共查询到20条相似文献,搜索用时 31 毫秒
1.
This study was designed for investigating the effect of Asparagus racemosus (AR) extract and chitosan (CTN) in facilitating the permeation of carvedilol (CDL) across rat epidermis. Transdermal flux
of carvedilol through heat-separated rat epidermis was investigated in vitro using vertical Keshary–Chien diffusion cells. Biophysical and microscopic manifestations of epidermis treated with AR extract,
CTN, and AR extract–CTN mixture were investigated by using differential scanning calorimetry, transepidermal water loss, scanning
electron microscopy (SEM), and transmission electron microscopy (TEM). Biochemical estimations of cholesterol, sphingosine,
and triglycerides were carried out for treated excised as well as viable rat epidermis. The antihypertensive activity of the
patches in comparison with that of oral carvedilol was studied in deoxycorticosterone acetate-induced hypertensive rats. The
permeation of carvedilol across excised rat epidermis was significantly higher (p < 0.05) when AR extract, CTN, or AR extract–CTN mixture was used as donor vehicle as compared to propylene glycol/ethanol
(7:3) mixture. Epidermis obtained after 12 h treatment of viable rat skin with AR extract–CTN mixture showed significantly
higher (p < 0.05) permeability to CDL as compared to that after treatment with AR extract or CTN alone. Further, the application of
patches containing AR extract–CTN mixture resulted in sustained release of CDL which was able to control the hypertension
in deoxycorticosterone acetate-induced hypertensive rats through 36 h. Estimation of micro constituents in rat epidermis revealed
maximum extraction of cholesterol, sphingosine, and triglycerides after treatment with AR extract–CTN mixture. This was manifested
in altered lipid and protein-specific thermotropic transitions. Further, increase in intercellular space, disordered lipid
structure, and corneocyte detachment as observed in SEM and TEM suggested great potential of AR extract for use as percutaneous
permeation enhancer. The developed transdermal patches of CDL containing AR extract–CTN mixture exhibited better performance
as compared to oral administration in controlling hypertension in rats. 相似文献
2.
Long Mo Guijing Lu Xiping Ou Dongsheng Ouyang 《Saudi Journal of Biological Sciences》2022,29(1):266-272
The main aim of this study is to optimize and evaluate transdermal patch of Carvedilol by the use of different polymer and different permeation enhancers which help to release drug in controlled action and thereby increase the bioavailability of the drug. Main objective was to avoid first pass metabolism of Carvedilol. Transdermal patches were developed by solvent evaporation method. The combination of Eudragit RS-100 as rate controlling polymer and Span 80 as a permeation enhancer was found to be ideal formulation (Formulation F7) with maximum drug release i.e. 100.29 ± 0.44 % within 12 h. Formulation F7 showed maximum bioavailability and showed maximum drop of BP at 6 h. From this study the conclusion was, transdermal patch of Carvedilol which contains Eudragit RS-100 polymer and Span 80 as penetration enhancer produced sustained and continued drug release. 相似文献
3.
The aim of the present investigation was to prepare glipizide matrix transdermal systems using the combinations of ethyl cellulose/polyvinylpyrrolidone and Eudragit RL-100/Eudragit RS-100. The systems were evaluated for various in vitro (drug content, drug permeation, scanning electron microscopy and drug-polymer interactions) and in vivo (acute and long-term hypoglycemic activity, biochemical and histopathological studies, skin irritation and pharmacokinetic studies in mice) parameters. Drug content of the patches was found to be more than 98%. Variations in drug permeation profiles were observed among various formulations. The scanning electron microscopy of the patches showed the formation of pores on the surface after in vitro permeation studies. The drug-polymer interaction results suggested no interaction between drug and polymers. The in vivo results revealed that the patches successfully prevented the severe hypoglycemia in the initial hours and they were also effective on chronic application. The transdermal route exhibited negligible skin irritation and produced better improvement with all the tested in vivo parameters compared to oral administration. 相似文献
4.
