betadex and piroxicam-beta-cyclodextrin

betadex has been researched along with piroxicam-beta-cyclodextrin* in 26 studies

Reviews

5 review(s) available for betadex and piroxicam-beta-cyclodextrin

ArticleYear
Piroxicam-β-cyclodextrin: a GI safer piroxicam.
    Current medicinal chemistry, 2013, Volume: 20, Issue:19

    Although NSAIDs are very effective drugs, their use is associated with a broad spectrum of adverse reactions in the liver, kidney, cardiovascular (CV) system, skin and gut. Gastrointestinal (GI) side effects are the most common and constitute a wide clinical spectrum ranging from dyspepsia, heartburn and abdominal discomfort to more serious events such as peptic ulcer with life-threatening complications of bleeding and perforation. The appreciation that CV risk is also increased further complicates the choices of physicians prescribing anti-inflammatory therapy. Despite prevention strategies should be implemented in patients at risk, gastroprotection is often underused and adherence to treatment is generally poor. A more appealing approach would be therefore to develop drugs that are devoid of or have reduced GI toxicity. Gastro- duodenal mucosa possesses many defensive mechanisms and NSAIDs have a deleterious effect on most of them. This results in a mucosa less able to cope with even a reduced acid load. NSAIDs cause gastro-duodenal damage, by two main mechanisms: a physiochemical disruption of the gastric mucosal barrier and systemic inhibition of gastric mucosal protection, through inhibition of cyclooxygenase (COX, PG endoperoxide G/H synthase) activity of the GI mucosa. However, against a background of COX inhibition by anti-inflammatory doses of NSAIDs, their physicochemical properties, in particular their acidity, underlie the topical effect leading to short-term damage. It has been shown that esterification of acidic NSAIDs suppresses their gastrotoxicity without adversely affecting anti-inflammatory activity. Another way to develop NSAIDs with better GI tolerability is to complex these molecules with cyclodextrins (CDs), giving rise to so-called "inclusion complexes" that can have physical, chemical and biological properties very different from either those of the drug or the cyclodextrin. Complexation of NSAIDs with β-cyclodextrin potentially leads to a more rapid onset of action after oral administration and improved GI tolerability because of minimization of the drug gastric effects. One such drug, piroxicam-β-cyclodextrin (PBC), has been used in Europe for 25 years. Preclinical and clinical pharmacology of PBC do show that the β-cyclodextrin inclusion complex of piroxicam is better tolerated from the upper GI tract than free piroxicam, while retaining all the analgesic and anti-inflammatory properties of the parent compound. In addition, the

    Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Dysmenorrhea; Female; Gastrointestinal Tract; Humans; Models, Molecular; Musculoskeletal Diseases; Pain; Piroxicam

2013
Piroxicam-beta-cyclodextrin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in rheumatic diseases and pain states.
    Drugs, 1994, Volume: 48, Issue:6

    Piroxicam-beta-cyclodextrin is a complex of the established nonsteroidal antiinflammatory drug (NSAID) piroxicam and an inert cyclic macromolecule, beta-cyclodextrin. In clinical trials in patients with rheumatic diseases or pain arising from other conditions, it was as effective an analgesic as standard piroxicam, and showed a faster onset of action on the first day of treatment. In short term pharmacodynamic studies in healthy volunteers, piroxicam-beta-cyclodextrin was equivalent to or tended to show less gastrointestinal mucosal toxicity than standard piroxicam, as assessed by endoscopy and faecal blood loss. However, no data are available on its comparative gastrointestinal mucosal effects from long term clinical trials using similar measures. Preliminary findings from a clinical study suggest piroxicam-beta-cyclodextrin caused fewer gastroduodenal lesions than tenoxicam. As with other NSAIDs, the majority of adverse events associated with piroxicam-beta-cyclodextrin in clinical trials were gastrointestinal in origin, with epigastric pain, heartburn and nausea the most common. Thus, piroxicam-beta-cyclodextrin is an effective agent in patients with rheumatic diseases or other pain states. When rapid analgesia is required in the initial treatment of acute pain, the faster onset of action of piroxicam-beta-cyclodextrin may be an advantage over the parent compound; however, this is unlikely to be important during long term therapy. The results of further long term trials are awaited before firm conclusions can be reached regarding the gastrointestinal tolerability of piroxicam-beta-cyclodextrin compared with that of standard piroxicam and other NSAIDs.

    Topics: Anti-Inflammatory Agents, Non-Steroidal; Arthritis; beta-Cyclodextrins; Cyclodextrins; Drug Combinations; Gastrointestinal Diseases; Humans; Piroxicam; Randomized Controlled Trials as Topic; Rheumatic Diseases

1994
Effects of piroxicam-beta-cyclodextrin on the gastrointestinal tract.
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    Piroxicam-beta-cyclodextrin (PBC), a complex of piroxicam with beta-cyclodextrin, was developed with the aim of improving the hydrosolubility and bioavailability of piroxicam. The complex is more rapidly absorbed, with a consequent reduction in the time of contact of piroxicam with the gastric and duodenal mucosa. It is hoped that the shorter contact time might reduce the local toxicity of piroxicam, but it is also possible that transiently higher local concentrations of the drug might worsen the injury to the gastro-duodenal mucosa. Four studies have been conducted in healthy volunteers in order to investigate the effects of PBC on the gastro-intestinal tract. In 3 of these trials, all of similar design, PBC (containing 20 mg of piroxicam) was compared with piroxicam 20mg and placebo given once daily with assessment of faecal blood loss using the 51Cr-labelled red-cell technique, and endoscopic appearance of gastroduodenal mucosa before and after 28 consecutive days of treatment. One study showed a significant difference in respect of faecal blood loss towards the end of the 4-week study period favouring PBC over piroxicam, while the 2 others showed comparable but non-significant trends in favour of PBC. In a fourth study, 32 non-patient volunteers received either piroxicam 20mg once daily; PBC 20mg equivalence; indomethacin 50mg twice daily; or placebo. The treatment was given double blind for 14 days. Endoscopy was performed and gastric potential differences were measured by neutral observers before and at the end of treatment. There were no significant differences in the endoscopic scores between the active treatment groups. The gastric potential difference showed greater changes with indomethacin and piroxicam than with placebo and PBC.(ABSTRACT TRUNCATED AT 250 WORDS)

