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At least 1,621 records · Page 90Linked to original sources
PubMed1998

Salivary secretion: stimulatory effects of chewing-gum versus paraffin tablets.

Paraffin tablets are commonly used in clinical saliva tests whereas chewing-gum is recommended to increase salivation in xerostomic patients. The aim of this study was to compare the effect on salivation of these stimuli. Saliva stimulated by chewing-gum or paraffin tablets was sampled on separate occasions from eight healthy subjects (25-45 yr). Whole or parotid saliva were collected for 6 min (1 min + 5 min) and 21 min (1 min + 5 min x 4), respectively. pH of saliva was measured with and without the addition of HC1 (titrated pH). Total parotid protein was measured using the microBSA-assay. Initially, flow rates were significantly higher during the chewing of gum vs. paraffin tablets (whole saliva 5.18 vs. 2.99 ml/min, parotid saliva 0.83 vs. 0.42 ml/min). Conversely, during final chewing periods, parotid flow rates, pH, and titrated pH were significantly higher during paraffin chewing. When comparing the stimuli, parotid protein output was higher initially during gum chewing, but in the final period paraffin chewing elicited the higher output. It was concluded that the clinical test of paraffin chewing gives a good estimate of the expected whole saliva response to chewing-gum. Furthermore, extended chewing of paraffin tablets seemed to influence parameters of parotid saliva positively.

Adult↗
PubMed2003

Comparative pharmacokinetics and safety of lansoprazole oral capsules and orally disintegrating tablets in healthy subjects.

BACKGROUND: Many individuals with acid-related gastrointestinal disorders have difficulty in swallowing oral agents. AIM: To compare the bio-availability of a single dose of lansoprazole orally disintegrating tablet with that of an intact capsule. METHODS: One hundred and twenty healthy subjects participated in two prospective, Phase I, open-label, two-period cross-over studies to receive lansoprazole, 15 mg or 30 mg. Within each study, subjects were randomized into two parallel cohorts consisting of 30 subjects per regimen, dispensed in opposing sequence over two periods separated by a 7-day washout period. Blood samples were collected on day 1 of both periods to determine the pharmacokinetic parameters. RESULTS: Tmax occurred at 1.8 and 2.0 h with the 15-mg and 30-mg tablets, respectively. Dose proportional increases in Cmax, AUCt and AUC infinity were observed in the 15-mg and 30-mg groups. The terminal elimination half-lives (t1/2) were identical in both dose groups (1.18 h). Lansoprazole administered as the orally disintegrating tablet was bio-equivalent to the intact capsule formulation with respect to Cmax, AUCt and AUC infinity. CONCLUSIONS: Lansoprazole orally disintegrating tablets, 15 mg and 30 mg, are bio-equivalent to the respective dose administered as the intact capsule. This novel dosage formulation represents an option for patients who have difficulty in swallowing oral agents.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2003

Gastrointestinal transit and release of 5-aminosalicylic acid from 153Sm-labelled mesalazine pellets vs. tablets in male healthy volunteers.

BACKGROUND: Mesalazine (5-aminosalicylic acid)-containing formulations, designed to optimize drug delivery to the ileo-caecal region, represent a cornerstone in the treatment of inflammatory bowel diseases. AIM: : To test, by means of pharmaco-scintigraphy, whether novel mesalazine-containing pellets release 5-aminosalicylic acid in the same target region as mesalazine tablets (Salofalk). METHODS: Fourteen healthy male volunteers received a single dose of either pellets or tablets containing 500 mg of mesalazine and 2 mg of 152Sm2O3 with a 1-week washout period. The gastrointestinal transit of 153Sm, incorporated into the formulations, was followed by gamma-scintigraphy. Mesalazine release was verified by assessing 5-aminosalicylic acid plasma pharmacokinetics. RESULTS: The formulations reached the ileo-caecal target region almost at the same time (3.3 +/- 1 and 3.8 +/- 1 h for pellets and tablets, respectively). Plasma 5-aminosalicylic acid tmax values were comparable and corresponded to the time during which the formulations were located in the target region. Plasma AUC values were significantly lower for pellets, which might be explained by a more prolonged release of 5-aminosalicylic acid. CONCLUSIONS: Novel mesalazine pellets and Salofalk tablets release active 5-aminosalicylic acid in the same target region and pass through the gastrointestinal tract under fasting conditions in healthy volunteers in a comparable time. From a comparison of in vitro dissolution and plasma concentration data, a slower and more prolonged release of 5-aminosalicylic acid from pellets is suggested.

