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At least 19 recordsLinked to original sources
PubMed1990

Bioavailability of doxycycline from dissolved doxycycline hydrochloride tablets--comparison to solid form hydrochloride tablets and dissolved monohydrate tablets.

Doxycycline (DC) is used either as solid form hydrochloride capsules, or as monohydrate tablets, which may be taken either as solid form tablets or dissolved in water. In this single dose (150 mg), crossover study on 15 healthy volunteers, the pharmacokinetic properties of DC from hydrochloride tablets taken either in dissolved or in solid form were compared with those observed after taking dissolved DC as a monohydrate tablet. The results of this study show that DC is absorbed rapidly (tmax 3.3-3.8 h) and with equal bioavailability (AUC values 52.9-58.5 mg/l x h) from both hydrochloride and monohydrate tablets. It can be concluded that taking the DC hydrochloride tablets in dissolved form does not affect the pharmacokinetics of DC, moreover the bioavailability of DC is comparable to that achieved after taking DC monohydrate tablets in dissolved form.

Biological Availability↗
PubMed2002

A new rapidly absorbed paracetamol tablet containing sodium bicarbonate. I. A four-way crossover study to compare the concentration-time profile of paracetamol from the new paracetamol/sodium bicarbonate tablet and a conventional paracetamol tablet in fed and fasted volunteers.

The primary objective of this four-way crossover study was to compare the concentration-time profile of paracetamol from a new rapidly absorbed paracetamol tablet containing sodium bicarbonate (PS) with a conventional paracetamol tablet (P), in a panel of 28 fed and fasted healthy volunteers. The results demonstrated that paracetamol was absorbed more rapidly from tablets containing sodium bicarbonate compared to conventional tablets, as indicated by a shorter tmax in both the fed and fasted state and a higher Cmax in the fasted state. The two formulations were bioequivalent with respect to area under curve (AUC). Food did not affect the extent of absorption from either formulation, as indicated by AUC, however, food did reduce the rate of absorption from both formulations, as indicated by a longer tmax and a lower Cmax. Metabolic activation of paracetamol to its oxidation metabolites, as assessed by combined partial clearances to subsequent secondary metabolites cysteine and mercapturic acid conjugates, indicated that the two formulations were bioequivalent in this respect.

Acetaminophen↗
PubMed1982

A comparison of the effect of combined frusemide and controlled-release potassium tablets (Diumide-K continus tablets) and frusemide and slow-K tablets in elderly patients with cardiac failure.

Serum potassium levels, weight, heart function and patient's opinion of therapy were assessed in a study comparing 40 mg of frusemide and 600 mg of controlled-release potassium chloride in a combined tablet to frusemide and potassium supplements given as separate tablets in thirty elderly patients in cardiac failure. Potassium levels were significantly higher, heart function was significantly improved and patient's opinion of therapy was better after the combined tablet therapy than both pre-trial and after the separate tablet therapy. There was no significant difference in weight reduction.

Aged↗
PubMed1999

Comparison of an orally disintegrating ondansetron tablet with the conventional ondansetron tablet for cyclophosphamide-induced emesis in cancer patients: a multicenter, double-masked study. Ondansetron Orally Disintegrating Tablet Emesis Study Group.

A total of 427 cancer patients receiving cyclophosphamide chemotherapy participated in this multicenter, double-masked, double-dummy, parallel-group, randomized study comparing the antiemetic efficacy and safety of an 8-mg conventional ondansetron tablet (OT, n = 212) taken twice daily with an 8-mg orally disintegrating ondansetron tablet (ODT, n = 215) taken twice daily for 3 days. In the primary efficacy analysis, complete or major control of emesis (0 to 2 emetic episodes) between days 1 and 3 was seen in 80% of OT and 78% of ODT patients. The 90% confidence interval for the differences between treatments was -8.6% to 4.4% (defined interval of equivalence, +/-15%), showing that the formulations were equivalent. In the secondary efficacy analysis, no significant differences were observed in the rates of complete control of emesis (no episodes of emesis) over 3 days (63% and 64% of the respective groups) and on day 1 (84% and 81%, respectively) and in the complete control of nausea over 3 days (37% and 43%, respectively) and on day 1 (59% and 61% of patients, respectively). The taste of ODT was acceptable to the majority of patients (89%) who received it. OT and ODT were both well tolerated. Thus 8 mg ODT twice daily represents a palatable, well-tolerated, and effective antiemetic treatment for the control of cyclophosphamide-induced emesis and nausea and provides equivalent treatment to OT 8 mg twice daily.

