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At least 1,063 records · Page 59Linked to original sources

[Sandwiched osmotic pump tablet for controlled release of water-insoluble drug].

AIM: To study sandwiched osmotic pump tablet for delivering water-insoluble drug for 24 hours. METHODS: Sandwiched osmotic pump tablet was prepared using nifedipine as the model drug. The effects of various formulation variables and orifice size on drug release were studied. The mechanical properties of cellulose acetate membrane were also investigated. RESULTS: Polyethylene oxide of drug layer and potassium chloride of push layer showed marked positive effects on drug release. In the range of 0.50 mm to 1.40 mm, orifice size hardly affects drug release. Cellulose acetate membrane is strong enough to assure the integrity of osmotic pump tablet and could sustain an internal pressure ranging from 0.34 MPa to 2.85 MPa. CONCLUSION: Sandwiched osmotic pump tablet can deliver water-insoluble drug constantly for 24 hours. Release media and agitation rate scarcely affect drug release. Compared with the commercialized push-pull osmotic pump tablet, sandwiched osmotic pump tablet is easy in preparation with exempting identification of drug layer before drilling.

Cellulose↗

Intra-gastric performance and bioavailability study of a new per-oral bioadhesive Verapamil HCl matrix tablet in dogs.

In a previous study, we developed a per-oral extended--release bioadhesive matrix tablet for verapamil HCl (VP). The system combined both strong bioadhesion and sustained release properties in vitro. The purpose of this study is to evaluate the in vivo performance of the prepared bioadhesive tablets (B). The conduction of a periodic X-ray imaging of the abdomen of beagle dogs, after administration of B containing 12% barium sulfate, was used to evaluate the intra-gastric performance. The VP concentrations in blood samples taken at specified times after oral administration of B to fasted beagle dogs were determined and compared with those obtained after administration of a commercial sustained release VP tablets (Manidon 120 R). The X-ray images showed that bioadhesive tablets remained almost at the same place in the stomach for at least 6 hours while it disappeared after 1 hour in case of the control tablets. No statistical difference was seen between the Cmax, tmax, AUC, t1/2, and MRT for B compared to Manidon. The Cmax was found to be 51.4 +/- 15.5 and 48.6 +/- 17.9 (ng/ml) for Manidon and B, respectively and the corresponding tmax were 7.0 +/- 1.9 and 6.0 +/- 0, respectively. The AUCO-. for Manidon and B were 949.84 +/- 245.11 and 722.92 +/- 144.42 ng.h/ml, respectively. So, the prepared B tablets can be considered bioequivalent to the commercial Manidon Retard product.

Adhesives↗

The efficacy of cholesterol-lowering action and side effects of garlic enteric coated tablets in man.

The present study aimed at investigating the cholesterol-lowering and side effects of garlic enteric coated tablets in comparison with placebo tablets. The study is a randomized double-blinded crossover design involving 116 volunteers. However, 16 of them did not complete the study. The remaining 100 volunteers were divided into two groups: 45 were in the trial group and the remaining 55 in the control group. The volunteers in the trial group were asked to take garlic tablets in the first three months, placebo in the second three months and discontinue all tablets in the last three months, while the volunteers in the control group started with three months of placebo followed by three months of garlic tablets and ended up with three months of tablets discontinuity. The results showed that there were no significant differences in the total serum cholesterol levels between the two groups at the end of three months or six months of the study. Side effects included headache, itching and complaints of garlic smell. No serious side effects relating to liver, kidney functions or hematologic side effects were detected

Adult↗

[A meta-analysis of treatment of infantile diarrhea with bifid triple viable bacterial tablet].

