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1.
The aim of this study was to microencapsulate caffeine by the emulsion technique, trying to control its release from a medicated chewing gum. Three formulations were prepared using alginate, alginate-starch, and alginate-starch with chitosan coating as the wall materials. These microcapsules were characterized with regard to the morphology studied by using an optical microscope and scanning electron microscopy (SEM), particle size, and encapsulation efficiency. The microcapsules were then incorporated into the chewing gums. The chewing gums were characterized by thermal behavior (by differential scanning calorimetry [DSC]), texture profile analysis [TPA], and sensory evaluation. Furthermore, the release of caffeine from the chewing gum was studied in vitro using the masticatory simulator and in vivo by a chew-out study. The microcapsules revealed a spherical form and high encapsulation efficiency, representing the success of the technique. The outcomes indicated that it is possible to encapsulate caffeine with the techniques employed and the microcapsules prolonged the release of caffeine throughout mastication. The chewing gum containing alginate-starch with chitosan-coated microcapsules showed the great potential of the microcapsule in controlling the release of the caffeine from the chewing gum, thereby delaying its bitterness.  相似文献   

2.
Chewing of gum contributes to the maintenance of oral health. Many oral diseases, including caries and periodontal disease, are caused by bacteria. However, it is unknown whether chewing of gum can remove bacteria from the oral cavity. Here, we hypothesize that chewing of gum can trap bacteria and remove them from the oral cavity. To test this hypothesis, we developed two methods to quantify numbers of bacteria trapped in chewed gum. In the first method, known numbers of bacteria were finger-chewed into gum and chewed gums were molded to standard dimensions, sonicated and plated to determine numbers of colony-forming-units incorporated, yielding calibration curves of colony-forming-units retrieved versus finger-chewed in. In a second method, calibration curves were created by finger-chewing known numbers of bacteria into gum and subsequently dissolving the gum in a mixture of chloroform and tris-ethylenediaminetetraacetic-acid (TE)-buffer. The TE-buffer was analyzed using quantitative Polymerase-Chain-Reaction (qPCR), yielding calibration curves of total numbers of bacteria versus finger-chewed in. Next, five volunteers were requested to chew gum up to 10 min after which numbers of colony-forming-units and total numbers of bacteria trapped in chewed gum were determined using the above methods. The qPCR method, involving both dead and live bacteria yielded higher numbers of retrieved bacteria than plating, involving only viable bacteria. Numbers of trapped bacteria were maximal during initial chewing after which a slow decrease over time up to 10 min was observed. Around 108 bacteria were detected per gum piece depending on the method and gum considered. The number of species trapped in chewed gum increased with chewing time. Trapped bacteria were clearly visualized in chewed gum using scanning-electron-microscopy. Summarizing, using novel methods to quantify and qualify oral bacteria trapped in chewed gum, the hypothesis is confirmed that chewing of gum can trap and remove bacteria from the oral cavity.  相似文献   

3.
Aims: To develop and assess a simple test for evaluating the mastication of visco‐elastic foods and prosthodontic success subsequent to treatment of older people. Method: The weight lost from chewing gum during mastication tests and the saliva secreted is weighed. The percentage of the original gum weight that is chewed out in a defined number of strokes is termed the Masticatory Effectiveness (ME) Material: Five edentate and three dentate volunteers were selected to provide a range of dental states and age. Four commercially available chewing gums of different origins and perceived hardness were tested, one without sweetener acted as a control for salivary stimulation. Intervention: Pre‐weighed samples of each gum were chewed, each for defined numbers of strokes. The saliva secreted was collected and weighed. The chewed gum was desiccated and the total weight loss of sweeteners chewed out provided an objective measure of chewing performance. Results: Weight loss showed large differences between gums, between subjects and the number of strokes. ME was significantly correlated with salivary secretion rates for two subjects. The interaction between subject and gum was statistically significant, established by an ANOVA model, the value of which is shown for multivariate studies. Differential success between gums of different thickness may provide evaluation of denture stability. Conclusions: Measuring the weight lost from gums during chewing provides a simple test of masticatory effectiveness of visco‐elastic foods. This has particular value both in functional assessment of older people and in physiological research.  相似文献   

