OBJECTIVETo observe clinical therapeutic effect of superficial needling at distal and proximal acupoints on primary dysmenorrhea (PD).

METHODSOne hundred and twenty cases of PD were randomly divided into a treatment group (n =60) and a control group (n = 60). The treatment group were treated with superficial needling at Sanyinjiao (SP 6) and the control group with oral administration of indometacin entric-coater tablets.

RESULTSOf the 120 cases, 116 cases completed the investigation. The total effective rate was 93. 3% in the treatment group and 75. 0% in the control group. The comprehensive therapeutic effect and the cured rate in the treatment group were significantly better than that in the control group (P<0. 001), with a more rapid effect and lasting a longer time than the control group.

CONCLUSIONClinical therapeutic effect of superficial needling at Sanyinjiao (SP 6) on primary dysmenorrhea is better than that of oral administration of indometacin entric-coater tablets.

Acupuncture Therapy ; Adult ; Dysmenorrhea ; therapy ; Female ; Humans ; Indomethacin ; administration & dosage ; therapeutic use ; Tablets, Enteric-Coated

OBJECTIVE: To compare the clinical efficacy between herb-separated moxibustion and conventional moxibustion on ankylosing spondylitis (AS) based on oral administration of sulfasalazine enteric-coated tablets. METHODS: A total of 64 patients with AS of cold-dampness obstruction type were randomly divided into an herb-separated moxibustion group and a conventional moxibustion group, 32 cases in each one. Based on oral administration of sulfasalazine enteric-coated tablets, the patients in the conventional moxibustion group were treated with moxibustion at the area with Dazhui (GV 14) to Changqiang (GV 1) as center and about 10 cm in width; the moxibustion was given for 1 hour. In the herb-separated moxibustion group, the gauze was soaked in the medicinal liquor and ginger juice, and placed on the same moxibustion area as the conventional moxibustion group, followed by moxibustion for 1 hour. The treatment in the two groups was given once a week, three treatments constituted a course and totally three courses were given. The symptom quantification score, occipital-wall distance, Schober test, C-reactive protein (CRP) and erythrocyte sedimentation rate (ESR) levels were observed before and after treatment in the two groups, and the clinical efficacy was evaluated. RESULTS: Compared before treatment, the symptom quantification score, occipital-wall distance, CRP and ESR levels were lower but the Schober test was higher after treatment in the two groups (all <0.05). The symptom quantification score, Schober test, CRP and ESR levels in the herb-separated moxibustion group were superior to those in the conventional moxibustion group (all <0.05), but no significant difference was observed on occipital-wall distance (>0.05). The total effective rate was 90.0% (27/30) in the herb-separated moxibustion group, which was higher than 73.3% (22/30) in the conventional moxibustion group (<0.05). CONCLUSION The herb-separated moxibustion combined with sulfasalazine enteric-coated tablets has significant efficacy for AS with cold-dampness obstruction type, which could obviously relieve pain symptoms, improve occipital-wall distance, Schober test and other physical signs, and improve the quality of life.
Acupuncture Points ; Humans ; Moxibustion ; Quality of Life ; Spondylitis, Ankylosing ; therapy ; Sulfasalazine ; Tablets, Enteric-Coated ; Treatment Outcome

OBJECTIVETo prepare the gastric retenting and chronopharmacologic drug delivery tablets containing sinomenine hydrochloride as a model drug, evaluate the effects of the coating layers formulation and technics on drug release behavior, and to elucidate the mechanism of drug release based on obtained results.

METHODThe gastric retenting and chronopharmacologic drug delivery tablets were prepared by press-coated technics. The types of disintegrants were chosen according to the expanding rate and the lag-time. The effects of formulation and technics of coating layer on the release characteristic of the drug were investigated by dissolution testing. The mechanism of drug release was proved by erosion test.

RESULTThe tablets had typical chronopharmacologic drug delivery properties with a lag time followed by a rapid release phase. CMS-Na was selected as the disintegrant. The lag-time was prolonged with the increase of the ratio of HPMC/carrrageenan and the amount of matrix material in coating layer. The compressing pressure and preparation method of coat material had minor influence on the lag-time of the tablets. Coating layer erosion and tablet core swelling were involved in the mechanism of drug release.

CONCLUSIONThe tablets had typical chronopharmacologic drug delivery properties. A suitable lag-time can be achieved by adjusting formulation of coating layer to meet the requirement of chronotherapy.

Chemistry, Pharmaceutical ; Drug Chronotherapy ; Drug Delivery Systems ; methods ; Humans ; Morphinans ; chemistry ; pharmacokinetics ; Stomach ; drug effects ; Tablets, Enteric-Coated ; chemistry ; pharmacokinetics

OBJECTIVETo explore the best technique parameters on preparing ophiopogon japonicus saponin enteric microsphere by spray drying technique.

