OBJECTIVETo optimize the formulation of immediate release tablet.

METHODThe immediate release tablet was prepared by using dry granules. The preparation was optimized by using orthogonal design which took the flow property of granules, the hardness, the disintegrating time and the dissolution rate of the tablet as indices.

RESULTThe optimized formulation contained 40% microcrystalline cellulose, 10% sodium carboxymethyl starch and 15% dextrin. The hardness disintegrating time and T50 of the tablet were 4.5 kg, 3 min, 5 min respectively.

CONCLUSIONIt is successful to prepare on immediate release tablet using the optimized formula above.

Cellulose ; Dextrins ; Drug Combinations ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; Panax ; chemistry ; Plants, Medicinal ; chemistry ; Salvia miltiorrhiza ; chemistry ; Solubility ; Tablets

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

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

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

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

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

We studied the mutation effect of subsites -3(Lys47), -7(146-152), and cyclization center (Tyr195) in active domain on product specificity of alpha-cyclodextrin glucanotransferase (alpha-CGTase) from Paenibacillus macerans sp. 602-1. The Lys47 was replaced by Thr47 and Tyr195 by Ile195, and the amino acids from 146 to 152 were replaced by Ile (named as delta6). All these mutant alpha-CGTases were actively expressed in E. coli BL21. Compared with the wild-type alpha-CGTase, the starch-degrading activities of all the mutant enzymes were declined. For mutant Y195I, the percentage of alpha-CD was decreased from 68% to 30%, and beta-CD was raised from 22.2% to 33.3%. Interestingly, gamma-CD was increased from 8.9% to 36.7% and became the main product, while the actual yield was increased from 0.4 g/L to 1.1 g/L. Mutant K47T and delta6 still produced alpha-CD as main product though the percentage of beta- and gamma-CD increased. Purified Y195I CGTase showed similar optimum temperature with the wild-type alpha-CGTase, but its optimum pH shifted from 5.0 to 6.0 with better pH stability. In summary, mutant Y195I CGTase has the potential to produce gamma-CD as the main product.
Escherichia coli ; genetics ; metabolism ; Glucosyltransferases ; genetics ; metabolism ; Mutant Proteins ; genetics ; metabolism ; Mutation ; Paenibacillus ; enzymology ; Recombinant Proteins ; genetics ; gamma-Cyclodextrins ; metabolism

Objective: To investigate the effect of sugammadex on postoperative nausea and vomiting(PONV) after intracranial aneurysm surgery. Methods: Data from intracranial aneurysms patients who met the inclusion and exclusion criteria and underwent interventional surgery in the Department of Neurosurgery, Peking University International Hospital from January 2020 to March 2021 were prospectively included. According to the random number table method, the patients were divided by 1∶1 into the neostigmine+atropine group (group N) and the sugammadex group (group S). Use an acceleration muscle relaxation monitor for muscle relaxation monitoring, and administer neostigmine+atropine and sugammadex to block residual muscle relaxation drugs after surgery. The incidence rates of PONV and severity, the appearance of anesthesia, and the correlation between PONV and postoperative complications were recorded in both groups during five periods after surgery: 0-0.5 hours (T1),>0.5-2.0 hours(T2),>2.0-6.0 hours (T3),>6.0-12.0 hours (T4) and >12.0-24.0 hours (T5). Group comparisons of quantitative data were performed by the independent sample t-test, and categorical data was performed by the χ² or rank sum test. Results: A total of 66 patients were included in the study, including 37 males and 29 female, aged (59.3±15.4) years (range: 18 to 77 years). The incidence rates of PONV of 33 patients in group S at different time periods of T1, T2, T3, T4, and T5 after surgery were respectively 27.3%(9/33),30.3%(10/33),12.1%(4/33),3.0%(1/33),0(0/33),and the incidence rates of PONV of 33 patients in the group N at different time periods of T1, T2, T3, T4 and T5 after surgery were respectively 36.4%(12/33),36.4%(12/33),33.3%(11/33),6.1%(2/33) and 0(0/33).The incidence of PONV was lower in the group S only in the T3 period after reversal than in the group N (χ²=4.227, P=0.040).However, there was no statistically significant difference in the incidence of PONV between the two groups of patients in other periods (all P>0.05). The recovery time for spontaneous breathing in patients in group S was (7.7±1.4) minutes, the extubation time was (12.4±5.3) minutes, and the safe exit time for anesthesia recovery was (12.3±3.4) minutes; the N groups were (13.9±2.0) minutes, (18.2±6.0) minutes, and (18.6±5.2) minutes, respectively; three time periods in group S were shorter than those in group N, and the differences were statistically significant (all P<0.05). The results regarding the occurrence of complications in patients with different levels of PONV at different time intervals after surgery in the two groups were as follows: in the T3 time period of group N, a significant difference was observed only in the occurrence of postoperative complications among patients with different levels of PONV (χ²=24.786, P<0.01). However, in the T4 time period, significant differences were found in the occurrence of postoperative complications among both the same level and different level PONV patients (χ²=15.435, 15.435, both P<0.01). Significant differences were also observed in the occurrence of postoperative complications among the same level and different level PONV patients in both the T3 and T4 time periods of group S (all P<0.01). Conclusion: Sugammadex can be used to reverse muscle relaxation in patients undergoing intracranial aneurysm intervention surgery,and it does not have a significant impact on the incidence of PONV, it can also optimize the quality of anesthesia recovery and reduce the incidence of complications after intracranial aneurysm embolization surgery.
Male ; Humans ; Female ; Sugammadex ; Postoperative Nausea and Vomiting/chemically induced* ; Neostigmine/adverse effects* ; Intracranial Aneurysm/surgery* ; gamma-Cyclodextrins/adverse effects* ; Atropine

Recently, increasing attention has been paid to beads, an innovative self-assembled drug delivery system prepared from cyclodextrins and oils. Beads are new core-shell minispheres containing poorly water-soluble drugs or lipophilic drugs dissolved in the lipid core without the use of organic solvents and surfactants. Therefore, beads with high drug loading and improved oral bioavailability have great potential for oral delivery of poorly water-soluble drugs and lipophilic drugs. The preparation mechanisms, formulations and methods, the in vitro and in vivo properties of beads were reviewed in order to provide the theoretical basis for further application of beads.
Administration, Oral ; Animals ; Biological Availability ; Drug Carriers ; Drug Delivery Systems ; Particle Size ; Solubility ; Soybean Oil ; administration & dosage ; chemistry ; pharmacokinetics ; alpha-Cyclodextrins ; administration & dosage ; chemistry ; pharmacokinetics