Preparation and evaluation of sirolimus sustained release tablets based on mesoporous silicon loaded self-microemulsion / 药学学报

Sirolimus self-microemulsion-mesoporous silicon sustained release tablets were prepared in order to improve the dissolution of the insoluble drug sirolimus and reduce its side effects. Firstly, sirolimus self-microemulsion was prepared and cured with mesoporous silicon. Secondly, the suitable excipients were selected according to the appearance, hardness and in vitro release rate. The sustained-release tablets with hydroxypropyl methylcellulose (HPMC) as skeleton material were prepared by powder direct pressing method, and the formulation was optimized by central composite design-response surface method to investigate the drug release in vitro. Finally, the pharmacokinetics was carried out in beagle dogs using the commercial sirolimus tablets as references. The final formulation of sustained-release tablets is as follows: 162 mg of sirolimus self-microemulsion-mesoporous silica (1∶1, w/w), 80 mg of HPMC K4M and 80 mg of carboxymethyl starch sodium, the microcrystalline cellulose is 168 mg. The results of in vitro release test showed that the self-made sustained-release tablets released slowly within 12 h, which conformed to the Ritger-Peppas model. The in vivo test results showed that compared with the commercial sirolimus tablets, the Cmax of the sustained-release tablets decreased by 49.47%, the Tmax of the sustained-release tablets was prolonged by 5.1 times, and the relative bioavailability was 105.81%. Sirolimus self-microemulsion-mesoporous silicon sustained-release tablets have good sustained-release effects in vitro and in vivo, which provides a reference for the solubilization of other insoluble drugs and the research and development of sustained-release preparations. Animal experiments and welfare processes were reviewed and approved by the Animal Ethics Committee of the 900TH Hospital of the Joint Logistics support Force.

Preparation and enhanced photodynamic therapy of supramolecular nanoparticles to overcome tumor hypoxia / 药学学报

The therapeutic effect of tumor photodynamic therapy is severely limited by the hypoxic tumor microenvironment. Inhibiting tumor celloxygen consumption is a more effective way than increasing its oxygen supply to overcome the tumor hypoxia and enhance photodynamic therapy. To carry out this strategy, the supramolecular nanoparticles VER-ATO-SMN loaded with photosensitizer verteporfin (VER), oxygen-consuming inhibitor atovaquone (ATO), and stabilizer polyvinylpyrrolidone (PVP)-K30 were prepared by the nanoprecipitation method, and the optimal prescription was screened and optimized by single factor experiments. The results showed that the optimal prescription for VER-ATO-SMN was ATO∶VER (w/w) = 1∶1, PVP-K30 = 100 mg, N,N-dimethylformamide∶water (v/v) = 1∶10. The morphology, particle size, particle dispersion index and encapsulation efficiency of supramolecular nanoparticles were characterized. The VER-ATO-SMN showed a spherical morphology and was well dispersed. The hydrodynamic size of VER-ATO-SMN was 101.21 ± 4.30 nm as determined by dynamic light scattering (DLS). The encapsulation efficiencies of VER and ATO in VER-ATO-SMN prepared with the optimal prescription were 70.86% and 77.52%, respectively. The VER-ATO-SMN exhibited good laser stability and also showed high stability in conditions which simulated the physiological solution. Compared with free VER and VER liposome, VER-ATO-SMN performed enhanced therapeutic effect at the cell level. The mechanism was that VER-ATO-SMN could effectively incorporate into cells and improving the intracellular oxygen concentration by reducing the oxygen consumption of tumor cells could increase the amount of reactive oxygen species generated by VER mediated photodynamic therapy. The in vivo anticancer efficacy results of tumor-bearing mice suggested that VER-ATO-SMN could effectively inhibit the tumor growth or even completely eliminate the tumor. All animal experiments were performed in line with national regulations and approved by the Animal Experiments Ethical Committee of 900 Hospital of the Joint Logistics Team.