    Topics: Administration, Oral; Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Controlled Clinical Trials as Topic; Cyclodextrins; Digestive System; Double-Blind Method; Drug Combinations; Female; Gastrointestinal Hemorrhage; Gastroscopy; Humans; Indomethacin; Male; Middle Aged; Piroxicam

1993
Piroxicam-beta-cyclodextrin in the treatment of acute pain of rheumatic disease.
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    Analgesics continue to be the mainstay of therapy in osteoarthritis. Non-steroidal anti-inflammatory drugs (NSAIDs) play an important role, particularly where there is a significant inflammatory component to the osteoarthritis. Piroxicam-beta-cyclodextrin (PBC) is a new formulation in which piroxicam has been complexed with beta-cyclodextrin, a cyclic oligosaccharide. This results in an increase in the rate of absorption of the active compound and, consequently, in an earlier onset of analgesic action. PBC, like piroxicam, is administered once daily. PBC has been used in the treatment of osteoarthritis. In comparison with piroxicam, PBC showed a more rapid analgesic-anti-inflammatory action after the first administration in patients with active osteoarthritis. Subsequent evaluations at the second, fifth and last day of treatment demonstrated a comparable efficacy of the two drugs. The efficacy and tolerability of PBC was compared with other NSAIDs given intramuscularly, such as diclofenac and ketoprofen. The three compounds provided marked pain relief within thirty minutes and this increased progressively until the third to fourth hour. The efficacy of oral PBC was comparable to that of intramuscular diclofenac or ketoprofen. In comparison with metamisole PBC achieved a more rapid and sustained reduction in pain intensity during the first twelve hours of treatment. This rapid and marked reduction in pain intensity with PBC was also observed in patients with low-back pain when compared with etodolac. In view of its efficacy, tolerability and rapid onset of action, piroxicam-beta-cyclodextrin appears to be an useful analgesic and a prominent progress in the treatment of acute rheumatic pain.

    Topics: Acute Disease; Adult; beta-Cyclodextrins; Controlled Clinical Trials as Topic; Cyclodextrins; Diclofenac; Dipyrone; Drug Combinations; Etodolac; Humans; Ketoprofen; Middle Aged; Pain; Piroxicam; Rheumatic Diseases

1993
Supermolecular inclusion of piroxicam with beta-cyclodextrin: a review of its pharmacological properties in laboratory animals.
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    Piroxicam-beta-cyclodextrin is a novel NSAID; it is a supermolecular inclusion complex designed to improve the risk:benefit ratio of piroxicam. In animal studies it has been shown to be as effective as piroxicam as an anti-inflammatory and analgesic agent but with a more rapid onset of action and reduced gastropathic effects.

    Topics: Administration, Oral; Animals; beta-Cyclodextrins; Cyclodextrins; Digestive System; Drug Combinations; Female; Inflammation; Male; Pain; Piroxicam

1993

Trials

13 trial(s) available for betadex and piroxicam-beta-cyclodextrin

ArticleYear
Evaluation of piroxicam-beta-cyclodextrin as a preemptive analgesic in functional endoscopic sinus surgery.
    Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas, 2010, Volume: 43, Issue:8

    The preemptive analgesic efficacy and adverse effects of preoperatively administered piroxicam-beta-cyclodextrin for post-endoscopic sinus surgery pain was determined in a prospective, double-blind, randomized, clinical study. Seventy-five American Society of Anesthesiologists status I-II patients, aged 18-65 years, were divided into three groups with similar demographic characteristics: group 1 received 20 mg piroxicam-beta-cyclodextrin, group 2 received 40 mg piroxicam-beta-cyclodextrin and group 3 received placebo orally before induction of general anesthesia. A blinded observer recorded the incidence and severity of pain at admission to the post-anesthesia care unit (PACU), at 15, 30, and 45 min in the PACU, and 1, 2, 4, 6, and 24 h postoperatively. All patients received patient-controlled morphine analgesia during the postoperative period and consumption was recorded for 24 h. During the PACU period, mean visual analogue scale values were significantly lower in groups 1 and 2 compared to group 3 (P < 0.05). During the postoperative period, morphine consumption was 3.03 +/- 2.54, 2.7 +/- 2.8, and 5.56 +/- 3.12 mg for each group, respectively (P < 0.05). As a side effect, bleeding was observed in groups 1 and 3, nausea and vomiting in all groups, and edema only in group 3. However, no significant differences were detected in any of the parameters analyzed, which also included epigastric pain, constipation/diarrhea and headache. Similar hematological test results were obtained for all groups. Preemptive administration of piroxicam-beta-cyclodextrin effectively reduced analgesic consumption, and 40 mg of the drug was more effective than 20 mg piroxicam-beta-cyclodextrin without side effects during the postoperative period.

