Study on the inclusion technic of hydroxypropyl-β-cyclodextrin in tea tree oil and evaluation of its included compounds / 国际中医中药杂志

Objective@#This study takes hydroxypropyl-β-cyclodextrin (HP-β-CD) as the inclusion materials to optimize the preparation technic of tea tree oil (TTO) and evaluate its pharmaceutical performance.@*Methods@#Take the production rate of HP-β-CD tea tree oil inclusion and entrapment rate as the evaluation index, taking the orthogonal test method to optimize the production technic of tea tree oil (HP-β-CD inclusion and using infrared (IR), differential thermal scanning (DSC) method to characterize the inclusion compound to analyze the stability of TTO-HP-β-CD.@*Results@#The best technic to produce HP-β-CD tea tree oil is as follow: the ratio of TTO and HP-β-CD should be equal to 1/10, at 40 ℃, within 1 h. The average drug loading shoud be 9.25% ± 3.25%. The IR, DSC characterization results showed that the characteristic peak of tea tree oil disappeared after the microspheres, which indicated the HP-β-CD encapsulated the tea tree oil with good compatibility. In 80 ℃ water bath, the TTO-HP-β-CD was stable with the retention rate 40% after 8 h, the retention rate was 4.32 times than that of the unwrapped tea tree oil.@*Conclusions@#The HP-β-CD tea tree oil obviously has higher rate of inclusion and stability. Therefore, it’s worth to promoting and being used in the pharmacy preparations and cosmetics field.

Preparation and characterization of nifedipine skeleton frame sustained release tablets with hydroxypropyl-beta-cyclodextrin and polyethylene glycolas as matrix / 重庆医学

Objective To prepare nifedipine (NP)skeleton frame sustained release tablets by adopting hydroxypropyl-beta-cy-clodextrin (HPC)and polyethylene glycol (PEG)as the matrix and to investigate its sustained release effect on NP.Methods NP skeleton frame sustained release tablets were prepared by the direct compression method after forming the inclusion complex with NP and HPC on a 1∶1 ratio and mixing with PEG.The in vitro drug release curves and the in vivo concentration-time curves of NP skeleton frame sustained release tablets were detected with the NP-PEG tablet without inclusion complex,NP-HPC tablet and NP powder capsule (NP capsule)as the control.Results The 5 h cumulative release rate of NP skeleton frame sustained release tablet in the simulated gastric fluid test(pH 1.2)was 36.4%,its sustained release effect was significantly stronger than that of the NP-HPC tablet group (80%,P<0.01)and the NP-PEG tablet group (100%,P<0.01).The in vivo test showed that AUC0-12 [(6 413±436)h/(ng·mL)],Cmax[(983±192)ng/mL]and tmax[(5.7±1.1)h]in the NP skeleton frame sustained release group were significantly higher than those in the NP-HPC tablet group,the NP-PEG tablet group and the NP Capsule group (all P<0.01 or 0.05).Conclusion NP skeleton frame sustained release tablets exhibits the sustained release effect on NP,can extend the NP in vitro release time,and improve the NP′s bioavailability,which is a novel NP sustained release tablet with excellent properties.

Current and Emerging Antifungal Agents in Japan / 대한의진균학회지

Currently available antifungal agents for the treatment of systemic fungal infections in Japan are smaller in number than those in the United States and Europe and probably in Korea. Therefore, the development of novel antifungal drugs for clinical use, including new formulations of approved agents, with advantages over and/or complimentary to existing agents is particularly needed in Japan. In this review, I have described historical perspectives of existing systemic antifungal agents and provided a brief overview of the current status of clinical development of several different categories of new drugs as follows: (1) liposomal amphotericin B; (2) itraconazole-hydroxypropyl-beta-cyclodextrin complexes; (3) phosphatyl fluconazole (phosfluconazole) ; (4) voriconazole; and (5) micafungin (FK463). At this moment, micafungin, a member of echinocandins attracts the greatest attention of Japanese medical mycologists because it has just been introduced into the clinic and has unique chemical and biological characteristics distinct from any other existing class of antifungal drugs. Micafungin, as well as other new drugs under clinical development, should constitute effective new options for the management of a variety of systemic fungal infections.