AIM: To explore the influencing factors in the release rate and give the application to the preparation. METHODS: Preparing ophiopogon saponin enteric microsphere by spray drying process,the accumulative release rate of acid and buffer solution were detected by colorimetric analysis. RESULTS: With the increase of Eudragit Ⅱ concentraction,the accumulative release rate tended to decrease.But ratio of drug and Eudragit Ⅱ,increased with the decrease in delay time on the break point. CONCLUSION: The concentration of Eudragit and the ratio of drug and material are the rey factors in the accumulative release rate in acid and buffer solution.

Objective To explore the prescription factor on Ophiopogon japonicus saponin enteric microsphere by spray drying technique. Methods Observing the type and content of enteric coating material, the type of plasticizer, the type and dosage of antistickiness material by single factor. Optimizing the prescription by orthogonal test design. Results Both Eudragit Ⅱ and micronization silica gel made in China could meet the need of the preparation. The best prescription included the proportion between drug and enteric coating material (1∶4), the dosage of castor oil (1%), and the dosage of micronization silica gel (1.5%). Conclusion O. japonicus saponin enteric microsphere accorded with the expecting demand. The kind of medical subsidiary material made in China will be the main raw material in producing the enteric microsphere. The study of prescription design will provide the basis for realizing microencap-sulation in Chinese materia medica.

AIM: To study compatibility rationality of combination of Paeonia lacliflora and Glycyrrhiza uralensis. METHODS: The effective combination of paeoniflorin(44% purity),glycyrrhizic acid(50% purity) and liquorice flavones(52% purity),glycyrrhizic acid(50% purity) and liquorice flavones(52% purity) were respectively administered to rats.Pharmacokinetic change of these constituents in rat blood was studied. RESULTS: The pharmacokinetic parameters of these constituents in rat blood showed that the increases in AUC and C_(max) of effective combination group were more than that of glycyrrhizic acid group or that of liquorice flavones group.T_(max) of the former was extended with respect to the latters.Clearance of effective combination markedly slowed down. CONCLUSION: The effective combination of paeonia lacliflora and Glycyrrhiza uralensis have the advantage of either Paeonia lacliflora or Glycyrrhiza uralensis.

With the deepening of modernization of traditional Chinese medicine (TCM), the method of quantification and standardization of TCM (i.e., quantitative characterization of TCM) has been more and more widely accepted by researchers. Chemometrics processes complicated data of TCM through applied mathematics, statistics and com-puter technology. And multivariable study was introduced into the quantitative characterization of TCM with great achievements. This article reviewed existed problems of quantitative characterization in TCM, the principles, char-acteristics, limitations, commonly used statistical methods and application conditions on quantitative characteriza-tion of TCM. With this review, a reference for further study of quantitative characterization of TCM was provided and a further research idea of combination with main methods of chemometrics was given.

Objective To explore how to decrease and prevent the occur-rence of catastrophic bleeding.Methods One case of serious bleeding caused by warfarin was analyzed, in view of the overall situation of the patient including disease and medication, and a resolution to reducing the risk of bleeding in our hospital was proposed.Results and Conclusion The patient′sphysical condition ( damage of liver and kidney function, hypoalbuminemia and fever) and drug interaction ( celecoxib, glucocorti-coid, Shenxiong glucose injection)may induce serious bleeding.Warfarin was influenced by many factors, and has a high probability of inducing adverse reactions.Pharmacists should make efforts to provide patients with safe and effective regimen and make medicine instruction.

OBJECTIVETo evaluate in vivo pharmacokinetics of Ophiopogonis Radix polysaccharide MDG-1 oily suspension injection prepared with different prescriptions in rats, and explore the feasibility of the long-acting drug delivery of MDG-1 Injection by using the oily suspension drug release system.

METHODMDG-1 microparticles were prepared by the anti-solvent precipitation method. Their size and size distribution were characterized. Castor oil with a high viscosity or aluminum stearate were added into soybean oil with a low viscosity, in order to prepare oily media with different viscosities, detect their rheological properties and screen out superior prescriptions for in vivo evaluation.