4.
Adequate salivary flow is important for patient comfort and maintenance of oral health. Xerostomia, or dry mouth, is a common clinical complaint. Masticatory and gustatory activity can stimulate salivary flow from functional salivary tissue and the use of sugarless mints and gums have been recommended to individuals who complain of xerostomia, but there are minimum clinical data. A clinical study assessing the effect on salivary flow rates and dental plaque pH of a sorbitol-sweetened chewing gum in subjects with the complaint of xerostomia was conducted. The chewing of the gum in this present study stimulated salivary flow in the subjects with xerostomia. Statistically significant stimulated whole mouth and parotid salivary flow rate increases were found when compared to unstimulated whole mouth and parotid salivary flow rates. Chewing of the sorbitol-sweetened gum also effectively reduced the drop in pH seen following the exposure to a fermentable carbohydrate. The findings of this present study indicate that chewing of a sorbitol-sweetened gum may be of benefit to patients with the complaint of xerostomia.  相似文献   

5.
The objective of this work was to develop matrix sustained-release tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as cost-effective, nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]/carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios, of 100∶0, 80∶20, 60∶40, 20∶80, 0∶100 of G gum (or X):HPMC, X gum:G gum, and triple mixture of these polymers (G gum, X gum, HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was, performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE8%), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor (f 2), pure HPMC and H8G2 were the most similar formulations to Topalgic-LP as the reference standard. Published: March 17, 2006  相似文献   

6.
The purpose of this work was to evaluate the potential of grewia gum (GG) as a suspending agent in pharmaceutical oral formulation using ibuprofen as model drug. Ibuprofen pediatric suspension (25 mg/5 mL) was formulated with grewia gum (0.5% w/v) as the suspending agent. Similar suspensions of Ibuprofen containing either sodium carboxymethylcellulose (Na-CMC) or hydroxymethylpropylcellulose (HPMC) were also produced. The suspensions were evaluated for ease of redispersion, sedimentation, rheological properties, and the effect of aging on the rheological properties at 25°C. The particle size and particle size distributions of the dispersed solute were determined. The redispersion time was 19, 11, and 0.5 min, respectively, for formulation containing Na-CMC, HPMC, and GG .The sedimentation volumes were 0.05, 0.05, and 0.125 mL, respectively, for Na-CMC, HPMC, and GG . Viscosities of suspensions at spindle speed of 25 rpm were of the order: GG > HPMC > Na-CMC when freshly prepared and of the order: HPMC > GG > Na-CMC within 6 months of storage. The particles size was 72.72, 73.82, 81.93, and 83.41 μm, respectively, for suspensions containing Na-CMC, ibuprofen alone, HPMC, and GG. Greatest hysteresis was observed in formulation containing HPMC. All the formulations were stable. It was our conclusion that the difference in the physicochemical properties of ibuprofen pediatric formulations was influenced more by the suspending agent used in the formulations than the drug. GG combined better redispersion with minimal changes in viscosity on storage compared to Na-CMC and HPMC as suspending agent. Thus GG may serve as a good suspending agent requiring no further aid in suspension redispersibility.KEY WORDS: grewia gum, oral pharmaceutical formulations, physicochemical properties, potential suspending agent  相似文献   

7.
Medicated chewing gums (MCGs) represent a unique platform for drug delivery. They have been defined as solid single-dose preparations, which may contain more than one active pharmaceutical ingredient (API) with base consisting primarily of gum that has to be chewed for a certain period of time. They mainly contain a tasteless masticatory gum base as the core with other minor nonmasticatory ingredients, such as flavors and sweeteners. Despite their advantages in drug delivery, MCGs remain a niche product due to the complexity of their formulation, lack of acceptable testing methods, and intricacy of their manufacturing. Few studies have been reported on their use, and most of the information on their composition and production could be found in patent search. The aim of this review is to provide an overview of gum composition, manufacturing process, and characterization. Due to the scarcity of studies concerning the evaluation of the mechanical properties of MCGs, greater emphasis was placed on the available performance tests and procedures for the estimation of their mechanical and textural properties. While very few tests have been recommended by the official pharmacopeias, several tests have been suggested for assessing the mechanical properties of MCGs in vitro. Properties, such as chewiness, elasticity, and firmness, of chewing gums during mastication are imperative quality attributes that have been found to strongly correlate with gum composition and mouth feel.  相似文献   