Adult↗
PubMed2000

Tolerability and efficacy of naratriptan tablets in the acute treatment of migraine attacks for 1 year. Naratriptan Long-Term Study Group.

OBJECTIVE AND DESIGN: This open-label study was conducted to evaluate the tolerability and efficacy of the 5HT1 agonist naratriptan with repeated use in the acute treatment of migraine attacks for 1 year. Four hundred and seventeen (417) migraine patients treated 15,301 migraine attacks over the course of the study. RESULTS: The results show that 84% of attacks treated with a single 2.5 mg dose of naratriptan were not associated with the occurrence of an adverse event. The percentage of attacks associated with an adverse event did not increase with number of doses used to treat a given attack (1 vs. 2) or duration of use (0-6 months vs. > 6-12 months). The only adverse events experienced in > 2% of attacks throughout the 1-year study were nausea (3% of attacks), hyposalivation (2% of attacks), and drowsiness/sleepiness (2% of attacks). Headache relief 4 h post-dose was reported in a median 70% of moderate or severe attacks and a median 86% of mild attacks treated with naratriptan tablets 2.5 mg. The percentages of patients reporting headache relief did not diminish as a function of increased duration of treatment (0-6 months vs. > 6-12 months) or frequency of use (for > 36 vs. < 36 attacks). The mean number of tablets taken per attack was 1.2. A second naratriptan 2.5 mg tablet was taken for headache recurrence in a mean 16% (median 8%) of attacks. CONCLUSION: The results of this study demonstrate that naratriptan tablets 2.5 mg taken for acute migraine attacks over a 1-year period are well-tolerated and effective.

Adult↗
PubMed2000

Rizatriptan tablet versus wafer: patient preference.

After taking both conventional oral rizatriptan tablets and oral disintegrating rizatriptan tablets in the treatment of migraine with or without aura, patients were permitted to select their formulation preference. All adult patients who had requested continuation of rizatriptan during a 6-month period were included in the study. Of the 367 patients studied, 188 selected the oral disintegrating tablet, while 179 preferred the conventional tablet. Although individual patients had strong preferences for one preparation over the other, no group preference was found.

Adult↗
PubMed2005

In vivo biopharmaceutical characterisation of a new formulation containing the antiepileptic drug lamotrigine in comparison to plain and dispersible/chewable lamotrigine tablets.

AIM: Two studies in healthy male volunteers were carried out to evaluate the pharmacokinetic profile of a new divisible formulation of lamotrigine (CAS 84057-84-1, Plexxo, Lamotrigin Desitin) in plasma in comparison to plain or dispersible lamotrigine tablets. METHODS: The plasma pharmacokinetics of lamotrigine were analysed after administration of single doses of 100 mg lamotrigine given as one tablet of the new formulation and either the plain or the dispersible reference formulation in two separate studies. In each study the data of 24 subjects were analysed according to the study protocol. Venous blood samples were taken at appropriate intervals up to 120 h after dosing. Concentrations of lamotrigine were determined in plasma by a validated HPLC method using UV detection. RESULTS AND CONCLUSION: In both studies, mean plasma concentration-time profiles of the new lamotrigine formulation and both reference formulations ran nearly in parallel. The pharmacokinetic mean data calculated from different subject groups of the two studies were very similar. The mean ratios of the main pharmacokinetic parameters and the corresponding 90% confidence intervals of AUC(0-t), AUC(0-inf) and C(max) were 103% (99.7-105.7), 103% (99.6-107.3) and 101% (95.2-106.6) for the comparison with the plain lamotrigine tablet and 100% (98.0-102.8), 100% (96.5-102.8) and 102% (99.1-105.3) for the comparison with the dispersible/chewable tablet, respectively. The most frequently reported adverse events possibly related to the administration of lamotrigine were headache and dizziness in both studies. It is concluded that the new divisible lamotrigine formulation is bioequivalent with regard to rate and extent of absorption to both the plain reference lamotrigine product and to the dispersible/chewable reference product.

