PVP only does not enhance the solubility of DHEA but a combination effect will manifeste once the substance is used concurrently with HPCD. In 5,59% HPCD solution, this solubility was enhanced by 115 times and in 5,59% HPCD solution adding 0,1% PVP it was enhanced by 139 times. There is a strict interaction between its components, different evidently from the physical mixed graphic
Povidone ; beta-Cyclodextrins ; Androsterone

An ideal reversal agent could be given at any time after the administration of a neuromuscular blocking agent, and should have no muscarinic side-effects. Sugammadex is a modified gamma-cyclodextrin designed to encapsulate rocuronium bromide, providing a rapid reversal of neuromuscular blockade. Sugammadex is a revolutionary investigational reversal drug currently undergoing Phase III testing whose introduction into clinical practice in Korea may change the face of clinical neuromuscular pharmacology. The dose of sugammadex for reversal of moderate block (when T2 is detectable) is approximately 2 mg/kg, the dose is 4-8 mg/kg for profound block (post-tetanic count 1-2) and a larger dose of 16 mg/kg for immediate reversal. The use of sugammadex has not been reported to be associated with recurrence of block provided a dose that is adequate for reversal has been used. Sugammadex appears to have an acceptable safety profile. Volatile agent such as sevoflurane seems not to influence the sugammadex ability to reverse the rocuronium neuromuscular blockade.
Androstanols ; gamma-Cyclodextrins ; Korea ; Methyl Ethers ; Neuromuscular Blockade ; Recurrence

OBJECTIVETo study optimal process conditions for the inclusion of volatile oil from Nardostachyos Radix et Rhizoma using saturated water solution method.

METHODThe optimal technology of inclusion was identified respectively by the utilization ratio of volatile oils and the yield of inclusion compound in an orthogonal experiment design, and the inclusion efficiency was evaluated by TLC, UV, IR, SE and GC-MS.

RESULTThe optimum preparation conditions for inclusion were established as follows: volatile oil: beta-CD was 1: 6, the inclusion temperature was 40 degrees C, the stirring speed and time were in 300 r x min(-1) and for 1 h. The analysis results showed that a new substance was conformed. The change of the volatile oil component was found before and after inclusion.

CONCLUSIONThe optimal process conditions are easy for operation, and high in utilization ratio of volatile oils and the yield of inclusion compound.

Nardostachys ; chemistry ; Oils, Volatile ; chemistry ; Technology, Pharmaceutical ; beta-Cyclodextrins ; chemistry

AIMTo establish a resolution method for alpha-cyclohexyl mandelic acid enantiomers by enantioselective extraction and to observe the effects of all kinds of tartaric esters, pH, the concentration of D-tartaric esters and beta-cyclodextrin on the enantioselectivity.

METHODSResolution of alpha-cyclohexyl mandelic acid enantiomers by enantioselective extraction with tartaric esters and beta-cyclodextrin has been studied.

RESULTSThe distribution behavior of alpha-cyclohexyl mandelic acid enantiomers in the separation system was studied. The effects of all kinds of tartaric esters, pH, the concentration of D-tartaric esters and beta-cyclodextrin on the enantioselectivity has been examined in the two-phase.

CONCLUSIONResults showed that the complex formed by D-iso-butyl-D-tartaric ester with R enantiomer is stabler than that with S enantiomer. With the increase of pH, the partition coefficient and separation factor decreased. The concentration of beta-cyclodextrin and D-tartaric ester had visible effect on the enantioselectivity.

Esters ; Mandelic Acids ; chemistry ; Stereoisomerism ; Tartrates ; chemistry ; beta-Cyclodextrins ; chemistry

Sugammadex is a modified gamma-cyclodextrin which is showing favorable outcomes regarding reversal of neuromuscular blockade, especially by rocuronium. It is designed to encapsulate rocuronium and being considered a new class of drugs as selective relaxant binding agents. It has given countless benefits to the patients at risk of incomplete or delayed recovery after neuromuscular block and has renown for another milestone in anesthesia practice. Recurrence of neuromuscular block has not been reported to be associated with the provided doses of sugammadex that are adequate for selected for reversal. Acceptable profiles are brought to light telling safety of sugammadex. However, some questions related to the twitch characteristics those resembled succinylcholine when reversal, the application for rocuronium anaphylaxis, and the hypersensitivity or anaphylaxis to sugammadex remain and are need of further investigation. It is imperative that potential problems that we need attention may include the patient's history of pulmonary disease and allergic disease for using sugammadex.
Anaphylaxis ; Androstanols ; Anesthesia ; gamma-Cyclodextrins ; Humans ; Hypersensitivity ; Light ; Lung Diseases ; Neuromuscular Blockade ; Patient Safety ; Recurrence ; Succinylcholine

