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1.
Article in Chinese | WPRIM | ID: wpr-920651

ABSTRACT

@#In this study, different functional layer formulations and process parameters were used to prepare the levomilnacipran hydrochloride sustained-release capsules, the influence of functional layer formulation and process factors on dose dumping was studied by comparing their release curves in 40% ethanol; and the risk of dose dumping of the self-developed drug was evaluated by the similar factors of the release curve of the self-developed drug and the reference drug.The results showed that as the coating weight increased, the degree of dose dumping decreased; when the concentration of ethanol in the coating liquid solvent was less than 80%, the dose dumping increased; as the atomization pressure and maturation time increase, the dose dumping became more serious. In 0% ethanol (purified water), 5% ethanol, 20% ethanol and 40% ethanol media, the self-developed and reference preparations had the same degree of dose dumping within the specified time, and rotation speed had no significant effect on the release of metformin in vitro. In summary, formulation factors such as coating weight gain, ethanol concentration in the coating solution solvent, and process factors such as atomization pressure and curing time have a serious impact on the dose dumping of sustained-release capsules.Under the optimal functional layer formulation and process, special attention should be paid to the control of risk of self-developed dose dumping.

2.
Article in Chinese | WPRIM | ID: wpr-907158

ABSTRACT

Objective To study the release profile of curcumin and piperine from the compound self-microemulsion. Methods The release of curcumin and piperine in vitro was investigated by dynamic dialysis under the condition of phosphate buffer of pH 4.8 and 7.5 with 0.75% Tween-80. Results The cumulative release rates of curcumin in pH 4.8 and pH 7.5 were 94.85% and 84.38% in 108 h, respectively. The cumulative release rates of piperine were 92.85% and 90.05% in 36 h, separately. Conclusion Curcumin and piperine in self-microemulsion have sustained release properties and released more in the acidic environment similar to the environment in tumors.

3.
China Pharmacy ; (12): 848-852, 2022.
Article in Chinese | WPRIM | ID: wpr-923192

ABSTRACT

OBJECTIVE To prepare cinnamaldehyde (CA) loaded liposomes bilayer-modified by bovine serum albumin (BSA)/chitosan (CTS)(BSA/CTS-Lip-CA) in order to improve the sustained-release effect and storage stability of the nanoparticles. METHODS Firstly,cinnamaldehyde loaded liposomes (Lip-CA)and blank liposomes (Lip-Blank)were prepared by thin film dispersion method. Then chitosan modified cinnamaldehyde loaded liposome (CTS-Lip-CA)and BSA/CTS-Lip-CA were obtained by electrostatic adsorption. Finally , the prepared liposomes were characterized , and their in vitro release characteristics and storage stability were investigated. RESULTS The particle size of BSA/CTS-Lip-CA was (177.8±4.0)nm and the Zeta potential was (-15.6±1.5)mV;they were in spherical shape ;FTIR analysis showed that the modification of BSA and CTS had no effect on the internal structure of liposomes. The results of in vitro drug release characteristics showed that the cumulative release of Lip-CA ,CTS-Lip-CA and BSA/CTS-Lip-CA within 10 hours were 82.9%,74.1% and 72.9% respectively. The results of storage stability showed that after 30 days of storage ,the particle sizes of Lip-CA ,CTS-Lip-CA and BSA/ CTS-Lip-CA were (134.2±2.1),(151.7±0.4),(164.8±1.5)nm;the retention rates of model drug CA were 65.4%,82.5% and 90.2% respectively. CONCLUSIONS BSA/CTS-Lip-CA is successfully prepared. It has a certain sustained-release effect and can improve the storage stability of the drug to a certain extent.