Administration, Oral↗
PubMed2003

Drug interaction of spirapril hydrochloride monohydrate and hydrochlorothiazide. A clinical study to compare the pharmacokinetics after administration of spirapril hydrochloride monohydrate tablets, hydrochlorothiazide tablets and fixed combination bi-layer tablets.

The potential influence of concomitantly administered hydrochlorothiazide (CAS 58-93-5) on the pharmacokinetics of spirapril (CAS 94841-17-5)/spiraprilat (CAS 83602-05-5) and of concomitantly administered spirapril on the pharmacokinetics of hydrochlorothiazide was investigated in an open, randomised, 3-way crossover study in 12 healthy male subjects. The test drug was a newly developed bi-layer tablet containing a fixed combination of spirapril hydrochloride monohydrate and hydrochlorothiazide (Quadroplus). The reference formulations were tablets containing solely spirapril hydrochloride monohydrate (Quadropril) or hydrochlorothiazide (produced exclusively for study medication). For spirapril, spiraprilat and hydrochlorothiazide the 90% confidence intervals of the AUC(0-infinity) as a measure for the extent of absorption were entirely included within the equivalence range of 0.8 to 1.25 and the 90% confidence intervals of the Cmax as a measure for the rate of absorption were entirely included within the extended equivalence range of 0.7 to 1.43. Therefore, bioequivalence was concluded for the test and reference formulations. The results suggest that hydrochlorothiazide does not interact in the fixed combination with the pharmacokinetics of spirapril and vice versa.

Adult↗
PubMed1991

Effects of tableting pressure on hydration kinetics of theophylline anhydrate tablets.

The effects of tableting pressure on hydration kinetics of types I and II theophylline anhydrate tablets at 95% relative humidity, 35 degrees C, have been studied by using various kinetic equations. Relations between tablet expansion and hydration were studied. Samples of 2 cm diameter tablets (1 g) were compressed at 5, 10 and 20 MPa. The hydration of types I and II tablets decreased with increased tableting pressure. The time required for 50% hydration of 2 cm diameter tablets, compressed at various pressures suggests that the tablet hydration rate was affected by the tableting pressure. Types I and II tablets expanded 11.37-16.75% in volume during hydration to the monohydrate. The thickness expansion of the tablets exceeded the diameter expansion as the tablet structure was not uniform owing to the orientation of particles during the compression. The final expansion ratio of the tablets increased with increased tableting compression pressure. The Hancock Sharp constant (m) and fitting of the kinetic data to a suitable model suggested that the hydration of theophylline anhydrate tablets followed the two-dimensional phase boundary equation (type I tablets) or the three-dimensional phase boundary equation (type II tablets).

Chemical Phenomena↗
PubMed1988

Effect of excipients on tablet properties and dissolution behavior of theophylline-tableted microcapsules under different compression forces.

Theophylline ethylcellulose microcapsules were tableted by compression with or without excipients [lactose or hydroxypropyl cellulose (HPC-H)]. Tablets without excipients had a crushing strength that was independent of the applied compression force and the particle size of the microcapsules used, but tablet thickness decreased with an increase in the particle size of the microcapsules. The dissolution characteristics of theophylline from tableted microcapsules without excipients were almost independent of the applied compression force, but showed a sustained-release behavior. However, the thickness, crushing strength, and dissolution properties of tablets containing excipients were found to be affected by the type of excipient. Tableted microcapsules containing lactose showed an increase in tablet crushing strength that correlated with an increase in the applied compression pressure, but the tablet thickness did not change. In contrast, tableted microcapsules containing HPC-H showed a decrease in tablet thickness with an increase in the applied compression pressure, but the tablet crushing strength was initially reduced and then increased with an increase in the compression force. There was a rapid release rate for theophylline from tableted microcapsules containing lactose; a zero-order release rate for theophylline was found in tableted microcapsules containing HPC-H. The insoluble compacted matrix formation, disintegration of tablet, rupture of microcapsules, and gel matrix formation may be responsible for the release behavior of theophylline-tableted microcapsules with or without excipients. The reduced surface area and porosity resulted in a prolongation of the release from tableted microcapsules compared with untableted microcapsules.