8.
PYCNOGENOL is an antioxidant phytochemical shown to have antiinflammatory activity in both the in vitro and in vivo models. This study compared the effects of chewing gums with and without PYCNOGENOL on gingival bleeding and plaque formation in 40 human subjects. In this double-blind study, subjects were assigned randomly to receive either control gums without PYCNOGENOL or experimental gums containng 5 mg PYCNOGENOL. Subjects used chewing gums for 14 days. Gingival bleeding and plaque scores were taken before and after the experiment. PYCNOGENOL chewing gums significantly reduced gingival bleeding, while no changes were noted in bleeding indexes in control subjects who used regular chewing gums. Subjects using regular control gums had significant increases of dental plaque accumulation during the two-week period. No increases in plaque accumulation were noted in subjects using PYCNOGENOL chewing gums. The data of this study suggest that the use of Pycnogenol chewing gums can minimize gingival bleeding and plaque accumulation.  相似文献   

9.
Abstract

Niosomes as drug delivery systems have the ability to decrease drugs' side effects and increase their therapeutic effectiveness. Metformin HCl is an oral antihyperglycemic agent belonging to biguanides. It is the most commonly chosen drug as a startup therapy for patients newly diagnosed with type 2 diabetes. This study aims to encapsulate metformin HCl inside niosomes to be used as a transdermal formulation helping to prolong its antidiabetic effect and investigate its ability to enhance wound healing in diabetic patients. Thin film hydration method was used to prepare metformin HCl niosomes using different proportions of Span 60, Span 40, Tween 80, and cholesterol. All formulations were characterized using transmission electron microscope, zeta potential, and vesicle size. In vitro release studies, stability studies and in vivo evaluation were conducted on selected niosomal formulations. The results of entrapment efficiency ranged from 13% to 32%. Vesicle sizes were determined in nano-range. The in vitro release profile of metformin HCl from niosomes occurred in two consecutive phases. Biological evaluation on diabetic rats revealed that metformin HCl niosomal gel given every 2 days showed a better sustained antidiabetic effect than oral doses given daily. It also showed an improvement in wound healing for diabetic rats given metformin formulations compared to nontreated ones.  相似文献   

10.
In a double-blind, placebo-controlled, crossover trial the effect of 2-mg nicotine chewing gum was studied in 43 smokers when they were smoking as inclined and when they were trying to stop smoking. Although 70% of the smokers stopped smoking during treatment, only 23% were still abstinent after one year. The effect of the nicotine, though significant, was small compared with the overall reduction in smoking. When the subjects were smoking as inclined cigarette consumption was reduced by an average of 37% on the nicotine gum compared with 31% on placebo gum, while avergage carboxyhaemoglobin (COHb) levels were reduced by 26% and 15% on the active and placebo gums respectively. When subjects tried to stop smoking there was a further considerable reduction in cigarette consumption, but no longer any difference between the two gums. Nevertheless, average COHb was still lower on the active gum. Plasma nicotine levels on the nicotine gum averaged only 10-7 ng/ml compared with 27-4 ng/ml after smoking. Better results could be expected with 4-mg nicotine gums.  相似文献   

