation experiments on
porcine buccal mucosa. The amount of drug permeated from mucoadhesive tablets presented a maximum value for the system containing
drug complexed with the methylated cyclodextrin derivative in presence of l-arginine. According to these results, the system containing the selected polymer mixture and the drug complexed with methyl-β-cyclodextrin
in presence of l-arginine showed a great potential as a buccal drug delivery formulation, in which a good compromise among mucoadhesion, dissolution,
and permeation properties was achieved. 相似文献
13.
The purpose of this research was to study mucoadhesive bilayer buccal tablets of propranolol hydrochloride using the bioadhesive
polymers sodium alginate (Na-alginate) and Carbopol 934P (CP) along with ethyl cellulose as an impermeable backing layer.
The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, mucoadhesive strength, swelling
index, in vitro drug release, ex vivo drug permeation, ex vivo mucoadhesion, and in vivo pharmacodynamics in rabbits. Tablets
containing Na-alginate and CP in the ratio of 5∶1 (F2) had the maximum percentage of in vitro drug release without disinte-gration
in 12 hours. The swelling index was proportional to Na-alginate content and inversely proportional to CP content. The surface
pH of all tablets was found to be satis-factory (7.0±1.5), close to neutral pH; hence, buccal cavity irritation should not
occur with these tablets. The mechanism of drug release was found to be non-Fickian diffusion and followed zero-order kinetics.
The formulation F4 was optimized based on good biodhesive strength (28.9±0.99 g) and sustained in vitro drug permeation (68.65%±3.69%
for 12 hours). The behavior of formulation F4 was examined in human saliva, and both the drug and the buccal tablet were found
to be stable. The formulation F4 was applied to rabbit oral mucosa for in vivo studies. The formulation inhibited isoprenaline-induced
tachycardia. The studies conducted in rabbits confirmed the sustained release as compared with intravenous administration.
Published: September 21, 2007 相似文献
14.
Bilayer nicotine mucoadhesive patches were prepared and evaluated to determine the feasibility of the formulation as a nicotine
replacement product to aid in smoking cessation. Nicotine patches were prepared using xanthan gum or carbopol 934 as a mucoadhesive
polymers and ethyl cellulose as a backing layer. The patches were evaluated for their thickness, weight and content uniformity,
swelling behavior, drug–polymers interaction, adhesive properties, and drug release. The physicochemical interactions between
nicotine and the polymers were investigated by Fourier transform infrared (FTIR) spectroscopy. Mucoadhesion was assessed using
two-arm balance method, and the in vitro release was studied using the Franz cell. FTIR revealed that there was an acid base interaction between nicotine and carbopol
as well as nicotine and xanthan. Interestingly, the mucoadhesion and in vitro release studies indicated that this interaction was strong between the drug and carbopol whereas it was weak between the
drug and xanthan. Loading nicotine concentration to non-medicated patches showed a significant decrease in the mucoadhesion
strength of carbopol patches and no significant effect on the mucoadhesion strength of xanthan patches. In vitro release studies of the xanthan patches showed a reasonable fast initial release profile followed by controlled drug release
over a 10-h period. 相似文献
15.
The aim of this work was the design of sustained-release mucoadhesive bilayered tablets, using mixtures of mucoadhesive polymers
and an inorganic matrix (hydrotalcite), for the topical administration of flurbiprofen in the oral cavity. The first layer,
responsible for the tablet retention on the mucosa, was prepared by compression of a cellulose derivative and polyacrylic
derivative blend. The second layer, responsible for buccal drug delivery, was obtained by compression of a mixture of the
same (first layer) mucoadhesive polymers and hydrotalcite containing flurbiprofen. Nonmedicated tablets were evaluated in
terms of swelling, mucosal adhesion, and organoleptic characteristics; in vitro and in vivo release studies of flurbiprofen-loaded
tablets were performed as well.
The best results were obtained from the tablets containing 20 mg of flurbiprofen, which allowed a good anti-inflammatory sustained
release in the buccal cavity for 12 hours, ensuring efficacious salivary concentrations, and led to no irritation. This mucoadhesive
formulation offers many advantages over buccal lozenges because it allows for reduction in daily administrations and daily
drug dosage and is suitable for the treatment of irritation, pain, and discomfort associated with gingivitis, sore throats,
laryngopharyngitis, cold, and periodontal surgery. Moreover, it adheres well to the gum and is simple to apply, which means
that patient compliance is improved.
Published: July 13, 2007 相似文献
16.
The purpose of research was to develop a mucoadhesive multiparticulate sustained drug delivery system of pravastatin sodium,
a highly water-soluble and poorly bioavailable drug, unstable at gastric pH. Mucoadhesive microparticles were formulated using
eudragit S100 and ethyl cellulose as mucoadhesive polymers. End-step modification of w/o/o double emulsion solvent diffusion
method was attempted to improve the purity of the product, that can affect the dose calculations of sustained release formulations
and hence bioavailability. Microparticles formed were discrete, free flowing, and exhibited good mucoadhesive properties.