Capsules↗
PubMed2000

Absorption of effervescent paracetamol tablets relative to ordinary paracetamol tablets in healthy volunteers.

OBJECTIVES: The aim of this study was to compare the rate of absorption between ordinary paracetamol tablets and effervescent paracetamol tablets. METHODS: Twenty healthy volunteers participated in an open randomised crossover study and were given a 1000-mg dose of either ordinary paracetamol tablets (2 x 500 mg Panodil tablets, SmithKline Beecham) or effervescent paracetamol tablets (2 x 500 mg Pinex Brusetablett, Alpharma AS) with a 3-week washout period in between. Blood samples were collected for 3 h. Maximum serum concentration (Cmax) and the time to maximum serum concentration (tmax) were recorded and the area under the concentration versus time curve (AUC) was calculated. RESULTS: The mean tmax was significantly shorter when paracetamol effervescent tablets were taken (27 min) rather than ordinary paracetamol tablets (45 min) (P = 0.004). There was no significant difference between the mean Cmax of 143 micromol/l with effervescent tablets and that of 131 micromol/l with ordinary tablets. The mean AUC(0-3 h) was significantly higher with paracetamol effervescent tablets (223.8 micromol x h x l(-1)) than with ordinary tablets (198.2 micromol x h x l(-1); P = 0.003). After 15 min, 17 (85%) subjects in the effervescent group had a serum concentration of 70 micromol/l (lower therapeutic serum concentration) or higher relative to only 2 (10%) subjects in the ordinary tablet group (P = 0.001). CONCLUSION: Paracetamol effervescent tablets are absorbed significantly faster than ordinary paracetamol. Thus, effervescent tablets might offer significantly faster pain relief when paracetamol is used.

Acetaminophen↗
PubMed1999

Reduction of tablet coloration at tableting for oily medicine (tocopheryl nicotinate).

The powder (TN-PO) which adsorbed D,L-tocopheryl nicotinate (TN) as an oily medicine was prepared using porous calcium silicate (Florite(R)RE, FLR) as an adsorbing carrier. Tablets (TN-TAB) were produced by compression of TN-PO at different compression pressures. As TN-PO was compressed at the higher TN content in TN-PO and compression pressure, the more TN was exuded from TN-PO, and an increase in the degree of tablet coloration was observed. Therefore, FLR or colloidal silica (AEROSIL(R)200, AER) was newly added to TN-PO at compression to reduce the degree of tablet coloration. Further, the effects of addition of FLR or AER on the crushing strength, friability, porosity and disintegration property of the tablet and the dissolution property of TN from the tablet were studied. After addition of FLR or AER, a similar reduction of tablet coloration was observed. When the addition percentage of FLR to TN-PO exceeded 30%, the crushing strength of the tablet increased significantly. On the other hand, when TN-PO added with AER was compressed, no change was observed in the crushing strength of the tablet. The disintegration time of the tablet with added FLR was shorter than that of the tablet with added AER. At every addition percentage studied, the tablet with added FLR showed a higher releasing ability of TN compared with the tablet with added AER. These results indicate that it is possible to reduce tablet coloration by adding FLR or AER at compression of TN-PO. Further, it is considered that the differences in the crushing strength, disintegration property and dissolution property of TN between the tablets with added FLR or AER resulted in different liquid adsorbing and holding mechanisms of FLR particles and AER particles.

Antihypertensive Agents↗
PubMed1993

Salbutamol in treatment of bronchial asthma--comparison of controlled release tablet with standard tablet.

