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Bioadhesive preparation can be attached to specific sites to control drug release rate, increase drug concentration and increase efficacy, which is based on natural or synthetic polymer material. In this paper, based on the physical properties of wet mass, a method for screening adhesion formulation was proposed, which was different from conventional way of screening optimal formulation, and astragalosides loaded bioadhesive pellets were prepared by extrusion-spheronization method (extrusion speed 30 r·min-1, spheronization speed 808 r·min-1, spheronization time 7.5 min) based on this formulation screening method, small living animal imaging technology and mucin from porcine stomach model were used to evaluate the in vivo and invitro adhesiveness behaviour of the pellets. According to the relationship between the physical properties of wet mass and the formability and adhesiveness of bioadhesive pellets, five key physical properties hardness (Ha), adhesiveness (Ad), springiness (Sp), cohesiveness (Co), chewiness (Ch) were selected as the index of screening optimal formulation, therefore a comprehensive evaluation model was established, which based on principal component analysis, to did digital ranking for these proposed adhesion formulation, the optimal formulation was determined: microcrystalline cellulose: (chitosan∶Carbomer 940 = 2∶1), the adhesive material dosage accounted for 20% of the excipient dosage, and the ratio of drugs to excipients was 1 : 4. All animal experiments have been approved by Ethics Committee of Shanghai University of Traditional Chinese Medicine. The in vivo and in vitro adhesive evaluation results showed the pellets had a clear advantage in intestinal adhesion over normal pellets, its also proved the scientificity and reliability of the method of screening bioadhesive formulation.
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Objective: Pueraria total flavonids (PTF) can treat cardiovascular and cerebrovascular diseases, but it has poor membrane permeability and oral bioavailability. Some excipients, such as carbomer, chitosan, and hydroxypropyl methylcellulose, can improve the oral bioavailability. Traditional in vitro evaluation techniques, including the rat intestinal perfusion and cell line models, cannot evaluate PTF absorption and holistic transporters. Methods: This study evaluated excipients’ adhesiveness and effect on PTF transport across Caco-2 cell monolayer. cDNA microarrays identified gene expression changes in Caco-2 cells exposed to PTF and PTF with excipients, and revealed the mechanism underlying the effect of excipients on PTF absorption. Results: In vitro adhesion and transport experiments across Caco-2 showed that excipients had higher adhesiveness to gastric mucosa and transport efficiency across Caco-2 cells than PTF alone. The interaction of PTF with excipients significantly changed the expression of some genes, which might influence the absorption rate of PTF. Conclusion: Different bioadhesive polymers can improve intestinal absorption of PTF, which was related to some genes affiliated to the ATP-binding cassette (ABC) and solute carrier transporter (SLC) to some extent.
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Objective: Because of the adhesion of Bletilla striata polysaccharide (BSP), it was mixed with sodium alginate (SA) as a composite carrier to prepare mucoadhesive PNS-BSP composite microspheres. Panax notoginseng saponins (PNS) dispersion with sustained release property was used as an encapsulating drug. Methods: The composite microsphere was prepared by ion cross-linking method. The formulation process was investigated and optimized by single factor test and orthogonal design. The microspheres were evaluated by scanning electron microscope (SEM), particle size distribution, DSC, swelling properties, in vitro mucoadhesive properties, and in vitro release characteristics. Results: PNS-BSP composite microspheres had good roundness, rough surface and wrinkles. The microspheres showed a narrow size distribution. PNS was uniformly dispersed in microspheres in an amorphous state. The microspheres prepared by the best prescription process were stable in process and reproducible. Compared with the microspheres prepared by directly adding PNS, the drug loading, encapsulation efficiency and yield of PNS dispersion microspheres were increased significantly, which were 10.34%, 51.25%, and 82.21%, respectively. The drug loading, encapsulation efficiency, and yield were 4.04%, 12.16%, and 61.35% of PNS microspheres. The addition of BSP increased the swelling properties of the SA microspheres, and significantly increased the retention rate in the stomach of rats. The release of ginsenoside Rg1 in PNS-BSP microspheres was released slower compared to PNS. Conclusion: The bioadhesion of microspheres was increased by the addition of BSP. The drug loading, encapsulation efficiency, and yield of the microspheres were increased by the preparation of PNS as a dispersion, and the microspheres also had a certain sustained-release effect.