METHODThe best technique parameters were investigated by orthogonal experimental design and by the target, such as surface appearances, encapsulated efficiency, etc.

RESULTThe best technique parameters included the inlet temperature (90 degrees C ), the feeding speed (10 mL x min(- 1)), and the rotate speed of atomizer (50 r x min(-1)).

CONCLUSIONOphiopogon japonicus saponin enteric microsphere accorded with the expecting demand. The main influencing factor was inlet temperature . It is suitable to industrialize in preparing Traditional Chinese Medicine microsphere.

Drug Compounding ; methods ; Microscopy, Electron ; Microspheres ; Ophiopogon ; chemistry ; Plants, Medicinal ; chemistry ; Saponins ; chemistry ; isolation & purification ; Tablets, Enteric-Coated ; chemistry ; Temperature

OBJECTIVETo explore the pharmacokinetics and bioequivalence of two kinds of enteric coated tablet of Zhengqing Fengtongning.

METHODA single dose of 45 mg kg(-1) test or reference preparation was administrated by randomized crossover way in 12 rabbits. The plasma concentrations of drug were determined by HPLC. The pharmacokinetics parameters and relative bioequivalence were calculated with 3p97 program.

RESULTThe concentration curves based on drug-time of both test and control preparations were presented by one-compartment model, tmax were (0.81 +/- 0.34), (0.60 +/- 0.30) h respectively, Cmax were (11.16 +/- 0.58), (11.90 +/- 1.44) microg mL(1) respectively, AUC(0-->t) were (61.58 +/- 6.70), (60.56 +/- 6.67) microg h mL(-1) respectively, relative bioavailability was (102.77% +/- 15.63)%. Suggesting no significant diffirence between the main pharmacokinetic parameters of two prepations.

CONCLUSIONThe two preparations are bioequivalent.

Animals ; Biological Availability ; Cross-Over Studies ; Drugs, Chinese Herbal ; pharmacokinetics ; Female ; Male ; Rabbits ; Random Allocation ; Tablets, Enteric-Coated ; Therapeutic Equivalency

We investigated the single- and multiple dose pharmacokinetics of a new controlled-release formulation (Orfil retard enteric coated tablet) of valproic acid in comparison with those of the plain tablet as a reference. Twelve healthy volunteers were given each formulation of 300 mg in the single-dose study. In the steady-state multiple-dose study, twelve epileptic patients received 1200 mg/day of the reference drug (300 mg 9 AM, 300 mg 3 PM, 600 mg 9 PM) and the test formulation (600 mg 9 AM, 600 mg 9 PM) with at least one week interval in cross-over manner. The AUC values of the test controlled release formulation were 91.7% (95% confidence interval: 78.4-100.4%) of the reference drug in the single-dose study and 98.2% (95% confidence interval: 86.2%-109.9%) in the steady-state study. The AUC's of the two formulations were not significantly different by ANOVA test. The Cmax and Tmax values of the test formulation were significantly different from the values of the reference in single-(Tmax: 158.4%, Cmax: 52.5% of the reference) and multiple-dose study (Tmax: 153.5% of the reference). The MRT values of the test formulation were also significantly greater (129.4% of the reference) in the single-dose study. Regarding the controlled-release characteristics of the test formulation, fluctuation index and percentage fluctuation of the twice a day dosage regimen of the test formulation were comparable with those of the thrice a day dosage regimen of the conventional tablet. Area deviation was even smaller in the test regimen of the controlled release formulation.(ABSTRACT TRUNCATED AT 250 WORDS)
Administration, Oral ; Adult ; Biological Availability ; Delayed-Action Preparations ; Epilepsy/blood/*drug therapy ; Humans ; Male ; Tablets ; Tablets, Enteric-Coated ; Valproic Acid/*pharmacokinetics