    Topics: Adolescent; Adult; Aged; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Dose-Response Relationship, Drug; Double-Blind Method; Endoscopy; Female; Humans; Male; Middle Aged; Pain Measurement; Pain, Postoperative; Piroxicam; Preoperative Care; Prospective Studies; Sinusitis; Young Adult

2010
Effects of piroxicam-beta-cyclodextrin sachets on abnormal postural sway in patients with chronic low back pain.
    Journal of clinical pharmacy and therapeutics, 2008, Volume: 33, Issue:5

    The clinical effects of piroxicam-beta-cyclodextrin (PBC) in sachet form have been surveyed in patients with osteoarthritic or acute pain in western countries, but scarcely studied in those with chronic low back pain (LBP), and never investigated in the field of postural sway. The aim of this study was to evaluate the clinical effects of PBC in sachet form prescribed in patients with chronic backache in local Asian when compared with those of plain piroxicam.. After randomized allocation and experimental exclusion, a total of 42 eligible patients were randomized into two groups, the sachet group (n = 23) and the piroxicam tablet group (n = 19). Both groups were administered the same dosage, orally per day (daily dose = 20 mg). The duration of trial was 28 days. Efficacy was assessed with pain score, disability index and postural sway.. The patients in sachet group showed greater improvement in pain score and disability index than those who took piroxicam tablets. There were significantly lower sway velocity and intensity at almost all different conditions than baseline profiles in both groups (P < 0.05). However, there was no significant difference of sway velocity and intensity in the piroxicam tablets group with regard to eyes open or eyes closed in 20 degrees dorsiflexion.. Piroxicam-beta-cyclodextrin (PBC) sachet may have greater improvement in the treatment of chronic LBP and possess the extended effects on postural abnormality relevant to chronic LBP.

    Topics: Administration, Oral; Adolescent; Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Chronic Disease; Dosage Forms; Drug Combinations; Female; Humans; Low Back Pain; Male; Middle Aged; Pain Measurement; Piroxicam; Postural Balance; Tablets; Young Adult

2008
Efficacy and tolerability of piroxicam-beta-cyclodextrin in the outpatient management of chronic back pain.
    Bratislavske lekarske listy, 2002, Volume: 103, Issue:12

    Piroxicam-beta-cyclodextrin (PBC) is the first nonsteroidal anti-inflammatory drug (NSAID), in which the active substance is complexed with the cyclic oligosaccharide cyclodextrin, which acts as an artificial receptor. This complex allows single molecules of the NSAID to be released adjacent to the gastrointestinal mucosa, instead of crystals. Since the piroxicam is immediately bioavailable in this formulation, the onset of action is similar to that of a parenteral drug. Since the time contact with gastric mucosa is reduced, the risk of direct-contact gastric irritation is also reduced. There is good evidence that PBC is beneficial in managing acute non-specific back pain (BP) but sufficient evidence on chronic BP is lacking.. Thirty-one eligible patients aged 18-85 years, resistant to previous therapy with different NSAIDs, were treated with PBC 20 mg once daily in a 40-day open-label noncomparative study. The patients experienced chronic BP defined as pain between the occipital region and gluteal fold, lasting for at least 6 weeks but not more than 6 months. Efficacy was assessed by changes in pain intensity, paravertebral tonus, functional impairment and morning stiffness using a 4-point numerical rating scale. Patients also self-assessed nocturnal and diurnal pain using the visual analogue scale. Tolerability was assessed by adverse events and routine laboratory evaluations. Global assessment of efficacy and tolerability by physician and patients was performed at the last visit.. Using intention-to-treat analysis, all efficacy assessments demonstrated statistically significant improvements over baseline at each follow-up. 90.3% of the patients evaluated the efficacy of PBC as improved or greatly improved, and investigators rated the treatment as improved or greatly improved in 87.1% of patients. Remission was achieved in 19.3% of the patients. Tolerability was also rated highly, with 83.9% of the patients characterizing PBC treatment as good or very good, and the investigators rated the treatment as good or excellent in 87.1% of the patients. Drug related adverse events were reported in 9.7% of patients and prompted discontinuation of the study medication in 3.2% of patients. No serious adverse events were reported.. These results suggest that the newly developed dosage form of piroxicam is effective and well tolerated in the treatment of patients with chronic BP. Thus, PBC, may be an important new treatment option in this condition. (Tab. 3, Fig. 3, Ref. 36.).

    Topics: Adolescent; Adult; Aged; Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Back Pain; beta-Cyclodextrins; Chronic Disease; Cyclodextrins; Drug Combinations; Female; Humans; Male; Middle Aged; Piroxicam

2002
Piroxicam concentrations in plasma and synovial fluid after a single dose of piroxicam-beta-cyclodextrin.
    International journal of clinical pharmacology and therapeutics, 2001, Volume: 39, Issue:1

    The efficacy of nonsteroidal anti-inflammatory drugs (NSAIDs) in rheumatic diseases depends on their concentrations within the joint. We determined piroxicam concentrations in plasma and synovial fluid (SF) after a single oral dose of 20 mg in the form of one tablet of piroxicam-beta-cyclodextrin.. 45 patients, aged 21 to 84 years, presenting with an effusion of the knee, related to degenerative or inflammatory joint disease, were included in this study after having given their written consent. One blood and one SF sample were drawn concomitantly in each patient from 0.5 to 48 h after NSAID administration. Piroxicam assays were performed by high performance liquid chromatography. Pharmacokinetic parameters were obtained from the mean plasma and synovial concentrations measured at various sampling times.. The peak concentration was higher in plasma (2.51+/-0.25 microg/ml) than in SF (1.31+/-0.76 microg/ml), but the elimination half-life was much longer in SF (90.7 h) than in plasma (32.5 h). The SF/plasma area under the concentration-time curve ratio (evaluating the quantity of NSAID transferred from the blood to the joint) was equal to 0.39.. Piroxicam contained in piroxicam-beta-cyclodextrin diffused well into the SF where its pharmacokinetic profile corresponded to that of a long half-life NSAID.

    Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Area Under Curve; Arthritis, Rheumatoid; beta-Cyclodextrins; Cyclodextrins; Drug Combinations; Female; Half-Life; Humans; Joint Diseases; Knee Joint; Male; Middle Aged; Piroxicam; Synovial Fluid

2001
Comparative population pharmacokinetic-pharmacodynamic analysis for piroxicam-beta-cyclodextrin and piroxicam.
    Journal of clinical pharmacology, 2000, Volume: 40, Issue:11

    Piroxicam (Feldene) is indicated for osteoarthritis and rheumatoid arthritis but not analgesia due to its delayed onset of pain relief. Piroxicam-beta-cyclodextrin (PBCD) was developed for pain indication by virtue of the increased absorption rate of piroxicam. Forty-eight patients received a single dose of PBCD or Feldene (10, 20, and 40 mg) in a randomized study, and piroxicam plasma concentration and pain relief were measured. The purpose of the study was to investigate the PK-PD relationship of piroxicam, determine the optimal dose, and evaluate the effect of increased absorption rate on analgesic effect of piroxicam for the pain model studied. The pharmacokinetic data were best described by a two-compartment model with first-order absorption. The absorption rate of PBCD (5/h) was faster than Feldene (1.41/h). Pain relief was found to be increasing with drug concentration in a hypothetical effect compartment (Emax model). The estimated half-life of the equilibration between plasma and effect site was about 2.34 hours. Monte Carlo simulation showed that the time when at least 50% of the patients have a 75% probability of achieving meaningful pain relief (pain intensity difference (PID > or = 1) for PBCD and Feldene at a dose of 20 mg was about 0.5 and 1.5 hours, respectively. PBCD demonstrated an advantage with an onset of pain relief 1 hour earlier than Feldene.

    Topics: Absorption; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Cyclodextrins; Dose-Response Relationship, Drug; Drug Combinations; Half-Life; Humans; Pain; Piroxicam

2000
Oral bioavailability of CHF1194, an inclusion complex of piroxicam and beta-cyclodextrin, in healthy subjects under single dose and steady-state conditions.
    European journal of clinical pharmacology, 1995, Volume: 47, Issue:6

    CHF1194 is an inclusion complex of beta-cyclodextrin with the nonsteroidal anti-inflammatory drug piroxicam. In man, beta-cyclodextrin acts as a carrier of piroxicam. As the inclusion complex of piroxicam-beta-cyclodextrin is wettable and more water soluble, the absorption rate of the drug is increased whilst its other pharmacokinetic characteristics remain unchanged. The aim of the present study in 12 healthy subjects was to compare the oral bioavailability of 20 mg piroxicam in a CHF1194 tablet and a plain piroxicam capsule after a single dose and after two weeks of once daily administration, and also to assess the plasma levels and urinary excretion of beta-cyclodextrin after CHF1194 administration. The two treatments were administered in cross-over fashion, separated by a wash-out period of three weeks. Piroxicam, 5'-hydroxypiroxicam and beta-cyclodextrin were monitored in plasma and urine for 120 h after the first and last doses. Clinical tolerance was excellent and no adverse event occurred during either phase of the study. The extent of absorption of piroxicam from the CHF1194 tablet after the single dose was equivalent to that after the plain piroxicam capsule, within confidence limits of less than 80-125%. After repeated dosing, CHF1194 yielded the same steady-state systemic concentrations of piroxicam and 5'-hydroxypiroxicam as the reference capsule, and similar excretion pattern of the metabolite. After both single and multiple dosing, piroxicam was absorbed more rapidly after CHF1194, an expected consequence of the complexation of piroxicam with beta-cyclodextrin.(ABSTRACT TRUNCATED AT 250 WORDS)

    Topics: Administration, Oral; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Biological Availability; Cross-Over Studies; Cyclodextrins; Drug Combinations; Female; Humans; Male; Piroxicam

1995
Evaluation of piroxicam-beta-cyclodextrin, piroxicam, paracetamol and placebo in post-operative oral surgery pain.
    International journal of clinical pharmacology research, 1994, Volume: 14, Issue:5-6

    Two hundred ninety-eight patients with post-operative pain after the surgical removal of an impacted third molar were randomly assigned, on a double-blind basis, to receive a single oral dose of piroxicam 20 mg, or piroxicam-beta-cyclodextrin equivalent to 20 mg piroxicam, or paracetamol 500 mg, or placebo. Using a semi-quantitative self-rating scale, patients rated their pain and its relief at 30-min intervals for the first 2 h, and then hourly for 4 h after treatment administration. All active medications were reported to be significantly superior to placebo. The three active drugs were comparable for the degree of analgesia up to the third hour, after which the effect of paracetamol decreased significantly as compared to piroxicam-beta-cyclodextrin and piroxicam. Piroxicam-beta-cyclodextrin and paracetamol were more rapid than piroxicam in inducing analgesia. The tolerability for the active drugs was comparable to that for placebo.

