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

The compound excipient containing sodium stearyl fumarate and plasdone S-630 was prepared by applying spray drying method. The basic physical properties of compound excipient were studied by solubility test, scanning electron microscope, differential scanning calorimeter, X-ray diffraction and Fourier transform infra-red spectroscopy. The effect of compound excipient on moisture absorption and ferulic acid in vitro dissolution of spray drying power of angelica were investigated. The results showed that the chemical constituents of compound excipient did not change before and after spray drying. The water soluble compound excipient can improve significantly moisture absorption and has application prospect.
Acetates ; chemistry ; Calorimetry, Differential Scanning ; Coumaric Acids ; administration & dosage ; chemistry ; Drug Compounding ; Excipients ; chemistry ; Fumarates ; chemistry ; Microscopy, Electron, Scanning ; Particle Size ; Povidone ; analogs & derivatives ; chemistry ; Solubility ; Spectroscopy, Fourier Transform Infrared ; Surface Properties ; Wettability ; X-Ray Diffraction

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

The aim of present study was to prepare buccal tablets of fluconazole for oral candidiasis. The dosage forms were designed to release the drug above the minimum inhibitory concentration for prolonged period of time so as to reduce the frequency of administration and to overcome the side effects of systemic treatment. The buccal tablets were prepared by using Carbopol 71G and Noveon AA-1 by direct compression method. Microcrystalline cellulose was used as the filler and its effect was also studied. The prepared dosage forms were evaluated for physicochemical properties, in vitro release studies and mucoadhesive properties using sheep buccal mucosa as a model tissue. Tablets containing 50% of polymers (Carbopol & Noveon) were found to be the best with moderate swelling along with favorable bioadhesion force, residence time and in vitro drug release. The in vitro drug release studies revealed that drug released for 8 h, which in turn may reduce dosing frequency and improved patient compliance in oral candidiasis patients.
Acrylates ; administration & dosage ; chemistry ; pharmacokinetics ; Acrylic Resins ; administration & dosage ; chemistry ; pharmacokinetics ; Adhesiveness ; Administration, Buccal ; Animals ; Candidiasis, Oral ; drug therapy ; Cellulose ; administration & dosage ; chemistry ; Delayed-Action Preparations ; Drug Combinations ; Drug Stability ; Excipients ; Fluconazole ; administration & dosage ; chemistry ; pharmacokinetics ; Mouth Mucosa ; metabolism ; Polymers ; administration & dosage ; Sheep ; Tablets

Pure and drug hydrophilic matrix tablets were prepared by direct compression method with theophylline as a model drug. The characteristics of four hydrophilic matrix polymers, hydroxypropylmethylcellulose (HPMC), polyethylene oxide (PEO), sodium alginate (NaAlg) and xanthan gum (XG), were compared by investigating the water absorption, swelling, erosion and gel layer strength. The sequence of water absorption rate was XG > NaAlg (H) > PEO > NaAlg (L) > HPMC; The sequence of swelling index was XG > PEO > HPMC > NaAlg; The sequence of erosion rate was NaAlg (L) > NaAlg (H) > PEO80 > PEO200 > PEO300 > XG approximately PEO400 approximately K4M > K15M > PEO600 approximately K100M; The sequence of the gel layer strength was PEO > HPMC > XG > NaAlg. For the PEO and HPMC matrix tablets, with the polymer molecular weight increased, the drug release mechanism was gradually transferred from mainly depending on the erosion to the diffusion; for SAL matrix tablets, the drug release mainly depends on erosion mechanism; and for XG matrix tablets, the drug release mainly depends on non-Fick diffusion mechanism. Comparison of the performance difference between the polymer materials will contribute to rational design and prediction of drug release behaviors from matrix tables and ultimately to achieve clinical needs.
Alginates ; chemistry ; Bronchodilator Agents ; administration & dosage ; Delayed-Action Preparations ; Drug Carriers ; Drug Compounding ; Drug Delivery Systems ; Excipients ; chemistry ; Glucuronic Acid ; chemistry ; Hexuronic Acids ; chemistry ; Hypromellose Derivatives ; Methylcellulose ; analogs & derivatives ; chemistry ; Molecular Weight ; Polyethylene Glycols ; chemistry ; Polymers ; chemistry ; Polysaccharides, Bacterial ; chemistry ; Tablets ; Theophylline ; administration & dosage ; 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

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

This study is to prepare the pantoprazole sodium enteric-coated tablet which is compacted by pellets. The enteric-coated pantoprazole sodium pellets were prepared by fluid bed coating technology. The pantoprazole sodium enteric-coated tablets were prepared by direct compression of the enteric-coated pellets and suitable excipients. In vitro dissolution method and scanning electron microscope method were used for the observation of the drug release behavior before and after compression of the pellets. The optimized formulation is: the coating level is 55%, the plasticizer content is 20%, the ratio of Eudragit L30D-55/NE30D is 8 : 2, enteric-coated pellets/excipients (MCC/PPVP/PEG 6000 = 2 : 1 : 1) is 5 : 5, the enteric-coated tablets release in artificial gastric fluid in 2 h is less than 10%, while in artificial intestinal fluid in 1 h is more than 85%. The release behavior of pantoprazole sodium enteric-coated pellets-type tablet is quite well. And it may be used in industrial production.
2-Pyridinylmethylsulfinylbenzimidazoles ; administration & dosage ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Drug Carriers ; Drug Compounding ; methods ; Excipients ; Microscopy, Electron, Scanning ; Plasticizers ; chemistry ; Polyethylene Glycols ; chemistry ; Polymethacrylic Acids ; chemistry ; Proton Pump Inhibitors ; administration & dosage ; chemistry ; Solubility ; Tablets, Enteric-Coated ; chemistry ; Technology, Pharmaceutical

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

This paper reported that a new type of floating osmotic pump of ambroxol hydrochloride was designed. Third method apparatus (Chinese Pharmacopeia 2010, appendix XD) was employed to simultaneously evaluate the release and floating behavior in vitro. The system was optimized using central composite design-response surface methodology. Similar factor (f2) between the release profile of self-made formulation and the target release profile was chosen as dependent factor. The amount of glucose (A, mg), pore former (B, %) and weight of coating (C, %) were employed as independent factors. Optimized formulation was: A (100.99 mg), B (1.70%), C (4.21%). The value of f2 (89.14) was higher than that of market capsules (69.02) and self-made tablets (72.15). It was showed that self-made capsules possessed character of zero-order release (r = 0.994 4) and drug release completely (>90%). It was showed in result of in vivo study that tmax and Cmax of self-made capsules were significantly lower than that of market capsules and self-made tablets. The correlation coefficient between the fraction of absorption in vivo and the release rate in vitro was 0.985 1, and relative bioequivalence of self-made capsules was 110.77%. Accordingly, self-made capsules displayed obviously characteristics of controlled release both in vivo and in vitro.
Absorption ; Administration, Oral ; Ambroxol ; administration & dosage ; chemistry ; pharmacokinetics ; Animals ; Area Under Curve ; Capsules ; Delayed-Action Preparations ; Dogs ; Drug Compounding ; methods ; Drug Delivery Systems ; Excipients ; Female ; Glucose ; chemistry ; Male ; Osmosis ; Osmotic Pressure ; Porosity ; Random Allocation ; Solubility ; Therapeutic Equivalency