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1.
Article in Chinese | WPRIM | ID: wpr-906000

ABSTRACT

Objective:To investigate the percutaneous permeability of sinomenine hydrochloride (SNH) and optimize the parameters of electroporation to achieve the best permeation enhancing effect on SNH. Method:The percutaneous permeability of SNH and the enhancement effect of electroporation were studied by <italic>in vitro</italic> diffusion cell method, and the enhancement effect of electroporation was further evaluated by <italic>in vivo</italic> study in mice. Result:Under steady-state condition, the permeation rates of SNH in stripped skin and intact skin of hairless mice were (385.81±12.88), (0.88±0.20) μg·cm<sup>-2</sup>·h<sup>-1</sup>, respectively. The permeation rate in stripped skin was 438 times higher than that in intact skin. The results of percutaneous permeation kinetics analysis showed that the solubility and diffusion coefficient of SNH in stratum corneum were relatively low, which were (70.82±9.63)×10<sup>3</sup> g·m<sup>-3</sup> and (3.07±1.52)×10<sup>-14</sup> cm<sup>2</sup>·s<sup>-1</sup>, respectively. Under the optimized electroporation conditions (voltage of 72 V, time of 60 min), the 24 h cumulative permeation amount of SNH through skin of mice was (10 008.39±1 961.57) μg·cm<sup>-2</sup>, and the steady-state permeation rate was (456.01±51.26) μg·cm<sup>-2</sup>·h<sup>-1</sup>, which were 5.4 times and 5.1 times higher than those of blank group, respectively. <italic>In vivo</italic> studies in mice showed that the contents of SNH in skin and muscle of electroporation group were 2.0 times and 1.5 times higher than those of blank group. Conclusion:The low solubility and low diffusion coefficient of SNH in the stratum corneum are the main factors hindering the percutaneous permeation of SNH. Electroporation can significantly increase the percutaneous permeation of SNH and its retention in skin and muscle of mice.

2.
China Pharmacist ; (12): 449-452, 2017.
Article in Chinese | WPRIM | ID: wpr-510092

ABSTRACT

Objective:To evaluate the therapeutic effects of sinomenine on T-helper cell type 1-mediated experimental colitis in-duced by 2,4,6-trinitrobenzene sulfonic acid (TNBS) in mice. Methods:Balb/c mice were divided into five groups:ethanol control group, TNBS model group, and sinomenine treatment groups (50, 100 and 200 mg·kg-1 ) with 10 ones in each. Colitis was induced by colonic instillation of TNBS dissolved in 0. 1 ml of 50% ethanol. Seven days after the colonic instillation of TNBS, sinomenine was given by gastric gavage once daily for 21 days. The mice were sacrificed on the 28th day, the injury degree of colonic mucosa was ob-served, the colon myeloperoxidase ( MPO) activity was determined, and the levels of inflammatory cytokines ( TNF-α, IL-17 and IL-23) were determined by ELISA. Results:Compared with those in TNBS model group, the body mass, gross injury score and histologi-cal findings in sinomenine groups at medium dose and high dose were significantly improved (P<0. 05), the activity of MPO signifi-cantly decreased (P<0. 05), and the protein levels of TNF-α, IL-17 and IL-23 in colonic mucosa were lower than those in TNBS group (P<0. 05). Conclusion:Sinomenine has notable therapeutic effect on TNBS-induced chronic colitis in mice, and the mecha-nism is related to the inhibition of Th1 cytokines by sinomenine.

