To prepare and evaluate dry powder inhalation (DPI) of extraction of Trollius chinensis Bunge (TCB). Orthodox design was employed to optimize the parameters of spray drying to prepare micronized TCB powder, the DPI was prepared by mixing micronized TCB powder and lactose. The results showed that the fine particle fraction (FPF) and emitted dose (ED) of micronized TCB powder was (21.07 +/- 1.74)%, (75.31 +/- 21.05)%, respectively, and for DPI was (56.4 +/- 2.2)%, (95.9 +/- 3.0)%, respectively. Therefore, the prepared DPI meeted requirements in the Chinese Pharmacopeia, indicating a good application prospect.
Administration, Inhalation ; Dry Powder Inhalers ; Excipients ; Plant Extracts ; administration & dosage ; isolation & purification ; Powders ; Ranunculaceae

OBJECTIVETo prepare sinomenine hydrochloride delayed-onset sustained-release tablets.

METHODThe tablets containing sinomenine hydrochloride were prepared by dry-compression coating technique with the ratio of HPMC in core tablet and the ratio of HPMC in coating film as the influence factors and the lag-time and release rate as the evaluation parameters. Experiments were done on the central composite design, the data were simulated by using multi-linear equation and second-order polynomial equation. The possibly optimal formulation was predicted by response surface method. The dissolution date (lag-time and release rate) of the tablets prepared under the optimum condition were compared with the predicted. The drug released mechanism of the tablet were studied by Model-fitted of drug released within 6-15 h with zero-order, Higuchi and Peppas equation, respectively.

RESULTThe lag-time and release rate were simulated using second-order polynomial equation, regression coefficients of the two parameters were 0.9901 and 0.9876, respectively. Bias between the observed and predicted values of lag-time and release rate were -3.15% and -0.34%, respectively. The lag-time of the tablet prepared under the optimum condition in vitro was about 6 h, then drug released from the tablet within 6-15 h was found to conform to zero-order kinetics and was controlled by bulk erosion mechanism.

CONCLUSIONSinomenine hydrochloride delayed-onset sustained-release tablets release drug slowly after lag time. The models developed in this study are proved to be highly predictable.

Chemistry, Pharmaceutical ; Delayed-Action Preparations ; administration & dosage ; Drug Delivery Systems ; methods ; Excipients ; administration & dosage ; Morphinans ; administration & dosage ; Pharmaceutical Preparations ; administration & dosage ; Tablets ; administration & dosage ; Technology, Pharmaceutical

The purpose of this study is to design push-pull osmotic pump (PPOP) tablets of famotidine using the expert system for the formulation design of osmotic pump of poor water-soluble drug which had been established by the authors. Firstly, the parameters which were requisite of the system input were obtained from literatures and experimental tests. Then the parameters were input into the system, and the program was run. The system displayed the designed formulations sequential. Finally, famotidine PPOP was prepared according to the designed formulations and the in vitro dissolution was carried out. It was found out that the target formulation of famotidine PPOP which could release for 24 hours was obtained in a very short period. Meanwhile, the practicability of the established expert system was proved.
Delayed-Action Preparations ; Drug Delivery Systems ; methods ; Excipients ; chemistry ; Expert Systems ; Famotidine ; administration & dosage ; chemistry ; Osmosis ; Solubility ; Tablets ; Water

Rheological properties of poloxamer 407 (brand named Pluronic F127) were examined by changing shear rate, temperature and the recovery properties of apparent viscosity after heating for several times. The results indicated that poloxamer 407 aqueous solution showed a Newtonian behavior at a low concentration while it might be a pseudoplastic fluid when the concentration reached a certain point. The thixotropy and the sol-gel transition temperature decreased with increasing the concentration (it could be an in situ gel at body temperature when the concentration of poloxamer 407 up to 15.25%). The results that obtained from the theological data would be useful in the application of poloxamer 407 such as in situ gel preparation.
Dose-Response Relationship, Drug ; Drug Compounding ; Drug Delivery Systems ; Excipients ; administration & dosage ; chemistry ; Poloxamer ; administration & dosage ; chemistry ; Rheology ; Shear Strength ; Solutions ; Temperature ; Viscosity ; Water

OBJECTIVETo study the solubilization effect of 2-hydroxypropyl-beta-cyclodextrin(HPCD) on paeonolum at various pH value.