OBJECTIVE: Duloxetine hydrochloride is a selective serotonin (5-hydroxytryptamine) and norepinephrine reuptake inhibitor. It is approved for effective treatment for major depressive disorder. The pharmacokinetics (PK) of duloxetine has been studied, but few pharmacokinetics properties in Chinese subjects are available. This study explored the dose proportionality and determined duloxetine levels in human plasma by comparing the PK properties after administration of single or multiple doses in healthy volunteers. METHODS: Thirty-six subjects were divided randomly into three groups and received a single dose of 15, 30, or 60 mg duloxetine. Those who received 30 mg continued on to the multiple-dose phase and received 30 mg daily for 7 days. Liquid chromatography/mass spectroscopy was applied to determine concentrations. The PK properties were calculated and included maximum plasma concentration (Cmax), time when maximum plasma concentration was reached (Tmax), time when half-maximum plasma concentration was reached (t1/2), area under the plasma concentration-time curve from time zero to the last measurable concentration (AUC0-t), mean concentration levels (AUC0-infinity), and apparent total clearance of the drug from plasma after oral administration (CL/F). RESULTS: The standard calibration curve was linear in the concentration range 0.11-112 ng/ml (r>0.992). Linear PK properties were found at doses of 15-60 mg. The Cmax and AUC were proportional to dose, but the Tmax and t1/2 did not increase with increasing dose. CONCLUSION: No significant differences in the PK parameters were found among the three groups during the single-dose phase. The AUC and Cmax were greater in the multiple-dose phase, indicating duloxetine accumulation following multiple-dose administration.
Administration, Oral ; Area Under Curve ; Asian Continental Ancestry Group ; Calibration ; Depressive Disorder, Major ; Humans ; Norepinephrine ; Plasma ; Serotonin ; Spectrum Analysis ; Tablets, Enteric-Coated ; Thiophenes ; Duloxetine Hydrochloride

OBJECTIVETo prepare enteric coated pellets containing panax notoginseng saponins.

METHODPanax notoginseng saponins loaded pellets were prepared by Extrusion-Spheronization method, and coated by Eudragit L30D-55 using Glatt fluid bed with the bottom spray process, central composite design was used to optimize the coating prescription.

RESULTThe drug release of enteric coated pellets of panax notoginseng saponins pellets would be lower than 5% in 2 h in simulated gastric fluid, but reach above 85% in 3 h in simulated human gastroenteric environment.

CONCLUSIONThe enteric coated pellets of panax notoginseng saponins have good acid residence to avoid panax notoginseng saponins from degrading in gastric acid.

Chemistry, Pharmaceutical ; methods ; Drug Stability ; Gastric Acid ; chemistry ; Gastrointestinal Tract ; drug effects ; Humans ; Models, Biological ; Panax notoginseng ; chemistry ; Saponins ; chemistry ; pharmacokinetics ; Tablets, Enteric-Coated ; chemistry

The study is to prepare taste masking and enteric-coated clarithromycin granules by melting and fluid bed coating technology. Clarithromycin and matrix materials were melted at a certain temperature, and then made into particles by fluidized bed coating. X-ray powder diffraction and scanning electron microscopy were used to identify the crystal and morphology of drug loading granules. In vitro dissolution method was used for the observation of the drug release behavior. The results showed that the drug particles size range was 0.2 - 0.6 mm; the crystal form of clarithromycin in the granule did not change; enteric-coated granules accumulated release in 0.1 mol L(-1) hydrochloric acid in 2 h was less than 10%, while in pH 6.8 phosphate buffer in 1 h was more than 80%. The taste masking and enteric-coated clarithromycin granules not only have good taste masking effect, but also have a good release behavior. It is expected to have better clinical application.
Clarithromycin ; administration & dosage ; chemistry ; Crystallization ; Drug Carriers ; Drug Compounding ; methods ; Excipients ; chemistry ; Microscopy, Electron, Scanning ; Particle Size ; Tablets, Enteric-Coated ; Taste ; Technology, Pharmaceutical ; methods ; X-Ray Diffraction

The present research was aimed to develop a high performance liquid chromatography (HPLC) method to determine oxaprozin in plasma and to evaluate the bioavailability of two oxaprozin enteric coated tablets. A C18 column was used to separate the plasma after protein precipitation and the mobile phase was methanol-12. 5mmol/L ammonium acetate buffer solution (pH=3.0)(71:29). The calibration curve was linear in the concentration range of 0. 50-70. 56 microg . mL-1, and the intra and inter-day RSDs were less than 12. 33% and 10. 42% respectively. A single dose of 0. 4 g reference preparation or test preparation of oxaprozin enteric coated tablets was administered to 20 healthy volunteers according to a randomized crossover study. AUC0-->264h were (4 917. 44 +/- 629. 57) microg . h . mL-1 and (4 604. 30+/-737. 83) microg . h . mL-1, respectively; Cmax were (52. 34+/-7. 68) microg . mL-1 and (48. 66+/-4. 87) microg . mL-1, respectively; Tmax were (18. 70+/-2.27) h and (19. 30+/-1. 63) h, respectively; The relative bioavailability of test preparation was 94.0% +/- 13. 7%. The method is simple, rapid and selective for oxaprozin determination. There is no significant difference in the main pharmacokinetic parameters between the test formulation and reference formulation and the two formulations are in bioequivalence.
Anti-Inflammatory Agents, Non-Steroidal ; blood ; pharmacokinetics ; Biological Availability ; Chromatography, High Pressure Liquid ; Cross-Over Studies ; Humans ; Propionates ; administration & dosage ; blood ; pharmacokinetics ; Tablets, Enteric-Coated