4.
Article in Chinese | WPRIM | ID: wpr-921635

ABSTRACT

In this paper, co-processed lactose SuperTab 40 LL was selected as fillers to study the preparation of musk sustained-release mini-tablets in the Xihuang multiple-unit drug release system. Musk sustained-release tablets containing different proportions of SuperTab 40 LL and MCC were prepared under various pressures, and then the compressibility and compactibility of these prescriptions were evaluated by Walker, Heckel and Ryshkewitch-Duckworth equations. In addition, the fluidity of the prescriptions was evaluated by parameters of Kawakita equation. There was a comprehensive analysis of the effect of SuperTab 40 LL on musk sustained-release mini-tablets combined with the appearance of SuperTab 40 LL and their tensile strength. The results shown that SuperTab 40 LL had better compression process through the Heckel equation, and the direct compression process of drug powders with excipients can be analyzed by the Kawakita and Ryshkewitch-Duckworth equations. As a new type of co-processed lactose, SuperTab 40 LL had a good fluidity and compactibility. SuperTab 40 LL may undergo particle crushing and plastic deformation during the compression process, which increased the contact area and bonding sites between the particles, and aggregated and shaped the mixed powder easy. Moreover, MCC showed a synergistic effect, and the combined application with SuperTab 40 ll could effectively improve the fluidity and compressibility of the musk sustained-release powder. When the ratio of SuperTab 40 LL and MCC was 2∶1, musk sustained-release mini-tablets had a high drug loading capacity and good compactibility in line with the design objectives.


Subject(s)
Delayed-Action Preparations , Drug Compounding , Excipients , Fatty Acids, Monounsaturated , Models, Theoretical , Powders , Tablets
5.
Article in Chinese | WPRIM | ID: wpr-904326

ABSTRACT

@#In order to evaluate the consistency of the release behavior between the self-made saxagliptin and metformin hydrochloride sustained-release tablets and the reference preparations in vitro, the similarity of the dissolution curves between the self-made preparations and the reference preparations in four dissolution mediums: HCl (pH 1.0), acetate buffer saline (pH 4.5), phosphate buffer saline (pH 6.8) and pure water, and the gel morphology and strength of the self-made preparations and the reference preparations in the HCl (pH 1.0) solution medium were compared.Results showed that in four dissolution mediums, the dissolution rates of saxagliptin in the self-made preparations and the reference preparations at 15 min were greater than 85%, and the ?2 similarity factors of metformin hydrochloride were 89, 83, 80, 86, all greater than 50, so the dissolution of the self-made preparations was consistent with those of the reference preparations.The volume expansion rate, water absorption rate and erosion rate were consistent with those of the reference preparations, and the gel strength of the self-made preparations was the same as that of the reference preparations.The in vitro release behaviors of the self-made preparations and the reference preparations are consistent, which provide a good guarantee for bioequivalence.

6.
Acta Pharmaceutica Sinica B ; (6): 2565-2584, 2021.
Article in English | WPRIM | ID: wpr-888872

ABSTRACT

Pulmonary administration route has been extensively exploited for the treatment of local lung diseases such as asthma, chronic obstructive pulmonary diseases and respiratory infections, and systemic diseases such as diabetes. Most inhaled medicines could be cleared rapidly from the lungs and their therapeutic effects are transit. The inhaled medicines with extended pulmonary exposure may not only improve the patient compliance by reducing the frequency of drug administration, but also enhance the clinical benefits to the patients with improved therapeutic outcomes. This article systematically reviews the physical and chemical strategies to extend the pulmonary exposure of the inhaled medicines. It starts with an introduction of various physiological and pathophysiological barriers for designing inhaled medicines with extended lung exposure, which is followed by recent advances in various strategies to overcome these barriers. Finally, the applications of the inhaled medicines with extended lung exposure for the treatment of various diseases and the safety concerns associated to various strategies to extend the pulmonary exposure of the inhaled medicines are summarized.