Adolescent↗
PubMed2005

Comparative bioavailability study with two gemfibrozil tablet formulations in healthy volunteers.

OBJECTIVE: To assess the bioequivalence of gemfibrozil (CAS 25812-30-0) 900 mg tablet formulation from EMS Farmaceutica as test formulation versus a 900 mg tablet formulation as reference in 36 healthy volunteers of both sexes. METHODS: The study was conducted using an open, randomized, two-period crossover design with a 1-week washout interval. Plasma samples were obtained over a 24-h period. Plasma gemfibrozil concentrations were analyzed by liquid chromatography coupled to tandem mass spectrometry (LC-MS-MS) with negative ion electrospray ionization using multiple reaction monitoring (MRM). From the gemfibrozil plasma concentration vs time curves, the following pharmacokinetic parameters were obtained: AUClast, AUC(0-inf) and Cmax. RESULTS: The limit of quantification was 0.05 microg/mL for plasma gemfibrozil analysis. The geometric mean and respective 90% confidence interval (CI) of Test/Reference percent ratios were 90.29 (81.39-100.17) for Cmax, 96.26 (90.33-102.59) for AUClast, 96.04 (90.21-102.23) for AUC(0-24 h) and 96.62 (90.82-102.78) for AUC(0-infinity). CONCLUSION: Since the 90% CI for AUClast, AUC(0-inf) and Cmax, ratios were within the 80-125% interval proposed by the U.S. FDA, it was concluded that gemfibrozil 900 mg tablet (test formulation) was bioequivalent to the 900 mg tablet reference formulation for both rate and extent of absorption.

Adolescent↗
PubMed2001

Bioavailability and pharmacokinetic profile of dihydroergotoxine from a tablet and from an oral solution formulation.

Dihydroergotoxine mesylate (DHETM, CAS 8067-24-1), the combination of the mesylates of four dihydrogenated ergot alkaloid derivatives (dihydroergocornine, dihydroergocristine, alpha-dihydroergocryptine and beta-dihydroergocryptine), is used mainly for age-related cognitive impairment. The bioavailability of DHETM was investigated in a cross-over study on 20 male healthy volunteers to whom two single doses of 9 mg DHETM were administered either in tablets (Orphol spezial) or in oral solution (Orphol forte). DHETM was assayed in serum with a double radioimmunoassay method displaying a satisfactory cross-reactivity with the principal components of DHETM. After administration of tablets the peak of DHETM was (mean +/- SE) 124 +/- 16 pg/ml, the tmax 1.15 +/- 0.21 h, the AUC 790 +/- 93 pg/ml x h and the terminal elimination half-life 7.54 +/- 1.23 h. After oral solution the peak of DHETM was 176 +/- 16 pg/ml, the tmax 0.50 +/- 0.04 h, the AUC 779 +/- 94 pg/ml x h and the terminal elimination half-life 6.13 +/- 0.76 h. The bioavailability of DHETM from tablets vs. that from oral solution differed only by a retard related to the dissolution time of DHETM from the tablets, but not for other pharmacokinetic parameters. The relatively high two single doses of 9 mg DHETM administered to the 20 subjects were well tolerated, causing only known and expected adverse reactions to DHETM (tiredness, headache and vertigo) that did not require discontinuation of the study.

Adult↗
PubMed2001

Bioequivalence of different prednisolone tablet formulations.