The objective of the present study was to develop membrane-moderated transdermal systems of ampicillin sodium and to evaluate
them with respect to various in vitro and in vivo parameters. The membrane-type transdermal systems were prepared using a
drug with various antinucleant polymers— hydroxypropyl methylcellulose (HPMC), methylcellulose (MC), cellulose acetate phthalate,
chitosan, sodium alginate (SA), and sodium carboxymethylcellulose—in an ethanol: pH 4.7 buffer volatile system by the solvent
evaporation technique with HPMC as the rate-controlling membrane for all the systems. The swelling properties of the polymers
were studied, and drug-polymer interaction studies were performed. The patches were subjected to various physicochemical studies,
in vitro release studies, permeation studies, and skin irritation studies. The best patch among the formulations was selected
for further in vivo studies. Compared to the other patches, SA exhibited the highest moisture content at 16%; a 21% moisture
uptake was found with MC. The release and permeation of the drug from the SA patch was found to be the maximum. The in vivo
study of the SA patch exhibited a peak plasma concentration Cmax of 126 μg/mL at Tmax 4 hours. Hence, it can be concluded that hydrophilic ampicillin sodium can be developed as a transdermal delivery system
with SA that is an alternative to intravenous administration and has minimal adverse effects.
Published: January 26, 2007 相似文献
5.
Dhaval P. Patel Chitral Mallikarjuna Setty Gaurav N. Mistry Santnu L. Patel Tarun J. Patel Pritesh C. Mistry Amar K. Rana Pritesh K. Patel Rishabh S. Mishra 《AAPS PharmSciTech》2009,10(2):437-442
Transdermal films of the furosemide were developed employing ethyl cellulose and hydroxypropyl methylcellulose as film formers.
The effect of binary mixture of polymers and penetration enhancers on physicochemical parameters including thickness, moisture
content, moisture uptake, drug content, drug–polymer interaction, and in vitro permeation was evaluated. In vitro permeation study was conducted using human cadaver skin as penetration barrier in modified Keshary–Chein diffusion cell.
In vitro skin permeation study showed that binary mixture, ethyl cellulose (EC)/hydroxypropyl methylcellulose (HPMC), at 8.5:1.5 ratio
provided highest flux and also penetration enhancers further enhanced the permeation of drug, while propylene glycol showing
higher enhancing effect compared to dimethyl sulfoxide and isopropyl myristate. Different kinetic models, used to interpret
the release kinetics and mechanism, indicated that release from all formulations followed apparent zero-order kinetics and
non-Fickian diffusion transport except formulation without HPMC which followed Fickian diffusion transport. Stability studies
conducted as per International Conference on Harmonization guidelines did not show any degradation of drug. Based on the above
observations, it can be reasonably concluded that blend of EC–HPMC polymers and propylene glycol are better suited for the
development of transdermal delivery system of furosemide. 相似文献
6.
Glibenclamide (GL)-loaded microcapsules (MC) and transdermal patches (TDP) were formulated and in vitro and in vivo parameters compared to find out the best route of drug administration. The formulation TDP1 having a drug–polymer ratio 1:1
showed comparatively higher GL release and better permeation across mice skin (p < 0.05). From the comparative study, it was concluded that the transdermal system of GL produced better improvement compared
to oral microcapsule administration (p < 0.05). The transdermal system exhibited comparatively slow and continuous supply of GL at a desired rate to systemic circulation
avoiding metabolism, which improved day-to-day glycemic control in diabetic subjects. Transdermal system of GL exhibited better
control of hyperglycemia and prolonged plasma half-life by transdermal systems (9.6 ± 1.2 h) in comparison with oral microcapsule
(5.84 ± 2.1 h), indicating that the drug, when administered by transdermal systems, will remain in the body for a longer period.
From the glucose tolerance test, transdermal route effectively maintained the normoglycemic levels in contrast to the oral
group (MC1), which produced remarkable hypoglycemia ranging from −12.6 ± 2.1% to −18 ± 2.3%. The significantly high (p < 0.05) area under the curve values observed with transdermal system (1,346.2 ± 92.3 ng ml−1 h−1) also indicate increased bioavailability of the drug from these systems compared to the oral route (829.8 ± 76.4 ng ml−1 h−1). 相似文献
7.
