OBJECTIVETo provide content-measuring evidences for establishing the quality criteria of dexamethasone acetate ulcer pasta.

METHODSContent of dexamethasone acetate was assayed by the isonicotinyl hydrazine (INH) colorimetry.

RESULTSThe good linear range was 6-16 microg/mL (r = 0.999 1). The average recovery of dexamethasone acetate was 98.9%, and relative standard deviation was low than 1% (n = 5).

CONCLUSIONIt is easy, convenient, accurate and dependable for INH colorimetry to determine the content of dexamethasone acetate.

Chromatography, High Pressure Liquid ; Dexamethasone ; analogs & derivatives ; Humans ; Oral Medicine ; Oral Ulcer

Dexamethasone sodium phosphate (DSP) is increasingly used in the treatment of ocular inflammatory diseases by systemic, periocular, and recently, intravitreal injection. We have developed a method for the determination of vitreous levels of DSP by reverse phase HPLC. In this method, co-elution of vitreous proteins with DSP is resolved by a prior sample clean-up procedure using Waters Sep-Pak C18 cartridge; the protein is separated and eluted with water while DSP, paraben and prednisone are eluted with methanol. DSP in the resulting sample is then separated by reverse phase HPLC and quantified by UV absorption at 254 nm. The recovery of DSP through the sample clean-up is 68.9 +/- 3.0%. DSP quantitation is linear from 0.1 mg to 1.0 mg per 1.0 ml vitreous. This method provides a simple, sensitive and reliable technique for determining the vitreous levels of DSP.
Animals ; Anti-Inflammatory Agents/*analysis ; Chromatography, High Pressure Liquid/*methods ; Dexamethasone/*analogs & derivatives/analysis ; Rabbits ; Reproducibility of Results ; Sensitivity and Specificity ; Vitreous Body/*chemistry

To investigate the effects of gossypol acetate on apoptosis in primary cultured cells from patients with acute lymphoblastic leukemia (ALL) and chronic lymphocytic leukemia (CLL) and its synergistic effect with dexamethasone. The apoptosis-inducing effect of gossypol acetate on primary cultured leukemia cells was analyzed by flow cytometry (FCM). The effect of gossypol acetate on survival rates of Raji cells and mononuclear cells (MNC) from normal bone marrow were evaluated by MTT assay. After co-treatment with gossypol acetate and dexamethasone, the apoptosis rate of Raji cells was detected by FCM. The results showed that gossypol acetate was able to induce apoptosis in primary cultured ALL cells at concentrations of ≥ 5 µmol/L. The effect was concentration and time dependent. Apoptosis-inducing concentration in CLL cells was higher than that in ALL cells. After exposing to 50 µmol/L gossypol acetate for 48 h, the apoptosis rate of ALL and CLL cells were (90.4 ± 6.2)% and (51.7 ± 10.3)% separately. No major growth inhibitory effect was observed in MNC from normal bone marrow when they were exposed to gossypol acetate at concentrations lower than 10 µmol/L. After exposing for 48 and 72 h, the IC(50) of gossypol acetate for MNC from normal bone marrow was 7.1 and 9.1 times as much as the IC(50) of Raji cells. Co-treatment with 10 µmol/L gossypol acetate and dexamethasone remarkably increased the apoptosis rate of Raji cells. It is concluded that the gossypol acetate has apoptosis-inducing activity in primary cultured leukemia cells from patients diagnosed as ALL and CLL in vitro. The inhibitory effect of gossypol acetate on MNC from normal bone marrow is less prominent than that on Raji cells. Co-treatment with gossypol acetate and dexamethasone notably amplified the pro-apoptosis activity of the latter in Raji cells.
Apoptosis ; drug effects ; Cell Line ; Dexamethasone ; pharmacology ; Gossypol ; analogs & derivatives ; pharmacology ; Humans ; Leukemia, Lymphocytic, Chronic, B-Cell ; pathology ; Precursor Cell Lymphoblastic Leukemia-Lymphoma ; pathology ; Tumor Cells, Cultured

