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PubMed1992

Bile acid and sterol solubilization in 2-hydroxypropyl-beta-cyclodextrin.

The use of 2-hydroxypropyl-beta-cyclodextrin has made it possible to prepare stable aqueous solutions of cholesterol, 26-hydroxycholesterol, 7 alpha-hydroxycholesterol, and monohydroxy bile acids such as lithocholic and 3 beta-hydroxy-5-cholenoic acids. These solutions are suitable for cell culture studies and for parenteral administration to animals.

2-Hydroxypropyl-beta-cyclodextrin↗
PubMed1992

Development of a lyophilized formulation of interleukin-2.

Native human interleukin-2 (IL-2) comprises a group of glycoproteins of MW 13,000-17,500. Recombinant human IL-2 (rhIL-2) (Cetus) is derived from E. coli and is not glycosylated. We have evaluated several processes for manufacturing rhIL-2, based on different chaotropic agents for solubilization of insoluble protein pastes. Formulation work carried out with material purified by one of these processes is reported here. Our studies have indicated that the presence of a stabilizer in the form of an amorphous excipient, such as amino acids, a non-ionic surfactant (polysorbate 80), hydroxypropyl-beta-cyclodextrin or human serum albumin was essential for preservation of rhIL-2 during lyophilization. Each of these formulations exhibited its own unique problems. We have overcome these problems through a systematic formulation development program and have been successful in developing several lyophilized formulations of rhIL-2 with optimum properties and performance.

2-Hydroxypropyl-beta-cyclodextrin↗
PubMedDate not supplied

Solubilization of ovine growth hormone with 2-hydroxypropyl-beta-cyclodextrin.

Studies were undertaken to determine the effects of 2-hydroxypropyl-beta-cyclodextrin (HPCD) on the solubility of ovine-Growth Hormone (o-GH) in aqueous solution. HPCD, which is believed to form inclusion complexes with hydrophobic amino acid residues of peptides, markedly increased o-GH solubility at all o-GH and all HPCD concentrations tested. In HPCD solutions, o-GH was completely solubilized between pH 7.5 and 8.5, while in water, o-GH was not solubilized until a pH of 11.5 was reached. Temperature and repeated freeze-thaw cycles had little effect on o-GH solubility in HPCD. Vigorous shaking of solution of o-GH in HPCD did not result in precipitation of the peptide. These studies document that HPCD enhances o-GH solubility in aqueous solutions. Preparations of GH in HPCD may eliminate solubility problems observed in current human GH preparations intended for parenteral use.

2-Hydroxypropyl-beta-cyclodextrin↗
PubMed1991

Piroxicam-beta-cyclodextrin: effects on gastrointestinal blood loss and gastric mucosal appearance in healthy men.

Thirty-six healthy men aged 20-31 years took part in a randomized, double-blind, double-dummy, parallel-group study to compare the effects of repeated doses of piroxicam-beta-cyclodextrin, piroxicam and placebo on faecal blood loss and the endoscopic appearances of gastric and duodenal mucosa. After an initial endoscopy, subjects received on day 0 autologous erythrocytes labelled with 51Cr. Complete daily faecal collections were then made from days 6 to 12. From days 13 to 40, subjects received daily by mouth either piroxicam-beta-cyclodextrin (containing 20 mg piroxicam), piroxicam 20 mg, or placebo. Complete faecal collections were made daily from days 13 to 41; blood samples for red-cell 51Cr activity were taken weekly. Endoscopy was repeated 16-20 h after the last dose of medication. Faecal blood loss was calculated from 51Cr activity of blood and faeces. Compliance with medication was confirmed by blood sampling on days 20, 27 and 34. General tolerability of the medication was good, although 1 subject was withdrawn from piroxicam-beta-cyclodextrin and 1 from piroxicam treatment because of abdominal pain. There were no clinically significant changes in haematology, biochemistry or urinalysis results in any subject. Endoscopic appearances deteriorated moderately in 3 subjects receiving piroxicam and 3 receiving piroxicam-beta-cyclodextrin, but did not deteriorate in any subject receiving placebo. There was a trend for cumulative blood loss to be higher for piroxicam than for the other treatments in the last 12 days of dosing.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMedDate not supplied

[Beta-cyclodextrin-piroxicam in the treatment of the active phase of osteoarthritic pathology].

