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1.
Journal of Pharmaceutical Practice ; (6): 108-113, 2024.
Article in Chinese | WPRIM | ID: wpr-1012790

ABSTRACT

Objective To prepare flumazenil sublingual tablets and study its bioavailability. Methods Flumazenil sublingual tablets were prepared by compressing flumazenil inclusion compound with hydroxypropyl-β-cyclodextrin as the inclusion material. In a double-cycle crossover trial, twelve beagle dogs were randomly divided into two groups, one group receiving flumazenil sublingual tablets and the other receiving flumazenil injections. LC-MS method was developed and validated to determine flumazenil plasma concentration. The pharmacokinetic parameters and bioavailability were calculated using WinNonlin pharmacokinetic software. Results In the pharmacokinetic study, AUClast of flumazenil injection and sublingual tablet was (8.41±2.15) and (8.86±2.83) h·ng·ml−1, respectively; Cmax was (10.96±2.62) and (6.36±2.14) ng/ml, respectively; tmax was (0.18±0.05) and (0.58±0.24) h, respectively. The bioavailability of flumazenil sublingual tablet was 52.68%. Conclusion Clathrates were used to prepare flumazenil sublingual tablets to achieve safe and efficient delivery. LC-MS method was established for the determination of flumazenil plasma concentration, and the advantages were simple, accurate and sensitive.

2.
Journal of Pharmaceutical Practice ; (6): 73-77, 2024.
Article in Chinese | WPRIM | ID: wpr-1006844

ABSTRACT

Objective To construct methoxy polyethylene glycol (mPEG) modified gold nanoparticles (AuNPs) loaded with doxorubicin (DOX) AuNPs-mPEG@DOX in order to reduce the toxicity and side effects of DOX. Methods AuNPs-mPEG@DOX was prepared and characterized by Z-Average, Zeta potential and UV-Vis spectroscopy. The impact of thiol-linked DOX (HS-DOX) at various dosage concentrations on the drug adsorption rate and drug loading of AuNPs-mPEG@DOX was investigated. Furthermore, a HPLC method was developed to accurately determine the content of unadsorbed HS-DOX in AuNPs-mPEG@DOX. The specificity, linearity, precision, stability and average recovery of this method were thoroughly investigated. The cytotoxic effect of AuNPs-mPEG@DOX on MCF-10A and MCF-7 cells was evaluated using a CCK-8 assay. Results AuNPs-mPEG@DOX was successfully prepared with Z-Average of (46.12±0.49) nm, Zeta potential of (18.60±1.51) nm and the maximum absorption wavelength of 530 nm. An efficient HPLC method for the detection of unadsorbed HS-DOX in AuNPs-mPEG@DOX was devised. The optimal dosage concentration of HS-DOX for AuNPs-mPEG@DOX was determined to be 11.18 μg/ml, resulting in a drug adsorption rate of (9.21±2.88)% and a drug loading rate of (2.01±0.62)%. Cytotoxicity experiments demonstrated that AuNPs-mPEG@DOX significantly reduced the toxic and side effects of DOX on normal breast cells. Additionally, AuNPs-mPEG@DOX and free DOX exhibited comparable cytotoxic effects on breast tumor cells when DOX concentration was equal to or greater than 4.75 μmol/L. Conclusion AuNPs-mPEG@DOX effectively reduce the toxicity of DOX, providing a reference for future research on reducing the toxicity of AuNPs-linked drugs.

3.
Journal of Pharmaceutical Practice ; (6): 1-5, 2024.
Article in Chinese | WPRIM | ID: wpr-1005419

ABSTRACT

Sprays have gained significant attention and widespread use due to their numerous advantages, including rapid action, safety, and convenience. They are widely used in various fields such as dermatology, respiratory disease treatment, wound repair, and central nervous system targeted drug delivery. With the in-depth research of new drugs and modern pharmaceutics, the development ideas of sprays are more diverse, and the application scenarios are increasingly extensive. In this review the clinical application status of sprays and the latest research progress were summarized. Then the quality control parameters were briefly introduced,which provided reference for the research and development of sprays.