3.
Article in Chinese | WPRIM | ID: wpr-852345

ABSTRACT

Objective To optimize the formulation of sinomenine hydrochloride transfersomes (SHTs) and to verify their therapeutic effects on rheumatoid arthritis in rats. Methods SHTs were prepared by ethanol injection method. Their formulation was optimized by an orthogonal test, which was based on the elasticity of transfersomes. Elasticity of transfersomes was measured by constant pressure extrusion method and entrapment efficiency was measured by HPLC combined with centrifugation ultrafiltration. The model of rheumatoid arthritis was established by subcutaneous injection of type II collagen into Wistar rats' tail. The therapeutic effects of the preparation on rheumatoid arthritis in rats were evaluated based on ankle joint score, swelling degree, level of TNF-α and IL-1β in serum as well as histological changes including inflammatory cell infiltration, pannus formation, cartilage destruction, and bone erosion. Results The optimized formulation was as follows: egg phospholipid 300 mg, cholesterol 30 mg, sinomenine hydrochloride 100 mg, sodium deoxycholate 60 mg, vitamin E 5 mg, phosphate buffered saline (pH 8.0) 23 mL, and absolute ethyl alcohol 2 mL. The optimized transfersomes had an average size of (83.31 ± 0.08) nm, Zeta potential of (-32.57 ± 3.27) mV, deformability index of 38.69 ± 1.66, drug content of (2.96 ± 0.27) mg/mL, and entrapment efficiency of (39.82 ± 0.97) %. The results of pharmacodynamical test revealed that the preparation could significantly reduce joint swelling caused by rheumatoid arthritis (P < 0.01) and lower TNF-α and IL-1β level in serum (P < 0.01), effectively alleviate inflammatory response and improve histological changes of ankle joint. Conclusion The preparation process for the transfersomes is feasible and their quality can be controlled. The optimized SHTs are effective for treatment of rheumatoid arthritis in rats.

4.
Article in Chinese | WPRIM | ID: wpr-853212

ABSTRACT

Objective: To clarify the percutaneous absorption characteristics of sinomenine hydrochloride (SIN-HCl) PEGylated transfersomes (SHPT) edge activated by volatile oils and to compare with others carriers. Methods: Various formulations of transfersomes [The representative formulations of SHPT contained different quantity of volatile oils including SHPT-A, SHPT-B, and SHPT-C; non-PEGylated transfersomes (SHT-A and SHT-B) corresponded to SHPT-A and SHPT-B; SHDT was edge activated by sodium deoxycholate], PEGylated liposomes (SHPL), and liposomes (SHLS) were prepared by ethanol injection method. Characterization of vesicles was based on results from particle size, morphology, elasticity, and entrapment efficiency (EE) studies. Elasticity was measured by constant pressure extrusion method and EE was measured by HPLC combined with centrifugation ultrafiltration. The skin permeation test was carried out with a Franz diffusion cell fitted with excised rat skin. The effects of vesicle types (SHPT, SHDT, SHLS, and SIN-HCl aqueous solution), DSPE-PEG 2000, and volatile oil in the SHPT on percutaneous permeation of SIN-HCl were investigated. Results: The SIN-HCl transfersomes and liposomes were mainly unilamellar vesicles with roundish shape and average size of 93-118 nm, without gathering property. The entrapment efficiency was of 11%-40%. The elasticity order of vesicles was SHPT-B > SHDT ≈ SHPT-A > SHT-B > SHT-A ≈ SHPL > SHLS > SHPT-C. The steady-state drug percutaneous permeation rate [J (μg∙cm-2∙h-1)] order of different vesicles was SHT-B (19.10 ± 5.74) > SHPT-B (17.06 ± 0.34) > SHDT (15.16 ± 0.55) > SHT-A (10.96 ± 0.99) > SHPT-A (9.42 ± 1.09) > SHLS (3.90 ± 0.67) > SHPT-C (3.51 ± 0.37) > SIN-HCl aqueous solution (2.26 ± 0.94). The cumulative permeated percentages [Qe (36 h)] of SHT-B and SHPT-B were (89.79 ± 6.67)%, and (84.01 ± 6.77)%, respectively. The Qe (36 h) of SHDT, SHLS, SHPT-C and SIN-HCl aqueous solution were (73.98 ± 10.55)%, (20.29 ± 3.21)%, (15.45 ± 3.04)%, and (10.33 ± 2.91)%, respectively. The lag time of SHPT-A, SHPT-B, SHT-A, SHT-B, and SHDT (0.3-0.6 h) were significantly reduced, compared to SHLS and SIN-HCl aqueous solution (3.5-3.8 h). Conclusion: SHPT edge activated by appropriate volatile oils has good elasticity and percutaneous absorption characteristics, which is better than that of liposomes and transfersomes edge activated by sodium deoxycholate to different degrees.