7.
China Pharmacy ; (12): 2327-2335, 2021.
Article in Chinese | WPRIM | ID: wpr-886912

ABSTRACT

OBJECTIVE:To optimize the form ulation of Zuojin pectin c apsules,and to prepare modern Zuojin pectin capsules with protective effects against gastric ulcers. METHODS :The formulation of Zuojin pectin capsules was optimized with orthogonal test with the contents of pectin ,soluble starch and dextrin as factors ,using formability ,moisture absorption and flow ability as indicators. Zuojin pectin capsule was prepared by wet granulation filling method with Zuojin extract powder as raw material. The contents of palmatine hydrochloride ,berberine hydrochloride ,evodiamine and rutaecarpin were evaluated by HPLC. Basket method was used to investigate the release behavior of the capsule in 0.1 mol/L HCl solution. The gastric ulcer model of rats was established by intragastric administration of 75% ethanol. Gastric ulcer index ,the inhibition rate of gastric ulcer and the pathological sections were used as indexes to investigate the protective effect of Zuojin pectin capsules (the doses were 54,108, 216 mg/kg)on gastric ulcer. RESULTS :The optimal formulation of Zuojin pectin capsules included 45% pectin,12% soluble starch,27% dextrin and 1% xylitol. Results of in vitro drug , release showed that palmatine hydrochloride and berberine, hydrochloride in Zuojin pectin capsules released 53.76% and No.54.82% respectively within 1 h,completely released at about 8 h, and conformed to the zero-order release behavior. 2492109374@qq.com Different doses of Zuojin pectin capsule could improve the ulcer injury of gastric tissue in gastric ulcer model rats to different extent ,and significantly reduced the gastric ulcer index(P<0.01),significantly increased the inhibition rate of gastric ulcer and the percentage of positive expression area of Schiff ’s iodate staining (P<0.01). CONCLUSIONS :Zuojin pectin capsule with protective effect on gastric ulcer and certain sustained- release effect is successfully prepared.

8.
International Eye Science ; (12): 1543-1547, 2021.
Article in Chinese | WPRIM | ID: wpr-886432

ABSTRACT

@#Diabetic macular edema(DME)is the foremost cause of vision impairment and even blindness in patients with diabetes mellitus. Nowadays, the approach in the treatment of DME involves laser photocoagulation, intravitreal injections of anti-VEGF agents or triamcinolone acetonide. However, they still have some limitations. In recent years, dexamethasone intravitreal implant, as a new treatment option, has brought therapeutic hope to DME patients who have poor response to other methods. Meanwhile, it has the advantages of good clinical efficacy, long duration, acceptable safety and good patient tolerability. In this paper, the research advances in dexamethasone intravitreal implant for DME are described.

9.
Article in Chinese | WPRIM | ID: wpr-882076

ABSTRACT

Objective To evaluate the pharmacokinetics of the new mesalazine enteric-coated sustained-release granules in SD rats and their distribution in the gastrointestinal tract, and to understand the preclinical pharmacokinetics and gastrointestinal distribution characteristics of the preparation. Methods Rats were administered orally to determine the drug concentrations in plasma samples and in the gastrointestinal tract. The commercially available mesalazine sustained-release granule was used as a reference to self-developed one to evaluate the process of absorption and elimination in vivo, relative bioavailability, and distribution in the gastrointestinal tract. Results The relative bioavailability of mesalazine enteric-coated sustained-release granule and non-enteric-coated one characterized by mesalazine was 89.62% ± 9.36%. After oral administration of mesalazine enteric-coated sustained-release granules, the drug has a high concentration distribution in the stomach within 2-8 hours, and gradually enters and remains in the jejunum, ileum and colon over time for 6-12 hours and then reaching a high concentration distribution in the colon. This help for the absorption of mesalazine, as well as the fixed-point release of the drug to produce a therapeutic effect. Conclusion The absorption and elimination process of mesalazine enteric sustained-release granule showed linear kinetic characteristics. There was no significant difference in pharmacokinetic parameters from the commercially available formulations, and it had a certain fluidity in the gastrointestinal tract. Good gastrointestinal distribution characteristics help the absorption of drugs in the body and the targeted release of the site of action