Effect of wuzhi capsules on the blood concentration of tacrolimus relative to diltiazem and CYP3A5 gene polymorphisms / 药学学报

To determine the relationship between the effect of wuzhi capsules on the blood concentration of tacrolimus as compared to diltiazem and with regard to cytochrome P450 (CYP)3A5 gene polymorphisms, 170 patients who underwent renal transplantation from November 2014 to March 2018 and used tacrolimus combined with diltiazem 30 mg bid were selected in this study retrospectively. Patients were divided into an observation group (105 patients) and a control group (65 patients) according to whether they used wuzhi capsules after the operation. The polymorphisms of CYP3A5*3 were determined and the effect of wuzhi capsules on the blood concentration of tacrolimus, as compared with that of diltiazem was determined in patients with different CYP3A5*3 genotypes. This study complies with relevant ethical norms. The results show that compared with diltiazem, an increase of tacrolimus C0/D was significantly correlated with the patient's CYP3A5*3 genotype in both the self-control and the control group. CYP3A5 expressers in the observation group were able to increase the tacrolimus C0/D by about 76.8% by replacing the wuzhi capsules with diltiazem, but this effect was not observed in CYP3A5 non-expressers. In CYP3A5 expressers wuzhi capsules had a greater ability relative to diltiazem to increase the blood concentration of tacrolimus.

Preparation of silymarin solid dispersions and dissolution rates of five constituents / 中成药

AIM To prepare silymarin solid dispersions and to evaluate the dissolution rates of five constituents.METHODS Taking F68 and PVPk30 as a combined carrier,the solid dispersions were prepared by solvent fusion method.Then the effects of combined carrier ratio and drug-carrier ratio on dissolution rates of silybin,isosilybin,silydianin,silycristin and taxifolin were investigated.RESULTS The optimal conditions were determined to be 1 ∶ 3 for combined carrier ratio,and 1 ∶ 5 for drug-carrier ratio.These five constituents displayed much higher dissolution rates in solid dispersions than those in raw medicine and physical mixture (silymarin-carrier).CONCLUSION Solid dispersions can significantly increase the dissolution rates of effective components in silymarin.

Preparation of mesoporous silica nanoparticles in different pore size and its use in the solidification of sirolimus loaded self-microemulsifying drug delivery system / 药学学报

The mesoporous silica nanoparticles (MSN) in different pore size and sirolimus (SRL) loaded self-microemulsifying drug delivery system (SMEDDS) were prepared. The results in morphology were collected by scanning electron microscope, transmission electron microscope, small-angle X-ray diffraction, and N2 adsorption-desorption. The results showed that the prepared MSN has ordered nanochannels with a pore size of 6.3, 8.1, 10.8 nm, respectively. The particle size of SRL-SMEDDS were measured by particle sizing system, which was 20.6±1.3 nm. The stirring method was developed to prepare SRL-SMEDDS-MSN. It was found that the optimal ratio of SRL-SMEDDS to MSN was 2:1, while the drug loading rate was near 0.83%, and the flow properties of SRL-SMEDDS-MSN were of good condition. The differential scanning calorimetry results proving a molecular or amorphous dispersed state of SRL in MSN while the suspension experiment has shown great reconstitution properties of SRL-SMEDDS-MSN. There is no significant influence on maximum drug release rate of different pore size of SRL-SMEDDS-MSN in 250 mL water within 2 h, while the results of the first 40 min have an obvious difference. Above all, MSN might provide a new strategy for the solidification of SMEDDS.