5.
Article in Chinese | WPRIM | ID: wpr-855426

ABSTRACT

Objective: To prepare sinomenine hydrochloride (SIN-HCl) liposomes with high entrapment efficiency (EE) and to illustrate the effects of drug quantity and particle size on EE. Methods: Centrifugation sedimentation-centrifugation ultrafiltration was employed to determine EE of liposomes. Thin film hydration (TFH), reverse phase evaporation (REV), and ether injection (EI) were screened based on EE and formability of liposomes. The effects of water type, pH value, ion concentration of hydration liquid, pH gradient active drug loading, lecithin-cholesterol ratio, and drug-lipid ratio on EE of liposomes were investigated. The relationship between EE and the factors affecting the drug quantity and particle size was probed with a comprehensive design experiment. The stability of typical liposomes was evaluated at 4 °C. Results: The optimal preparation technology was TFH for SIN-HCl liposomes and citrate buffer solution (CBS) was the best hydration liquid. The liposome EE increased with the increase of pH values of CBS. When the pH value of CBS was fixed, the EE increased as a result of decrease in the ion concentration of CBS. pH gradient active drug loading led to increase of EE. The preferable hydration liquid for liposomes was CBS with pH value of 2.5. The optimal ratio of soybean lecithin to cholesterol was 6:1. Increasing ratios of SIN-HCl to soybean lecithin from 1:6 to 6:6 led to a slight decrease in EE of liposomes without probe signification. A quantitative relationship was established between the EE and drug quantity and liposome size. The EE of SIN-HCl liposomes prepared by certain particle size and drug quantity could reach over 80%. The typical liposomes showed a good stability. Conclusion: The technology of pH gradient active drug loading is able to prepare SIN-HCl liposomes with high EE.

6.
Article in Chinese | WPRIM | ID: wpr-855223

ABSTRACT

Objective: To prepare the solid lipid nanoparticle (SLN) thermosensitive gel of sinomenine hydrochloride (SH) for intra-articular injection and to investigate its in vitro drug release behavior. Methods: Poloxamer 407 (P-407) and Poloxamer 188 (P-188) were used as gel matrix to prepare the gel, and the gelatinization temperature was applied as a target to optimize the prescription. The SH-SLN was prepared based on the microemulsion technique, and the gel system containing SH-SLN was obtained by cold-dissolving methods. The content of SH was determined by HPLC, in vitro release characteristics of SH-SLN thermosensitive gel were investigated by dialysis method. Results: The optimal gel prescription was finally confirmed as 18% P-407, 5% P-188, and 0.6% HPMC. The gelatination temperature for SH-SLN thermosensitive gel was (34.5 ± 0.2)°C, and the in vitro accumulated release rates of SH in the SLN thermosensitive gel system were (57.79 ± 0.36)% after 24 h and (75.16 ± 0.12)% after 48 h. Conclusion: The SH-SLN thermosensitive gel has the temperature sensitivity and obvious sustained-release effect. The combination of nanoparticle thermosensitive gel will be used as a new drug delivery for intra-articular injection.

7.
Article in Chinese | WPRIM | ID: wpr-840021

ABSTRACT

Objective: To study the characteristics and mechanism of transdermal delivery of sinomenine hydrochloride (SH) through mouse skin treated by solid silicon microneedle arrays. Methods: The amount of SH was determined by HPLC system. Hairless rat skin was pretreated with microneedle arrays. The side-by-side diffusion cell method was used to investigate the effects of needlepoint shape, different insertion forces, retention time, and number of microneedles on transdermal SH delivery. Skin samples treated by microneedles were made into paraffin sections for histological examination and were viewed by brightfield microscopy. Results: The skin pretreated with microneedle arrays had a remarkable enhancement of SH transport compared with passive diffusion group (P<0.01); the flat tipped microneedles were more effective than the sharp tipped microneedles in enhancing the skin permeability. The accumulation of SH increased with the enhancement of insertion force; however, when the insertion force exceeded 5.0 N, the accumulation of SH no longer increased. The skin permeability was enhanced with the increase of retention time; when the retention time exceeded 1.0 min, it no longer increased SH accumulation. Although skin permeability increased with the microneedle number, there was no linear correlation was found. Histological examination showed that microneedle piercing created micro-conduits in skin. Conclusion: Microneedles can create conduits in rat skin and greatly increase the skin permeability of SH; microneedle arrays provide an efficient and promising technology for transdermal drug delivery of SH.