4.
Journal of Pharmaceutical Practice ; (6): 14-17, 2023.
Article in Chinese | WPRIM | ID: wpr-953752

ABSTRACT

Reactive oxygen species(ROS) responsive liposomes are prepared based on the high level of ROS expression in the tumor microenvironment, enabling precise drug delivery to the tumor site. With the addition of photosensitizer, the controllability of drugs in liposomes can be further enhanced.

5.
Journal of Pharmaceutical Practice ; (6): 273-276, 2023.
Article in Chinese | WPRIM | ID: wpr-973683

ABSTRACT

Tetrodotoxin (TTX) is a neurotoxin found in puffer fish and other marine organisms. It has been used as an inhibitor of voltage-gated sodium channels (VGSCs), which could selectively bind to the α-subunit on the outer vestibule of VGSCs, preventing sodium ions from entering the channel, resulting in pharmacological activities. As a typical sodium channel blocker, TTX shows a significant analgesic effect. TTX could selectively block Na+ channels without affecting other ion channels, therefore it could reduce the probability of adverse reactions caused by commonly used antiarrhythmic drugs. In addition, TTX has a significant role in detoxification and prevention of renal failure, so TTX has great potential as a medicine. The structure and physicochemical properties, mechanism of action, pharmacological activities and preparations of tetrodotoxin have been reviewed in this paper, so as to provide a general support for the evaluation of its druggability and application in the field of pharmacy.

6.
Journal of Pharmaceutical Practice ; (6): 182-186, 2023.
Article in Chinese | WPRIM | ID: wpr-965570

ABSTRACT

Objective To establish a detection method for the determination of tetrodotoxin (TTX) in sustained-release microspheres. Methods The HPLC separation of tetrodotoxin was performed on an Agilent ZORBAX SB-C18 column (4.6mm×150mm,5 μm) with acetonitrile, 8mmol/L sodium heptane sulfonate containing 0.005% TFA (5:95) (pH 4.0) as the mobile phase. The flow rate was 1.0 ml/min. The UV detection wavelength was 200 nm and the column temperature was 30 °C. Results The method had good specificity and linearity of TTX in the concentration range of 1−20 μg/ml. The intra-day precision, inter-day precision, stability and repeatability of the method were good, and the average recoveries were found between 98.0% and 102.0%. Conclusion This study established an HPLC method which was suitable for the determination of tetrodotoxin sustained-release microspheres. The method is accurate and reliable within the applicable range, with strong specificity, which could lead to quantitative detection.

7.
Acta Pharmaceutica Sinica B ; (6): 3124-3138, 2022.
Article in English | WPRIM | ID: wpr-939960

ABSTRACT

Tumor-associated macrophages (TAMs), one of the dominating constituents of tumor microenvironment, are important contributors to cancer progression and treatment resistance. Therefore, regulation of TAMs polarization from M2 phenotype towards M1 phenotype has emerged as a new strategy for tumor immunotherapy. Herein, we successfully initiated antitumor immunotherapy by inhibiting TAMs M2 polarization via autophagy intervention with polyethylene glycol-conjugated gold nanoparticles (PEG-AuNPs). PEG-AuNPs suppressed TAMs M2 polarization in both in vitro and in vivo models, elicited antitumor immunotherapy and inhibited subcutaneous tumor growth in mice. As demonstrated by the mRFP-GFP-LC3 assay and analyzing the autophagy-related proteins (LC3, beclin1 and P62), PEG-AuNPs induced autophagic flux inhibition in TAMs, which is attributed to the PEG-AuNPs induced lysosome alkalization and membrane permeabilization. Besides, TAMs were prone to polarize towards M2 phenotype following autophagy activation, whereas inhibition of autophagic flux could reduce the M2 polarization of TAMs. Our results revealed a mechanism underlying PEG-AuNPs induced antitumor immunotherapy, where PEG-AuNPs reduce TAMs M2 polarization via induction of lysosome dysfunction and autophagic flux inhibition. This study elucidated the biological effects of nanomaterials on TAMs polarization and provided insight into harnessing the intrinsic immunomodulation capacity of nanomaterials for effective cancer treatment.