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Objective To study the mechanism of bioadhesive materials(Chitosan,Carbomer and hydroxypropyl methyl cellulose(HPMC))on promoting panax notoginseng saponins(PNS)′s oral absorption by microarray.Methods The study was divided into four groups.PNS,PNS-chitosan,PNS-carbomer and PNS-HPMC,microarray were used to investigate the change of genes expression level affiliated to the solute carrier transporter(SLC)and the ATP-binding cassette(ABC)after transpor-ting across Caco-2 cell monolayer,to explore the mechanism of bioadhesive materials′effect on PNS′s absorption.Results Comparing with PNS group ，chitosan and carbomer could significantly increase gene expression level affiliated to SLC transporter ，chitosan could decrease multi-resistant genes and P-gp efflux genes expression level affiliated to ABC transporter . HPMC had no obvious effect on SLC and ABC transporter .Conclusion Chitosan and carbomer increase PNS′s oral due to genes change affiliated to SLC and ABC transporter that could promote absorption and inhibit efflux .The promotion mechanism of HPMC absorption was that it could prolong retention time on absorption site .
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Objective To prepare salvianolic acid bioadhesive floating pellets; To prolong its residence time in vivo; To improve the oral bioavailability. Methods Salviae miltiorrhizae total phenolic acid adhering floating pellets were prepared by extrusion-spheronization. Chitosan, HPMC and carbomer were used as adherent material, stearyl alcohol was used as floating material and MCC as forming agent. The in vitro release of two adherent floating pellets were prepared and their bioavailability in rats were investigated. Results The results of in vitro release test showed that the salvianolic acid B in the blank pellets was completely released at 4 h, and the two adherent floating pellets prepared in vitro were released for 12 h. The results of pharmacokinetic studies in rats showed that after intragastric administration of salvianolic acid, salvianolic acid chitosan pellets and salvianolic acid HPMC pellets, Tmaxwere (12.00±2.74)min, (17.00±7.58)min and (27.00±12.55)min, respectively. The relative bioavailability of salvianolic acid chitosan pellets and salvianolic acid HPMC pellets were 177.08% and 172.03%, respectively. Conclusion Salvia total phenolic acid adherent floating pellets release slowly in vitro, and floating pellets can prolong the retention time in vivo and increase the oral bioavailability of salvianolic acid in rats.
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Objetivo: Desarrollar una nueva técnica para la transferencia de cianometacrilato de muy baja densidad sobre las superficies internas y externas del corazón. Material y métodos: Se combinó el cianometacrilato curado por luz ultravioleta de muy baja densidad con colorante comercial para demostrar su capacidad de transferencia sobre las superficies externas e internas de un modelo de corazón in vitro. Se mezclaron 0,5 ml de cianometacrilato con 0,2 ml tinta, y el material se inyectó sobre la superficie del corazón en aire seco, lo que permite su fijación durante 2-3 seg. A continuación, toda la preparación se sumergió en solución salina y se agitó vigorosamente para eliminar el compuesto no ligado. Se realizó un experimento similar sin cianometacrilato y con cianometacrilato de alta viscosidad (3000 cps). Se comprobó visualmente después del lavado que una cantidad significativa del compuesto se liga a las superficies del corazón en comparación con la tinta sola. Luego, se investigó la transferencia efectiva del compuesto a las superficies internas y externas del corazón después de haber sumergido el tejido en solución salina. Entre diversas técnicas, la de pincelado fue la más efectiva para la transferencia orientada del compuesto. Mediante esta técnica fue muy fácil transferir el compuesto sobre las superficies endocárdica y epicárdica. También otras áreas específicas, como la orejuela auricular izquierda, las superficies internas del ventrículo izquierdo en el origen del músculo papilar y el ápex ventricular izquierdo, fueron investigadas exitosamente. La fuente de luz ultravioleta fue un dispositivo en forma de lapicera basado en un diodo emisor de luz. Luego del tratamiento con luz ultravioleta, se observó cierta precipitación del compuesto en algunas zonas. El experimento se repitió con tres muestras para determinar el resultado. Conclusiones: La transferencia de cianometacrilato de muy baja viscosidad curado por luz ultravioleta es potencialmente útil para el estudio de las superficies internas y externas del corazón. Esta técnica podría servir para la transferencia de factor de crecimiento.