8.
Article in Chinese | WPRIM | ID: wpr-855622

ABSTRACT

Objective: To study the preparation of sinomenine hydrochloride (SH) loaded nano flexible liposomes and investigate the mechanism of the flexible liposomes for enhanced in vitro transdermal drug delivery. Methods: The SH loaded nano flexible liposomes were prepared by film dispersion method, and the effects of concentration of phosphatidylcholine (PSC), cholesterol (CH), and propyleneglycol (PG) on the entrapment efficiency of SH were also investigated. The SH content was determined by HPLC. The physical property was evaluated by the atomic force microscope (AFM), transmission electron microscope (TEM) and photon correlation spectrometer (PCS). The side-by-side diffusion cells were used to evaluate transdermal delivery of SH by nano flexible liposomes. At the end of the transdermal experiment, the treated skin was carefully observed by scanning electron microscopy (SEM). Results: The SH loaded nano flexible liposomes were prepared by film dispersion method with the PSC (3%), CH (0.02%), and PG (25%); The SH entrapment efficiency was (66±2.3)%. The prepared nano flexible liposomes had a closed spherical or elliptical shape showed by AFM images, the TEM images appeared as multi-lamellar vesicles. The calculated mean size was (170±26) nm, the zeta potential values of -(43±3.4) mV. The SH loaded nano flexible liposomes caused the structure of stratum corneum (SC) layer disturbed and disordered the intercorneocyte domain wider, this increased the skin permeability of drug. Conclusion: The SH loaded nano flexible liposomes are obviously resulted in a remarkable enhancement of the SH transdermal drug delivery, which could act as a new nanodimensional vehicle for transdermal delivery of SH.

9.
Article in Chinese | WPRIM | ID: wpr-855555

ABSTRACT

Objective: To develop a method for determining the entrapment efficiency of sinomenine hydrochloride (SM-HCl) liposomes and to illuminate the drug retention property in the liposomes. Methods: Thin film hydration method was employed to prepare SM-HCl liposomes. HPLC was used to determine drug content of the liposomes. A Kromasil ODS C18 column (250 mm x 4.6 mm, 5 μ) was used with an isocratic elution composed of methanol, water, and ethylenediamine in the ratio of 55 : 45 : 0.225 at a flow rate of 1.0 mL/min. The column was maintained at 30 °C. The UV detector was set at 265 nm. Centrifugation sedimentation combined with centrifugation ultrafiltration was used to determine drug entrapment efficiency of the liposomes. The entrapment efficiencies of an SM-HCl liposome sample (hydrated with citric buffer solution at pH 7.0) and its diluted sample were compared. Results: The pharmaceutical excipients and solvents for analysis had no interference with the determination of sinomenine. Sinomenine had a good linear relation in the range of 9.82-78.6 μg/mL (r = 0.999 7), the intra-day and inter-day precisions were with RSD≤2.1% and the averaged recovery was within 99.29%-100.8%. SM-HCl solution (50 μL) was able to saturate the drug absorption of ultrafiltration films. The entrapment efficiencies of the SM-HCl liposome sample (hydrated with citric buffer solution at pH 7.0) and its double-volume diluted sample were 33.16% and 14.75%, respectively. Conclusion: HPLC and centrifugation sedimentation combined with centrifugation ultrafiltration are able to determine the entrapment efficiency of SM-HCl liposomes efficiently and accurately. Initial filtrate (50 μL) should be discarded in the process of ultrafiltration in order that the drug concentration in filtrate may be equal to that of external aqueous phase of liposomes. The retention of sinominine in the liposomes is poor, although it has considerable affinity to the lipid bilayers.

