AIM:To study the effect of different quantities of carboxymethyl chitosan(CMCT) modification to the pharmacokinetic performance of PTX-LP in rats.METHODS:Plasma was extracted with tert-butyl methyl ether and Norethisterone was employed as internal standard after i.v.unmodified PTX-LP,(0.1)%CMCT modified PTX-LP and(0.2)%CMCT modified PTX-LP in rats.Plasma samples were analyzed on a C_(18) column at 227 nm and the mobile phase was methanol and water(6535,v/v).RESULTS:The plasma concentration-time profile in rats after iv.unmodified PTX-LP,(0.1)% CMCT modified PTX-LP and(0.2)% CMCT modified PTX-LP follow bi-exponential disposition.T_(1/2?) are(11.20),(15.55) and(30.6) h respectively,AUC were(2541.99),(2748.78) and(3451.64)(mg?L~(-1)?min) for each of them.CONCLUSION:Significant changes of in vivo pharmacokinetic performance have been found after CMCT modification to PTX-LP in rats by comparison with unmodified LP.T_(1/2?) and circulation time in plasma have been lengthened and AUC has been improved in some extent.We found that this kind of long circulating action had some correlation with the quantities of CMCT employed.

OBJECTIVETo prepare the oridonin submicron emulsion and characterize their properties.

METHODHigh pressure homogenization method was employed to prepare the oridonin submicron emulsion and such properties as size, Zeta potential and viscosity were characterized.

RESULTThe results showed that the submicron emulsions was formed with the drug loading 1 g L(-1), particle size of (138.87 +/- 0.60) nm, zeta potential of (47.27 +/- 2.31) mV, pH value of (6.02 +/- 0.03) and viscosity of (1.78 +/- 0.015) MPa s, respectively.

CONCLUSIONThe method is feasible and the submicron emulsions has stable properties. Experiments offer a new formulation of oridonin for clinical application.

Chemistry, Pharmaceutical ; Diterpenes, Kaurane ; chemistry ; Emulsions ; chemistry ; Particle Size ; Viscosity

Objective To design a handhold emergency suction apparatus, in order to meet the needs of clinical therapy, field and on-site emergency treatment. Methods The apparatus was divided into such components as handle, grab handle, L tie, piston, waste liquid tank and its cap, and the junction between the parts, and then the optimum design of the components were performed. Results Through the optimum design, the apparatus was improved from the aspects of portability, easy-to-use and reliability. Conclusion It is proved by practice that the apparatus also can reduce the labor intensity of healthcare staff, and definitely satisfy the clinical rescue and the treatment needs.

The purpose of this study was to develop a novel phospholipidas-based in-situ gel sustained-release formulation of levobupivacaine hydrochloride injection. Appropriate formulation was screened based on the factors such as phospholipid type, ratio of phospholipid to ethanol, ratio of water to phospholipid-ethanol mixture, which indicated typical in-situ gel profiles. Pharmacokinetic study using beagles showed that there were delayed tmax and prolonged t1/2 in levobupivacaine plasma-time profile after administration of the phospholipidas-based in-situ gel formulation if compared to commercially available conventional levobupivacaine hydrochloride injection. Pharmacodynamic studies conducted on guinea-pig demonstrated that it maintained 48-72 hr regional anesthesia, much longer than that of the anesthesia in the group receiving conventional injection. Hence, this novel in-situ gel intended for injection is worthy of development.

In this report, a series of novel piperidine-substituted thiophene[3,2-]pyrimidine derivatives were designed to explore the hydrophobic channel of the non-nucleoside reverse transcriptase inhibitors binding pocket (NNIBP) by incorporating an aromatic moiety to the left wing of the lead . The newly synthesized compounds were evaluated for anti-HIV potency in MT-4 cells and inhibitory activity to HIV-1 reverse transcriptase (RT). Most of the synthesized compounds exhibited broad-spectrum activity toward wild-type and a wide range of HIV-1 strains carrying single non-nucleoside reverse transcriptase inhibitors (NNRTI)-resistant mutations. Especially, compound exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR). Moreover, the RT inhibition activity, preliminary structure-activity relationship and molecular docking were also investigated. Furthermore, exhibited favorable pharmacokinetics (PK) profiles and with a bioavailability of 33.8%. Taken together, the results could provide valuable insights for further optimization and compound holds great promise as a potential drug candidate for the treatment of HIV-1 infection.

Novel therapies are urgently needed to improve global treatment of SARS-CoV-2 infection. Herein, we briefly provide a concise report on the medicinal chemistry strategies towards the development of effective SARS-CoV-2 inhibitors with representative examples in different strategies from the medicinal chemistry perspective.