Progress in study of spectrum-effect relationship of traditional Chinese medicine and discussions / 中国中药杂志

Spectrum-effect relationship of traditional Chinese medicine is a scientific method based on fingerprint of traditional Chinese medicine, which studied the correlations between fingerprint and activity. The method revealed the activity related peaks and clarified the active components. It provided directions and thoughts for the clarification of pharmacodynamic material basis and establishment of evaluation method to reflect the inherent quality of traditional Chinese medicine. In this text we would make a systematic review about the progress in the study of spectrum-effect relationship of traditional Chinese medicine after summarized the latest years of investigations from researchers at home and abroad, including the establishment of fingerprint, efficacy evaluation, and data processing. The key problems in each part were clarified and corresponding discussions were made, providing thoughts and advices for the following study of spectrum-effect relationship of traditional Chinese medicine. At last we made a expecting on the development trend of spectrum-effect relationship of traditional Chinese medicine.

Fingerprint and spectrum-effect relationships on Tripterygium glycosides preparation / 中国中药杂志

Tripterygium glycosides preparation which extracted from the traditional Chinese herb Tripterygium wilfordii (TWHY), was widely used to treat the autoimmune diseases. Previous works demonstrated that TWHF had potent anti-inflammatory and immunosuppressive properties. But the different quality and high incident rate of side effects of different manufactures inhibited its clinical application. Since TWHF had been generally known to play a therapeutical effect by synergism of multiple constituents, it was necessary to build the relationship between the HPLC fingerprint and bioactivity so as to ensure the quality safety and efficacy. The HPLC fingerprint showed that description and content of peaks from different manufactures were diverse. Only 11 common peaks were found. In this study, mice spleen cells stimulated by Con A were used to test the proliferation inhibition bioactivity of TWHF preparations, which were incubated with 30, 15, 7.5, 3.75, 1.88 and 0.94 mg x L(-1) TWHF preparations for 48 h. The results showed that mice spleen cells proliferation was inhibited by all TWHF preparations significantly compared with the control group, which suggested the TWHF preparations showed immune suppress activity. The TWHF preparations from 7 manufacture showed different IC50 value, which might belong to different contents which showed in the HPLC fingerprint. Moreover, a relationship between the HPLC fingerprint and the bioactivity were established to identify important constituents by grey relational analysis (GRA). The result showed that all the contents were relative with the IC50, especially No. 5 and 10 peaks, but No. 1 peak, which was proved to be triptolide, had few contribute to the inhibition of mice spleen cells proliferation. The study of relationship between the HPLC fingerprint and the IC50 by GRA could help to investigate mechanism of bioactive and provide an evidence for the quantification of multi-constituents.

Isolation, purification and identification of polysaccharides from Gynura divaricata / 中国中药杂志

The purpose of this study was to isolate and purify polysaccharide from Gynura divaricata and analyze its monosaccharide composition. A water-soluble crude polysaccharide was obtained by hot water extraction, ethanol precipitation and deproteinization after degreasing. The crude polysaccharide then purified with DEAE-Sepharose Fast Flow column chromatography and dialysis. The monosaccharide composition and structure were analyzed by HPLC, UV spectrophotometer and 1H-NMR. The results showed that the purity and molecular weight of GDPS-2 and GDPS-3 were 87.3%, 2.03 x 10(4) Da and 90.9%, 4.29 x 10(4) Da, respectively. The UV spectrophotometer and 1H-NMR data suggested that glycosidic bond of GDPS-2 and GDPS-3 were a type. Both GDPs-2 and GDPs-3 were homogeneous polysaccharides, and GDPs-2 was mainly composed of glucuronic acid and xylose at a molar ratio of 1.1:0.63. GDPs-3 was mainly composed of rhamnose, glucuronic acid, galactose, xylose and galacturonic acid at a molar ratio of 0.32:6.0:0.21:1.75:4.3.

Progress of animal research on electro-acupuncture treatment for depression(△) / 中国医学科学杂志(英文版)

This paper summarized the Chinese literatures in the previous 5 years about the pre-clinical animal researches on the application of electro-acupuncture (EA) treatment for depression, searched in China National Knowledge Infrastructure (CNKI). The efficiency of EA treatment for depression and the mechanism of it were discussed, to shed light on new ideas and new fronts for the further research on depression in clinical or pre-clinical fields.