Thermosensitive in situ gel is a novel drug delivery system which can form gel in situ after injection of the polymer solution into the body and releases the drug in a controlled manner, thus provides a promising strategy for localized drug delivery. The aim of the present work is to investigate the characteristics including gelation temperature, sol-gel transition temperature (T(s-g)), gel strength, stable viscosity, erosion and drug release behavior of the thermosensitive in situ gel which are composed of different concentrations of poloxamer Pluronic F127 and F68. The gelation temperature was determined by tube-reverse method. Rheological measurements were carried out to evaluate T(s-g), stable viscosity and gel strength. Erosion of the gels and release of dexamethasone sodium phosphate (DSP) from the gels were investigated by membrane-free method and HPLC. Increased F127 concentration in gel decreased the gelation temperature, T(s-g) as well as erosion of the gel and drug release rate, while viscosity and gel strength rose accordingly. However, increased F68 in gel could lead to the opposite result. The poloxamer solution below T(s-g) is Newtonian fluid with comparatively low viscosity, but shows the characteristics of the pseudoplastic fluid when temperature rises near to T(s-g). Drug release was controlled by the erosion of the gel matrix, and both of them followed the zero-order kinetics. An optimized formation containing 22.5% F127 and 2.5% F68 showed more desirable characteristics which meet the clinical requirements and is of potential in future clinical therapy.
Delayed-Action Preparations ; Dexamethasone ; administration & dosage ; analogs & derivatives ; chemistry ; Drug Delivery Systems ; methods ; Gels ; Poloxamer ; administration & dosage ; chemistry ; Rheology ; Temperature ; Viscosity

OBJECTIVETo investigate the therapeutic effect of combined injection of pingyangmycin (PYM) & dexame thasone (DXM) for the treatment of maxillofacial and cervical venous malformations.

METHODSFrom August 1995 to October 2008, 116 cases with maxillofacial and cervical venous malformations were retrospectively analyzed. The injection dilute was made with PYM 8 mg, DXM 10 mg and 2% lidocaine 2.0 ml (PYM 2 mg/ml). The PYM diluent 1.0-4.0 ml (including the PYM 2-8 mg) was injected into the tumor according to the patients age, tumor size and location. For children, PYM 2-4 mg was injected for one treatment. The needle should be inserted into tumor perpendicularly or from the edge of tumor. After withdrawing blood, the drug was injected into the tumor slowly. The injection could be repeated every 7-10 days. The clinical signs were recorded; ultrasonography and chest X-ray were performed to evaluate the therapeutic effect.

RESULTS1-5 treatments of injection were performed in the 116 patients. The tumor shrinked and disappeared after treatment with PYM 2-40 mg and DXM 5-50 mg. The patients were followed up for 3-5 years with no occurrence and complication.

CONCLUSIONSIt's safe, effective and practical to treat maxillofacial and cervical venous malformations by combined injection of PYM and DXM. The cosmetic appearance and function can be preserved at the most.

Adolescent ; Antineoplastic Combined Chemotherapy Protocols ; administration & dosage ; Bleomycin ; administration & dosage ; analogs & derivatives ; Child ; Dexamethasone ; administration & dosage ; Humans ; Injections ; Maxilla ; Neck ; Retrospective Studies ; Vascular Malformations ; drug therapy ; Veins ; abnormalities

OBJECTIVESince human mast cell is an important source of cytokines, it is of importance to understand the effects of anti-allergic drugs on cytokines modulation in mast cells. In the present study, we aimed at observing whether IL-4 could be released from human mast cell line (HMC-1) after the stimulation of PMA + A23187, and the effects of systemic glucocorticosteroid, dexamethasone, topical glucocorticosteroid, budesonide and H1 antagonist, desloratadine on IL-4 release and mRNA expression.

METHODSHMC-1 was stimulated with 25 ng/ml phorbol 12-myristate 13-acetate (PMA) and 2.5 x 10(-7) mol/L ionomycin (A23187) and cultured for 6 hours, 12 hours and 24 hours respectively in the presence or absence of 10(-6)-10(-10) mol/L concentrations of test drugs. Culture supernatants were collected and the levels of IL-4 were assayed by enzyme-linked immunosorbent assays (ELISA). The mRNA expression of IL-4 was measured by semiquantitative reverse transcription-polymerase chain reaction (RT-PCR).

RESULTSHMC-1 expressed IL-4 mRNA and the resulting protein production of IL-4 released after being stimulated with PMA plus A23187. Dexamethasone, budesonide and desloratadine had potent inhibitory effect on IL-4 release at any concentrations and time points, with significant deference (P < 0.05) compared to the control cells. The inhibitory effect did not show time-dependent and concentration-dependent manner. Desloratadine and budesonide showed neither up-regulatory nor down-regulatory effects on IL-4 mRNA expression at the test concentrations, however, desloratadine could down-regulate IL-4 mRNA expression.