    Topics: Acetaminophen; Adolescent; Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Cyclodextrins; Double-Blind Method; Drug Combinations; Female; Food Additives; Humans; Male; Middle Aged; Molar, Third; Pain, Postoperative; Piroxicam; Surgery, Oral; Surveys and Questionnaires; Tooth Extraction

1994
Interrelationships between Helicobacter pylori infection, nonsteroidal antiinflammatory drugs and gastroduodenal disease. A prospective study in healthy volunteers.
    Digestive diseases and sciences, 1994, Volume: 39, Issue:5

    Helicobacter pylori and nonsteroidal antiinflammatory drugs independently cause gastroduodenal mucosal injury but the relationship between them remains unclear. We have performed a double-blind, parallel-group, placebo-controlled prospective study in 77 healthy volunteers aged 19-35 years who were randomly allocated to indomethacin (N = 15), one of three oxicams (piroxicam, chlortenoxicam, or CHF 1194; N = 36), or placebo (N = 26). Esophagogastroduodenoscopy was performed before and after four weeks of treatment and the mucosal appearances graded. Colonization with H. pylori was established at each endoscopy and gastrointestinal symptoms were assessed by daily diary card. Seven subjects (9%) were positive for H. pylori before treatment (one placebo, one indomethacin, and five an oxicam); their H. pylori status remained unchanged. Two of 70 H. pylori-negative subjects became H. pylori-positive (2.9%), both of whom had received placebo. The endoscopic score deteriorated in 1/6 drug-treated H. pylori-positive subjects and in 0/1 taking placebo. Of the H. pylori-negative subjects whose endoscopic score deteriorated, three (13%) were taking placebo, four (28.6%) indomethacin, and eight (25.8%) an oxicam. Upper gastrointestinal symptoms were reported in eight (30.8%) of the subjects taking placebo (one subject negative for H. pylori became positive), eight (53.3%) indomethacin (one H. pylori-positive), and 10 (27.8%) an oxicam (one H. pylori-positive). There were no statistically significant differences between the H. pylori-negative and H. pylori-positive groups whether on drug or placebo.(ABSTRACT TRUNCATED AT 250 WORDS)

    Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Cyclodextrins; Double-Blind Method; Drug Combinations; Dyspepsia; Endoscopy, Gastrointestinal; Gastric Mucosa; Gastrointestinal Diseases; Helicobacter Infections; Helicobacter pylori; Humans; Indomethacin; Male; Piroxicam; Prospective Studies

1994
Supermolecular inclusion of piroxicam with beta-cyclodextrin: pharmacokinetic properties in man.
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    Piroxicam beta-cyclodextrin is a novel inclusion complex in which the piroxicam molecule has higher wettability and faster dissolution characteristics than plain piroxicam. Pharmacokinetic studies comparing piroxicam beta-cyclodextrin with plain piroxicam have been carried out in both patients and healthy subjects. The absorption rate of piroxicam from the complex, determined using tmax, absorption rate constant (Ka) and plasma concentrations at 15 min and 30 min post-dose, is considerably faster than that for plain piroxicam. This difference, that can be demonstrated with both tablet and sachet formulations, is still present during repeated dose administration and when the drugs are administered after food. After absorption from piroxicam beta-cyclodextrin formulations, the kinetic disposition of piroxicam and bioavailability parameters are identical to those for plain piroxicam. The more rapid rise in piroxicam plasma concentrations and the reduced contact time of piroxicam in the upper gastrointestinal-tract may be reasons for the reduced incidence of gastrointestinal complaints and gastrointestinal bleeding and the rapid attainment of pain relief with piroxicam beta-cyclodextrin. The most rapid relief of pain will be achieved using piroxicam beta-cyclodextrin sachets administered in the fasting state, since piroxicam is immediately bioavailable in this formulation and the onset of action is similar to that for injectable piroxicam.

    Topics: Absorption; Administration, Oral; Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Cross-Over Studies; Cyclodextrins; Digestive System; Drug Combinations; Female; Follow-Up Studies; Food; Humans; Male; Molecular Structure; Piroxicam

1993
Rheumatic diseases--clinical experience with piroxicam-beta-cyclodextrin.
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    The clinical relevance of piroxicam-beta-cyclodextrin (PBC) in the long-term treatment of osteoarthritis and rheumatoid arthritis is reviewed. Two hundred and twenty-five patients--one hundred with rheumatoid arthritis and one hundred and twenty five with osteoarthritis--were enrolled in a double-blind, randomised, controlled study versus piroxicam. Drugs were administered once-daily, for twelve weeks. The indices of efficacy (pain intensity, severity of inflammation, functional impairment evaluated at 0,2,4,8 and 12 weeks showed the good analgesic effect of piroxicam without significant differences between its two formulations. Tolerance appeared to be better in the group of patients treated with PBC than in the one treated with piroxicam. Both the incidence and severity of side effects were lower for patients treated with PBC. The majority of side effects were related to the gastrointestinal tract. The study suggests that PBC, used in the long term treatment of rheumatic diseases, improves the safety of piroxicam without affecting its efficacy. In another study, thirty patients with chronic osteoarthritis were randomly assigned to receive PBC or tenoxicam daily for eight weeks. Both drugs effectively reduced pain, inflammation, and functional limitation of the affected joints. Endoscopy revealed minor post-treatment mucosal lesions; these tended to be less severe with PBC than with tenoxicam. The clinical experience in the long-term treatment of rheumatic conditions indicates that the microencapsulation of piroxicam as piroxicam-beta-cyclodextrin has provided a new drug with a superior tolerability compared to the parent compound without affecting its high efficacy on the symptoms of the primary disease.