The relative bioavailability of different prednisolone (CAS 50-24-8) tablet formulations (Prednisolon Ferring 2, 5, and 20 mg) was investigated in comparison to a reference formulation. The study was performed in a GCP/ICH-conform manner using a randomized cross-over design in 13 healthy volunteers. With respect to the pharmacokinetic parameters Cmax (maximal prednisolone concentration), AUC0-12 h (area under the concentration-time curve until 12 h after drug intake), AUC0-infinity (area under the concentration-time curve until infinity), and t1/2 (elimination half-life time), 10 x 2 mg prednisolone tablets did not show any relevant differences as compared to the reference (1 x 20 mg) meaning that the 90% confidence intervals were within the given 0.80-1.25 limits for the decision of bioequivalence. Although not statistically significant, tmax (time to reach the maximal prednisolone plasma concentration) was 11 min shorter regarding the test preparation as compared to the reference. The pharmacokinetic parameters of 4 x 5 prednisolone tablets were also well in accordance with the reference. The most important parameters Cmax, AUC and t1/2 were within the defined limits for the acceptance of bioequivalence and, in addition, tmax did not show any significant differences. The 20 mg prednisolone tablet formulation showed almost identical parameters of Cmax, AUC, t1/2 und tmax in comparison to the reference substance. Taken together, the results of the bioavailability parameters indicate the bioequivalence of the three prednisolone test preparations as compared to the reference.

Adult↗
PubMed1984

[Therapeutic effect of intravaginal application of estriol tablets in the treatment of pathological cervical factor as a cause of sterility].

81 women were included in a prospective randomised 12-year personal study. The "pathological cervical factor" was confirmed by periovulatory daily examination of the quality of the cervical mucus, using a new modified scheme of cervical score by examining the oestrogenic activity in the vaginal smear and results of sperm-penetration tests after Sims- Huhner , partly also by periovulatory determination of the concentration of luteinising hormone in the serum. The presence of ovulatory cycles could also be determined by regular registration of the cycle length, measurement of the basal body temperature and partly by premenstrual endometrium biopsies; these determinations were of course effected during cycles without therapy. All 81 cases with abnormal preovulatory production of cervical mucus were treated in a total of 234 cycles by intravaginal application of oestriol tablets 1 to maximal 3 mg daily for 1 or more subsequent cycles. On the basis of these criteria, the quality of cervical mucus and postcoital tests improved with a satisfying intravaginal resorption of the oestriol tablets; no side effects were seen. After this therapy, very good results were obtained with intravaginally administered oestriol tablets in 59.3% of the patients with a pregnancy rate of 27.2%; 24.7% of the cases only showed a moderate improvement of the mucus; 16.0% did not respond to oestriol treatment and, therefore, had to be considered as therapeutic failures. The present study again confirms the results of other investigators on the local effectiveness of intravaginal application of oestriol tablets.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed2004

Vaginal prostaglandin E2 gel versus tablet in the induction of labour at term--a retrospective analysis.

Our aim in this retrospective analysis was to compare labour outcomes between 145 consecutive women with unfavourable cervices, who received prostaglandin E2 vaginal gel (1-2 mg) for labour induction over a 3-month period, and 149 women receiving a prostaglandin E2 vaginal tablet (3 mg) over the following 3 months. Our results showed that cervical dilatation in the gel group was significantly more than in the tablet group at transfer to labour ward [4 cm (SD 2.5 cm) versus 3.3 cm (SD 2 cm), mean difference -0.7, 95% CI -1.2 to -0.2, P=0.01), with fewer women requiring oxytocin augmentation, but this was not statistically significant (41.4% versus 50%, RR 0.8, 95% CI 0.7-1.1). There were no significant differences in the mode of delivery in the number delivering vaginally within 24 hours of the induction (60.4% in the gel group versus 56.2% in the tablet group, RR1.1, 95% CI 0.9-1.4), in the number of doses of PGE2 administered, or in the neonatal outcomes between the two groups. In conclusion, there were no significant differences in labour or neonatal outcomes between prostaglandin E2 gel or tablet use in the induction of labour in this retrospective analysis.

Administration, Intravaginal↗
PubMedDate not supplied

Tableting of coated ketoprofen pellets.

Ketoprofen pellets were prepared by the method of extrusion-spheronization, and a film coating of guar gum and Eudragit NE was applied to drug cores using pan technology. In an attempt to design a tablet which, on peroral administration, disintegrates rapidly, releasing intact coated pellets which maintain the integrity of both the cores and their release retarding membrane, Avicel PH101, lactose DT and magnesium stearate were used as excipients to prepare tablets comprising ketoprofen pellets or microcapsules. Preliminary experiments were conducted on uncoated pellets to determine the optimum compression force required to prepare tablets of satisfactory mechanical properties and release profiles. Coated pellets containing ketoprofen were used to investigate the influence of excipients levels. In an attempt to minimize problems associated with blending and segregation of microcapsules and excipients, placebo spheres of Avicel PH101 and lactose DT were produced by the method of extrusion-spheronization. The use of placebo spheres produced tablets with improved drug content uniformity and disintegration time. The tensile strength of such compacts was enhanced by excluding magnesium stearate from the mixes without significant problems of sticking or picking. The use of placebo pellets resulted in significant damage to drug microcapsules, which was attributed to the higher hardness and density of the excipients pellets. The role of membrane coating in protecting the drug core during compression was also evaluated.