METHODPhase-solubility method was adopted to study the solubilization effect at 25 degrees C and UV spectrohotometer was used to determine paeonolum content.

RESULTSThe apparent solubility of paeonolum was significantly enhanced by increased HPCD concentration. The apparent stability constant of paeonolum compounds was calculated up to 1 425 in which pH was 3 and HPCD concentration was 133.33 mmol x L(-1). The solubility of paeonolum came up to 10 mg x mL(-1).

CONCLUSIONHPCD is an ideal solubilizer for paeonolum.

2-Hydroxypropyl-beta-cyclodextrin ; Acetophenones ; administration & dosage ; chemistry ; isolation & purification ; Drug Stability ; Excipients ; Hydrogen-Ion Concentration ; Paeonia ; chemistry ; Plants, Medicinal ; chemistry ; Solubility ; beta-Cyclodextrins

Insoluble breviscapin was chosen as the model drug. Bi-layer osmotic pump technology and gel matrix technology were used to prepare the breviscapin sustained and controlled release preparations. Dissimilarity factors (f1) and similarity factors (f2) were applied as similar judgment index to compare the effects of in vitro conditions on the release behavior of different types of breviscapin sustained and controlled release preparations. The tolerance of in vitro release conditions of bi-layer osmotic pump technology and gel matrix technology were studied. The results showed that in vitro release conditions have a greater impact on the gel matrix sustained release formulations, while have almost no effects on the osmotic pump controlled release formulations. Therefore, osmotic pump controlled release technology is less affected by the drug release environment. And it has a very good application prospect.
Delayed-Action Preparations ; Drug Carriers ; Excipients ; Flavonoids ; administration & dosage ; Hypromellose Derivatives ; Methylcellulose ; analogs & derivatives ; chemistry ; Osmolar Concentration ; Osmosis ; Polyethylene Glycols ; chemistry ; Rotation ; Technology, Pharmaceutical ; methods ; Temperature

The distribution fate and solubilization behavior of indomethacin through the intestinal tract were investigated with in vitro lipolysis model, by comparing the Capmul MCM and Labrafil M 1944 CS type I lipid formulations. The results showed that the more favorable solubilization was in the aqueous digestion phase from each lipid formulations for indomethacin. The lipolysis rate and extent were decided with chemical constitution of the lipid excipients, which meant that less indomethacin was transferred from the long chain polar oil lipid solution into the aqueous digestion phase. Increasing the concentration of indomethacin in the lipid formualitons from a solution to a suspension led to a linear increase in the concentration of indomethacin attained in the aqueous digestion phase from lipid formulations. This study also implied that adverse effects of the lipolysis rate and extent on drug absorption were could be taken into consideration when screening lipid formulations. Lipid suspensions likely had better enhancement of drug absorption. Last, this study demonstrated that a potential basis for optimizing and assessing type I lipid formulations and also researching in vivo-in vitro correlations of lipid formulations were provided by an in vitro lipolysis model.
Caprylates ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Digestion ; Excipients ; Glycerides ; chemistry ; Indomethacin ; administration & dosage ; pharmacokinetics ; Lipolysis ; Models, Biological ; Polyethylene Glycols ; chemistry ; Solubility ; Suspensions

AIMTo study the erosion behaviour during dissolution of matrices using different molecular weight polyethylene oxide (PEO) as hydrophilic polymer.

METHODSPEO hydrophilic matrix tablets with no added drug and excipients were prepared by direct compression method. The erosion rates of matrices comprised of pure or blending PEO polymers were evaluated in distilled water at (37 +/- 0.5) degrees C with rotating rate of 50 r x min(-1). The relationship between PEO molecular weight and erosion rate of matrices was investigated by experimental and mathematical model methods.