Salbutamol in controlled release tablet form was compared to salbutamol in standard tablet form for the management of patients with bronchial asthma. A total of twenty asthmatic patients enrolled in the study were classified into two groups, ten patients each, for a cross-over study. Group 1 received controlled release tablets for a 2 to 3 week period, and were then shifted to standard tablets for another similar period. Group 2 received standard tablets first and was then shifted to controlled release tablets. Patients were required to record symptom scores during therapy, including sleep disturbance, chest tightness, wheezing, cough, sputum production and inhalational bronchodilator use. Measurements of peak expiratory flow rate (PEFR) were also done, as well as record made of side effects experienced. The result showed that a lower symptom score was found in patients receiving controlled release tablets than in patients receiving standard tablets (p < 0.001 for sleep disturbance, p < 0.005 for sputum formation and p < 0.001 for total score). There was a higher PEFR in patients receiving controlled-release tablets than in patients receiving standard tablets (p < 0.001). Side effects with tremor were observed in 30% of both groups of patients with a slightly higher degree in the patients receiving standard tablets (statistically not significant). In conclusion, salbutamol of controlled release tablet form obtains a better therapeutic response than standard tablets in the management of patients with bronchial asthma.

Adult↗
PubMed2001

Efficacy, tolerability, and patient satisfaction with 50- and 100-mg sumatriptan tablets in those initially dissatisfied with the efficacy of 50-mg sumatriptan tablets.

BACKGROUND: Both 50- and 100-mg sumatriptan tablets are effective and well tolerated in the acute treatment of migraine. However, given a choice between the 2 doses, many patients in clinical practice and clinical studies prefer the 100-mg dose. OBJECTIVE: This study was designed to assess whether patients initially dissatisfied with the efficacy of 50-mg sumatriptan tablets would be satisfied with 100-mg sumatriptan tablets. METHODS: In phase 1 of the study, triptan-naive patients with migraine (International Headache Society diagnosis) received open-label treatment of 3 migraine attacks with 50-mg sumatriptan tablets. At the end of phase 1, those who were dissatisfied with the efficacy but satisfied with the tolerability of 50-mg sumatriptan tablets entered phase 2 and were randomized in a double-blind, parallel-group fashion to receive either 50- or 100-mg sumatriptan tablets for the treatment of 3 attacks. Patients who were satisfied with the efficacy or dissatisfied with the tolerability of the 50-mg tablets in phase 1 were given the option of continuing open-label treatment with 50-mg sumatriptan tablets in phase 2. The primary end point was the percentage of patients satisfied with medication at the end of phase 2 double-blind treatment. Patient satisfaction with specific medication attributes was assessed using the Patient Perception of Migraine Questionnaire. RESULTS: Seven hundred twenty-two patients were enrolled in phase 1 of the study (the intent-to-treat population), 609 of whom had evaluable satisfaction data at the end of open-label treatment. Three hundred twenty-six (54%) of these patients were satisfied with 50-mg sumatriptan tablets, whereas 283 (46%) were not satisfied. Among those who were dissatisfied, lack of efficacy was cited as the sole reason for dissatisfaction by 242 (86%). Two hundred thirty-one of those who were dissatisfied with efficacy only and wished to continue the study were randomized to double-blind treatment with either 50-mg sumatriptan tablets (n = 123; 82% female, 18% male; mean age, 37.6 years) or 100-mg sumatriptan tablets (n = 108; 86% female, 14% male; mean age, 36.0 years). The remaining 310 patients elected to continue open-label treatment with 50-mg sumatriptan tablets. At the end of double-blind treatment, 64 of 101 patients (63%) in the 100-mg group indicated that they were satisfied with treatment, compared with 55 of 113 (49%) in the 50-mg group (P = 0.031). Across the 3 attacks treated in the double-blind phase. headache relief 2 hours postdose was reported by 47% to 53% of patients in the 50-mg group and 45% to 60% of patients in the 100-mg group. The overall incidence of patients reporting > or =1 adverse event was 19% (23/123) in the 50-mg group and 22% (24/108) in the 100-mg group. CONCLUSIONS: For most patients, 50 mg is the appropriate starting dose of sumatriptan tablets. In patients who experience inadequate relief with 50 mg, increasing the dose to 100 mg is an appropriate therapeutic option.

Adult↗
PubMed2002

Comparative pharmacokinetics of lovastatin extended-release tablets and lovastatin immediate-release tablets in humans.