11.
Development of palatable formulations for pediatric and geriatric patients involves various challenges. However, an innovative development with beneficial characteristics of marketed formulations in a single formulation platform was attempted. The goal of this research was to develop solid oral flexible tablets (OFTs) as a platform for pediatrics and geriatrics as oral delivery is the most convenient and widely used mode of drug administration. For this purpose, a flexible tablet formulation using cetirizine hydrochloride as model stability labile class 1 and 3 drug as per the Biopharmaceutical Classification System was developed. Betadex, Eudragit E100, and polacrilex resin were evaluated as taste masking agents. Development work focused on excipient selection, formulation processing, characterization methods, stability, and palatability testing. Formulation with a cetirizine-to-polacrilex ratio of 1:2 to 1:3 showed robust physical strength with friability of 0.1% (w/w), rapid in vitro dispersion within 30 s in 2–6 ml of water, and 0.2% of total organic and elemental impurities. Polacrilex resin formulation shows immediate drug release within 30 min in gastric media, better taste masking, and acceptable stability. Hence, it is concluded that ion exchange resins can be appropriately used to develop taste-masked, rapidly dispersible, and stable tablet formulations with tailored drug release suitable for pediatrics and geriatrics. Flexible formulations can be consumed as swallowable, orally disintegrating, chewable, and as dispersible tablets. Flexibility in dose administration would improve compliance in pediatrics and geriatrics. This drug development approach using ion exchange resins can be a platform for formulating solid oral flexible drug products with low to medium doses.  相似文献   

12.
The aim of this paper was to evaluate the performance of different swellable polymers in the form of layered matrix tablets to provide controlled therapeutic effect of metoprolol tartrate for twice daily administration. Seven different swellable polymers (carrageenan, hydroxypropylmethyl cellulose, pectin, guar gum, xanthan gum, chitosan, and ethyl cellulose) were evaluated alone or in combination as release-retardant layer. Tablets were tested for weight variation, hardness, diameter/thickness ratio, friability, and drug content uniformity and subjected to in vitro drug-release studies. In addition, the target-release profile of metoprolol tartrate was plotted using its clinical pharmacokinetic data, and the release profiles of the tablets were evaluated in relation to the plotted target release profile. Carrageenan was determined as the best polymer in two-layered matrix tablet formulations due to its better accordance to the target release profile and was selected for preparing three-layered matrix tablets. Carrageenan formulations exhibited super case II release mechanism. Accelerated stability testing was performed on two- and three-layered matrix tablet formulations of carrageenan. The tablets were stored at 25°C/60% relative humidity and 40°C/75% relative humidity for 6 months and examined for physical appearance, drug content, and release characteristics. At the end of the storage time, formulations showed no change either in physical appearance, drug content, or drug-release profile. These results demonstrated the suitability of three-layered tablet formulation of carrageenan to provide controlled release and improved linearity for metoprolol tartrate in comparison to two-layered tablet formulation.  相似文献   

13.
Soft chewable dosage forms are a new approach to improve the compliance of medication for special patient populations. Based on their texture, they are chewed several times before they get swallowed. A suitable dissolution method based on in vivo chewing data was developed. The method covers parts of dissolution within the oral cavity (simulation of chewing) as well as the dissolution of the swallowed bolus within the gastrointestinal tract. Chewing was simulated by the help of a steel tooth assembled to a texture analyzer and wedge gliding on an inclined plane, imitating the occlusal glide. Chewing cycles of non-brittle, elastically deformable foods were predicted by a multiple linear regression (R adj?=?0.985) using hardness, stickiness, fat/water content, and softening behavior as independent variables. Cross-validation of three sets of chewing data led to a root mean square error of prediction of 0.408 or 0.658 chewing cycles, respectively. The new method is able to distinguish between different soft chewable formulations which had been approved as similar by the dissolution method of the European Pharmacopoeia. Furthermore, it provides information about the drug content released within the time of chewing (7–15%).  相似文献   