    Topics: Adult; Aged; Aged, 80 and over; Antirheumatic Agents; Arthritis, Rheumatoid; beta-Cyclodextrins; Cyclodextrins; Double-Blind Method; Drug Combinations; Drug Therapy, Combination; Female; Humans; Male; Middle Aged; Osteoarthritis; Pain; Piroxicam

1993
[Analgesic efficacy and the tolerance for piroxicam-beta-cyclodextrin compared to piroxicam, paracetamol and placebo in the treatment of postextraction dental pain].
    Minerva stomatologica, 1993, Volume: 42, Issue:5

    Acute postoperative pain is a common experience in oral surgery practice. Non-steroidal anti-inflammatory drugs (NSAIDs) are quite effective against mild to moderate pain and they are generally better suited in ambulatory outpatients than narcotic analgesics. The analgesic activity of piroxicam, a well known NSAID has been documented in many pain states. Piroxicam can be administered once daily because of its long half-life, but its absorption in the gastrointestinal tract is slow as it is its onset of action. Piroxicam-beta-cyclodextrin (PBCD) is a new formulation of piroxicam which is the product of supermolecular encapsulation of piroxicam with the cyclic oligosaccharide beta-cyclodextrin. PBCD is absorbed much faster than standard piroxicam, and its action as an analgesic is consequently more rapid. The purpose of this study was to assess the efficacy and the rapidity of action of piroxicam-beta-cyclodextrin in comparison with standard piroxicam, paracetamol and placebo following surgical extraction of impacted third molars.. The study population was composed of 32 patients of both sexes and in good health. To be included into the study, patients must have had third molar removal resulting in acute post-surgical pain of at least moderate intensity. The patients were then randomly assigned to one of four treatment groups. PBCD 20 mg tablets; piroxicam 20 mg capsules; paracetamol 500 mg tablets, or placebo. The study was conducted according to a double-blind, double-dummy design. Pain intensity and pain relief were recorded at 0.5, 1, 1.5, 2, 3, 4 hours after a single dose of the study drugs, by means of a Keele-type rating scale. Rescue analgesics were not allowed before one and a half hour after taking the study drugs. A global evaluation of study drugs was expressed by patients at the end of the observation period.. Treatment groups were homogeneous for demographic characteristics of the patients and for pain intensity at the time of medication with study drugs. All patients who received placebo requested supplemental analgesics, while none of the patients treated with the active drugs needed rescue analgesics. PBCD and paracetamol were comparable for their analgesic effect, while the time lag before a significant reduction of pain intensity with piroxicam was longer. Piroxicam and PBCD were superior to paracetamol because they showed a substantial analgesic effect through the 4-hour study duration, while paracetamol did not induce a complete relief from pain.. One of the most commonly utilized model for the evaluation of analgesics is the third molar extraction pain. Our study clearly differentiated between active drugs and placebo. Furthermore, while PBCD and paracetamol showed a rapid effect, piroxicam was slow in inducing pain relief. The analgesic and anti-inflammatory activity of PBCD and piroxicam brought about the resolution of pain and inflammation consequent to the dental extraction. Paracetamol, a pure analgesic, was not equally active and pain persisted, even if at a low grade, throughout the observation period; probably this was due to local inflammation and edema. The results of our study appear to confirm the pharmacokinetic data on PBCD, which showed that therapeutic blood levels are reached faster with PBCD than with the standard piroxicam formulation. This results should be confirmed in studies with an adequate number of patients.

    Topics: Acetaminophen; Adolescent; Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Cyclodextrins; Double-Blind Method; Drug Combinations; Drug Tolerance; Female; Humans; Male; Middle Aged; Molar, Third; Pain Measurement; Pain, Postoperative; Piroxicam; Placebos; Tooth Extraction

1993
Placebo-controlled comparison of piroxicam-beta-cyclodextrin, piroxicam, and indomethacin on gastric potential difference and mucosal injury in humans.
    Digestive diseases and sciences, 1992, Volume: 37, Issue:12

    The acute gastroduodenal mucosa injury and gastric potential difference (GPD) drops provoked by 14-day administration of 20 mg/day of a new piroxicam formulation (piroxicam-beta-cyclodextrin), 20 mg/day standard piroxicam and 100 mg/day indomethacin were evaluated and compared in a randomized, double-blind, placebo-controlled study carried out on 64 volunteers. Endoscopic examinations, performed after 14-day treatment, demonstrated that piroxicam-beta-cyclodextrin was less gastrolesive (mean endoscopic score +/- SE = 0.56 +/- 0.2) than either piroxicam (2.06 +/- 0.5) or indomethacin (2.25 +/- 0.5) (p < 0.01). The drop in GPD after a single dose of the assigned drug was considerably greater for piroxicam and indomethacin than for piroxicam-beta-cyclodextrin (p < 0.01), which registered similar values to placebo. Since GPD is an expression of the anatomo-functional integrity of the gastric barrier, the results indicate that piroxicam-beta-cyclodextrin exerts less direct acute damage on the gastric mucosa. Therefore, when administered short-term, piroxicam-beta-cyclodextrin appears to be less gastrolesive than either indomethacin or the standard piroxicam formulation.