The pharmacokinetics of lovastatin and its active metabolite lovastatin acid was evaluated in 9 healthy subjects in a three-period crossover study following a single oral dose of lovastatin extended-release (ER) tablets and lovastatin immediate-release (IR) tablets. Participants were dosed with lovastatin IR 40 mg tablets following a standard breakfast, lovastatin ER 40 mg tablets following a standard breakfast, and lovastatin ER 40 mg tablets underfasting conditions. Serial plasma samples were collected for up to 48 hours postdose and assayed for lovastatin and lovastatin acid using a liquid chromatography/mass spectroscopy/mass spectroscopy method. Lovastatin ER tablets, unlike lovastatin IR tablets, exhibited delayed- and extended-release characteristics. The relative bioavailability, in terms of area under the curve values, of lovastatin (156%) and lovastatin acid (124%) was greater from lovastatin ER tablets as compared with lovastatin IR tablets when given with breakfast. An even greater increase in the bioavailability of lovastatin (261%) and lovastatin acid (231%) was observed when the lovastatin ER tablets were administered under fasting conditions. Thus, greater gastrointestinal tract drug absorption of lovastatin from lovastatin ER tablets was demonstrated. Ingestion of a standard breakfast prior to administration of lovastatin ER tablets decreased absorption of lovastatin by approximately 40%, relative to lovastatin ER tablets under fasting conditions.

Adult↗
PubMed2002

Application of fluidized hot-melt granulation (FHMG) for the preparation of granules for tableting; properties of granules and tablets prepared by FHMG.

The objective of this study was to investigate the properties of granules and tablets prepared by a novel Fluidized Hot-Melt Granulation (FHMG) technique. Macrogol 6000 (polyethylene glycol 6000, PEG 6000), macrogol 20000 (polyethylene glycol 20000, PEG 20000), and glyceryl monostearate (GMS) were used as binders with different levels of viscosity and water solubility. The properties of both granules and tablets were compared with those obtained using the Standard Tablet Formulation (STF, lactose/corn starch/hydroxypropylcellulose/ magnesium stearate: 66/30/3.5/0.5) for fluidized-bed granulation, which is widely used for wet granulation. To obtain suitable flowability as granules for tabletting, the content of the melting material should be approximately 10 w/w%. The rate of increase in the mean diameter of the granules during FHMG was affected by both the melting temperature and the viscosity of the melting material used in the granules. The compression properties of granules prepared by FHMG were also investigated, demonstrating that these granules had a high pressure transmittance. The hardness and the disintegration time of tablets obtained from granules prepared by FHMG were influenced by the properties of the melting material, such as its compaction behavior, solubility, and wettability. No significant differences of hardness were observed when compared to STF tablets. Tablets prepared from FHMG granules disintegrated within 15 min, whereas the STF tablets showed faster disintegration. It was also demonstrated that the hardness and disintegration time of tablets prepared from FHMG granules were not affected by the tablet porosity. Therefore, tablets with a constant quality may be obtainable under a wide range of compression forces. The results of this study suggested that FHMG is a useful method of preparing granules for tableting without using any solvents or water.

Drug Compounding↗
PubMed2001

Assessing tablet bond types from structural features that affect tablet tensile strength.

PURPOSE: The aim of this article was to study the possibility of assessing the structural features affecting tablet tensile strength to obtain information on the dominating bond types, i.e. interparticulate attractions, in tablets. METHODS: The features of the internal tablet structure considered to be important for tablet tensile strength were assessed using a simple tablet model for tablets made from seven materials: potassium chloride, sodium chloride, sodium bicarbonate, lactose, sucrose, microcrystalline cellulose, and ascorbic acid. RESULTS: Tablet porosity and particle size (measured as external specific surface area by permeametry) were the structural features that best correlated with tablet tensile strength. These features were described by a "structural factor," which was combined with tablet tensile strength, as an "interaction factor," to reflect the dominating bond types in tablets. CONCLUSION: The qualitative results gave dominating bond types in the tablets studied that matched the results of earlier studies, thus supporting the applicability of the method.

Models, Chemical↗
PubMed2002

Investigation of the effect of tablet surface area/volume on drug release from hydroxypropylmethylcellulose controlled-release matrix tablets.