RESULTSThe gravimetric erosion experimental results indicated that the power-law relationship which relates the polymer erosion rate and weight average molecular weight: k infinity (M(w)) -1.30 4 was proved to have great potential utility in predicting the degree of polymer erosion of matrices comprised of either intermediate molecular weight (97. 98 x 10(4) - 553. 36 x 10(4)) or blends of lower and higher molecular weight polymers. Based on the semiempirical equation for mass transfer rate: Jp = (fp < Dp > (2/3) v (-1/6) omega (1/2)) C(p,dis), a theoretical mathematic model was developed for describing the relationship between PEO erosion rate and PEO weight average molecular weight: Jp infinity M(-1.241), where the exponent of -1. 241 was very close to the exponent of - 1. 130 4 obtained from practical determination.

CONCLUSIONPEO was proved to be a good candidate of hydrophilic polymer and appeared to have great potential for controlled release applications. The mathematic model presented together with the utilization of the erosion behaviour discussed in our study could provide a guide line to predict the degree of polymer erosion for other intermediate polymer grades and / or mixture of the polymers utilized in this study, which could play an active role in designing PEO hydrophilic sustained delivery systems.

Delayed-Action Preparations ; chemistry ; Drug Carriers ; chemistry ; Drug Delivery Systems ; Drug Stability ; Excipients ; chemistry ; Molecular Weight ; Polyethylene Glycols ; administration & dosage ; chemistry ; Polymers ; Solubility ; Tablets ; Water

This study is to report the evaluation of the micromeritic properties of LubriTose AN, which is expected to provide preliminary theoretical basis for the direct compression technology. From the aspects of flowability, compressibility and dilution potential, the angle of repose, flow velocity, the Carr' index, tensile strength, elastic recovery, yield pressure and the lubricating ability of LubriTose AN were determined. Also, model drugs were selected to investigate the dilute potential under the desirable compressing performance. Compared to the physical mixtures, the flowability of LubriTose AN was better, and the deformation mechanism was the same with anhydrous lactose, both brittle deformation. The compressibility and compaction of LubriTose AN was slightly better than that of physical mixtures under low and moderate pressure. The dilution potential of LubriTose AN were high for most of hydrophobic drugs. The lubricate ability was desirable under different rotational speeds. LubriTose AN is an excellent co-processed excipient, which is helpful for the promotion and improvement of the tablet manufacturing level.
Drug Compounding ; Elasticity ; Excipients ; chemistry ; Glycerides ; chemistry ; Ibuprofen ; administration & dosage ; chemistry ; Lactose ; chemistry ; Lubricants ; chemistry ; Lubrication ; Particle Size ; Pressure ; Technology, Pharmaceutical ; methods ; Tensile Strength

To prepare verapamil hydrochloride (VH) core-in-cup tablets with tri-layered tablet and four-layered tablet as core tablets, separately, which can provide biphasic release with double-pulsatile and multi-phasic release, core tablets were prepared by direct compression method, and core-in-cup tablets by dry-compression coated technology. The parameter, time-lag (T(lag)), was used to evaluate the influence of factors, such as the weight of the top cover layer, the amount of hydroxypropylmethylcellulose (HPMC), and the compression load on VH release. With the increase of the weight and HPMC amount of the top cover layer, the first lag time T(lag1) was prolonged. The second lag time T(lag2) of core-in-cup tablet with four-layered tablet as core tablet increased with the increasing amount of HPMC K100M. With the increase of compression load among the range (6 - 10 kg x cm(-2)), the two lag times were prolonged. Core-in-cup tablets with double-pulsatile and multi-phasic release released VH after the first lag time (4 -5 h), then kept sustained release for 12 h or 13 h, finally released rapidly. The drug in the core-in-cup tablet only released from the top cover layer. T(lag) is determined by the erosion rate of the inhibitor layers (the top cover layer and the sustained-release layer of the multi-layer core tablet).
Delayed-Action Preparations ; Drug Carriers ; Drug Compounding ; methods ; Drug Delivery Systems ; Excipients ; chemistry ; Hypromellose Derivatives ; Methylcellulose ; analogs & derivatives ; chemistry ; Tablets ; Verapamil ; administration & dosage