10.
Article in Chinese | WPRIM | ID: wpr-433248

ABSTRACT

AIM : To prepare a phase-specific drug delivery system withfloating and pulsatile release of sinome-nine hydrochloride and evaluate in vitro drug release behavior. METHODS: The floating and pulsatile-release of coat-core tablets were prepared by press-coated technics. The effects of factors influencing release characteristic of the drug were investigated by dissolution test, and to elucidate the mechanism of drug releaseof the tablets with erosion and water-uptake test. RESULTS: The tablets had typical floating and pulsatile release properties with a lag time rapid release. The lag-time was shortened with the increase of expansion ratio of tablet core and rotation speed of stirrer. The lag-time was prolonged with the increase of pH and ionic strength of dissolution media.CONCLUSION: The tablet could float and rapidly release drug at the predetermined time.

11.
Article in Chinese | WPRIM | ID: wpr-379770

ABSTRACT

Objective To study the effect of phonophoresis on transdermal delivery of sinomenine hydrochloride ( SH ) gel in vitro. Methods Ultrasound at one of two frequencies ( 800 kHz or 1 MHz) was applied with a sonicator with a transducer in this study. The skin of male Sprague-Dawley rats was used as the model and SH gel was used as the ultrasound couplant. The permeation rate of SH was detected using a modified Franz diffusion cell maintained at 32±0.5℃ and filled with 20% polyethylene glycol 400 physiological saline solution. The transdermal phonophoresis experiments were carried out in five groups: Group Ta, f=800 kHz, / = 0.75 W/cm2, t = 10 min:Group Tb,f=1 MHz,I=0.7 W/cm2, t=10 min; Group Tc,f=1 MHz,I=0.35 W/cm2, t=10 min; Group Td,f=800 kHz, I = 1.5 W/cm2, t = 10 min and Group Tc,f=800 kHz, I=1.5 W/cm2,t=5 min. There was also a control group (C) in which the SH was allowed to diffused passively. Samples were withdrawn at the indicated intervals and the concentration of SH was determined by high-performance liquid chromatography. The transdermal parameters such as average accumulated delivery quantity per unit area Q8h, average transdermal steady delivery rate J, and Tlag were calculated. Results The Q8h and Js of the control group were 20.65±10.23 μ/cm2 and 3.02±0.11μ/cm2/h respectively. The phonophoresis parameters in groups Ta and Tb were, on average, significantly higher than in the control group. The parameters in group Tb were significantly larger, on average, than in Te. In group Td the parameters were significantly larger than in groups Ta and Te. Conclusions The results show that phonophoresis can enhance the transdermal delivery of SH. Phonophoresis variables such as frequency and time influence its effects on drug permeation. Almost no change was observed in the structure of the skin after phonophoresis, though under a scanning electron microscope the surface of the corneum appeared rough and porous. Phonophoresis is there-fore an effective and safe method for SH transdermal delivery, and the effect is positively relation with the applied intensity and exposure time.

12.
Article in Chinese | WPRIM | ID: wpr-480372

ABSTRACT

Aim: To establish a linear additive model for the predication of in vitro sinomenine hydrochloride release from the combination of immediate release, enteric-coated and sustained-release pellets based on the release profiles of each pellet type. Methods: Immediate release pellets were manufactured by extrusion/spher-onization technology. The operation of bottom-spraying in the fluid-bed equipment was conducted to enteric-coating using Eudragit~(R) L-30D-55 and sustained-release coating using Surelease~(R) . In vitro sinomenine hydrochloride release profiles of both uncoated and coated pellets were fitted to the chosen mathematical equations offered by the curve fitting toolbox of Matlab~(R) before a linear additive model was created based upon the best-to-fitting equations. The proportion of each pellet type in the combined format to generate the desired 24 h sinomenine hydrochloride release profile was solved by Matlab~(R). The predicted and assayed sinomenine hydrochloride release from the polled pellets was compared. Results: It was shown that the actual sinomenine hydrochloride release profiles of each pellet type were approximate to those of predicted ones. A linear additive model of the appropriate mathematical equations of each pellet was proven to be capable of controlling in vitro release of sinomenine hydrochloride multiple-unit pellets. Conclusion: A multiple-unit combined system of the selected pellets, as a novel sustained-release system, was successfully prepared. In vitro release performance of the calculated combination of each pellet type could be guaranteed by this approach in designing sustained-release drug delivery system.