Background: Cyan methacrylate is a compound with remarkable adhesion properties used in different specific areas, including medicine, where it can be applied in some entities and is also subject of research in the field of cardiology Objective: The aim of this study was to develop a novel technique for the transfer of very-low viscosity cyan methacrylate on the inner and outer surfaces of the heart. Methods: Very-low viscosity ultraviolet curable cyan methacrylate was mixed with commercially available dye to demonstrate its ability of transfer on the inner and outer surfaces of an in-vitro heart model. Cyan methacrylate (0.5 ml) was mixed with 0.2 ml of ink, and the material was injected on the surface of the heart in dry air, allowing its fixation for 2-3 seconds. Subsequently, the whole preparation was immersed in saline, and was vigorously shaken to remove the unbound compound. A similar experi-ment was performed without cyan methacrylate, and with high viscosity cyan methacrylate (3000 cps). A significant amount of the compound was visually found to attach to the surfaces of the heart compared with ink alone. Then, after soaking the tissue in saline solution, effective transfer of the compound was assessed on the inner and the outer surfaces of the heart. Results: Among various techniques, the paintbrush technique was the most effective one for the targeted transfer of the com-pound. With this specific areas, such as instead of specific areas, as technique, it was easier to transfer the compound on the epicardial and endocardial surfaces. Also, other specific areas, as the left atrial appendage, the left ventricular inner surfaces at the origin of the papillary muscle and the left ventricular apex were successfully investigated. The ultraviolet light source was a pen-shaped device based on a light emission diode. Some compound precipitation was observed in some areas following ultraviolet treatment. The experiment was repeated with three different samples to determine the results. Conclusions: Very-low viscosity ultraviolet curable cyan methacrylate transfer is potentially useful to study the inner and outer surfaces of the heart. This technique could be useful for growth factor transfer.
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Objective: To optimize the formula and preparation technology of cantharidin chitosan bioadhesive microspheres.Methods: The microspheres were prepared by a spray drying method.A single-factor experiment was used to study the effect of chitosan with different molecular weight on the gastric mucosa adhesion rate were also studied, and the effects of different drug loading ratio, concentration of chitosan acetic acid solution and speed of peristaltic pump on the loading rate were also studied.The cantharidin entrapment efficiency as the studying index, a response surface method was used to further optimize the formula.Results: The best formula and preparation process of cantharidin chitosan bioadhesive microspheres were as follows: the concentration ratio of antharidin to chitosan was 19.83% , the concentration of chitosan acetic acid solution was 0.77% , and the peristaltic pump flow rate was 9.225 ml·min-1.With the best formula, the entrapment efficiency of cantharidin chitosan bioadhesive microspheres was 90.14%.Conclusion: The microsphere preparation by the spray drying method is stable and repeatable.Cantharidin chitosan bioadhesive microspheres have high entrapment efficiency and promising biological adhesion.