The anti-inflammatory and analgesic activity of the beta-cyclodextrin-piroxicam (beta CDP) complex was assessed in a randomized single-blind controlled parallel study vs nabumetone (NAB). Forty patients, 18 men and 22 women aged 18 to 65 and suffering from chronic osteoarthritis, were treated. Both drugs were orally administered, once a day in the morning, for 4 consecutive weeks. PI and SPID, evaluated for 24 hours following the first drug administration, showed a quicker onset of the analgesic action of beta CDP, with statistically significant differences between treatments (p less than 0.05). In the medium-term treatment, beta CDP proved to be more effective on joint swelling, spontaneous pain, pain on passive movement and functional limitation. Both treatments were well tolerated but a higher gastro-intestinal side-effect incidence was recorded in NAB group.

Adult↗
PubMedDate not supplied

[Osteoarthritic disease: therapy with oxicam derivatives].

Two groups, each composed of 20 elderly patients suffering from osteoarthritis characterised by intense pain, were treated for 4 weeks with the oral formulation of two modern oxicam derivatives (tenoxicam capsules and beta-cyclodextrin-piroxicam tablets respectively). The analysis of the results showed that both drugs have an excellent antalgic effect. After the first dose the action of beta-cyclodextrin-piroxican was quicker and more marked, with statistically significant differences between treatments for the first 4 hours. At the end of the study period the two drugs proved to be equally effective, with a more pronounced symptomatic effect of beta-cyclodextrin-piroxican. No side effects serious enough to warrant suspension of treatment were observed: the only side effects reported were gastric adverse events (pyrosis, gastralgia) in both groups, having an incidence of 50% (tenoxicam) and 15% (beta-cyclodextrin-piroxicam) respectively.

Aged↗
PubMed1990

[A multicenter clinical study of oral topical administration of G-512 on chemotherapy-associated intraoral mucosal lesions of patients with hematological malignancies. G-512 Therapeutic Study Group for Intraoral Mucosal Lesions].

We evaluated the usefulness of PGE2 on chemotherapy-associated oral mucosal lesions of the patients with hematological malignancies and compared the efficacy of the troche with that of the tablet. One hundred and fifty three patients were given 0.5 mg of these PGE2 topically three times daily. One hundred and fourty five cases were evaluable (Tablet; 85, Troche; 60). 1) Symptoms and signs were improved in 102/144 (70.8%) and 102/145 (70.3%), respectively. The overall response rate was 70.3%. 2) The improvement rates were 77.5% (55/71), 85.7% (6/7) and 62.7% (32/51) in leukocyte count-increased, -unchanged and -decreased patients, respectively. 3) No background factor of the patients except performance status affected the improvement rate. 4) Higher improvement rate was noted in the PGE2 early starting group (within 5 days after the appearance of oral lesions) than the late group (6 days and thereafter) (76.5% v.s. 55.8%: U-test p less than 0.1, chi2-test p less than 0.05). 5) There was no difference in the efficacy rate between the tablet and the troche. 6) Mild side effects were seen in 10 cases. These results suggest that topical administration of PGE2 is safe and useful for improving chemotherapy-associated oral mucosal lesions of patients with hematological malignancies.

Administration, Oral↗
PubMedDate not supplied

Efficacy and gastrointestinal tolerability of beta-cyclodextrin-piroxicam and tenoxicam in the treatment of chronic osteoarthritis.

Thirty patients aged 26 to 70 years with a history of chronic osteoarthritis of at least eight years were randomly assigned to receive 20 mg daily of beta-cyclodextrin-piroxicam (beta-CDP) or tenoxicam for eight weeks. Both drugs effectively reduced pain, inflammation, and functional limitations of the affected joints. Endoscopy revealed minor posttreatment hemorrhagic lesions and erosions; these tended to be less severe in the group treated with beta-CDP than with tenoxicam. Slight to moderate gastrointestinal symptoms were reported by one patient treated with beta-CDP and three patients treated with tenoxicam; the symptoms were poorly correlated with endoscopic findings. It is concluded that both drugs are safe and effective in the control of symptoms in patients with chronic osteoarthritis.

Adult↗
PubMed1989

Effects of 2-hydroxypropyl-beta-cyclodextrin on the aqueous solubility of drugs and transdermal delivery of 17 beta-estradiol.

The effect of 2-hydroxypropyl-beta-cyclodextrin (2-HPCD) on the aqueous solubility of 18 drugs possessing different physiochemical properties was investigated. The largest increase in aqueous solubility was obtained with very lipophilic drugs with low aqueous solubility and the enhancement was larger at low temperature than at high temperature. In many cases a linear relationship exists between the drug solubility and the 2-HPCD concentration. Ionization of a drug molecule enhanced the solubility effects of 2-HPCD, resulting in greater aqueous solubility than if either method was used by itself. 2-HPCD was found to be an effective transdermal permeability enhancer.

2-Hydroxypropyl-beta-cyclodextrin↗
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↗