10.
Acta Pharmaceutica Sinica ; (12): 1712-1718, 2021.
Article in Chinese | WPRIM | ID: wpr-881565

ABSTRACT

Methotrexate (MTX) injection has a short half-life and significant toxic side effects. In order to overcome the demerits of MTX injection, MTX@COF was prepared for subcutaneous injection by loading MTX in crosslinked cyclodextrin metal-organic framework (COF) in this study. The cationic lipid material (2, 3-dioleoyl-propyl)-trimethylamine (DOTAP) was then coated on the MTX@COF surface by solvent evaporation. Different surface charge characteristics were observed in the coated MTX@COF@DOTAP with no significant change in particle morphology. The in vitro release behaviors of sustained-release particles were investigated in water and phosphate buffer (pH 7.4), and the in vivo release characteristics were evaluated for pharmacokinetics in rats. The in vitro release results showed that the cumulative release of MTX, MTX@COF and MTX@COF@DOTAP within 6 h was 92.70%, 36.31% and 18.19% in water, respectively; the cumulative release of MTX, MTX@COF and MTX@COF@DOTAP within 4 h was 90.82%, 79.37% and 58.30% in phosphate buffer, respectively; the results showed that MTX@COF can significantly delay the release of MTX, the modification to MTX@COF by DOTAP can further delay the release of MTX. Pharmacokinetic studies in rats showed that the mean retention time [MRT(0-t)] and the time to peak (Tmax) of the subcutaneous injection of MTX@COF@DOTAP group were significantly prolonged compared with the MTX@COF group and the MTX group. The area under the concentration-time curve [AUC(0-t)] of the MTX@COF@DOTAP subcutaneous injection group was 1.8 times high as that of the MTX group. In this study, MTX@COF@DOTAP particles had a certain sustained-release effect, and could prolong the bioavailability of MTX by subcutaneous injection, which provided a new idea for the development of new MTX dosage forms.

11.
Article in Chinese | WPRIM | ID: wpr-881260

ABSTRACT

@#Dental resin materials have been widely used in the treatment of dental defects. However, the polymerization shrinkage of the resin materials tends to cause microleakage and accumulation of bacterial plaque, which leads to secondary dental caries. Endowing dental resin with antibacterial properties is an important way to solve this problem. Adding antibacterial agents to dental resin is the main method to give it antibacterial properties. Antimicrobial agents are mainly divided into three types: release type, non-release type and mixed type. In terms of antibacterial effects, the selection and addition of antibacterial agents will affect the antibacterial and mechanical properties of dental resin materials; and the long-term antibacterial effect of antimicrobial agents in the oral cavity remains to be verified; as antimicrobial agents or other environmental factors can lead to drug resistance and even dormant persistent bacteria. In recent years, researchers have been committed to improving the antibacterial effect by modifying antibacterial agents. The sustained release of antimicrobial agents via carriers is also the main research direction. This paper reviews the research progress on the antibacterial properties of dental resin materials.

12.
Article in Chinese | WPRIM | ID: wpr-846291

ABSTRACT

Objective: Using polydopamine (PDA) as a carrier to construct a Salviae Miltiorrhizae Radix et Rhizoma (SMRR) nano-delivery system (PDA-SMRR), which can load a large number of SMRR water-soluble components and better exert antioxidation and antistress effect. Methods: PDA-SMRR nanoparticles (PDA-SMRR) were prepared, and the prescription process was investigated and optimized by single-factor experiments. The particle size, potential, and morphology of the nanoparticles were examined by a laser particle size analyzer and a transmission electron microscope. The drug loading and cumulative release rate were analyzed by dialysis. The cardiomyocytes of neonatal rats were extracted and cultured. The CCK-8 experiment was used to investigate the biological safety of PDA-SMRR and verify the protective effect of PDA-SMRR on oxidative stress-induced cardiomyocytes. Results: The optimal drug loading process was pH value 3.5, drug loading time was 12 h, drug loading temperature was room temperature, and PDA-SMRR was successfully prepared. The morphology and size of the nanoparticles were regular and uniform. The particle size and Zeta potential were (459.2 ± 4.5) nm, (3.01 ± 0.3) mV; In vitro release experiments indicated that SMRR was released slowly by the delivery system. CCK-8 experiments showed that PDA-SMRR had good biological safety and nanoparticles can reduce damaged cardiomyocytes caused by oxidative stress. Conclusion: PDA-SMRR can be used as a multi-component medicine depot for SMRR, with high drug loading and sustained release effect, which can effectively reduce the damage of oxidative damage on myocardial cells.