Effects of electroacupuncture on circadian rhythm of temperature and melatonin in depression rats model induced by chronic stress / 中国针灸

<p><b>OBJECTIVE</b>To observe the effects of electroacupuncture (EA) on circadian rhythm of temperature and melatonin (MT) in depression rats model induced by chronic stress, so as to explore the biological mechanism of EA for depression.</p><p><b>METHODS</b>Twenty-four SD rats were randomly divided into a control group, a model group and an EA group, 8 cases in each one. Rats in the control group were treated with normal diet for 21 days without any treatment. In the model and EA group, rat model was established by chronic unpredictable stress combined with solitarily feeding method, and rats in the EA group was treated with EA at "Baihui" (GV 20), "Yintang" (GV 29) 1 h before stress stimulation everyday, 2 Hz in frequency and intensity was favorable with the head of rat slightly shivering. The needles were retained for 20 min, once a day for totally 21 days. After EA treatment, open-field experiment was adopted to observe the behavioral improvement; the rats temperatures were monitored at six time points (2:00, 6:00, 10:00, 14:00, 18:00, 22:00) and orbital blood sampling was collected. The level of serum MT was tested by enzyme linked immunosorbent assay. The circadian rhythm changes of temperature and serum MT in each group were compared.</p><p><b>RESULTS</b>The numbers of horizontal movement and vertical movement in the model group were obviously lower than those in the control group (both P < 0.05), while those in the EA group were significantly improved compared with those in the model group (both P < 0.01). The circadian rhythm of temperature and MT disappeared in the model group, which was improved into normal level after EA treatment.</p><p><b>CONCLUSION</b>The electroacupuncture has regulation effects on circadian rhythm of temperature and melatonin in depression rat model induced by chronic stress.</p>

Effect of propranolol gel on infantile hemangiomas / 中华整形外科杂志

<p><b>OBJECTIVE</b>To evaluate the efficacy and security of propranolol gel in treatment of Infantile hemangiomas.</p><p><b>METHODS</b>51 consecutive infants with hemangiomas from October 2010 to September 2011 in Department of General Surgery Fuzhou General Hospital of Nanjing Military Command were treated with propranolol hydrochloride 3% gel. Changes in hemangioma size, texture, color, tumor blood flow peak were recorded.</p><p><b>RESULTS</b>The results were evaluated using Achauer system, responses of IHs to propranolol were considered scale I (poor) in 4 patient (17.24%), scale II (moderate) in 18 patients (24.14%), scale III (good) in 22 patients (44.83%) and scale IV (excellent) in 7 patients (13.79%). The response of superficial hemangiomas was significantly better than other hemangiomas (P < 0.05), and no significant differences in response among different primary sites (P > 0.05).</p><p><b>CONCLUSIONS</b>Topical use of propranolol hydrochloride 3% gel is an effective option for superficial hemangiomas.</p>

Validation and comparison of pharmacogenetics-based warfarin dosing algorithms in Han Chinese patients / 中华心血管病杂志

<p><b>OBJECTIVE</b>To assess whether the existing three types of pharmacogenetics-based Warfarin dosing algorithms appropriately predict the actual maintenance dose in Han Chinese mechanical heart valve replacement patients (n = 130).</p><p><b>METHODS</b>The patients' CYP2C9 and VKORC1 genetic polymorphisms were detected by PCR-RFLP. The genotype of CYP2C9, VKORC1 and other information were used to calculate predicted doses. Accuracy of the models was assessed using the absolute value of the difference between predicted dose and actual dose, calculated on both an absolute and percentage basis. Actual weekly dose was also regressed on predicted weekly dose, from which we obtained R(2) values. Clinical accuracy of the predictions was assessed by computing the proportion in which the predicted dose was 20% or more below the actual dose (under dosed), within 20% of the actual dose (ideally dosed), or 20% or greater above the actual dose (over dosed).</p><p><b>RESULTS</b>The average absolute error is the smallest for the predictions made by the Wen model (3.74 mg/wk), followed by the Ohno model (4.07 mg/wk) and IWPC model (5.05 mg/wk). R(2) was 40.2% in the Wen model, 38.2% in the Ohno model and 26.7% in the IWPC model. When comparing the percentage of patients for whom the predicted doses were ideal, the Wen model works the best (50.0%) in low-dose group (≤ 21 mg/wk), but the Ohno model works the best (85.29%) in middle-dose group (21 - 49 mg/wk), followed by the Wen model.</p><p><b>CONCLUSION</b>The best accuracy is achieved by the Wen model and the best clinical accuracy is obtained by the Ohno model for predicting the actual maintenance dose in Han Chinese mechanical heart valve replacement patients.</p>