A. B. Shreya Renuka S. Managuli Jyothsna Menon Lavanya Kondapalli Aswathi R. Hegde Kiran Avadhani 《Journal of liposome research》2016,26(3):221-232
Context: Asenapine maleate (ASPM) is an antipsychotic drug for the treatment of schizophrenia and bipolar disorder. Extensive metabolism makes the oral route inconvenient for ASPM.Objective: The objective of this study is to increase ASPM bioavailability via transdermal route by improving the skin permeation using combined strategy of chemical and nano-carrier (transfersomal) based approaches.Materials and methods: Transfersomes were prepared by the thin film hydration method using soy-phosphatidylcholine (SPC) and sodium deoxycholate (SDC). Transfersomes were characterized for particle size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency, surface morphology, and in vitro skin permeation studies. Various chemical enhancers were screened for skin permeation enhancement of ASPM. Optimized transfersomes were incorporated into a gel base containing suitable chemical enhancer for efficient transdermal delivery. In vivo pharmacokinetic study was performed in rats to assess bioavailability by transdermal route against oral administration.Results and discussion: Optimized transfersomes with drug:SPC:SDC weight ratio of 5:75:10 were spherical with an average size of 126.0?nm, PDI of 0.232, ZP of??43.7?mV, and entrapment efficiency of 54.96%. Ethanol (20% v/v) showed greater skin permeation enhancement. The cumulative amount of ASPM permeated after 24?h (Q24) by individual effect of ethanol and transfersome, and in combination was found to be 160.0, 132.9, and 309.3?μg, respectively, indicating beneficial synergistic effect of combined approach. In vivo pharmacokinetic study revealed significant (p?0.05) increase in bioavailability upon transdermal application compared with oral route.Conclusion: Dual strategy of permeation enhancement was successful in increasing the transdermal permeation and bioavailability of ASPM. 相似文献
8.
《Journal of liposome research》2013,23(2):119-125
AbstractValsartan (VLT) is a highly selective and orally active antihypertensive drug. However, its oral administration is associated with drawbacks like low bioavailability. The objective of this study was to design and develop a transdermal delivery system for VLT using ethosomal carriers to investigate their enhanced transdermal delivery potential. VLT ethosomes were prepared by cold method. VLT ethosomes were characterized by scanning electron microscopy. The prepared ethanolic liposomes were characterized to be spherical having low polydispersity of nano-size range with good entrapment efficiency. ETC5 ethosomal suspension with 4% of phospholipon 90H and 40% of ethanol was found to have highest entrapment efficiency, i.e. 80.230?±?0.8748%. The permeation study of ethosomes was evaluated by ex vivo diffusion study through rat abdominal skin using Franz’s diffusion cells and ETC5 ethosomal suspension was found to have highest permeation with flux of 92.819?±?1.539?µg/cm2/h, when compared to the permeation profiles of drug solutions either in water or in a water–ethanol mixture. Transdermal application of ethosomal VLT on Wistar rats showed better and prolonged antihypertensive activity in comparison to orally administered VLT suspension by virtue of transdermal permeation through Wistar rat skin. Histopathological study of skin applied with ETC5 showed intercellular permeation across skin by dissolving intercellular lipids in epidermis without causing any rigorous changes in the skin cellular structure. In conclusion, ethosomes enabled the transdermal permeation of VLT, which amply proves its superiority over oral administration for antihypertensive treatment. 相似文献
9.