13.
China Pharmacy ; (12)2007.
Article in Chinese | WPRIM | ID: wpr-531183

ABSTRACT

OBJECTIVE:To investigate the degradation kinetic characteristics of Sinomenine hydrochloride aqueous solution.METHODS:The colorimetric method was used to determine the degradation kinetic parameters of Sinomenine hydrochloride aqueous solution under various pH solutions,various ionic strength and various dielectric constant conditions.RESULTS:With comparative regression analysis of linear fitting,the degradation kinetic order of Sinomenine hydrochloride aqueous solution was determined as n=1.The higher the pH in Sinomenine hydrochloride aqueous solution was,the higher the degradation kinetic rate constant was.The Sinomenine hydrochloride aqueous solution degraded slowly at the field of lower pH(pH5).The higher the ionic strength of Sinomenine hydrochloride aqueous solution was,the higher the degradation kinetic rate constant was.As the dielectric constant of solution increased,so did the degradation kinetic rate constant.CONCLUSION:It was found that the degradation of Sinomenine hydrochloride followed apparent first-order kinetics.The degradation kinetic rate was affected by pH remarkably and positively correlated with ionic strength and dielectric constant.

14.
Article in Chinese | WPRIM | ID: wpr-580293

ABSTRACT

Objective To establish a method for the determination of content in Sinomenine Hydrochloride external applied powder. Methods Diamonsil ODS C_(18) (250 mm ? 4.6 mm, 5 ?m) column was used in HPLC with mobile phase of phosphate buffer (0.01 mol/L K_2HPO_4 solution, and 1%0 triethylamine, pH was adjusted to 3.0)-MeOH (80 : 20). The flow rate was 1.0 mL/min and the detection wavelength was 265 rim. Results The linear range of Sinomenine Hydrochloride was 0.446~4.46 ?g and the regression equation was Y=9.01 ? 10~6X+102803 (r=0.9999). The average recovery was 99.2%, RSD=0.68% (n =9). Conclusion This method is rapid and accurate with good reproducibility. It can be applied to control the quality of Sinomenine Hydrochloride external applied powder.

15.
Article in Chinese | WPRIM | ID: wpr-581155

ABSTRACT

Objective To optimize the formulation of sinomenine hydrochloride pulsatile drug delivery tablets by central composite design-response surface method.Methods The tablets containing sinomenine hydrochloride were prepared by dry-compression coating technique.The influence factors included the amount of sodium carboxymethyl starch in core tablets, the ratio of HPMC/carrrageenan,and the amount of matrix materials in coating film.The evaluation parameter was lag time.Experiments were done on the central composite design,and the data were simulated using multi-linear equation and second-order polynomial equation.The possibly optimal formulation was predicted by response surface method.The lag time of the tablets prepared under the optimum condition was compared with the predicted.Results The lag time was simulated using second-order polynomial equation and the regression coefficient was 0.993 7.The lag time in vitro of the tablets prepared under the optimum conditions was about 6 h,then drug released in pulsatilerelease character.Bias between the observed and predicted values of the lag time was within ?4.43%.Conclusion The sinomenine hydrochloride pulsatile tablets could release drug quickly in vitro at the predetermined time.Central composite design-response surface method can be used to optimize the formulation and the model developed in this study proves to be highly predictable.

16.
Article in Chinese | WPRIM | ID: wpr-580272

ABSTRACT

Objective To study the formulation and preparation factors influencing in vitro release mechanism of drug from?-carrageenan/konjac glucomannan hydrophilic matrix tablets.Methods The matrix tablets containing sinomenine hydrochloride as a model drug were obtained by direct compression method or wet granulation technique.The effects of the ratios of?-carrageenan/konjac glucomannan,the amount of matrix materials,the kinds of diluent agent,tablet size,preparation method,and compressing pressure on release mechanism of the matrix tablets were studied by evaluating the n value in the Peppas equation. Results The release mechanism of the matrix tablets was non-Fickian release that coupled diffusion and erosion modle.With a decrease in the ratio of?-carrageenan/konjac glucomannan,a decrease in the amount of matrix materials,a decrease in the water-solubility of diluent agents,an increase in tablet size,and a decrease in compressing pressure,the ratio of drug diffusion was increased.Preparation method had little influence on drug release mechanism.Conclusion Drug could be slowly released from the matrix tablets containing?-carrageenan/konjac glucomannan as matrix material,the main factors influencing drug release mechanism are the ratio of?-carrageenan/konjac glucomannan,the amount of matrix materials, the kinds of diluent agent,tablet size,and compressing pressure.