8.
Journal of Pharmaceutical Practice ; (6): 520-524, 2021.
Article in Chinese | WPRIM | ID: wpr-904752

ABSTRACT

Objective To compare the differences in the anti-tumor growth effects of organisms with different injections of CT26 tumor cell RNA loaded into nanoliposomes. Methods The extracted tumor RNA was loaded into nanoliposomes to prepare tumor RNA nanoliposome vaccines, and the related properties of nanoliposome vaccines were investigated. The particle size of nanoliposome vaccines was (120.0±12.1)nm and zeta potential was (3.39±0.56)mV. Tumor RNA nanoliposome vaccines were injected into different parts of the mice to test and analyze the influence of different injections on the growth of colon cancer transplanted tumors in mice. Results Tumor RNA nanoliposome vaccines were used to inject tumor-transplanted mice in different ways. Compared with underarm injection, intraperitoneal injection enhanced the organism's anti-tumor immune response and inhibited the growth of transplanted tumors more effectively. The H&E staining of important organs in mice was compared and no obvious organic lesions were found in the organs. Conclusion Intraperitoneal injections of nanoliposome loaded with tumor RNA can enhance the body's anti-tumor immune response more effectively than underarm injections.

9.
Journal of Pharmaceutical Practice ; (6): 211-214, 2021.
Article in Chinese | WPRIM | ID: wpr-876851

ABSTRACT

Nanomaterials, with the advantages of unique microstructure, have been widely used in the fields of material manufacturing, microelectronics and computer technology, medicine and health, environment and energy. Compared with traditional hemostatic materials, nanomaterials can improve the bioavailability and stability of traditional hemostatic drugs to a certain extent, enhance the controlled and targeted release of drugs, which lay a good foundation for the development of new-style modern hemostatic nanomaterials. This paper reviews the advanced design and application progress of various nanomaterials in hemostasis, such as liposomes, nanoparticles, self-assembled nano peptides, nanofibers, etc. Finally, the challenges and prospects of hemostatic nanomaterials are briefly described.

10.
Journal of Pharmaceutical Practice ; (6): 30-33,54, 2018.
Article in Chinese | WPRIM | ID: wpr-790828

ABSTRACT

Objective To study the effect of flumazenil on hypnotic mice induced by diazepam and zolpidem ,and to eval-uate the possibility of flumazenil oral administration .Methods First ,Kunming mice were injected intraperitoneally with nor-mal saline and sodium pentobarbital (S + W) ,diazepam and pentobarbital sodium (D + W) ,zolpidem and pentobarbital sodi-um (Z + W) .The hypnotic effect of diazepam and zolpidem on prolonging the sleep time of pentobarbital sodium would be ver-ified by (D + W) group and (Z + W) group .Then the mice were injected intraperitoneally with flumazenil .The sleep time was used as the evaluation index to evaluate the effect of flumazenil against hypnosis . Finally , the oral administration of flumazenil was observed against hypnosis ,which was evaluated by using sleep time as an index .Results Compared with the control group (S+W) ,the diazepam group (D+W) and the zolpidem group (Z+W) significantly prolonged the sleep time in-duced by pentobarbital sodium (P<0 .001 ,P<0 .05);After Intraperitoneal injection of flumazenil ,compared with the diazepam group (D+W) and the zolpidem group (Z+W) ,the sleep time of the diazepam group [F(ip)+D+W] and the zolpidem group [F(ip)+Z+W] were significantly shorter (P<0 .001 ,P<0 .05);After oral administration of flumazenil ,the sleep time of the diazepam group [F(ig)+ D+ W] and the zolpidem group [F(ig)+ Z+ W] were also significantly shorter (P< 0 .001 ,P<0.05) .Conclusion Flumazenil ,whether intraperitoneal injection or intragastric administration ,could antagonize the hypnotic effect of diazepam and zolpidem .It was proved that oral administration of flumazenil had the same effect compared with intrap-eritoneal injection of flumazenil ,which provided the possibility of preparation of oral administration of flumazenil .

11.
Journal of Pharmaceutical Practice ; (6): 485-489, 2017.
Article in Chinese | WPRIM | ID: wpr-790801

ABSTRACT

Flumazenil ,a benzodiazepine antagonist ,specifically binds the benzodiazepine receptors in central nervous system and reduces the release of gamma-aminobutyric acid .It is used for the reversal of sedative effects of benzodiazepine and benzodiazepine-induced anesthesia .In this article ,the clinical applications of flumazenil and the developments of different dos-age forms were reviewed .

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