The purpose of this study was to investigate physicochemical characteristics and in vitro release of zidovudine from monolithic film of Eudragit RL 100 and ethyl cellulose. Films included 2.5% or 5% (w/w) zidovudine of the dry polymer weight were prepared in various ratios of polymers by solvent evaporation method from methanol/acetone
solvent mixture. The release studies were carried out by vertical Franz cells (2.2 cm2 area, 20 ml receptor fluid). Ex vivo studies were done on Wistar rat skin within the films F6 (Eudragit RL100) and F7 (Eudragit RL100/Ethylcellulose, 1:1) consisting
5% (w/w) zidovudine in comparison with the same amount of free drug. Either iontophoresis (0.1 and 0.5 mA/cm2 direct currents, Ag/AgCl electrodes) or dimethyl sulfoxide (pretreatment of 1% and 5%, w/w, solutions) were used as enhancers. Films consisting of ethyl cellulose under the ratio of 50% (w/w) gave similar release profiles, and the highest in vitro cumulative released amount was achieved with F6 film which gave the closest results with the free drug. This result could
be due to the high swelling capacity and re-crystallization inhibition effect of RL 100 polymer which also influenced the
film homogenization. All the films were fitted to Higuchi release kinetics. It was also observed that both 0.5-mA/cm2 current and 5% (w/w) dimethyl sulfoxide applications significantly increased the cumulative permeated amount of zidovudine after 8 h; however,
the flux enhancement ratio was higher for 0.5-mA/cm2 current application, especially within F6 film. Thus, it was concluded that Eudragit RL100 film (F6) could be further evaluated
for the transdermal application of zidovudine. 相似文献
10.
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
11.
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
12.
The Role of the Conformational Profile of Polysaccharides on Skin Penetration: The Case of Hyaluronan and Its Sulfates
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Francesco Cilurzo Giulio Vistoli Chiara G. M. Gennari Francesca Selmin Fabrizio Gardoni Silvia Franzè Monica Campisi Paola Minghetti 《化学与生物多样性》2014,11(4):551-561
The literature data suggest the capacity of biomacromolecules to permeate the human skin, even though such a transdermal permeation appears to be governed by physicochemical parameters which are significantly different compared to those ruling the skin permeation of small molecules. On these grounds, the present study was undertaken to investigate the in vitro diffusion properties through the human epidermis of hyaluronic acid and their sulfates. Low‐ and medium‐molecular‐weight hyaluronic acids and the corresponding derivatives at two degrees of sulfation were then tested. In vitro studies evidenced that the sulfated polymers permeate better than the corresponding hyaluronic acid, despite their vastly greater polarity, while the observed permeation markedly decreases when increasing the polymer's molecular weight regardless of the sulfation degree. Using a fluorescent‐labeled polysaccharide, it was also evidenced that hyaluronans have a great affinity for corneocytes and likely cross the stratum corneum mainly through a transcellular route. The molecular‐dynamics study revealed how the observed permeations for the investigated polysaccharides can be rationalized by monitoring their conformational profiles, since the permeation was found to be directly related to their capacity to assume extended and flexible conformations. 相似文献
13.
Timolol Maleate (TiM), a nonselective β-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from poor oral bioavailability (50%) due to its first pass effect and a short elimination half-life of 4?h; resulting in its frequent administration. Transdermal formulation may circumvent these problems in the form of protransfersomes. The aim of this study is to develop and optimize transdermal protransfersomal system of Timolol Maleate by film deposition on carrier method where protransfersomes were converted to transfersomes upon skin hydration following transdermal application under occlusive conditions. Two 23 full factorial designs were employed to investigate the influence of three formulation variables which were; phosphatidyl choline: surfactant molar ratio, carrier: mixture and the type of SAA each on particle size, drug entrapment efficiency and release rate. The optimized formulation was evaluated regarding permeation through hairless rat skin and compared with oral administration of aqueous solution on male Wistar rats. Optimized protransfersomal system had excellent permeation rate through shaved rat skin (780.69?μg/cm2/h) and showed six times increase in relative bioavailability with prolonged plasma profile up to 72?h. A potential protransfresomal transdermal system was successfully developed and factorial design was found to be a smart tool in its optimization. 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 purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive patches
of propranolol hydrochloride using the hydrophobic polymer Eudragit L-100 as the base matrix. The hydrophilic polymers Carbopol
934 and polyvinyl pyrrolidone (PVP) K30 were incorporated into the Eudragit patches, to provide the patches with bioadhesive
properties and to modify the rate of drug release. The patches, which were prepared by the solvent casting method, were smooth
and elegant in appearance; were uniform in thickness, weight, and drug content; showed no visible cracks; and showed good
folding endurance. A 32 full factorial design was employed to study the effect of independent variables like hydrophilic polymers Carbopol 934 and
PVP K30, which significantly influenced characteristics like swelling index, ex vivo mucoadhesive strength, in vitro drug
release, and ex vivo residence time. A stability study of optimized Eudragit patches was done in natural human saliva; it
was found that both drug and buccal patches were stable in human saliva. It can be concluded that the present buccal formulation
can be an ideal system to improve the bioavailability of the drug by avoiding hepatic first-pass metabolism.