13.
Article in Chinese | WPRIM | ID: wpr-846204

ABSTRACT

Objective: To prepare resveratrol (Res) nanoparticles grafted with polyamide-amine dendrimer (PAMAM) modified by lactose acid (LA) and evaluate them in vitro. Methods: After partial carboxylation of G3.0 PAMAM terminal (PAMAM-COOH) which synthesized by divergence method. Res was bonded through esterification reaction and LA was grafted on the surface of the carrier through amidation reaction. Nuclear magnetic resonance (1H-NMR) and infrared spectroscopy (IR) were used for characterization. La-PAMAM-Res/Res nanoparticles were prepared by physical encapsulation using LA-PAMAM-Res and Res, and the encapsulation rate was detected by dialysis method. The drug load of the two kinds of nanoparticles was detected by high performance liquid chromatography (HPLC), the particle size was investigated by laser particle size analysis method, the drug release performance in vitro was determined by dialysis method, and the biosafety was evaluated by hemolytic experiment. The cytotoxicity and anticancer activity of PAMAM, PAMAM-COOH, Res, LA-PAMAM-Res and LA-PAMAM-Res/Res were investigated by MTT assay. Results: LA- PAMAM-Res and La-PAMAM-Res/Res nanoparticles were prepared. The encapsulation rate of LA-PAMAM-Res/Res was (75.1 ±2.2) %, the drug loading rates of LA-PAMAM-Res and LA-PAMAM-Res/Res were (7.2 ± 0.9) % and (18.4 ± 1.1) %, respectively. The particle size was (126.3 ± 3.4) nm and (251.0 ± 15.7) nm, respectively. After 72 h, the drug release in vitro was (23.83 ± 0.43)% and (35.28 ± 0.72)%, respectively. The hemolysis rate of both nanoparticles was less than 5%, and the carrier PAMAM-COOH showed less cytotoxicity than PAMAM, and both LA-PAMAM-Res and LA-PAMAM-Res/Res maintained anti-tumor proliferative activity. Conclusion: LA-PAMAM-Res and LA-PAMAM-Res/Res nanoparticles with sustained drug release, good biocompatibility, low cytotoxicity and anticancer activity were prepared, and LA-PAMAM-Res/Res increased the drug load of Res.

14.
Article in Chinese | WPRIM | ID: wpr-846170

ABSTRACT

Objective: To compare the effects of softeners including ethanol, propylene glycol and mixed alcohol (ethanol-propylene glycol 2:8) on the preparation of glabridin ethosomes (GLA-ES), and provide the selection basis of the softeners for studying the ethosomes of insoluble drugs. Methods: GLA-ES were prepared by injection-ultrasonic binding method with ethanol, propylene glycol and mixed alcohol (ethanol-propylene glycol, 2:8) as softeners. The morphology, size, Zeta potential, entrapment efficiency, stability, and in vitro drug release of GLA-ES were investigated. Tyrosinase activity on melanoma B16-OVA cells were detected to evaluate the inhibition of GLA-ES on the synthesis of melanin, the experiment of potassium ferricyanide reducing power was performed to evaluate the antioxidant effect of GLA-ES, and human epidermal HaCaT cells and rat skin were used for preliminary safety evaluation. Results: GLA-ES were yellow translucent liquid, containing vesicular phospholipid bilayer structure, the average particle size of GLA-Et-ES, GLA-PG-ES and GLA-MA-ES were (34.24 ± 0.29), (62.31 ± 1.66) and (41.20 ± 1.13) nm, respectively; The Zeta potential were (-41.0 ± 1.8), (-32.9 ± 0.2) and (-35.8 ± 1.6) mV, the entrapment efficiency were (91.47 ± 2.39)%, (87.33 ± 1.31)% and (91.39 ± 3.59)%, respectively, which had good stability of storage at 4 ℃ for 20 d, in vitro drug release behaviors of GLA-ES fitted Higuchi equation, implying their sustained release properties. Compared with the glabridin suspension, the inhibitory effects of GLA-Et-ES, GLA-PG-ES and GLA-MA-ES on tyrosinase activity in melanoma B16-OVA cells were increased by 38.07%, 19.58% and 40.42%, respectively. The results of potassium ferricyanide reducing power also showed that GLA-ES had a stronger in vitro antioxidant effect than the glabridin suspension; GLA-ES were nearly nontoxic on normal cells and had no irritation to rat skin. Conclusion: GLA-ES can be obtained by hree kinds of softeners, which can inhibit the synthesis of melanin and enhance the antioxidant effect with good safety. The present research will provide the basis for further developing skin-whitening cosmetics or pharmaceutical external preparation. For the insoluble drugs such as glabridin, when mixed alcohol (ethanol-propylene glycol) was selected as the softener to prepare ethosome, it exhibited better encapsulation efficiency and stability than that of ethanol or propylene glycol as the softener alone.