    Topics: Adult; beta-Cyclodextrins; Cyclodextrins; Double-Blind Method; Drug Combinations; Female; Gastric Acidity Determination; Gastric Mucosa; Gastroscopy; Humans; Indomethacin; Male; Membrane Potentials; Piroxicam

1992
Comparison of faecal blood loss, upper gastrointestinal mucosal integrity and symptoms after piroxicam beta-cyclodextrin, piroxicam and placebo administration.
    European journal of clinical pharmacology, 1989, Volume: 36, Issue:6

    In order to evaluate the gastric tolerance of the new piroxicam formulation CHF 1194 (piroxicam complexed with beta-cyclodextrin), a double-blind randomized trial was carried out in 21 young healthy volunteers comparing CHF 1194 with piroxicam and placebo. Faecal blood loss measurement by the Cr-51 labelled red blood cell technique, upper gastrointestinal endoscopic evaluation, titration of gastric pH and gastric biopsies before, during and after treatment were used to assess drug tolerability. Four out of 7 volunteers in the piroxicam-treated group withdrew because of severe gastrointestinal symptoms and oesophageal and/or gastroduodenal lesions, while all subjects treated with CHF 1194 or placebo completed the treatment. There was a significant difference between the endoscopic scores of the piroxicam and placebo groups, whereas no differences were found between CHF 1194 and placebo, nor between piroxicam and CHF 1194. Daily mean gastrointestinal blood loss was greater in the piroxicam group than in either the CHF 1194 or placebo groups, but the difference was not significant, due to the small number of piroxicam-treated subjects who completed the study. When administered for a short period to healthy young subjects, CHF 1194 caused less gastric damage and was better tolerated than piroxicam.

    Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Clinical Trials as Topic; Cyclodextrins; Dextrins; Double-Blind Method; Drug Combinations; Female; Gastric Mucosa; Gastrointestinal Hemorrhage; Gastroscopy; Humans; Hydrogen-Ion Concentration; Male; Piroxicam; Random Allocation; Starch

1989

Other Studies

8 other study(ies) available for betadex and piroxicam-beta-cyclodextrin

ArticleYear
Triple-component nanocomposite films prepared using a casting method: Its potential in drug delivery.
    Journal of food and drug analysis, 2018, Volume: 26, Issue:2

    The purpose of this study was to fabricate a triple-component nanocomposite system consisting of chitosan, polyethylene glycol (PEG), and drug for assessing the application of chitosan-PEG nanocomposites in drug delivery and also to assess the effect of different molecular weights of PEG on nanocomposite characteristics. The casting/solvent evaporation method was used to prepare chitosan-PEG nanocomposite films incorporating piroxicam-β-cyclodextrin. In order to characterize the morphology and structure of nanocomposites, X-ray diffraction technique, scanning electron microscopy, thermogravimetric analysis, and Fourier transmission infrared spectroscopy were used. Drug content uniformity test, swelling studies, water content, erosion studies, dissolution studies, and anti-inflammatory activity were also performed. The permeation studies across rat skin were also performed on nanocomposite films using Franz diffusion cell. The release behavior of films was found to be sensitive to pH and ionic strength of release medium. The maximum swelling ratio and water content was found in HCl buffer pH 1.2 as compared to acetate buffer of pH 4.5 and phosphate buffer pH 7.4. The release rate constants obtained from kinetic modeling and flux values of ex vivo permeation studies showed that release of piroxicam-β-cyclodextrin increased with an increase in concentration of PEG. The formulation F10 containing 75% concentration of PEG showed the highest swelling ratio (3.42±0.02) in HCl buffer pH 1.2, water content (47.89±1.53%) in HCl buffer pH 1.2, maximum cumulative drug permeation through rat skin (2405.15±10.97 μg/cm

    Topics: Administration, Cutaneous; Animals; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Drug Carriers; Drug Delivery Systems; Male; Microscopy, Electron, Scanning; Nanocomposites; Piroxicam; Polyethylene Glycols; Rats; Rats, Sprague-Dawley; X-Ray Diffraction

2018
Piroxicam/2-hydroxypropyl-beta-cyclodextrin inclusion complex prepared by a new fluid-bed coating technique.
    Journal of pharmaceutical sciences, 2009, Volume: 98, Issue:2

    This work was aimed at investigating the feasibility of fluid-bed coating as a new method to prepare cyclodextrin inclusion complex. The inclusion complex of the model drug piroxicam (PIX) and 2-hydroxypropyl-beta-cyclodextrin (HPCD) in aqueous ethanol solution was sprayed and deposited onto the surface of the pellet substrate upon removal of the solvent. The coating process was fluent with high coating efficiency. Scanning electron microscopy revealed a coarse pellet surface, and a loosely packed coating structure. Significantly enhanced dissolution, over 90% at 5 min, was observed at stoichiometric PIX/HPCD molar ratio (1/1) and at a ratio with excessive HPCD (1/2). Differential scanning calorimetry and powder X-ray diffractometry confirmed absence of crystallinity of PIX at PIX/HPCD molar ratio of 1/1 and 1/2. Fourier transform-infrared spectrometry and Raman spectrometry revealed interaction between PIX and HPCD adding evidence on inclusion of PIX moieties into HPCD cavities. Solid-state (13)C NMR spectrometry indicated possible inclusion of PIX through the pyridine ring. It is concluded that fluid-bed coating has potential to be used as a new technique to prepare cyclodextrin inclusion complex.