Published: June 22, 2007 相似文献
16.
A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance diffusion rate and oral bioavailability
of valsartan. The solubility of valsartan was checked in different oils, surfactants, and cosurfactants and ternary phase
diagrams were constructed to evaluate the microemulsion domain. The valsartan SMEDDS was prepared using Capmul MCM (oil),
Tween 80 (surfactant), and polyethylene glycol 400 (cosurfactant). The particle size distribution, zeta potential, and polydispersity
index were determined and were found to be 12.3 nm, −0.746, and 0.138, respectively. Diffusion rate of valsartan was measured
by in vitro dialysis bag method using phosphate buffer pH 6.8 as diffusion media. Developed high-performance liquid chromatography method
was used to determine drug content in diffusion media. Oral bioavailability of valsartan SMEDDS was checked by using rabbit
model. Results of diffusion rate and oral bioavailability of valsartan SMEDDS were compared with those of pure drug solution
and of marketed formulation. Diffusion of valsartan SMEDDS showed maximum drug release when compared to pure drug solution
and marketed formulation. The area under curve and time showed significant improvement as the values obtained were 607 ng h/mL
and 1 h for SMEDDS in comparison to 445.36 and 1.36 h for market formulation suggesting significant increase (p < 0.01) in oral bioavailability of valsartan SMEDDS. 相似文献
17.
Ramesh Gannu Chinna Reddy Palem Shravan Kumar Yamsani Vamshi Vishnu Yamsani Madhusudan Rao Yamsani 《AAPS PharmSciTech》2010,11(2):976-985
The purpose of the present study was to develop and optimize reservoir-based transdermal therapeutic system (TTS) for buspirone
(BUSP), a low bioavailable drug. A three-factor, three-level Box–Behnken design was employed to optimize the TTS. Hydroxypropyl
methylcellulose, d-limonene and propylene glycol were varied as independent variables; cumulative amount permeated across rat abdominal skin
in 24 h, flux and lag time were selected as dependent variables. Mathematical equations and response surface plots were used
to relate the dependent and independent variables. The statistical validity of polynomials was established, and optimized
formulation factors were selected by feasibility and grid search. Validation of the optimization study with seven confirmatory
runs indicated high degree of prognostic ability of response surface methodology. BUSP-OPT (optimized formulation) showed
a flux 104.6 μg cm−2 h−1, which could meet target flux. The bioavailability studies in rabbits showed that about 2.65 times improvement (p < 0.05) in bioavailability, after transdermal administration of BUSP-OPT compared to oral solution. The ex vivo–in vivo correlation was found to have biphasic pattern and followed type A correlation. Reservoir-based TTS for BUSP was developed
and optimized using Box–Behnken statistical design and could provide an effective treatment in the management of anxiety. 相似文献
18.