OBJECTIVE: To assess the efficacy and safety of bifid triple viable bacterial tablet in treatment of infantile diarrhea. METHODS: According to the requirements of Cochrane systematic review, a thorough literature search was performed among Chinese Digital Hospital Library (www.chkd.cnki.net) and Chinese Biomedical Literature Disk Database (CBMdisk). A meta analysis was performed on a total of 1326 patients involved in 12 papers which met the inclusion criteria. RESULTS: Publication bias analysis showed that the funnel plot was symmetrical. Test for heterogeneity showed that the groups treated with bifid triple viable bacterial tablet and antibiotics or anti-viral agents or placebo control had clinical homogeneity and statistical homogeneity (P = 0.66, 0.67, 0.85, respectively, I(2) = 0%), which allowed to use fixed effect model analysis. The bifid triple viable bacterial tablet and Smecta did not have statistical homogeneity (P = 0.02, I(2) = 70.9%), therefore random effect model analysis was applied. Incorporation analysis showed that in comparison of the bifid triple viable bacterial tablet versus antibiotics or anti-viral agents or placebo control, the odds ratios were 5.34, 4.74 and 6.43, respectively, and 95% CIs were [2.81, 10.16], [2.47, 9.09], and [2.61, 15.83], on test for overall effect, Z = 5.11, 4.67 and 4.04, P < 0.00001. In the forest plot the 95% CI horizontal line of incorporation odds ratio droped to the right side of the vertical line indicating the border of effectiveness. However, no statistically significant difference was found between bifid triple viable bacterial tablet and Smecta. CONCLUSION: The clinical evidences available so far indicated that treatment of infantile diarrhea with bifid triple viable bacterial tablet is safe and effective although rigorously designed large sample size randomized double blind clinical trials are required to further demonstrate and support the conclusion.

Administration, Oral↗

Development and validation of dissolution tests for fexofenadine hydrochloride capsules and coated tablets.

PURPOSE: This study describes the development and validation of dissolution tests for fexofenadine hydrochloride capsules and coated tablets using an HPLC method. METHOD: The appropriate conditions were determinate after testing sink conditions, dissolution medium, and agitation intensity. The apparatus, paddle and basket, were applied to tablets and capsules, respectively. Fexofenadine hydrochloride capsules, products A and B, and coated tablets, products A, B and C were evaluated. The best dissolution conditions tested, for the products in each respective pharmaceutical dosage form were applied to evaluate the dissolution profiles. The parameters of difference factor, similar factor, and dissolution efficacy were employed. RESULTS: Optimal conditions to carry out the dissolution tests were 900 ml of 0.01 M hydrochloric acid as dissolution medium, basket at 100 rotation per minute (rpm) stirring speed for capsules and paddle at 75 rpm for tablets. The dissolution profiles for tablets products A, B, and C and for capsules products A and B were not similar. CONCLUSION: The developed and validated dissolution tests satisfactorily describes the time-course of the drug release. The obtained results provided adequate dissolution profiles. The HPLC method was validated to quantify fexofenadine capsules and coated tablets from the dissolution tests.

Capsules↗

Stability of levamisole oral solutions prepared from tablets and powder.

PURPOSE: To study the stability of levamisole oral solutions (25 mg/mL) prepared from powder and tablets stored at 4 +/- 3 degrees C and 23 +/- 2 degrees C in amber glass prescription bottles. METHODS: Levamisole 25 mg/mL solutions were prepared from commercially available 50-mg tablets or from pure powder in sterile water. Levamisole concentrations were determined in duplicate by a stability-indicating HPLC method at 0, 1, 2, 3, 4, 7, 14, 30, 60 and 90 days. The initial and final pHs of solutions were measured. RESULTS: The recovery of levamisole from tablets was 100 +/- 2.1%. No color or odour changes were observed during the study period. The oral solutions prepared from powder were stable at least 90 days stored at 4 and 23 degrees C. The oral solutions prepared from tablets were stable at least 90 days at 4 degrees C and 15 days when stored at 23 degrees C. The initial pH of solutions prepared from powder and tablets were 5.30 and 4.55, respectively. Initial and final pH values were significantly different (p<0.001) for the two solutions. CONCLUSIONS: Levamisole 25 mg/mL oral solutions can be prepared from tablets or powder with sterile water for irrigation and stored for 90 days under refrigeration, taking account of the lack of microbiological contamination.

Administration, Oral↗

Assessment of Albizia zygia gum as a binding agent in tablet formulations.

Albizia gum has been evaluated as a binding agent in tablet formulations in comparison with gelatin BP. Compressional properties were analyzed using density measurements and the compression equations of Heckel and Kawakita as assessment parameters, while the mechanical properties of the tablets were assessed using the crushing strength and friability of the tablets. Drug release properties of the tablets were assessed using disintegration time and dissolution time as assessment parameters. Formulations containing Albizia gum as a binding agent show a faster onset and higher amount of plastic deformation under compression pressure than those containing gelatin. The crushing strength, disintegration and dissolution times of the tablets increased with increased binder concentration while their friability decreased. Albizia gum produced tablets with better mechanical properties and longer disintegration and dissolution times than those containing gelatin BP. This suggests that Albizia gum could be useful as a binding agent especially when high mechanical strength and slower release rates are desired.