    Topics: 2-Hydroxypropyl-beta-cyclodextrin; Aerosols; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Crystallography, X-Ray; Dosage Forms; Ethanol; Feasibility Studies; Kinetics; Magnetic Resonance Spectroscopy; Microscopy, Electron, Scanning; Piroxicam; Powder Diffraction; Solubility; Solvents; Spectroscopy, Fourier Transform Infrared; Spectrum Analysis, Raman; Surface Properties; Technology, Pharmaceutical

2009
Impact of piroxicam beta-cyclodextrin on the efficacy of the intrauterine device in a rat model.
    The European journal of contraception & reproductive health care : the official journal of the European Society of Contraception, 2007, Volume: 12, Issue:2

    To elucidate the effect of piroxicam beta-cyclodextrin (PbetaCD), a non-steroidal anti-inflammatory drug (NSAID), on the efficacy of the intrauterine device (IUD) in a rat model.. Forty nulliparous female Wistar rats were allocated to one of four groups, comprising each 10 of these animals. Group I: neither IUD nor medication; group II: IUD, but no medication; group III: IUD and PbetaCD; and group IV: PbetaCD only. In groups II and III, a string of 3/0 silk suture of 2 cm long was transcervically placed in one of the horns of the bicornuate uterus of the rat. Rats in group III were treated during the 18 days following IUD placement with 3 mg/kg/day PbetaCD administered via a feeding tube; group IV received PbetaCD for the same length of time, but had no IUD inserted. The rats were then mated. Thereafter, vaginal smears were taken and assessed daily, in the early morning, for the presence of spermatozoa. The day when spermatozoa were detected was considered to be the first day of gestation. On gestational day 19, both uterine horns of all rats were evaluated for the presence and number of embryos.. In group II, mean embryo counts in the horn with or without IUD were 1.0 +/- 0.2 and 4.5 +/- 0.3, respectively (p < 0.01). The comparison of group II with group I showed that the presence of an IUD in one horn did not affect the mean embryo counts in the contralateral horn (4.5 +/- 0.3 versus 5.1 +/- 0.9, p > 0.05). In groups II and III, mean numbers of embryos in the horn with IUD were 1.0 +/- 0.2 and 2.7 +/- 0.4, respectively (p < 0.01). No difference in the mean embryo counts was observed between group I (5.1 +/- 0.9) and IV (4.8 +/- 0.9; p > 0.05).. The IUD had a contraceptive effect in the rat model. The IUD in one horn did not affect the number of embryos in the contralateral horn. In this model, IUDs appear to exert a local effect, i.e. counteracted by PbetaCD. This drug had no adverse effect on the fertility of rats without IUD in situ.

    Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Embryo Implantation; Female; Intrauterine Devices; Models, Animal; Piroxicam; Pregnancy; Rats; Rats, Wistar

2007
[Corneal edema and systemic NSAIDs].
    Journal francais d'ophtalmologie, 2007, Volume: 30, Issue:6

    We report a case of a transient corneal edema related to systemic NSAID treatment.. A 48-year-old woman treated with a systemic NSAID [piroxicam B-cyclodextrin (Brexin) and naproxen (Apranax)] presented with a corneal edema and a transient decrease in visual acuity for a period of 24 h. No ocular etiology was found to explain this corneal edema. Another treatment with Apranax was follow by another corneal edema.. Corneal edema could be related to systemic NSAID treatment.

    Topics: Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Corneal Edema; Female; Humans; Intervertebral Disc Displacement; Lumbar Vertebrae; Middle Aged; Naproxen; Piroxicam; Recurrence

2007
Quantitative determination of piroxicam in a new formulation (piroxicam-beta-cyclodextrin) by derivative UV spectrophotometric method and HPLC.
    Journal of pharmaceutical and biomedical analysis, 2001, Volume: 26, Issue:2

    A derivative ultraviolet (UV) spectrophotometric method for the determination of piroxicam in piroxicam--beta-cyclodextrin tablets was developed. Phosphate buffer (pH 7.8, 0.1 M) and ethanol were used as a solvent system throughout the study. In this study, determination of piroxicam was conducted by using first order derivative amplitudes at 261.4 nm (n=4). Standards for the calibration graph ranging from 2.40 to 20.0 microg/ml were prepared from working standard. The proposed method is accurate with 99.70%+/-0.50 recovery value and precise with coefficient of variation (CV) of 1.29. The results were compared with those obtained using a high-performance liquid chromatography (HPLC) procedure. A reversed-phase C(18) column with aqueous phosphate buffer:methanol, 60:40, v/v, mobile phase was used. UV detector was set at 254 nm. Calibration solutions used in HPLC were ranging from 5 to 20 microg/ml. Results obtained in HPLC were comparable to those obtained by derivative UV spectrophotometric method.

    Topics: Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Cyclodextrins; Drug Combinations; Piroxicam; Spectrophotometry, Ultraviolet

2001
Pharmacokinetic profile of piroxicam beta-cyclodextrin, in rat plasma and lymph.
    General pharmacology, 1997, Volume: 28, Issue:5

    1. The absorption of piroxicam into the blood of rats is significantly slower after oral administration of piroxicam beta-cyclodextrin than of free piroxicam. 2. The pharmacokinetic profiles of piroxicam in rat lymph were very similar in both groups. 3. Bioavailability of piroxicam in plasma is higher after treatment with the inclusion product than with free piroxicam. On the other hand, bioavailability in lymph is higher when free piroxicam is administered.

    Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Biological Availability; Cyclodextrins; Drug Combinations; Hematocrit; Lymph; Male; Piroxicam; Rats; Rats, Wistar

1997
Prizes!
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    Topics: Anti-Inflammatory Agents, Non-Steroidal; Awards and Prizes; beta-Cyclodextrins; Cyclodextrins; Drug Combinations; Humans; Osteoarthritis; Piroxicam

1993
Macrocyclic molecules and their pharmacological applications.
    European journal of rheumatology and inflammation, 1993, Volume: 12, Issue:4

    Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Cyclodextrins; Digestive System; Drug Combinations; Humans; Molecular Structure; Piroxicam

1993
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