17.
Article in Chinese | WPRIM | ID: wpr-578483

ABSTRACT

Objective To prepare the sinomenine hydrochloride multivesicular liposomes with high entrapment efficiency and sustained release character.Methods Multiple emulsion method was used to prepare the sinomenine hydrochloride multivesicular liposomes.Uniform design was applied to optimize the formulation and pharmaceutical process.The shape,the particle size,and the release charcter of the liposome were evaluated.Results The sinomenine hydrochloride multivesicular liposomes prepared were spherical and the size of majority particles was in the range of 20—30 ?m and well distributed.The encapsulation efficiency was more than 80% and its in-vitro release profile accorded well with the Higuchi model with t1/2 up to 52.7 h.Conclusion The formulation and pharmaceutical process of the sinomenine hydrochloride multivesicular liposomes are stable and feasible with the high encapsulation efficiency and good sustained-release character.

18.
Article in Chinese | WPRIM | ID: wpr-576435

ABSTRACT

Objective To prepare sinomenine hydrochloride transfersomes and evaluate their qualities. MethodsThree different preparation methods including film dispersion, reverse phase evaporation, and ethanol injection methods were compared according to the encapsulation efficiency of transfersomes. Uniform design was applied to optimize the formulation and pharmaceutical process of reverse phase evaporation. The particle size, the appearance, the Z-potential, and the stability were also evaluated. ResultsThe transfersomes prepared by reverse-phase evaporation method possessed the highest encapsulation efficiency. The ideal combinations of preparation and formulation were: soya lecithin/sodium cholate was 200/30 mg/mg, chloroform/PBS was 5 mL/mL, pH of PBS was 6.5, added sinomenine hydrochloride was 10 mg. The transfersomes obtained were milky white translucent suspension, with a mean encapsulation efficiency of 62.2%. The shape of their particles was spherical or similar to spherical under microscope, which was smooth and disconglutinated with an average diameter of 96.4 nm, and a Z-potential of-35.93 mV. Aggregation or deposition was not observed after exposure under the temperature of 4 ℃ for 30 d. ConclusionThe preparation process of sinomenine hydrochloride transfersomes is feasible, the quality of obtained transfersomes is stable.It is expected to provide a new preparation for clinical use of sinomenine hydrochloride.

19.
Article in Chinese | WPRIM | ID: wpr-581278

ABSTRACT

AIM: To study the formulation and preparation factors on vitro drug release from sinomenine hydrochloride delayed-onset sustained-release tablet. METHODS: With hydrophilic matrix materials as excipient,the tablets containing hydrochloride sinomenine as a model drug were prepared by direct compression. The effect of the type and amount of tablet core matrix materials(HPMC K15M,HPMC K4M,xanthan gum and carrageenan),the type and amount of coating matrix materials,the preparation of coating materials and the pressure on in vitro drug release of the tablets were studied. RESULTS: The lag time of the tablet was 4 ~ 5 h and drug release slowly in 24 h. The type and the amount of the core matix materials and the coating matrix materials play an important role on lag time and drug release(P

20.
Article in Chinese | WPRIM | ID: wpr-580947

ABSTRACT

AIM: The drug release characteristics of ?-carrageenan/konjac glucomannan matrix tablet were elvated by in vitro dissolution experiment. METHODS: Sinomenine hydrochloride was used as model drug,the matrix tablet containing ?-carrageenan and konjac glucomannan as matrix material were prepared by wet granulation technique. Drug release and tablet erosion in different pH values,ionic strength of media and rotation speeds were studied by in vitro dissolution experiment. The data of drug release and matrix tablet erosion were confirmed in Peppas and zero order equation,respectively. RESULTS: Among the rate of drug release in different media,0. 1 mol/L HCl was the fastest,distilled water was the second,pH6. 8 PBS was the slowest. The rate of drug release decreased with increasing the ionic strength of media(P 0. 1). The rate of drug release increased with increasing the rotation speeds(P

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