RESULTThe average size of microparticles was 21.81 microm, and the span between them was 2.63. The in vivo evaluation was conducted for prescriptions of mixed oil (soybean oil/castor oil, 2: 3) and soybean oils gelled by 2% and 4% aluminium stearate. Among them, the prescription of soybean gelled by 4% aluminium stearate could significantly reduce C(max) and prolong the apparent t1/2, with the MDG-1 release time of several days.

CONCLUSIONIt is feasible to achieve the long-acting MDG-1 drug delivery by using oily media with a high viscosity.

Animals ; Chemistry, Pharmaceutical ; methods ; Drug Delivery Systems ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; pharmacokinetics ; Male ; Ophiopogon ; chemistry ; Plant Oils ; chemistry ; Polysaccharides ; administration & dosage ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Viscosity

Oral solid rapidly-disintegrating dosage form has aroused general concern increasingly because of its characteristics about convenient taking, rapid absorption, high bioavailability and not serious adverse drug reaction. This article introduced its mechanism, which was rapid disintegration, fast dissolution or the promoting dissolving action of supplementary material. This dosage form included dispersible tablets, fast dissolving tablets, fast releasing tablets, droppills, granules and tablets by solid dispersible technology, quick-liquefying chewable tablets and dry elixir. It will become a new way for promoting bioavailability in traditional Chinese medicine difficultly-dissolving composition, create up a new dosage form for treating emergency case by traditional Chinese medicine and give a new thinking for studying new supplementary materials. In brief, oral solid rapidly-disintegrating dosage form will have good prospect in the field of traditional Chinese medicine.
Administration, Oral ; Capsules ; chemistry ; Cellulose ; Drug Delivery Systems ; Drugs, Chinese Herbal ; administration & dosage ; Polyethylene Glycols ; Porosity ; Povidone ; Solubility ; Tablets ; chemistry ; Technology, Pharmaceutical ; methods

The paper is to report the observation of pharmacokinetic changes of the characteristic ingredients in the combinations of different-dose herbs of Shaoyao-Gancao decoction. After the establishment of HPLC analytical method of plasma effective constituents, rats were orally administered with different-dose herbs of Shaoyao-Gancao decoction. Blood samples at different times after administering these decoctions were collected, and then were analyzed by HPLC fingerprints technology. Pharmacokinetic parameters of characteristic peaks were analyzed by SPSS 15.0 software and DAS 2.0. At last, we looked for the correlation of those pharmacokinetic parameters and the dosage of Gancao. The best dose of Shaoyao-Gancao decoction was at the ratio of 4 to 4, which was consistent with the dose commonly used in ancient times. The absorption of characteristic peaks from Shaoyao-Gancao decoction was related with the dosage of Gancao, and there existed interaction between each characteristic ingredients. There existed the right dose-ratio of Shaoyao and Gancao to get the best effect. The absorptions of effective constitutents were mutual waxing and waning in order to increase biological effects together. It's demonstrated the compatibility connotation at a right dose-ratio of Shaoyao-Gancao decoction through the angle of pharmacokinetics.

The pharmacokinetics of a long-circulating PEGylated Radix Ophiopogonis polysaccharide (ROP) was investigated in rats following i.v. or s.c. administration at three dose levels (9, 20, 50 mg x kg(-1)). A moderate coupling reaction between the hydroxyl-activated ROP and the amino-terminated mPEG was chosen to produce PEGylate ROP. The grafting degree of the prepared conjugate was 1.03, and the molecular mass of mPEG used was 20 kDa. High-performance gel permeation chromatorgraphy with fluorescein isothiocyanate prelabeling was established to determine levels of the conjugate in plasma. The results showed that the elimination half-life of the conjugate following s.c. administration was basically identical to that after iv administration. An accurate linear correlation was observed between administration doses and areas under the curve of plasma conjugate level vs. time profile, regardless of the administration route. The absolute bioavailability of the conjugate following sc administration was approximately 56%, and the mean in vivo residence time was 52.1 h, increased 2.4 times compared to those of iv administration. In general, linear pharmacokinetics was observed for the conjugate within the dose range studied, and sc should be a promising administration route for the conjugate.

Animals ; Diabetes Mellitus, Experimental ; drug therapy ; Insulin Resistance ; Stilbenes ; pharmacology ; therapeutic use