Effect of CYP3A4*18B, CYP3A5*3 gene polymorphism on dosage and concentration of tacrolimus in renal transplant patients / 药学学报

The effect of CYP3A4*18B and CYP3A5*3 on concentration/dosage x body surface area ratios (C/D'), adverse effects and acute rejection of tacrolimus in renal transplant patients were investigated. The CYP3A4*18B genotypes of 227 renal transplant patients were determined by PCR-RFLP method. The differences of C/D' ratios, adverse reactions and acute rejection were compared among all of the genotype groups treated with tacrolimus. The frequencies of CYP3A4*18 and CYP3A5*3 alleles in renal transplant patients were 30.8% and 74.2%, respectively. No significant association was found between the C/D's of tacrolimus and CYP3A4*18B genotypes when they were classified by two CYP3A5 genotypes (P > 0.05). While after the effects of CYP3A4*18B genotype were eliminated, the C/D' ratio of tacrolimus in patients with CYP3A5*1/*1 and *1/*3 genotype group was significantly lower than those with CYP3A5*3/*3 genotype groups (P < 0.01). There is no significant difference in adverse effects and acute rejection among different genotypes (P > 0.05).

Preparation of in situ gel systems for the oral delivery of ibuprofen and its pharmacokinetics study in beagle dogs / 药学学报

The in situ gel systems can form gel in situ after administration to achieve sustained release, thus provides a promising strategy for drug delivery systems. The aim of this study was to design and prepare in situ gel systems for the oral delivery of ibuprofen (IBU-ISG) and study its pharmacokinetics in Beagle dogs. The characteristics of the basic material of gellan gum (Kelcogel, Kel) and sodium alginate (Manugel, M) were studied through investigating the complex viscosity of the Kel or M solution with or without different concentrations of calcium ion or sodium citrate to ascertain the amount range of the excipients. The measurement of complex viscosity of the solution (0. 5% Kel and 1% M) with different concentrations of sodium citrate and calcium ion was carried out to select the suitable proportion of calcium ion and sodium citrate. The formulation of binary IBU-ISG was optimized by monitoring the complex viscosity before gelling in vitro release property. The optimized formulation contains 1.0% sodium alginate, 0.5% gellan gum, 0. 21% sodium citrate and 0.056% calcium chloride. A single oral dose of IBU-ISG and reference formulation (IBU suspension) were given to each of the 6 healthy Beagle dogs, ibuprofen in plasma at different sampling times was determined by RP-HPLC. The pharmacokinetics parameters in 6 Beagle dogs were calculated. The Tmax of IBU-ISG and reference formulation were (1.8 +/- 0.6) and (0.4 +/- 0. 1) h. The Cmax values were (29.2 +/- 7.6) and (37.8 +/- 2.2) microg x mL(-1). The T(1/2) were (2.3 +/- 0.5) and (2.0 +/- 0.9) h, and the AUC(0-t) were (131.0 +/- 38.6) and (117.3 +/- 23.1) microg x mL(-1) x h, respectively. The binary IBU-ISG was successfully prepared.