15.
Article in Chinese | WPRIM | ID: wpr-846102

ABSTRACT

Objective: To prepare the rhynchophylline nanosuspensions and lyophilized powder, and study its sustained-release tablets. Methods: Rhynchophylline nanosuspensions were prepared by microprecipitation combined with high pressure homogenization method, and the particle size and zeta potential were determined. Scanning electron microscopy (SEM) was employed to observe the appearances of nanosuspensions. Nanosuspensions were prepared into lyophilized powder using lactose as freeze-dried protectors. HPMC (hydroxypropyl methyl cellulose) was used as hydrophilic matrix to prepare the sustained-release tablets. Single factor investigation and orthogonal experiments were employed to optimize the formulation of rhynchophylline nanosuspensions sustained-release tablets, and the model fitting was also been studied. Results: The particle size and zeta potential of rhynchophylline nanosuspensions were (153.7 ± 4.9) nm and (-18.54 ± 1.32) mV, respectively. The appearances of rhynchophylline nanosuspensions were spherical or nearly spherical. After orthogonal optimization, the cumulative release rate of rhynchophylline nanosuspensions sustained-release tablets was 92.53% in 12 h. The optimized formulation of hydrogel matrix sustained-release tablets was better accorded with Higuchi model: ln(1-Mt/M∞)=0.286 0 t1/2-0.069 0 (r=0.992 4). The drug release from hydrogel matrix sustained-release tablets were controlled by diffusion and degradation. Conclusion: The obtained rhynchophylline nanosuspensions has small particle size. The prepared hydrogel matrix sustained-release tablets can control the release of rhynchophylline nanosuspensions in a slow characteristic.

16.
Article in Chinese | WPRIM | ID: wpr-845149

ABSTRACT

Objective: To evaluate the in vitro release degree, release mechanism and dose dumping of test tablet and reference tablet Lyrica® CR. The in vivo pharmacokinetics of the test tablet and the reference tablet were further investigated using the Beagle dog as a model. Methods: With Pfizer's pregabalin sustained-release tablets(Lyrica® CR)as the reference listed drug, the in vitro release behavior was evaluated using an automatic dissolution apparatus, and similarity factor(f2)method was used to analyze the in vitro release similarity between the reference tablet and the test tablet. The in vitro release equation was fitted to evaluate the drug release mechanism. Study was conducted on dose dumping of preparations based on the relevant guiding principles of the United States, Europe and China. Finally, the pharmacokinetic parameters of the test tablet and the reference tablet in Beagle dogs were compared. Results: The f2 of the test tablet and the reference tablet were more than 80 in all five release media, and there was no sudden release in the release medium containing ethanol. The pharmacokinetic parameters of the reference tablet and the test tablet were as follows: The Tmax was(6.00±2.19)and(4.00±2.19)h, the Cmax was(19.35±11.43)and(17.25±7.77)μg/ml, and the AUC0-t was(340.37± 220.66)and(281.65 ± 196.25)h•μg/ml for the reference tablet and the test tablet, respectively. Conclusion: In this study, the release curve of the test tablet was similar to that of the reference tablet in the five media. The drug was released slowly without sudden release, and the release mechanism in vitro was similar. There was no significant difference in pharmacokinetic parameters between the test tablet and the reference tablet in beagle dogs, and the relative bioavailability was more than 80%.

17.
Acta Pharmaceutica Sinica ; (12): 2719-2727, 2020.
Article in Chinese | WPRIM | ID: wpr-837509

ABSTRACT

The aim of this study is to prepare acetaminophen sustained-release tablets by hot melt extrusion 3D printing technology based on the concept of "Quality by Design" (QbD). Firstly, the failure mode and effect analysis (FMEA) was used to determine the critical process parameters (CPPs), then full-factor experimental design was used to analyze the critical quality attributes (CQAs) and to establish the design space. The results showed that the content of plasticizer, the path spacing and the shell numbers are independent variable for the experimental design. The design space was concluded to be plasticizer content: 9%, and the shell number: 3-5, the path spacing: 1.05-1.2 mm. In this study, 3D printing technology was used to prepare acetaminophen sustained-release tablets in accordance with the concept of QbD, which improved the durability of the process and ensured the uniform and controllable quality of the preparation and also provided experimental basis for personalised medicine.