14.
唾液的增加加速了含羧甲基壳聚糖口香糖的抗菌效果   总被引:1,自引:0,他引:1  
目的:本论文采用了含羧甲基壳聚糖的口香糖,咀嚼这种口香糖的机械效果加速了其对口腔细菌的抑制作用,还比较口腔嗽洗液和咀嚼口香糖的抗菌效果,证明了通过咀嚼这种口香糖加速了唾液的分泌.方法:从青岛大学口腔科的老师和学生中选取了12名健康的受试者.在测试前取受试者的唾液测试细菌含量.在测试口香糖的试验中,受试者咀嚼5分钟口香糖然后休息5分钟.在测试口腔嗽洗液时,受试者用10ml嗽洗液漱口30秒后,休息9分30秒.同一天中这些测试步骤在50分钟内连续不断的进行了5次.5次测试后分别在0、30和60min收集被试者的唾液测试细菌含量.在测试唾液分泌的试验中,受试者每天咀嚼三次口香糖持续两天.结果:与使用口腔嗽洗液相比,咀嚼含羧甲基壳聚糖口香糖的受试者,在三个取样时间内口腔细菌的含量基本都明显减少,但是在60分钟的取样时间结果有点差异.咀嚼含羧甲基壳聚糖的口香糖明显提高了唾液的分泌量.结论:咀嚼含羧甲基壳聚糖的口香糖具有明显的抗菌效果.目前的研究结果强有力的证明了:使用像壳聚糖以及其衍生物这样的天然物质,对我们的口腔健康以及生活质量都有很大的帮助.  相似文献   

15.
16.
Recently, we reported that 1,2-dipalmitoyl-sn-glycero-3-phosphoglyceroglycerol (DPPGOG) prolongs the circulation time of thermosensitive liposomes (TSL). Since the only TSL formulation in clinical trials applies DSPE-PEG2000 and lysophosphatidylcholine (P-lyso-PC), the objective of this study was to compare the influence of these lipids with DPPGOG on in vitro stability and heat-induced drug release properties of TSL. The content release rate was significantly increased by incorporating DPPGOG or P-lyso-PC in TSL formulations. DPPC/DSPC/DPPGOG 50:20:30 (m/m) and DPPC/P-lyso-PC/DSPE-PEG2000 90:10:4 (m/m) did not differ significantly in their release rate of carboxyfluorescein with >70% being released within the first 10s at their phase transition temperature. Furthermore, DPPC/DSPC/DPPGOG showed an improved stability at 37 degrees C in serum compared to the PEGylated TSL. The in vitro properties of DPPGOG-containing TSL remained unchanged when encapsulating doxorubicin instead of carboxyfluorescein. The TSL retained 89.1+/-4.0% of doxorubicin over 3 h at 37 degrees C in the presence of serum. The drug was almost completely released within 120s at 42 degrees C. In conclusion, DPPGOG improves the in vitro properties in TSL formulations compared to DSPE-PEG2000, since it not only increases the in vivo half-life, it even increases the content release rate without negative effect on TSL stability at 37 degrees C which has been seen for DSPE-PEG2000/P-lyso-PC containing TSL.  相似文献   

17.
An attempt was made to formulate medicated chewing gum to prevent motion sickness using natural gum base for faster onset of action and easy administration, anywhere and anytime, without access to water. To avoid the discard issue of gum cud, natural gum base of Triticum aestivum (wheat grain) was explored because of its biodegradable and biocompatible nature and easy availability. Prolamin, extracted from wheat, showed good chewing capacity, elasticity, high water retention capacity, antifungal activity, and compatibility with the drug. Formulations were prepared based on a two-factor and three-level factorial design. Amount of calcium carbonate (texturizer) and gum base were selected as independent variables. Elasticity and drug release were considered as the dependent variables. All batches were evaluated for the content uniformity, elasticity study, texture study, in vitro drug release study, and chewiness study. Results revealed that medicated chewing gum containing 80 mg of calcium carbonate and 500 mg of gum base showed good elasticity and more than 90% drug release within 16 min. Thus, this study suggested that both good elasticity and chew ability and abundant availability of wheat grain can act as a potential gum base for medicated chewing gum.KEY WORDS: biodegradable gum, gum base, medicated chewing gum, plasticizer, wheat prolamin  相似文献   