CONCLUSIONSHMC-1 could express and produce IL4 after stimulation. Dexamethasone, budesonide and desloratadine all had inhibitory effects on IL-4 release from HMC-1. In addition, desloratadine could also inhibit the IL-4 mRNA expression.

Budesonide ; pharmacology ; Cell Line ; Dexamethasone ; pharmacology ; Humans ; Interleukin-4 ; biosynthesis ; Loratadine ; analogs & derivatives ; pharmacology ; Mast Cells ; drug effects ; metabolism ; Tetradecanoylphorbol Acetate ; pharmacology

BACKGROUNDNon-infectious endophthalmitis was reported to occur after cataract surgery or intravitreal injections. This study reported a series of patients having non-infectious endophthalmitis after pars plana vitrectomy in the same two operation rooms during the same period to estimate the risk factors for non-infectious endophthalmitis after vitrectomy.

METHODSMedical records of patients who presented with severe non-infectious endophthalmitis following vitrectomy between May 13 and June 8, 2011, were reviewed. The presenting symptoms and signs were collected, including visual acuity, intraocular pressure, cornea and anterior chamber activity. The treatments and results of microbiology examination were also recorded and analyzed.

RESULTSTen patients were identified with severe non-infectious endophthalmitis, presenting 1 day after pars plana vitrectomy. Three eyes (30%) had previous intraocular surgeries, four (40%) had proliferative diabetic retinopathy, and one (10%) got pars plana vitrectomy combined with phacoemulsification and intraocular lens implantation. All the patients were initially treated with topical and/or oral steroids. Only two patients had intravenous antibiotics because of the atypical presentation. One eye had paracentesis because of high intraocular pressure and the aqueous sample was sent for microbiological examination. The culture of the aqueous, air in the operation room, the swab from hand of surgeons, infusion fluid, and vitrectomy effluent were all negative for bacteria and fungi. The inflammation regressed rapidly after the initial treatment.

CONCLUSIONSIntraocular surgery history, poor general health status, longer operation time, and more surgical procedures are the risk factors for non-infectious endophthalmitis after vitrectomy. It responds well to steroids.

Adult ; Aged ; Dexamethasone ; administration & dosage ; Endophthalmitis ; drug therapy ; etiology ; Female ; Humans ; Intraocular Pressure ; Male ; Middle Aged ; Prednisolone ; administration & dosage ; analogs & derivatives ; Vitrectomy ; adverse effects

OBJECTIVETo explore the clinical efficacy and safety of lenalidomide plus low dose dexamethasone for treating patients with multiple myeloma (MM).

METHODSA total of 19 MM patients were enrolled to receive the therapeutic schedule of lenalidomide plus dexamethasone in our hospital from May 2013 to June 2015. Lenalidomide 25 mg was taken orally daily for 21 days and resting for 7 days, and dexamethasone 10 mg was taken orally daily on the day 1-4, 7-10 and 13-16. The regimens were Rd (lenalidomide and dexamethasone, n = 12), and RCd (lenalidomide, ifosfamide and dexamethasone, n = 7).

RESULTSAmong 19 patients received 1 cycle of treatment 3 patients achieved complete remission (CR), 3 patients achieved very good partial remission (VGPR), 10 patients achieved partial remission (PR) and 3 patients in stable disease (SD) with an overall response rate (ORR = CR + VGPR + PR) of 84%; their ORR rate was 89% after 2 cycles of treatment. In the early stage of treatment, the renal function was improved in 4 out of 5 patients with renal dysfunction. And the common adverse reactions were hematologic toxicity in 4 patients, 1 degree rash in 5 patients, and gastrointestinal side effects in 4 patients.

CONCLUSIONThe lenalidomide plus dexamethasone regimen has a good anti-multiple myeloma effect, which can control the disease rapidly and overcome the multidrug resistance in MM, improving the poor prognosis with renal dysfunction, and showing high remission rate in the patients exposed to bortezomib with low toxicity.