The purpose of the present work was to investigate the innovative self-assembling system, "beads", prepared by continuously shaking alpha-cyclodextrin and soybean oil without the use of organic solvents and surfactants at room temperature. Berberine hydrochloride previously dissolved in soybean oil was chosen as a model drug to explore the shape, structure, drug loading and in vitro release of beads. The particle size and drug loading of berberine hydrochloride-loaded beads were (2.25 +/- 0.23) mm and (67.02 +/- 0.64) microg x g(-1), respectively. Confocal microscopy showed that the core-shell structure of beads could contain poorly water soluble drugs or lipophilic drugs in the lipid core. The drug release rate and cumulative releases of beads were both higher than those of raw medicine of berberine hydrochloride in simulated intestinal fluid. These results suggested that beads were the novel and potential lipid-based drug delivery system for lipophilic or poorly water soluble traditional Chinese medicine.
Berberine ; administration & dosage ; Drug Delivery Systems ; Particle Size ; Solubility ; Soybean Oil ; administration & dosage ; alpha-Cyclodextrins ; administration & dosage

OBJECTIVETo study the cyclodextrin inclusion complexes of Dragon's blood for improving the drug solubility and the preparation.

METHODThe inclusion complexes were prepared with beta-cyclodextrin, HP-beta-cyclodextrin, SBE-beta-cyclodextrin and confirmed by DTA. The activity of the inclusion complex was tested by animal experiments. Inclusion complexes tablets were prepared and the dissolution test was performed.

RESULTThe solubility of inclusion complexes was increased to 13. 75-168. 39 times. The activity of the inclusion complex was markedly improved, and dissolution rate was 78.69%.

CONCLUSIONThe cyclodextrin inclusion complexes of Dragon's blood have a good solubility, dissolution rate and pharmacological activity.

2-Hydroxypropyl-beta-cyclodextrin ; Cyclodextrins ; chemistry ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Plant Extracts ; chemistry ; Solubility ; Tablets ; chemistry ; beta-Cyclodextrins ; chemistry

OBJECTIVETo study the preparation of Venenum Bufonis beta-cyclodextrin inclusion complexes.

METHODAn 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.

RESULTThe 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%.

CONCLUSIONBall grinding method is the best method for the preparation of Venenum Bufonis beta-cyclodextrin inclusion complexes.

Amphibian Venoms ; administration & dosage ; chemistry ; Animals ; Bufanolides ; Bufo bufo ; Cholenes ; analysis ; Cyclodextrins ; Drug Carriers ; Drug Stability ; Materia Medica ; administration & dosage ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods ; beta-Cyclodextrins

OBJECTIVETo study the volatile regularity of menthol and borneol in granule and lozenge at different temperature.

METHODKinetic method with GC being detection technique.

RESULTThe volatility of menthol and borneol acts as a pseudo first-order reaction in open system. Under the same condition, the volatile rate of menthol and borneol in granule is four times as fast as that in lozenge, and the volatile rate of borneol is faster than that of menthol.

CONCLUSIONThis study can be applied to improve the quality of lozenges containing menthol or/and borneol.

Bornanes ; administration & dosage ; chemistry ; Cyclodextrins ; Drug Carriers ; Drug Stability ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Menthol ; administration & dosage ; chemistry ; Tablets ; Temperature ; Volatilization ; beta-Cyclodextrins

OBJECTIVETo determine the major factors affecting the conversion efficiency of naringin-HP-beta-CD that was enzymed to prepare naringenin were determined and select the process condition with high conversion efficiency, stable and suitable for industrial production.

METHODThe dropping method was used to prepare naringin-HP-beta-CD, which was hydrolyzed by snailase to obtain naringenin. With the bioconversion rate as the index, the effects of pH value, temperature, reaction time, dosage of enzyme and concentration of naringin-HP-beta-CD on conversion rate of naringenin were detected for the purpose of optimizing the preparation condition. the conversion efficiency of naringin-HP-beta-CD was verified by scanning calorimetry, and the Hydrolysis product was identified by H-NMR, and 13C-NMR.

RESULTThe optimum enzymolysis of naringin-HP-beta-CD with snailase was 98.4% under the conditions of 37 degrees C, a pH 5.0 acetic acid- sodium acetate buffer solution for 12 hours. The substrate concentration was 30 g x L(-1) and the weight ratio of enzyme and substrate was 3: 5. Under the optimum enzymolysis condition, the conversion rate of naringin-HP-beta-CD was higher than naringin that was not entrapped with HP-beta-CD, with 272.25 reaction product relative molecules. The structure of naringenin was confirmed by the analysis of 1H-NMR and 13C-NMR.

CONCLUSIONNaringin which is entrapped with HP-beta-CD to prepare naringenin can significantly improve the conversion efficiency by shortening the reaction time, increasing the concentration of the substrate and reducing the amount of enzyme. Therefore, the process is stable and it was suitable for industrialization.

2-Hydroxypropyl-beta-cyclodextrin ; Flavanones ; chemistry ; isolation & purification ; Hydrolysis ; Solubility ; beta-Cyclodextrins ; chemistry