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The present study was designed to prepare and compare bio-adhesive pellets of panax notoginseng saponins (PNS) with hydroxy propyl methyl cellulose (HPMC), chitosan, and chitosan : carbomer, explore the influence of different bio-adhesive materials on pharmacokinetics behaviors of PNSbio-adhesive pellets, and evaluate the correlation between in vivo absorption and in vitro release (IVIVC). In order to predict the in vivo concentration-time profile by the in vitro release data of bio-adhesive pellets, the release experiment was performed using the rotating basket method in pH 6.8 phosphate buffer. The PNS concentrations in rat plasma were analyzed by HPLC-MS-MS method and the relative bioavailability and other pharmacokinetic parameters were estimated using Kinetica4.4 pharmacokinetic software. Numerical deconvolution method was used to evaluate IVIVC. Our results indicated that, compared with ordinary pellets, PNS bio-adhesive pellets showed increased oral bioavailability by 1.45 to 3.20 times, increased C, and extended MRT. What's more, the release behavior of drug in HPMC pellets was shown to follow a Fickian diffusion mechanism, a synergetic function of diffusion and skeleton corrosion. The in vitro release and the in vivo biological activity had a good correlation, demonstrating that the PNS bio-adhesive pellets had a better sustained release. Numerical deconvolution technique showed the advantage in evaluation of IVIVC for self-designed bio-adhesive pellets with HPMC. In conclusion, the in vitro release data of bio-adhesive pellets with HPMC can predict its concentration-time profile in vivo.
Subject(s)
Animals , Male , Acrylic Resins , Adhesives , Chitosan , Drug Carriers , Drug Liberation , In Vitro Techniques , Intestinal Absorption , Methylcellulose , Panax notoginseng , Chemistry , Plant Extracts , Metabolism , Pharmacokinetics , Rats, Sprague-Dawley , Saponins , Metabolism , PharmacokineticsABSTRACT
Bio-adhesive drug delivery system (BDDS) is a novel drug delivery system, which can prolong the retention time of the preparation, improve the stability of the drug, and improve the mucosa absorption and the targeting of the drug. With the development of polymer materials over the past 30 years, BDDS made a great progress. This paper reviews the muco-adhesion theory, adhesive materials, and methods to evaluate muco-adhesive properties and applications in traditional Chinese medicine according to domestic and foreign literatures, in order to provide new ideas for further studies.
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Objective:To establish a method to determine the contents of pantoprazole sodium bioadhesive tablets. Methods:An HPLC method was adopted. The determination was performed on a HYPERSIL ODS-2 (150 mm × 4. 6 mm, 5μm) column with mobile phase consisting of 0. 01 mol·L-1 dipotassium phosphate solution –methanol (60 ∶40) at the flow rate of 1. 0 ml·min-1 . The de-tection wavelength was set at 289 nm, the column temperature was maintained at 30 ℃ and the sample size was 20 μl. Results:The linear range of pantoprazole sodium was 1. 28-20. 60μg·ml-1,(r=0. 999 8) . The average recovery was 99. 52%(RSD=1. 43%, n=9). Conclusion:The method is simple, accurate and reliable, and can be used for determining the content of pantoprazole sodium bioadhesive tablets.
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OBJECTIVE: To explore the effects of different bio-adhesive materials on in vitro adhesion and retention in artificial gastric acid fluid of Panax notoginseng saponins(PNS) bio-adhesive pellets. METHODS: PNS bio-adhesive pellets were prepared with different bio-adhesive materials.The in vitro adhesion of PNS bio-adhesive pellets was determined by the tissue retention method, using HPLC method to determine the contents of PNS(including notoginseng saponins R1, ginseng saponin Rg1 and ginseng saponin Rb1) retained in the pellets after a certain period of time in artificial gastric acid fluid. RESULTS: The contents of PNS retained in PNS bio-adhesive pellets prepared with chitosan and chitosan-carbomer after being placed in artificial gastric acid fluid for 2 h were the largest, which were (27.60±7.45)% and (19.80±3.55)% for R1, (27.01±5.49)% and (19.67±1.39)% for Rg1 and (47.07±6.26)% and (51.08±7.44)% for Rb1, respectively.For in vitro adhesion, HPMC and HPMC-carbomer combination was the best, followed by chitosan and chitosan-carbomer combination. CONCLUSION: PNS bio-adhesive pellets prepared with chitosan and chitosan-carbomer combination bio-adhesive materials can protect PNS from degradation in artificial gastric acid fluid and have good adhesion property.