Albizzia↗

In vitro evaluation of marketed antimalarial chloroquine phosphate tablets.

BACKGROUND & OBJECTIVES: The aim of the present study is to investigate the physicochemical equivalence of seven brands of tablets containing chloroquine phosphate, an antimalarial purchased from different retail pharmacy outlets. METHODS: The quality and physicochemical equivalence of seven different brands of chloroquine phosphate tablets were assessed. The assessment included the evaluation of uniformity of weight, friability, crushing strength, disintegration and dissolution tests as well as chemical assay of the tablets. RESULTS: All the seven brands of the tablets passed the British Pharmacopoeia (BP) standards for uniformity of weight, disintegration and crushing strength. One of seven brands failed the friability test. One of the brands did not comply with the standard assay of content of active ingredients. Dissolution test passes the pharmacopoeial standards for chloroquine phosphate tablets. There were no significant differences in the amounts of chloroquine phosphate released from the different brands. INTERPRETATION & CONCLUSION: Out of the seven brands of anti-malarial chloroquine phosphate tablets only one brand fails to meet BP quality specifications which shows constant market monitoring of new products to ascertain their equivalency to pharmacopoeial standards.

Animals↗

Transbuccal tablets of carbamazepine: formulation, release and absorption pattern.

Tranbsuccal drug administration is an attractive method, as it has several advantages especially with respect to peroral delivery. Here we report: i) the aptitude of carbamazepine (CBZ) to penetrate porcine buccal mucosa and reconstituted human oral (RHO) epithelium; ii) three different tablet formulations for transbuccal administration; iii) the drug release rate from tablets. CBZ permeation through the buccal mucosa was investigated by using two different bi-compartmental open models: Franz cells for porcine buccal mucosa and Transwell diffusion cells system for RHO epithelium. Results, expressed as drug flux (Js) and permeability coefficients (Kp), indicated that CBZ well penetrates the membrane and arrives in the acceptor phase. Js and Kp resulted 7x10(-2) mg/cm2h and 0.23 cm/h for in vitro experiments and 1.81 x 10(-2) mg/cm2h and 4.57 x 10(-2) cm/h for ex vivo experiments. The flux is extensively affected by the membrane thickness. The CBZ release from three different formulations of tablets, prepared with loaded microspheres, loaded matrices, and conventional compressed physical mixture of components was studied. Using the new formulated "non-conventional" tablets prolonged drug release was obtained. Loaded matrix tablets discharged CBZ faster than microsphere tablets (17% and 12% in about 2.5 h respectively). Results indicate the possibility of administering CBZ on buccal mucosa.

Absorption↗

[The study of the in vivo-in vitro correlation of the naftopidil sustained-release tablet in dog].

We studied the correlation of sustained-release tablet of naftopidil between the in vitro release and the in vivo absorption in the dog. The release rate (X) of naftopidil sustained-release tablet in artificial gastric fluid was determined and the naftopidil concentration in plasma was determined after a single oral dose of 100 mg naftopidil (tablet or sustained-release tablet) in the dog. The absorbed fraction(F) and in vivo absorption rate (A) of the NAF sustained-release tablet in the dog at different time were calculated by W-N method and deconvolution method, respectively. Then the regression equations between F or A and X of the corresponding time point were obtained: F=2. 1533X - 27. 636(r = 0.9927) and A=2.3452X - 25.474(r= 0.9938). W-N method and deconvolution method both indicated that the correlation between the in vitro release and the in vivo absorption in the dog of the NAF sustained-release tablet was good.

Animals↗

[Effects of fufangdenshen tablets on human atherosclerotic plasma protein using proteomic technique].

OBJECTIVE: To research the effects of fufangdenshen tablets on atherosclerotic plasma protein using proteomic technique and further explore its potential molecular mechanism to cure atherosclerosis. METHOD: The plasma of normal, atherosclerosis and cured group were collected, and the albumin in plasma was removed. Proteomic protocol involved of 2-DE, image analysis and spectrometry detection was used to detect regulated plasma protein by fufangdenshen tablets. RESULT: 3 decreased expressed and 6 higher protein in atherosclerotic plasma could be recovered by fufangdenshen tablets. The levels of fibrinogen, Granzyme C and immunoglobulin were decreased by fufangdenshen tablets. CONCLUSION: The levels of fibrinogen, Granzyme C in atherosclerotic plasma could be decreased by fufangdenshen tablets. The effects of fufangdenshen tablets on atherosclerosis included that: inhibition of adhesion of monocyte, inhibition of proliferation and migration of VSMC, and weakening of inflammation.