Studies on preparation of sustained-release Shuxiong formulation, a traditional Chinese medicine compound recipe, using time-controlled release techniques / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare a sustained-release formulation of traditional Chinese medicine compound recipe by adopting time-controlled release techniques.</p><p><b>METHOD</b>Shuxiong tablets were chosen as model drug. The prescription and technique of core tablets were formulated with selecting disintegrating time and swelling volume of core tablets in water as index. The time-controlled release tablets were prepared by adopting press-coated techniques, using PEG6000, HCO and EVA as coating materials. The influences of compositions, preparation process and dissolution conditions in vitro on the lag time (T(lag)) of drug release were investigated.</p><p><b>RESULT</b>The composition of core tablets was as follow: 30% of drug, 50% MCC and 20% CMS-Na. The T(lag) of time-controlled release tablets was altered remarkably by PEG6000 content of the outer layer, the amount of outer layer and hardness of tablet. The viscosity of dissolution media and basket rotation had less influence on the T(lag) but more on rate of drug release.</p><p><b>CONCLUSION</b>The core tablets pressed with the optimized composition had preferable swelling and disintegrating properties. The shuxiong sustained-release formulations which contained core tablet and two kinds of time-controlled release tablets with 3 h and 6 h of T(lag) could release drug successively at 0 h, 3 h and 6 h in vitro. The technique made it possible that various components with extremely different physicochemical properties in these preparations could release synchronously.</p>

Preparation of Shuxiong micropellets by centrifugal granulation technology / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare shuxiong micropellets.</p><p><b>METHOD</b>Shuxiong micropellets were prepared by using a centrifugal granulator. The formulation composition and process factors were optimized investigated by adopting several indices such as size distribution, repose angle, bulk density and friability as indexes.</p><p><b>RESULT</b>The optimal process parameters were as follows. The ratio of fine intermediate product and MCC was 3:1 (w/w), the adhesive agent was 3% HMPC solution, the rotating rate of plate was 200 r x min(-1), the blower rate was 15 x 20 L x min(-1), the rate of air flow was 15 L x min(-1), the spray air pressure was 0.5 MPa, the rotating of spray solution pump was 5-25 r x min(-1) and the rotating rate of powder feed machine was 5-25 r x min(-1).</p><p><b>CONCLUSION</b>Under the optimal conditions, micropellets prepared by using centrifugal granulator hadpossessed prefect shape and surface characteristics and the yield of shuxiong pellets was 90.5%.</p>

Pharmacodynamics of compound danshen pH-dependent delayed release pellets in dogs / 药学学报

<p><b>AIM</b>To prepare the compound danshen pH-dependent delayed release pellets and filled them in capsules and then study thier pharmacodynamics.</p><p><b>METHODS</b>The pH-dependent delayed release pellets were prepared by coating with HPMC, Eudragit L-30D-55 and Eudragit L100-Eudragit S100 (1:6), separately, and mixed in proper proportion to prepare the two pH-dependent delayed release systems T1 and T2. The release of delayed release pellets was determined according to the method of China Pharmacopoeia (2000) in the simulated gastrointestinal pH conditions. The pharmacodynamic,parameters were evaluated by serum pharmacology method.</p><p><b>RESULTS</b>The compound danshen pH-dependent delayed release pellets were prepared with the characteristics of pH dependent delayed release profile in vitro. In single oral dose, the pharmacodynamic parameters of rapid release tablets R Emax (%) and Tmax (h) were 34.63% and 0.58 h, respectively. Tmax S of delayed-release pellets T1 and T2 were extended to 2.42, 3.17 h and Emax S (%) were declined to 13.57%, 14.52%. The relative bioavailabilities of T1 and T2 were 99.3%, 133.6% , respectively. In multiple oral doses of R the pharmacodynamic parameter of DF was 7.32 and those T1, T2 DF were 3.40, 3.03, respectively.</p><p><b>CONCLUSION</b>The compound danshen pH-dependent delayed release capsules have characteristics of pH dependent releasing in vitro and characteristics of delayed release in vivo. In multiple oral (loses the DF of delayed release capsules was lower than that of rapid release tablet at steady state.</p>