Capsules↗
PubMed2006

Design and evaluation in vitro of controlled release mucoadhesive tablets containing chlorhexidine.

This investigation deals with the development of buccal tablets containing chlorhexidine (CHX), a bis-bis-guanide with antimicrobial and antiseptic effects in the oral cavity, and able to adhere to the buccal mucosa to give local controlled release of drug. A mucoadhesive formulation was designed to swell and form a gel adhering to the mucosa and controlling the drug release into the oral cavity. Some batches of tablets were developed by direct compression, containing different amounts of hydroxypropylmethylcellulose (HPMC) and carbomer; changing the amount ratio of these excipients in formulations, it is possible easily modulate the mucoadhesive effect and release of drug. The in vitro tests were performed using the USP 26/NF paddle apparatus, a specifically developed apparatus, and a modified Franz diffusion cells apparatus. This last method allows a simultaneous study of drug release rate from the tablets and drug permeation through the buccal mucosa. Similar tests have also been carried out on a commercial product, Corsodyl gel, in order to compare the drug release control of gel with respect to that of the mucoadhesive tablet, as a formulation for buccal delivery of CHX. While the commercial formulation does not appear to control the release, the formulation containing 15% w/w methocel behaves the best, ensuring the most rapid and complete release of the drug, together with a negligible absorption of the active agent as required for a local antiseptic action in the oral cavity.

Adhesiveness↗
PubMed2006

Development of sustained-release tablets containing sodium valproate: in vitro and in vivo correlation.

We have developed a 200 mg and 400 mg sustained-release sodium valproate tablet that allows effective blood concentration of the active drug with once-a-day dosing. The controlled dissolution or sustained release of the drug was attained by a membrane-controlled system. A single-coating system did not adequately control the dissolution rate, and therefore double-coated tablets were prepared and a human pharmacokinetic study was conducted. With the 200 mg VPA-Na tablets, the nonfasting C(max) was only 20% higher than the fasting C(max). An in vitro dissolution test was conducted to predict the effects of food on drug dissolution after administration of this tablet. A relatively good correlation was observed between the absorption profiles and the dissolution profiles of the drug.

Acrylic Resins↗
PubMed2006

The influence of drug-excipient and drug-polymer interactions on butt adhesive strength of ranitidine hydrochloride film-coated tablets.

The influence of fillers and polymeric films on adhesive strength of hydroxypropyl methylcellulose (HPMC) and Eudragit E100 films coated on ranitidine HCl tablets containing either spray-dried rice starch (SDRS) or lactose monohydrate as fillers after storage at 45 degrees C/75% RH for four weeks was investigated by the use of butt adhesion technique. The adhesive strength of film-coated tablets of fillers without drug was found to slightly decrease after storage. In contrast, the adhesive strength of drug-containing film-coated tablets significantly reduced, the degree of which was higher for Eudragit E100 than HPMC. Physicochemical characterization by employing differential scanning calorimetry (DSC) and diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS) revealed that the drug was obviously incompatible with lactose and possibly mild interaction with Eudragit E100 was suggested. The results indicated that the adhesive strength of film-coated tablets would be affected not only by the drug-excipient interaction, but also by the drug-polymeric film interaction.

Adhesiveness↗
PubMed2006

High-throughput evaluation of non-swellable controlled release matrix tablets.