18.
Semlali A  Leung KP  Curt S  Rouabhia M 《Peptides》2011,32(5):859-867
We investigated the toxicity of synthetic antimicrobial decapeptide KSL-W on normal human gingival epithelial cell cultures, its effect on Candida albicans adhesion and growth, and the activation of epithelial cell innate immunity. Our results indicate that KSL-W had no toxic effect on cell adhesion or growth, suggesting its safe use with human cells. Pre-treating C. albicans with KSL-W attenuated the yeast's virulence as demonstrated by its reduced adhesion and growth on engineered human oral mucosa epithelium and the subsequent decreased expression of some innate defense molecules by targeted epithelial cells. Indeed, the expression of Toll-like receptors and human β-defensins was reduced in tissues infected with KSL-W-treated Candida. Proinflammtory cytokine secretion (IL-1β and IL-6) by the epithelial cells was also regulated by KSL-W in a manner similar to that of antifungal molecule amphotericin B. These findings therefore show that KSL-W is safe for use with human cells and is able to attenuate Candida virulence by modulating its effects on host innate immunity. This study proposes the potential application of KSL-W peptide as an alternative antifungal agent.  相似文献   

19.
We hypothesized that interindividual differences in motor activities during chewing and/or swallowing were determining factors for the transfer of volatile aroma from the in-mouth air cavity (IMAC) toward the olfactory mucosa. In our first experiment, we looked for changes in IMAC volume after saliva deglutition in 12 healthy subjects. The mean IMAC volume was measured after empty deglutition using an acoustic pharyngometer device. Based on the time course of the IMAC volume after swallowing, we discerned two groups of subjects. The first group displayed a small, constant IMAC volume (2.26 mL ±0.62) that corresponded to a high tongue position. The second group displayed a progressive increase in IMAC (from 6.82 mL ±2.37 to 22.82 mL ±3.04) that corresponded to a progressive lowering of the tongue to its resting position. In our second experiment, we investigated the relationship between IMAC volume changes after deglutition and the level of aroma release at the nostril. For this purpose, the release of menthone was measured at the nostril level in 25 subjects who consumed similar amounts of a mint tablet. The subjects were separated into two groups corresponding to two levels of menthone release: high (H) and low (L). The mean volume of IMAC was measured during and after empty deglutition. Group H displayed a small, constant amplitude of IMAC volume change after deglutition, while Group L displayed a progressive increase in IMAC. It is likely that Group H continuously released the aroma through the veloglossal isthmus as the mint was consumed, while Group L trapped the aroma in the oral cavity and then released it into the nasal cavity upon swallowing. These results show that the in vivo aroma release profile in humans depends closely on the different motor patterns at work during empty deglutition.  相似文献   

20.
This study describes the formulation and physicochemical characterization of poly(acrylic acid) (PAA) organogels, designed as bioactive implants for improved treatment of infectious diseases of the oral cavity. Organogels were formulated containing a range of concentrations of PAA (3-10% w/w) and metronidazole (2 or 5% w/w, representing a model antimicrobial agent) in different nonaqueous solvents, namely, glycerol (Gly), polyethylene glycol (PEG 400), or propylene glycol (PG). Characterization of the organogels was performed using flow rheometry, compressional analysis, oscillatory rheometry, in vitro mucoadhesion, moisture uptake, and drug release, methods that provide information pertaining to the nonclinical and clinical use of these systems. Increasing the concentration of PAA significantly increased the consistency, compressibility, storage modulus, loss modulus, dynamic viscosity, mucoadhesion, and the rate of drug release. These observations may be accredited to enhanced molecular polymer entanglement. In addition, the choice of solvent directly affected the physicochemical parameters of the organogels, with noticeable differences observed between the three solvents examined. These differences were accredited to the nature of the interaction of PAA with each solvent and, importantly, the density of the resultant physical cross-links. Good correlation was observed between the viscoelastic properties and drug release, with the exception of glycerol-based formulations containing 5 and 10% w/w PAA. This disparity was due to excessive swelling during the dissolution analysis. Ideally, formulations should exhibit controlled drug release, high viscoelasticity, and mucoadhesion, but should flow under minimal stresses. Based on these criteria, PEG 400-based organogels composed of 5% or 10% w/w PAA exhibited suitable physicochemical properties and are suggested to be a potentially interesting strategy for use as bioactive implants designed for use in the oral cavity.  相似文献   

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