DSC and DRS showed stable character of drug in microparticles and absence of drug polymer interaction. The drug to polymer
ratio and surfactant concentration had significant effect on mean particle size, drug release, and entrapment efficiency.
Microparticles made with drug: eudragit S100 ratio of 1:3 (F6) exhibited maximum entrapment efficiency of 72.7% and ex vivo mucoadhesion time of 4.15 h. In vitro permeation studies on goat intestinal mucosa demonstrated a flux rate (1,243 μg/cm2/h) that was 169 times higher than the flux of pure drug. The gastric instability problem was overcome by formulating the
optimized microparticles as enteric-coated capsules that provided a sustained delivery of the highly water-soluble drug for
12 h beyond the gastric region. The release mechanism was identified as fickian diffusion (n = 0.4137) for the optimized formulation F6. Conclusively, a drug delivery system was successfully developed that showed delayed
and sustained release up to 12 h and could be potentially useful to overcome poor bioavailability problems associated with
pravastatin sodium. 相似文献
17.
The purpose of this research was to prepare and evaluate sustained release mucoadhesive tablets of Itraconazole. It is practically
insoluble in aqueous fluids hence its solid dispersion with Eudragit E100 was prepared by spray drying. This was formulated
in matrix of hydrophilic mucoadhesive polymers Carbopol 934P (CP) and Methocel K4M (HPMC). The formulation was optimized using
a 32 factorial design. Amounts of CP and HPMC were taken as formulation variables for optimizing response variables i.e. mucoadhesion
and dissolution parameters. The optimized mucoadhesive formulation was orally administered to albino rabbits, and blood samples
collected were used to determine pharmacokinetic parameters. The solid dispersion markedly enhanced the dissolution rate of
itraconazole. The bioadhesive strength of formulation was found to vary linearly with increasing amount of both polymers.
Formulations exhibited drug release fitting Peppas model with value of n ranging from 0.61 to 1.18. Optimum combination of polymers was arrived at which provided adequate bioadhesive strength and
fairly regulated release profile. The experimental and predicted results for optimum formulations were found to be in close
agreement. The formulation showed C
max 1898 ± 75.23 ng/ml, t
max of the formulation was 2 h and AUC was observed to be 28604.9 ng h/ml 相似文献
18.
Miguel Montenegro-Nicolini Patricio E. Reyes Miguel O. Jara Parameswara R. Vuddanda Andrónico Neira-Carrillo Nicole Butto Sitaram Velaga Javier O. Morales 《AAPS PharmSciTech》2018,19(8):3376-3387
The buccal mucosa appears as a promissory route for biologic drug administration, and pharmaceutical films are flexible dosage forms that can be used in the buccal mucosa as drug delivery systems for either a local or systemic effect. Recently, thin films have been used as printing substrates to manufacture these dosage forms by inkjet printing. As such, it is necessary to investigate the effects of printing biologics on films as substrates in terms of their physical and mucoadhesive properties. Here, we explored solvent casting as a conventional method with two biocompatible polymers, hydroxypropyl methylcellulose, and chitosan, and we used electrospinning process as an electrospun film fabrication of polycaprolactone fibers due to its potential to elicit mucoadhesion. Lysozyme was used as biologic drug model and was formulated as a solution for printing by thermal inkjet printing. Films were characterized before and after printing by mechanical and mucoadhesive properties, surface, and ultrastructure morphology through scanning electron microscopy and solid state properties by thermal analysis. Although minor differences were detected in micrographs and thermograms in all polymeric films tested, neither mechanical nor mucoadhesive properties were affected by these differences. Thus, biologic drug printing on films was successful without affecting their mechanical or mucoadhesive properties. These results open way to explore biologics loading on buccal films by inkjet printing, and future efforts will include further in vitro and in vivo evaluations. 相似文献
19.
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
20.
Supriya S. Shidhaye Pritesh V. Thakkar Neha M. Dand Vilasrao J. Kadam 《AAPS PharmSciTech》2010,11(1):416-424
The purpose of this study was to develop and optimize formulations of mucoadhesive bilayered buccal tablets of pravastatin sodium using carrageenan gum as the base matrix. The tablets were prepared by direct compression method. Polyvinyl pyrrolidone (PVP) K 30, Pluronic® F 127, and magnesium oxide were used to improve tablet properties. Magnesium stearate, talc, and lactose were used to aid the compression of tablets. The tablets were found to have good appearance, uniform thickness, diameter, weight, pH, and drug content. A 23 full factorial design was employed to study the effect of independent variables viz. levels of carrageenan gum, Pluronic F 127 and PVP K30, which significantly influenced characteristics like in vitro mucoadhesive strength, in vitro drug release, swelling index, and in vitro residence time. The tablet was coated with an impermeable backing layer of ethyl cellulose to ensure unidirectional drug release. Different penetration enhancers were tried to improve the permeation of pravastatin sodium through buccal mucosa. Formulation containing 1% sodium lauryl sulfate showed good permeation of pravastatin sodium through mucosa. Histopathological studies revealed no buccal mucosal damage. It can be concluded that buccal route can be one of the alternatives available for the administration of pravastatin sodium. 相似文献