Drug release from controlled-release (CR) matrix tablets involves the permeation and diffusion of water through the system. In this study, a new methodology is proposed for the measurement of water permeation and simultaneous drug release from the inert, non-swellable CR matrix tablet of diltiazem (DLT) and a correlation is made between these two processes. Cylindrical matrices were readily prepared by direct compression of pellets obtained by extrusion-spheronization. Water transport was studied using tritiated water (HTO) as a permeant in a Franz-diffusion cell and simultaneously drug release was measured. Further, dissolution was performed on USP XXI/XXII dissolution apparatus I using demineralized water. Matrices showed a steady water-uptake up to 6 h and the steady state for HTO permeation lasting from 6-h to 24-h Flux of water permeated and flux of drug released correlated well. Thus, HTO permeation through the matrix tablet and the proposed methodology can be used as a tool and/or surrogate marker for evaluation of controlled release matrix tablets. This methodology can be coined as "high-throughput" in terms of amount of labor and resources required in comparison to that of dissolution.

Delayed-Action Preparations↗
PubMedDate not supplied

Evaluation of polyvinyl acetate dispersion as a sustained release polymer for tablets.

Kollicoat SR 30D is a unique 30% aqueous dispersion of polyvinvyl acetate stabilized by polyvinyl-pyrrolidone intended for preparation of sustained release products. Detailed evaluation of this polymer dispersion as a sustained release coating for active pharmaceutical ingredients of two diverse classes of drugs was studied. A water insoluble drug (ibuprofen) and a water soluble drug (ascorbic acid) were selected as model active drugs. Ibuprofen was granulated using a GPCG-1 fluid bed processor prior to tableting, to improve the particle size and particle flow properties. In this process a 2(3) factorial design was implemented to evaluate the optimum process parameters such as spray rate, inlet air temperature and the inlet air velocity. The statistical model selected was Y(ijkl) = mu + tau(i) + beta(j) + theta(k) + (taubeta)ij + (betatheta)jk + (tautheta)ik + (taubetatheta)ijk + epsilon(ijkl). The factorial design showed that the spray rate, inlet air temperature, and inlet air velocity had a significant effect (p value <0.05) on the particle size. Significant improvement was observed in the flow properties of the granules. The granules were coated with Kollicoat SR30D dispersion using top spray method in the fluid bed processor. The dissolution studies showed that the release of ibuprofen decreased with an increase in the coating levels of Kollicoat SR 30 D. In the case of ascorbic acid, preparation of sustained release coated commercial granules was not possible due to the difficulty in coating a highly soluble drug particle. However, the coated granules when compressed into tablets showed some sustainability. Ibuprofen tablets manufactured with coated granules with a 15 g polymer for 300 g batch showed dissolution parameters of t50 and t90 at 4.2 hr and 7.5 hr, respectively. An approximate zero-type of release was observed when the polymer content was increased to 45 g for 300 g batch. Ascorbic acid tablets made with coated commercial granules having a total polymer content of 45 g per a 500 g batch showed an average dissolution t50 and t90 at 1.0 hr and 4.55 hr, respectively. When the total polymer content was increased to 60 g, per 500 g, the average dissolution t50 and t90 delayed to 1.40 hr and 7.20 hr, respectively.

Analysis of Variance↗
PubMed2001

Evaluation of the tablet coating by the conventional spouted-bed process.

The purpose of this paper was to present an analysis of the tablet coating by the conventional spouted-bed process. To analyze the equipment performance, the rate of increase of the tablets mass, K1, and the adhesion coefficient eta were determined as a function of the feed flow rate of coating suspension Ws; of the Reynolds number Rep; of the flow rate of atomizing gas Wat, and of the cone base angle gamma. To analyze the product quality, the uniformity of coating mass deposition onto the tablet's surface was used. Three different procedures for description of kinetics growth, weighing method, image analysis, and measurements with a micrometer were used to verify the validity of the commonly used weighing method. Comparison between experimental results of kinetics growth with estimates obtained by a literature model was also performed. A tendency toward an increase in K1 and in eta with the feeding flow rate of coating suspension Ws was detected. The weighing method can be used for the process analysis. The kinetics of growth can be described by the growth model used. The variable that produce more pronounced effect on K1 and eta was the feed flow rate of coating suspension, the weighing method describes very well the increase of particle diameter with coating time, the growth model can be used for the describe the kinetics of growth during the coating operation, and the coating does not deposit uniformly onto the tablet's surface.

Chemistry, Pharmaceutical↗