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The aim of the present study is to formulate tenofovir loaded gelatin nanoparticles by two step desolvation method for targeted release of drug by varying the concentration of polymer and cross-linking agent. Entrapment efficiency for all the formulations was found to be within 67.32 ± 1.24 % to 92.11 ± 1.13 %. Average particle size of different tenofovir loaded gelatin nanoparticle formulations was found within the range of 294.9 - 445.3 nm. In-vitro drug release study for glutaraldehyde cross linked gelatin nanoparticles were found between 67.09 % ± 1.423 – 82.41 % ± 1.874 after 8 h of dissolution. F5 (850 mg gelatin, 0.2 ml glutaraldehyde) was considered as the best formulation based on the entrapment efficiency and drug release from nanoparticle core. Kinetics study was performed for all the formulations and best fit model for drug release was determined depending on R squared values. HPMC K15M was used as a bioadhesive polymer as well as a gelling agent. Three different gel formulations were prepared by varying concentration of HPMC K15M and incorporated with the best formulation, F5. Membrane permeation and bio-adhesion study revealed F5B gel (5% HPMC K15M) as an optimum formulation with suitable bioadhesive strength and membrane permeability.
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We evaluated the histological dental pulp state in vivo after indirect pulp capping using sildenafil or LG-nitro-L-arginine (L-NAME), incorporated into a new bioadhesive thermoresponsive system (BTS). Male Wistar rats were subjected to an upper and lower first molar class I cavity preparation followed by indirect pulp capping with sildenafil or L-NAME. Calcium hydroxide (CaOH2) was used as a control. The teeth and surrounding bone were properly dissected and processed for Nissl's staining. Pulp state was evaluated considering the morphological aspects of the inflammatory response, type of inflammatory infiltrate, organization of the odontoblast layer, blood vessel condition, and presence of abscesses or necrosis. The results were expressed as average of observations. The most intense inflammatory response was observed 3 days after the cavity preparation. No identified changes were detected in the dental pulp response of the molars treated with L-NAME compared with those treated with CaOH2. A dual effect was observed in the teeth treated with sildenafil. While low sildenafil concentration (0.015% w w-1) promoted effects comparable to CaOH2, at a higher concentration (0.15% w w-1), sildenafil caused a severe inflammatory response and pulp necrosis. This pioneering suggest that NO pathway activity may be a determinant in the process of dental pulp healing.
Avaliou-se o estado histológico da polpa dental in vivo após capeamento pulpar indireto usando sildenafil ou LG-nitro-L-arginine (L-NAME), incorporados num novo sistema bioadesivo termorresponsivo (BTS). Ratos Wistar machos foram sujeitos ao preparo cavitário, classe I nos primeiros molares superiores e inferiores, seguido de capeamento pulpar indireto com sildenafil ou L-NAME incorporados em BTS. Hidróxido de cálcio (CaOH2) foi usado como controle positivo. Os dentes e tecidos adjacentes foram adequadamente dissecados e processados para a coloração de Nissl. O estado da polpa foi avaliado quanto aos aspectos morfológicos e tipo do infiltrado inflamatório, organização da camada de odontoblastos, condições dos vasos sanguíneos e presença de abcesso ou necrose. A reposta inflamatória mais intensa foi observada três dias após o preparo cavitário. Nenhuma alteração foi detectada na polpa dental dos molares tratados com L-NAME comparados com aqueles tratados com CaOH2. Um efeito dual foi observado nos dentes tratados com sildenafil. Enquanto baixas concentrações de sildenafil (0.015% v v-1) promoveram efeitos comparáveis com o CaOH2, altas concentrações (0.15% v v-1) causaram uma severa resposta inflamatória e necrose pulpar. Este estudo pioneiro sugere que a atividade da via do NO pode ser determinante no processo de cicatrização.