The purpose of this study was to investigate the influence of tablet surface area/volume (SA/Vol) on drug release from controlled-release matrix tablets containing hydroxypropylmethylcellulose (HPMC). Soluble drugs (promethazine HCl, diphenhydramine HCl, and propranolol HCl) were utilized in this study to give predominantly diffusion-controlled release. Drug release from HPMC matrix tablets with similar values of SA/Vol was comparable within the same tablet shape (i.e., flat-faced round tablets) and among different shapes (i.e., oval, round concave, flat-faced beveled-edge, and flat-faced round tablets). Tablets having the same surface area but different SA/Vol values did not result in similar drug release; tablets with larger SA/Vol values hadfaster release profiles. Utility of SA/Vol to affect drug release was demonstrated by changing drug doses, and altering tablet shape to adjust SA/Vol. When SA/Vol was held constant, similar release profiles were obtained with f2 metric values greater than 70. Thus, surface area/volume is one of the key variables in controlling drug release from HPMC matrix tablets. Proper use of this variable has practical application by formulators who may need to duplicate drug release profiles from tablets of different sizes and different shapes.

Delayed-Action Preparations↗
PubMed2003

Hydroxypropyl methylcellulose based cephalexin extended release tablets: influence of tablet formulation, hardness and storage on in vitro release kinetics.

The object of this study was to develop hydroxypropyl methylcellulose (HPMC) based cephalexin extended release tablet, which can release the drug for six hours in predetermined rate. Twenty-one batches of cephalexin tablets were prepared by changing various physical and chemical parameters, in order to get required theoretical release profile. The influences of HPMC, microcrystalline cellulose powder (MCCP), granulation technique, wetting agent and tablet hardness on cephalexin release from HPMC based extended release tablets were studied. The formulated tablets were also characterized by physical and chemical parameters. The dissolution results showed that a higher amount of HPMC in tablet composition resulted in reduced drug release. Addition of MCCP resulted in faster drug release. Tablets prepared by dry granulation was released the drug slowly than the same prepared with a wet granulation technique. Addition of wetting agent in the tablets prepared with dry granulation technique showed slower release. An increase in tablet hardness resulted in faster drug release. Tablets prepared with a wet granulation technique and having a composition of 9.3% w/w HPMC with a hardness of 10-12 kg/cm(2) gave predicted release for 6 h. The in vitro release data was well fit in to Higuchi and Korsmeyer-Peppas model. Physical and chemical parameters of all formulated tablets were within acceptable limits. One batch among formulated twenty-one batches was successful and showed required theoretical release. The effect of storage on in vitro release and physicochemical parameters of successful batch was studied and was found to be in acceptable limits.

Cephalexin↗
PubMed1989

The United States experience with oral controlled-release morphine (MS Contin tablets). Parts I and II. Review of nine dose titration studies and clinical pharmacology of 15-mg, 30-mg, 60-mg, and 100-mg tablet strengths in normal subjects.

The results of nine US multicenter, sequential crossover, dose titration studies of controlled-release oral morphine (MS Contin 30 mg tablets [MSC], Purdue Frederick, Norwalk, CT) are reviewed in Part I. The studies demonstrated the prolonged analgesic efficacy of the preparation in the treatment of patients with moderate to severe cancer-related pain. Approximately 93% of the patients achieved satisfactory to excellent analgesia on a 12-hour regimen when appropriate dose titration was allowed. The remaining patients were successfully maintained on an 8-hour regimen. The preparation was well-tolerated and comparable in safety to immediate-release oral morphine. In global evaluations, MSC was judged to be significantly (P less than 0.05) more effective, and with significantly (P less than 0.05) fewer side effects than both the prestudy opioid analgesics and 4-hour immediate-release oral morphine. Patients had a broad range of morphine requirements (mean daily MSC dose, 240 mg; range, 60 mg/day to 1800 mg/day); therefore various MSC tablet strengths were developed. Part II presents three studies in which the MSC formulations (15-mg, 60-mg, and 100-mg tablets) were compared to the 30-mg tablet within three randomized, single-dose, two-way crossover, analytically blinded bioavailability protocols, to determine bioequivalence and dose proportionality. The maximum morphine concentration, time of maximum morphine concentration, and area under the plasma morphine versus 12-hour and 24-hour time curve (AUC 0.12; AUC 0.24) were determined in each study. There were no significant differences between the values associated with MSC 1 X 30 mg tablet and 2 X 15 mg tablets (study 1), MSC 2 X 30 mg tablets and 1 X 60 mg tablet (study 2), and MSC 3 X 30 mg tablets and 1 X 100 mg tablet (study 3, values adjusted to dose of 90 mg), except for one marginally significant difference in study 3 (AUC 0.24; P = 0.04) which was not clinically or biopharmaceutically significant. The results showed that MSC 15-mg, 30-mg, 60-mg, and 100-mg dosage strengths are bioequivalent and dose proportional, and, therefore, therapeutically interchangeable. It was concluded that with routine assessment of the patient and adherence to the principles of analgesic dosing, MSC can be successfully used to control cancer-related pain. Furthermore, the availability of various MSC tablet strengths can be expected to facilitate the analgesic management of a patient population with widely differing opioid requirements.

