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At least 55 records · Page 3Linked to original sources
PubMed2006

Validation of direct assay of an aqueous formulation of a drug compound AZY by chiral supercritical fluid chromatography (SFC).

Supercritical fluid chromatography (SFC) is increasingly being recognized as a powerful technique for analysis of pharmaceutical compounds in various dosage forms. Assay of aqueous formulations of research compounds by SFC is, however, a relatively unexplored area primarily due to the potential problems associated with it. This work describes the development of a direct assay of a chiral drug compound AZY in a 100% aqueous formulation by SFC, and its qualification following ICH and FDA validation guidelines on chromatographic methods. The results indicated that SFC has the potential for assaying aqueous formulations of research compounds with high degree of selectivity, accuracy, precision, robustness, sensitivity, and linearity over a wide range of concentrations. This work also confirmed a previous hypothesis that direct formulation assay by SFC approach is applicable to both acidic and basic pharmaceutical compounds with equal degree of success.

Amylose↗
PubMed2003

[Effect of acupuncture-drug compound anesthesia on alteration of immune function in patients undergoing open-heart surgery].

OBJECTIVE: To observe the effect of electro-acupuncture (EA) on alteration of immune function of patients undergoing open-heart surgery with cardiopulmonary bypass (CPB), and to appraise the value of acupuncture-drug compound anesthesia in the operation. METHODS: Thirty patients undergoing atrial septal defect repairing operation were selected and divided into three groups, Group A was the general anesthesia group; Group B, the acupuncture anesthesia group and Group C, the general anesthesia plus EA group. Peripheral venous blood of patients was collected at different time points, i.e. before anesthesia, before CPB, 30 min and 24 hrs after CPB, to determine natural killer cells activity (NKCA), and the levels of interferon-gamma (IFN-gamma) and interleukin-2 (IL-2) in supernatant of cell culture were also tested. RESULTS: NKCA was significantly lowered in Group A before CPB but increased in Group B, while no evident change was found in Group C, so the level of NKCA in Group B was significantly higher than in the other two groups. It lowered in all the three groups after CPB, especially evidently in Group B, so as to cause the NKCA level in Group B lower than that in Group A. The lowering further progressed, 24 hrs after CPB, NKCA in Group B was more reduced than that in Group C. Levels of IFN-gamma and IL-2 lowered in all the three groups after CPB, and further lowered at time point of 24 hrs after CPB, but the parameters in Group C were significantly higher than those in Group B. CONCLUSION: EA could enhance NKCA, but acupuncture anesthesia couldn't inhibit the suppressive effect of CPB on NKCA, IL-2 and IFN-gamma, suggesting that the immunosuppression induced by stress has a prior effect. General anesthesia plus EA yielded better effect than general anesthesia and acupuncture anesthesia, but it could't improve the immunosuppression completely, indicating that the compound anesthesia could partially improve the immunosuppression induced by CPB.

Acupuncture Analgesia↗
PubMed2006

A novel method for oral delivery of drug compounds to the neonatal SMNDelta7 mouse model of spinal muscular atrophy.

Spinal muscular atrophy (SMA) is a devastating motor neuron disease that is one of the leading genetic causes of infant mortality. Currently, there is no cure for SMA. Mouse models that genetically and phenotypically resemble SMA have been generated and have the potential to be used for the discovery of novel therapeutics. Oral administration is a commonly used mode of drug delivery in humans as well as in rodents. Unfortunately, there is no method of drug delivery that can accurately and reliably deliver drug compounds orally to neonatal mice. In this report, we describe a novel method to orally administer compounds to neonatal SMA mice. Oral delivery to neonatal mice, usually starting at postnatal day 4 (PND04), is both rapid and safe to the pup. Oral delivery of two different commonly used vehicle formulations, distilled water and 2-hydroxypropyl-beta-cyclodextrin, does not affect the survival of SMA mice. After oral delivery for 3 days, 5-bromo-2'-deoxyuridine could be detected in the kidneys, brains and spinal cords of treated non-SMA as well as SMA neonatal pups. In conclusion, we have developed a method by which drugs can be safely and reliably administered orally to neural targets of neonatal mice. This approach offers a simple and rapid means by which potential therapeutics for SMA can be identified.

Administration, Oral↗
PubMedDate not supplied

QSPR correlation of melting point for drug compounds based on different sources of molecular descriptors.