Aged↗

Comparative microbial contamination levels in wet granulation and direct compression methods of tablet production.

Raw materials used for tablet production were assessed for their microbiological quality. Tablets were produced by wet granulation and direct compression methods and assessed for compliance with B.P. specifications. Samples from the production stages in the two tabletting processes were assessed for microbial levels and for absence from designated microbial species- E.coli, Ps.aeruginosa, S.aureus and salmonella species. The effect of the microbial levels of the raw materials and the formulation technology on the microbial levels of the produced tablets were also investigated. Results indicated that the microbial levels of the tablets were influenced by the microbial quality of the starting raw materials, the production environment and the method of production. Generally, tablets produced by direct compression method gave lower microbial levels than those of the wet granulation method. The compaction process exert lethal effect on the survival of microorganisms.

Drug Compounding↗

Comparative bioavailability of three batches of four commercial acetaminophen tablets.

The aim of this investigation is to evaluate four brands of acetaminophen tablets and three batches of each brand for their in vitro properties and in vivo bioavailabilities using urinary excretion data. All batches dissolved at least 80% of their acetaminophen content within 30 minutes. The differences between the dissolution rates of the batches were not found statistically significant except the batches of brand C. With respect to their dissolution rates, the brands have the following order: A less than B less than C less than D. Statistical analysis of the percent bioavailabilities and the elimination rate constants showed that there was no significant difference between brands and or between the batches. The percent excreted in the first three hours was found to be significantly different between the solution and tablet A, between tablet A and tablet C, and between Tablet A and Tablet D.

Acetaminophen↗

The search for an optimized treatment of hypoglycemia. Carbohydrates in tablets, solutin, or gel for the correction of insulin reactions.

Recommendations for the treatment of insulin reactions are based more on habit than data. We investigated the efficacy in correcting blood glucose levels and alleviating clinical symptoms of hypoglycemia of seven orally administered carbohydrates--glucose in solution, tablets, and gel; sucrose in solution and tablets; a hydrolized polysaccharide solution; and orange juice--each of which provided 15 g of carbohydrate. Forty-one type I diabetic patients recently treated with insulin agreed to submit to artificially induced hypoglycemia by an intravenous injection of insulin. Corrective therapy was given when patients experienced symptoms and asked for treatment. Mean blood glucose levels 10 minutes after ingestion were found to be similar whether correction was dispensed with the tablets and the solutions of glucose, those of sucrose, or the polysaccharide preparation. However, almost no increment was obtained at this time point with the gel or the fruit juice. Fifteen and 20 minutes after carbohydrate intake, blood glucose levels were higher with the tablet forms than with the solutions, although differences only became signifiant for sucrose. Glycemic responses were again consistently lower with the sucrose gel and the orange juice. Clinical symptoms were alleviated in 14.0 +/- 0.8 minutes (mean +/- SEM) with sucrose and glucose in solution or tablets. We conclude that in moderately severe hypoglycemia, ingestion of 15 g of carbohydrate in the form of glucose or sucrose tablets or as a solution provides an effective therapy; both sugars seem equivalent. Even if sucrose lumps are better recommended in terms of cost and availability, they may not be recommendable in terms of palatability. Glucose gel or orange juice cannot be recommended, at least in light of our experimental procedure and at the dosage used therein.

Adult↗

Comparative pharmacokinetics and antihypertensive effects of the nifedipine tablet and capsule.

The pharmacokinetics and antihypertensive effects of the nifedipine tablet and capsule have been examined in six male patients with diastolic pressure greater than 95 mm Hg despite metoprolol therapy. On two separate mornings, a 20 mg nifedipine tablet or 2 X 10 mg nifedipine capsules were administered with metoprolol 100 mg following a 12-h fast. Both capsule and tablet significantly reduced blood pressure (BP), with the maximum fall occurring at 45 min for the capsule and 4 h for the tablet. Two patients developed postural hypotension after the capsule and a third experienced flushing and palpitations. The maximum nifedipine plasma concentration after the capsule was 257 ng/ml compared with 50 ng/ml for the tablet, and the time of maximum concentration was significantly earlier for the capsule. Although the nifedipine capsule results in a fivefold higher maximum plasma concentration and is associated with a more rapid reduction in blood pressure than the tablet, its use may be limited by postural hypotension and other untoward symptoms.