Antineoplastic Combined Chemotherapy Protocols ; Dexamethasone ; administration & dosage ; therapeutic use ; Humans ; Ifosfamide ; therapeutic use ; Multiple Myeloma ; drug therapy ; Remission Induction ; Thalidomide ; administration & dosage ; analogs & derivatives ; therapeutic use

This study was aimed to compare the efficacy and adverse effects of PD (bortezomib + dexamethasone) and VAD (vincristine + adriamycin + dexamethasone) as regimens for treatment of multiple myeloma patients. 21 and 31 multiple myeloma patients were enrolled in the PD and VAD groups respectively which received 2 to 5 courses of treatments, and both clinical effects and adverse reactions were observed. In the all 52 patients, 48 were newly diagnosed and the other 4 patients had accepted 1 to 2 courses of M2 or MP treatment, but didn't get PR. In 52 patients, 4, 4, 8 and 5 patients accepted 2, 3, 4 and 5 courses of PD regimen respectively, while 6, 11, 12 and 2 patients accepted 2, 3, 4 and 5 courses of VAD regimen respectively. The results indicated that the rate of good efficacy (both CR and VGPR) in PD group was 57.1%, while the rate of good efficacy in VAD group was 16.1%, there was significant difference (p = 0.0052). The percentage of patients who got CR, VGPR and PR in PD and VAD groups were 95.2% and 74.2% respectively, there was no significant difference (p = 0.1108). The incidences of adverse effects in 2 groups were similar, which included hematological toxicity, liver and kidney functional lesion, peripheral neuropathy, infection, interstitial pneumonia. It is concluded that compared with conventional VAD chemotherapy, PD may improve CR and VGPR rate in newly diagnosed patients with multiple myeloma, meanwhile it does not bring about more and worse toxicity.
Adult ; Aged ; Antineoplastic Combined Chemotherapy Protocols ; therapeutic use ; Bleomycin ; analogs & derivatives ; therapeutic use ; Dexamethasone ; therapeutic use ; Doxorubicin ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Multiple Myeloma ; drug therapy ; Treatment Outcome ; Vincristine ; therapeutic use

The objective was to explore the in vitro effects of growth inhibition and apoptosis induction of 2-methoxyestradiol (2ME2), an estrogen derivative, on seven myeloma cell lines NCI-H929, HS-sultan, KM3, SKO-007, CZ-1, U266 and LP-1and to observe its synergistic effects in combination with some other drugs, such as dexamethasone, As(2)O(3), thalidomide and zoledronic acid. Seven myeloma cell lines NCI-H929, HS-sultan, KM3, SKO-007, CZ-1, U266 and LP-1 were cultured at different concentrations with or without dexamethasone, As(2)O(3), thalidomide and zoledronic acid. Cell viability was assessed by trypan blue assay, plasma cell labeling index (PCLI) was detected by BrdU assay, terminal-deoxynucleotidyl transferase mediated dUTP nick end labeling (TUNEL) assay were used to determine apoptosis cells in situ. Synergistic effects of 2ME2 in combination with other drugs were judged by King's formula. The results showed that after treatment with 1, 4, 8, 12, 16 micromol/L 2ME2 at 12, 24, 36 and 48 hours respectively, 2ME2 caused a dose- and time-dependent inhibition of the cell viability. The concentration of 50% growth inhibition (IC(50)) was between (20.8 +/- 0.27) and (34.1 +/- 0.57) micromol/L. After treatment with 12 micromol/L 2ME2 within 24 hours, 2ME2 led to a progressive decline in the fraction of S-phase cells by BrdU assay, plasma cell labeling index (PCLI) declined from (30.14 +/- 4.28)% to (14.71 +/- 6.27)% (P < 0.05). After treatment with 1, 4, 8, 12, 16 micromol/L 2ME2 at 12, 24, 36 and 48 hours respectively, 2ME2 can induce a dose- and time-dependent apoptosis of myeloma cell lines. The percentage of apoptosis was between 9% - 33% (P < 0.05). Q value of synergistic effects was between 1.13 to 1.43. It is concluded that 2ME2 can inhibit proliferation and induce apoptosis of myeloma cell lines and has synergistic effects with dexamethasone, As(2)O(3), thalidomide and zoledronic acid.
Apoptosis ; drug effects ; Arsenicals ; pharmacology ; Cell Proliferation ; drug effects ; Dexamethasone ; pharmacology ; Dose-Response Relationship, Drug ; Drug Synergism ; Estradiol ; analogs & derivatives ; pharmacology ; Humans ; Multiple Myeloma ; pathology ; Oxides ; pharmacology ; Time Factors ; Tumor Cells, Cultured