Context: Avanafil (AVA) is used in the treatment of erectile dysfunction, but is reported for its poor aqueous solubility. Solid lipid nanoparticles (SLNs) are lipid carriers that can greatly enhance drug solubility and bioavailability.Objective: This work was aimed to formulate and optimize AVA SLNs with subsequent loading into hydrogel films for AVA transdermal delivery.Materials and methods: AVA SLNs were prepared utilizing homogenization followed by ultra-sonication technique. The prepared SLNs were characterized for particle size, charge, surface morphology and drug content. The optimized SLNs formulation was incorporated into transdermal films prepared using HPMC and chitosan. Hydrogel films were evaluated for ex-vivo rat skin permeation using automated Franz diffusion cells. The permeation parameters and the release mechanism were evaluated. The transdermal permeation of the prepared AVA SLNs through the skin layers was studied using confocal laser scanning microscope.Results: Lipid concentration and % of oil in lipid had a pronounced effect on particle size while, entrapment efficiency was significantly affected by lipid concentration and % of cholesterol. The optimized AVA SLNs showed particle size and entrapment efficiency of 86?nm and 85.01%, respectively. TEM images revealed spherecity of the particles. High permeation parameters were observed from HPMC films loaded with AVA SLNs. The release data were in favor of Higuchi diffusion model. The prepared AVA SLNs were able to penetrate deeper in skin layers.Conclusion: HPMC transdermal film-loaded AVA SLNs is an effective and alternative to per-oral drug administration. 相似文献
19.
The purpose of this research was to mask the intensely bitter taste of ondansetron HCl and to formulate a rapiddisintegrating
tablet (RDT) of the taste-maske drug. Taste masking was done by complexing ondansetron HCl with aminoalkyl methacrylate copolymer
(Eudragit EPO) in different ratios by the precipitation method. Drug-polymer complexes (DPCs) were tested for drug content,
in vitro taste in simulated salivary fluid (SSF) of pH 6.2, and molecular property. Complex that did not release drug in SSF
was considered taste-masked and selected for formulation RDTs. The complex with drug-polymer ratio of 8∶2 did not show drug
release in SSF; therefore, it was selected. The properties of tablets such as tensile strength, wetting time, water absorption
ratio, in vitro disintegration time, and disintegration in the oral cavity were investigated to elucidate the wetting and
disintegration characteristics of tablets. Polyplasdone XL-10 7% wt/wt gave the minimum disintegration time. Tablets of batch
F4 containing spray-dried mannitol and microcrystalline cellulose in the ratio 1∶1 and 7% wt/wt Polyplasdone XL-10 showed
faster disintegration, within 12.5 seconds, than the marketed tablet (112 seconds). Good correlation between in vitro disintegration
behavior and in the oral cavity was recognized. Taste evaluation of RDT in human volunteers revealed considerable taste masking
with the degree of bitterness below threshold value (0.5) ultimately reaching to 0 within 15 minutes, whereas ondansetron
HCl was rated intensely bitter with a score of 3 for 10 minutes. Tablets of batch F4 also revealed rapid drug release (t90, 60 seconds) in SGF compared with marketed formulation (t90, 240 seconds;P<.01). Thus, results conclusively demonstrated successful masking of taste and rapid disintegration of the formulated tablets
in the oral cavity.
Published: June 22, 2007 相似文献
20.
Screening of Venlafaxine Hydrochloride for Transdermal Delivery: Passive Diffusion and Iontophoresis
The objective of the study was to investigate in vitro transdermal delivery of venlafaxine hydrochloride across the pigskin by passive diffusion and iontophoresis. For passive
diffusion, experiments were carried out in Franz diffusion cell whereas for iontophoretic permeation, the diffusion cell was
modified to contain both the donor and return electrode on the same side of skin. Anodal iontophoresis was carried out using
a current density of 0.5 mA/cm2. Donor concentrations used were 585.5 mg/ml (saturated solution) and 100 mg/ml. Experiments initially performed to determine
the transport efficiency of venlafaxine ions showed promising results. Iontophoresis increased the permeation rate at both
concentration levels over their passive counterparts (P < 0.01), but surprisingly higher steady-state flux was obtained from lower donor drug load (P < 0.01). The favorable pH of the unsaturated solutions is suggested to be the cause for this effect. Mild synergistic effect
was observed when iontophoresis was carried out incorporating peppermint oil in the donor but the same was not found in passive
diffusion. Highest steady-state flux obtained in the experiment was 3.279 μmol/cm2/h when peppermint oil (0.1%) was included in the donor. As the maintenance requirement of venlafaxine hydrochloride is approximately
9.956 μmol/h, the results suggested that the drug is a promising candidate for iontophoretic delivery. 相似文献