Aged↗

[Pharmacokinetics of clarithromycin granule and tablet in children].

It has been known that clarithromycin (TE-031, A-56268), a new macrolide antibiotic (ML), achieves higher concentrations in blood, is better excreted into urine and is better distributed into various tissues than conventional MLs. We investigated the pharmacokinetics of TE-031 in children upon oral administration of the drug in the following method. TE-031 granular preparation with a potency of 100 mg/g was given to 6 boys (5 years 4 months-14 years 0 month) with dose levels of 5 mg/kg and 10 mg/kg for each 3 boys. A tablet preparation with each tablet containing 50 mg of TE-031 was administered to 4 boys and 2 girls (8 years 5 months-11 years 6 months) with dose level of 2 tablets (i.e., 100 mg) and 3 tablets (i.e., 150 mg) for each 3 children. All administrations were done at 30 minutes before meal. Then, to conduct a cross-over test, the granule preparation was given orally to the 3 children mentioned above who was given 2 tablets and the 1 of 3 cases that were given 3 tablets at the same dose levels (100 mg and 150 mg) respectively. A bioassay was used to determine concentrations in blood of active antibiotic compounds and an high performance liquid chromatography (HPLC) was used to determine unchanged TE-031 and its main metabolite, M-5. Urinary concentrations of active antibiotic compounds were also determined by the bioassay and the HPLC was used to determine concentrations and proportions of unchanged TE-031 and its metabolites, M-1, M-4, M-5, M-6 and M-7 to figure out the urinary recovery rate in the first 6 hours. The results of these experiments are summarized as follows. 1. As was mentioned above, TE-031 was administered orally to 2 groups of children at dose levels of 5 mg/kg and 10 mg/kg, respectively. Mean serum levels of total active antibiotic compounds reached their maximum in 1 and 2 hours for the 5 mg/kg and the 10 mg/kg dosage groups, respectively, at 1.28 and 3.62 micrograms/ml, respectively. Mean half lives of serum concentrations in the 2 groups were quite similar, with values of at 2.1 and 2.0 hours, respectively. Mean serum concentrations of unchanged TE-031 determined by the HPLC method reached their peaks in 1 hour after administration in either of the 5 and 10 mg/kg dosage groups at peak levels of 0.65 micrograms/ml and 2.67 micrograms/ml, respectively. Thus, dose-response relationships were observed with TE-031 and M-5.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗

Pharmaceutical development of ondansetron tablets.

Ondansetron tablets contain ondansetron base as the hydrochloride dihydrate, lactose, microcrystalline cellulose, starch and magnesium stearate. Tablets sampled at the beginning and end of the compression process have good content uniformity and drug content, showing that there is no segregation or loss of the drug substance during tabletting. The release of drug substance is related to the tablet disintegration time. Tablets with disintegration times of 3 and 10 min release 85% of the drug substance in approximately 6 and 20 min respectively. Satisfactory bioavailability has been demonstrated. The tablets have good stability, and have a shelf life of 2 years when stored below 30 degrees C.

Antiemetics↗

UV spectrophotometric determination of hydralazine hydrochloride in tablets: collaborative study.

A UV spectrophotometric method for the determination of hydralazine hydrochloride in tablets was collaboratively studied by 5 laboratories. The method is based on conversion of hydralazine to a tetrazolo [5,1-alpha]phthalazine derivative which shows an absorption maximum at about 274 nm. Each collaborator received blind duplicate samples of 2 commercial powdered composites from 10 and 100 mg tablets, and 1 synthetic tablet formulation. Each collaborator also received a set of 10 tablets for determination of content uniformity. The pooled mean recovery of hydralazine hydrochloride from the synthetic formulation was 101.2 +/- 0.94%. The mean assay values for 10 and 100 mg tablets were 95.6 +/- 0.98 and 101.0 +/- 0.73% of the declared amounts, respectively, with corresponding CV values of 1.02 and 0.73%. The pooled mean for individual tablet assay was 99.8 +/- 3.26% of the declared value, with a CV of 3.29%. The method has been adopted official first action.

Hydralazine↗