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PubMedDate not supplied

Pharmacokinetics of dipyridamole-beta-cyclodextrin complex in dogs.

Plasma concentrations and urinary and fecal excretion of intact dipyridamole were followed in dogs after oral administration of dipyridamole-beta-cyclodextrin complex (dip-beta-CD) (capsules containing 37.5 and 75 mg of active principle), of commercial dipyridamole and of dipyridamole. HCl (tablets and capsules of 75 mg of active principle, respectively), according to a crossover design. Dip-beta-CD afforded significantly shorter lag-times, higher Cmax, smaller interindividual variations of plasma concentrations and greater urinary excretion than the other two preparations, as a consequence of a better bioavailability of the former one. This amelioration seems to be due not only to an increased wettability and water solubility of the product, but also to a finer molecular dispersion in the gastrointestinal fluids which favors the contact of dipyridamole with a greater absorption surface.

Administration, Oral↗
PubMed1987

Inhibition of experimental and spontaneous pulmonary metastasis of murine RCT (+) sarcoma by beta-cyclodextrin-benzaldehyde.

The effect of beta-cyclodextrin-benzaldehyde (CDBA) on pulmonary metastasis in C3H/He mice was examined. In experimental metastasis that was induced by iv injection of 1 X 10(6) RCT (+) cells, the highest inhibition was observed in the mice that were treated daily with CDBA (5 mg/day) for 1 week before tumor cell inoculation and further treated for 3 weeks after inoculation, when compared with those in other experimental groups that were given only pretreatment or posttreatment. The inhibitory effect was dose-dependent. In spontaneous metastasis that was induced by sc injection of 3 X 10(6) RCT (+) cells, the inhibition of metastasis was also observed in the mice treated with CDBA (5 mg/day) in the same manner as described above. However, the development of the primary tumor was not inhibited. CDBA-treated tumor-bearing mice showed almost as much NK activity as normal mice. Furthermore, although injection of 5-fluorouracil suppressed this activity to about 50% of that in normal mice, the combined treatment with CDBA could maintain the NK cell activity at the normal level. The results suggested that the inhibition of pulmonary metastasis might be induced by a combined effect of CDBA; that is, the direct inhibition of tumors and the maintenance of NK cell activity.

Animals↗
PubMed1988

[Inhibition of pulmonary metastases in mice by beta-cyclodextrin-benzaldehyde].

The effect of beta-cyclodextrin-benzaldehyde (CDBA) on the pulmonary metastasis in C3H/He mice was examined. When mice were treated daily with CDBA, 3 weeks later the number of lung nodules developed after i.v. inoculation of 1 X 10(6) RCT (+) cells was significantly decreased. The mean numbers of the lung nodules were 69.9 and 73.4 in the water-and cyclodextrin (CD)-treated mice, respectively. However, these were 17.8, 9.8 and 2.9 in 0.5, 5 and 25 mg/mouse per day CDBA-treated mice, respectively. And also, daily treatment of CDBA prolonged the survival time of the tumor bearing mice in both experimental and spontaneous metastasis studies. Two or three weeks after subcutaneous inoculation of RCT (+) cells (1 X 10(6) cells) to the foot pad, left hindlimbs were amputated and then mice were daily treated or untreated with CDBA. Five weeks after tumor inoculation, the number of lung nodules was counted. Twenty eight point six and 100% of untreated mice had lung metastases when amputation was carried out 2 (earlier operation group) and 3 (latero peration group) weeks after tumor inoculation. However, in CDBA-treated mice, these values were noticeably decreased, that is, 6.7% and 60% in earlier and later operation groups, respectively. Furthermore, in the later operation group, mean number of the lung nodules in CDBA-treated mice was only 2.7 while this was 12.9 in untreated mice. These data suggest that CDBA improve the survival time of tumor bearing mice through the inhibition of the lung metastasis.

Administration, Oral↗
PubMed1987

Enhanced percutaneous absorption of homogenized tolnaftate/beta-cyclodextrin polymer ground mixture.

The absorption of tolnaftate after external application of tolnaftate-cyclodextrin polymer homogenized ground mixtures was investigated in comparison with that of tolnaftate alone and non-homogenized mixtures. To evaluate their percutaneous absorption, samples were applied to the shaved back skin of mice. It was found that homogenized ground mixture samples showed the highest level of percutaneous absorption, and also resulted in the highest blood level concentrations.

Animals↗
PubMed1985

Internalization of cycloheptaamylose-dansyl chloride complex during labelling of surface membrane in living Paramecium aurelia cells.

Internalization of cycloheptaamylose-dansyl chloride complex during surface labelling of living long-term starved Paramecium aurelia cells has been observed. This process may be inhibited by pretreatment of the ciliates with dichloroisoproterenol. Uptake of cycloheptaamylose-dansyl chloride may be visualized only after UV preirradiation: the appearance of orange-fluorescing vacuoles of diameter 2.3-4.5 micron may then be observed. Microspectrographic analysis performed on the cells and dansyl derivatives indicates that this fluorescence is produced by a photochemical reaction of dansyl chloride - released from CDC complex inside the digestive vacuoles-under the influence of UV irradiation.

Animals↗
PubMed1994

Evaluation of piroxicam-beta-cyclodextrin, piroxicam, paracetamol and placebo in post-operative oral surgery pain.

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.

Acetaminophen↗
PubMedDate not supplied

Piroxicam-beta-cyclodextrin in induced migraine attacks: a SPECT study with Tc-99m HM-PAO split-dose method.

To verify the effect of piroxicam-beta-cyclodextrin (P-B-CD), a novel non-steroidal anti-inflammatory compound, on regional cerebral blood flow (rCBF) during migraine attacks, 7 female patients (mean age: 37.4 years), suffering from migraine without aura, were studied. The patients, after induction of a migraine-like attack with sublingual nitroglycerin (NTG), underwent a rCBF evaluation using Single Photon Emission Computerized Tomography (SPECT) and Tc-99m examethyl-propylene-amino-oxyma split-dose method before and after oral administration of P-B-CD (20 mg). In addition, a spontaneous migraine attack and NTG test in 7 control subjects were investigated. All patients observed relief of pain, evaluated by direct and indirect parameters (Pain Intensity; Pain Intensity Difference; Sum of Pain Intensity Difference). SPECT revealed a uniform and symmetrical distribution of the radiocompound in 5 out of 8 patients, while in the remaining 3 symmetrical parietal or parieto-occipital areas of decreased tracer uptake were detected. In these cases, the intake of P-B-CD cancelled out the cerebral perfusion abnormality.

Adolescent↗
PubMed1993

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Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1993

Rheumatic diseases--clinical experience with piroxicam-beta-cyclodextrin.

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.

Adult↗