Five linear QSPR models for melting points (MP) of drug-like compounds are developed based on three different packages for molecular descriptor generation and a combined set of all descriptors. A data set of 323 gaseous, liquid, and solid compounds was used for this study. Two models from the combined set of descriptors based on stepwise regression and genetic algorithm (GA) descriptor selection methods have acceptable prediction abilities. The statistical results of these models are r2 = 0.673 and root-mean-square error (RMSE) of 40.4 degrees C for stepwise regression-based quantitative structure-property relationships (QSPRs) and r2 = 0.660 and RMSE of 41.1 degrees C for GA-based QSPRs. Interpretation of descriptors of all models showed a strong correlation of hydrogen bonding and molecular complexity with melting points of drug-like compounds.

Databases as Topic↗
PubMed1999

Discriminative effects of compound drug stimuli: a focus on attention.

Discrimination research has increasingly used compound stimuli emerging from drugs acting through multiple neurotransmitter systems or from injections of drug mixtures that approximate "street-wise" drug-taking behaviors. Accompanying this trend has been an interest in the role of cognitive factors in drug discrimination learning. Accounts of multidimensional drug stimuli have focused mainly on specific neuronal mechanisms, and have largely ignored the contribution of stimulus information to the perception of internal events or to the selection processes, heretofore called attention mechanisms, which may underlie the observer's idiosyncratic response to drug administration. It is argued here that research in drug discrimination may benefit from a more detailed consideration of the processes by which an observer interacts with the emergent stimulus properties of drug administration. Therapeutic intervention initiatives may critically depend on knowing the interactions between the specific attributes of the drug experience that capture the attention of the individual and that may later acquire stimulus control over complex drug-taking behaviors.

Animals↗
PubMed2003

Direct plasma analysis of drug compounds using monolithic column liquid chromatography and tandem mass spectrometry.

A monolithic silica column high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method has been developed for the high-speed direct simultaneous determination of a drug discovery compound and its major circulating metabolite (M-72) in rat plasma. This methodology makes use of flow programming and an alkyl-bonded silica rod column for fast macromolecule removal and chromatographic separation without the need for significant sample preparation. The matrix ionization suppression effect on the monolithic column HPLC-MS/MS system was investigated using the postcolumn infusion technique. After 200 plasma injections on a 50 x 4.6 mm monolithic silica column, consistent column efficiency of close to 39,000 theoretical plates/m and reproducible retention times for the analytes were observed. The apparent on-column recoveries of 12 test compounds in rat plasma samples were greater than 90%. The proposed fast direct plasma injection method was tested over a 3-day period with the interday coefficient of variation less than 15% for both analytes.

Calibration↗
PubMed2005

Release characteristics of anionic drug compounds from liquid crystalline gels I: Passive release across non-rate-limiting membranes.

Liquid crystalline gels (LCG) offer the formulator dynamic and flexible vehicles, into which actives, enhancers and other adjuvants with a wide range of physicochemical properties can be incorporated. This is achievable because of the biphasic oil/water composition of the gel. In this paper, the suitability of an isotropic liquid crystalline gel is investigated for a range of anionic drug molecules, with particular emphasis on sodium diclofenac. Parameters, which have been investigated, include the mode of vehicle preparation, the effect of the concentration of the drug and how buffering the gel and/or the receptor medium affect the release profiles. Such profiles have been measured for the sodium salts of benzoate, salicylate and indomethacin. The passive release from the standard system was found to adhere to matrix-controlled diffusion. An increase in concentration leads to a non-linear increase in the cumulative release of sodium diclofenac from the gels. In direct contrast to the result reported for cationic salbutamol base, optimum release from the gel was achieved when neither the receptor medium nor the aqueous phase of the gel was buffered. The percentages released of the sodium salts of benzoate, salicylate and indomethacin, after 24 h, were determined to be 25, 26 and 19%, respectively, and these are significantly greater than the release of sodium diclofenac. This suggests that diclofenac undergoes ion-pairing or complexation within the gel, which inhibits its diffusion from the vehicle. Future papers will report on the incorporation of enhancers and the effects of iontophoresis on the release profiles of drugs from these gels, and ultimately on the transdermal transport of drugs from these vehicles across human and porcine skin.

Agar↗