18.
Article in Chinese | WPRIM | ID: wpr-828940

ABSTRACT

OBJECTIVE@#To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS).@*METHODS@#Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software.@*RESULTS@#LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05).@*CONCLUSIONS@#Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Delayed-Action Preparations , Male , Rats , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry , Trichosanthes
19.
Article in Chinese | WPRIM | ID: wpr-817643

ABSTRACT

@#【Objective】To prepare rapamycin(RAPA)sustained-release film and to evaluate its dissolution.【Methods】RAPA sustained- release film was created by using polymer polyactioglyconic acid (PLGA),copolymer of polyactic acid(PLA)and polyglycolic acid(PGA). Drug content of the sustained-release film was determined using specificity test,recovery,relative standard deviation(RSD)and stability test. Then,the dissolution of the sustained- release film was analyzed.【Results】The concentration of RAPA had a linear relationship with peak area,which ranged between 0.408 μg/mL and 40.8 μg/mL through the standard curve. The specificity test of the drug content determination indicated the excipient of the film and the solution with 0.3% sodium dodecyl sulfate(SDS)did not affect in determining the RAPA content. The recovery and RSD were excellent through drug content determination in blank films,which had three different levels of RAPA concentrations. The mean RAPA content of the sustained-release films was(112.6±10.1)μg(RSD 8.99%)through the drug content determination of the films,and the stability of RAPA with 0.3% SDS was good within 15 days. In addition,dissolution test of the sustained- release film indicated that the amount of drug release reached a high level and sustained up to 15 days.【Conclusion】 The RAPA sustained-release film with certain behavioral characteristic parameters had a stable drug content and favorable sustained-release property,and it may have certain application potential in anti-proliferation after glaucoma filtering surgery.

20.
Article in Chinese | WPRIM | ID: wpr-847720

ABSTRACT

BACKGROUND: The repair of peripheral nerve defects by nerve conduit bridging can provide a suitable microenvironment for nerve regeneration. On one hand, it can provide a unique channel for nerve regeneration, prevent the invasion of peripheral connective tissue and the formation of scars. On the other hand, it can maintain endogenous and exogenous neurotrophic factors, growth factors and other stimulants to promote axon growth. OBJECTIVE: To observe the therapeutic effect of chitosan/polyvinyl alcohol catheter injected with brain-derived neurotrophic factor sustained-release microspheres to bridge peripheral nerve defects. METHODS: Chitosan/polyvinyl alcohol nerve conduit was prepared by repeated freeze-thaw technique. The brain-derived neurotrophic factor microspheres were obtained by polymer-alloys combined with oil-oil emulsion/solvent evaporation method. A 15 mm sciatic nerve defect model was made in the right hindlimb of 60 adult male Sprague-Dawley rats. They were selected and randomly divided into four groups (n=15 per group): group A implanted with autogenous sciatic nerve; group B implanted with chitosan/polyvinyl alcohol nerve catheter, injected with normal saline; group C implanted with chitosan/ polyvinyl alcohol nerve catheter, injected with brain-derived neurotrophic factor solution; group D implanted with chitosan/polyvinyl alcohol nerve catheter, injected with brain-derived neurotrophic factor sustained-release microspheres. General observation, histological inspection, and electrophysiological determination were performed at 4 months after the surgery. This study was approved by the Research Ethics Committee of the Second Hospital of Hebei Medical University. RESULTS AND CONCLUSION: (1) Gross anatomy showed that muscle atrophy in group A and group D was lighter than that in the other two groups. The grafts in four groups were all adhered to the peripheral tissues, and the nerve in the autotransplantation segment was strongly adhered to the peripheral tissues. In group D, the regenerated nerve had connected the distal and proximal nerves, and the regenerated nerve filled the conduit. (2) Electrophysiological examination showed that the latency of group D was shorter than that of groups B and C (P 0.05). (3) Histological observation showed that there were regenerated nerve fibers in groups B, C, and D. The diameter, number and thickness of myelin sheath of group D were larger than those of group B and group C (P 0.05). (4) The results showed that the injection of brain-derived neurotrophic factor microspheres into chitosan/PVA catheter had a long-term promoting effect on peripheral nerve regeneration.

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