Administration, Oral↗
PubMed2002

A double-blind, single-dose comparison of the analgesic efficacy of tramadol/acetaminophen combination tablets, hydrocodone/acetaminophen combination tablets, and placebo after oral surgery.

BACKGROUND: Improved clinical outcomes have been documented with combinations of oral analgesic agents, particularly those with complementary activities. However, because not all combinations or dose ratios lead to enhanced analgesia or reduced adverse events (AEs), each combination and dose ratio must be evaluated individually in carefully designed preclinical and clinical trials. OBJECTIVE: The goal of the study was to compare the efficacy and safety of 37.5 mg tramadol/325 mg acetaminophen tablets (T/APAP), 10 mg hydrocodone bitartrate/650 mg acetaminophen tablets (HC/APAP), and placebo in the treatment of postoperative dental pain. METHODS: This was a single-center, double-blind, parallel-group, placebo- and active-controlled study in adults with at least moderate pain (score > or =50 on a 100-mm pain visual analog scale) after extraction of > or =2 impacted third molars. Patients were randomized to receive 1 or 2 T/APAP tablets, 1 HC/APAP tablet, or placebo. Scores for hourly pain relief (PAR), pain intensity difference (PID), and combined PAR and PID (PRID) were based on reported pain at 30 minutes and each successive hour for 8 hours. Primary efficacy measures were summary pain intensity and pain relief scores (total pain relief [TOTPAR], sum of pain intensity differences [SPID], and sum of pain relief and pain intensity differences [SPRIDI) for 0 to 4 hours, 4 to 8 hours, and 0 to 8 hours. Secondary efficacy measures were hourly PAR, PID, and PRID scores; onset and duration of pain relief; time to remedication with a supplemental analgesic agent; and patients' overall assessment of medication. RESULTS: Two hundred adults took part in the study (50 per treatment group) and were included in the efficacy and safety analyses. T/APAP 75/650 mg and HC/APAP were statistically superior to placebo on the primary efficacy measures of TOTPAR, SPID, and SPRID (P < or = 0.024), as well as on hourly PAR, PID, and PRID over 6 hours (P < or = 0.045). All active treatments were statistically superior to placebo in terms of onset of pain relief (P < or = 0.001), duration of pain relief (P < or = 0.024), time to remedication (P < 0.001), and patients' overall assessment of medication (P < 0.001). A statistically significant dose response with T/APAP (2 tablets > 1 tablet > placebo) was seen for TOTPAR, SPID, and SPRID (all, P < or = 0.018). The median time to onset of pain relief was approximately 34.0 minutes with 2 T/APAP tablets and 25.4 minutes with HC/APAP. Although the median time to onset of pain relief was shorter with HC/APAP, two T/APAP tablets had comparable efficacy to HC/APAP. The median time to remedication with a supplemental analgesic agent was 169.0 minutes in the T/APAP 75/650 mg group and 204.0 minutes in the HC/APAP group. However, the duration of pain relief, as defined by time to remedication, was not significantly different between these 2 groups. The overall incidence of AEs was lower with T/APAP (0% treatment-related AEs) than with HC/APAP (4%) or placebo (10%). The incidence of nausea (18% T/APAP, 36% HC/APAP) and vomiting (12% T/APAP, 30% HC/APAP) was approximately 50% lower with 2 T/APAP tablets than with HC/APAP (P < 0.05). CONCLUSIONS: T/APAP tablets provided effective, rapid (< or = 34 minutes), dose-dependent analgesia for the treatment of postoperative dental pain. Two T/APAP tablets provided analgesia comparable to that provided by HC/APAP with better tolerability.

Acetaminophen↗