Diversity of invasiveness and matrix metalloproteinases expression profile of human gastric carcinoma xenografted in different tissue environments / 中华病理学杂志

<p><b>OBJECTIVE</b>To study the effect of tissue environment on the invasiveness of carcinoma cells and the implication of expression of matrix metalloproteinases.</p><p><b>METHODS</b>Tissue from a human gastric carcinoma was transplanted and passaged subcutaneously in nude mice. After the 3rd passage, the xenografts were also transplanted into the abdominal cavity of nude mice. The invasiveness of xenografts at the two locations were observed morphologically and the expressions of MMP-2, MMP-7, MMP-9, MMP-13, TM1-MMP, TM2-MMP and TM3-MMP were monitored by immunohistochemistry.</p><p><b>RESULTS</b>The subcutaneous xenografts of human gastric carcinoma in nude mice presented as expanding outgrowths with limited invasion. Except for MMP-7, the other 6 MMPs (MMP-2, MMP-9, MMP-13, TM1-MMP, TM2-MMP, TM3-MMP) were not expressed in the neoplastic cells nor in the tumor stroma. In contrast, the intra-peritoneal xenografts displayed an invasive growth pattern accompanied by more fibrous stroma. All MMPs examined were expressed in the tumor cells at the invasive fronts and in the adjacent stroma.</p><p><b>CONCLUSIONS</b>Invasiveness and expression of MMPs were obviously diverse in human gastric carcinoma cells when grafted at different anatomic locations in nude mice, thus indicating: (1) There exists a close interaction between tumor cells and surrounding stromal cells. The tissue environment may play a definitive role in the tumor phenotype. (2) The expression of MMPs is closely related to the growth pattern and the invasiveness of tumor cells. MMPs produced by the stroma cells at the invasion front may be linked to the invasiveness of neoplastic cells.</p>

Studies on diclofenac sodium pulsatile release pellets / 药学学报

<p><b>AIM</b>To investigate the preparation of diclofenac sodium pulsatile release pellets (DS-PRP), the release in vitro and the pharmacokinetics of the drug.</p><p><b>METHODS</b>Diclofenac sodium (DS) core pellets prepared by extrusion-spheronization technology were coated in a mini-fluidized bed spray coater with swelling material as the inner coating swelling layer and ethylcellulose aqueous dispersion as the outer coating controlled layer. The effects of formulation and medium on pulsatile release of DS were investigated under release rate test. Pharmacokinetic and bioavailability study in eight human subjects were performed by HPLC method.</p><p><b>RESULTS</b>The delayed-release time and release rate of DS from DS-PRP were influenced obviously by the swelling material, the concentration of SDS in medium, the coating level of the inner swelling layer and the outer controlled layer. In vitro, the delayed-release time T0.1 was 3.1 h, and the pulsed-release time T0.1-0.2 was 1.2 h. In vivo, the delayed-release time Tlag was 2.8 h, and the bioavailability was (91 +/- 12)%.</p><p><b>CONCLUSION</b>The release of drug from DS-PRP was shown to be in pulsed way both in vitro and in vivo.</p>

Study on the preparation of venenum bufonis beta-cyclodextrin inclusion complexes / 中国中药杂志

<p><b>OBJECTIVE</b>To study the preparation of Venenum Bufonis beta-cyclodextrin inclusion complexes.</p><p><b>METHOD</b>An optimal condition was established by the uniform design. Under the optimal conditions the Venenum Bufonis beta-cyclodextrin inclusion complexes were prepared with 5 different methods.</p><p><b>RESULT</b>The ball grinding method was superior to other four methods. The bufadienolide inclusion rate of Venenum Bufonis beta-cyclodextrin prepared with ball grinding method was 85.42%.</p><p><b>CONCLUSION</b>Ball grinding method is the best method for the preparation of Venenum Bufonis beta-cyclodextrin inclusion complexes.</p>