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Rats , Dental Pulp Capping , Dental Pulp Necrosis , Sildenafil CitrateABSTRACT
Se desarrollaron sistemas poliméricos bioadhesivos del tipo película polimérica y comprimido empleando el biopolímero pullulan, para el transporte de digluconato de clorhexidina, el cual es un principio activo utilizado como alternativa terapéutica en el tratamiento de la gingivitis y de la enfermedad periodontal. Inicialmente, se evaluó la capacidad del polímero para formar películas y tabletas, luego, fueron propuestas formulaciones de cada uno de los sistemas. A las películas y comprimidos obtenidos se les determinaron propiedades mecánicas y de transporte, actividad antiséptica, caracterización de las microestructuras obtenidas, además, se comprobó la liberación del fármaco desde los sistemas estudiados. Con las formulaciones seleccionadas se determinó su capacidad mucoadhesiva in vitro, empleando como sustrato mucosa oral porcina.
As a therapeutic alternative in the transport of active substances in treatment of gingivitis and periodontal disease, bioadhesive polymeric systems type polymeric film and tablet were developed using the biopolymer pullulan. First, the ability of pullulan polymer to form films and tablets was evaluated and formulations were proposed for each system. Mechanical and transport properties, as well as antiseptic activity and microstructures characteristics were determined for these polymeric systems. Drug release behavior in the studied systems was also verified. The in vitro mucoadhesive capacity was determined with the formulations selected, using porcine oral mucous membrane like substrate.
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To study the bioavailability of pueraria flavonoids bio-adhesive and floating pellets, the absorption of puerarin was studied using Caco-2 cell monolayer by liquid chromatography (HPLC) method, comparing the Papp of pueraria flavonoids bio-adhesive and floating pellets with different bio-adhesive materials. Drugs were administered at a dose of 100 mg·kg-1 via ig. The plasma concentration of puerarin was determined by HPLC, the pharmacokinetics were calculated with the WinNonlin 6.0 software. The results showed that the Papp of bio-adhesive and floating pellets with hydroxypropyl methylcellulose (HPMC)-cabomer was largest, which had a significant difference (P0-t of pueraria flavonoids bio-adhesive and floating pellets was 1.79 times of pueraria flavonoids, the Cmax of pueraria flavonoids bio-adhesive and floating pellets and pueraria flavonoids had a significant difference (P<0.05). What's more the MRT had prolonged. In conclusion, pueraria flavonoids bio-adhesive and floating pellets with HPMC-cabomer could significantly facilitate the transport of puerarin on Caco-2 cellular monolayers. The bioavailability of pueraria flavonoids bio-adhesive and floating pellets with HPMC-cabomer was increased more than pueraria flavonoids with a sustained release effect.
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Bioadhesive delivery systems with sustained release characteristics can promote the absorption and increase the bio-availability of drugs by prolonging the residence time on the applied site. The evaluation of adhesion property of bioadhesive drug deliv-ery systems is important because the sustained release effect and the absorption are closely related with the adhesion. The methods for the evaluation of the adhesive properties of bioadhesive drug delivery systems in vitro were summarized in the article, including determi-ning the minimum peel force, measuring the residues on mucosa surface, determining the retention time on mucosal surface, measuring the swelling and the viscosity of fluid and so on, and the operation of some methods were described simply as well.
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@#The aim of this study was to conduct the preparation and pharmaceutical characterization of a new type of terbinafine hydrochloride bioadhesive film-forming gel. The viscosity of the gel of(13 299±51)mPa ·s, pH of 3. 50±0. 50, and the shearing viscosity of(196±4)g/cm2 was found. This new gel turned out to be a layer of solid film on the application site in a very short time. The remaining solid ratio of the resulting film was estimated to be(50. 74±2. 81)%; the tensile strength was(1. 17±0. 21)MPa; and the breaking elongation was(21. 42±3. 24)%. In vitro release behavior of terbinafine hydrochloride from the film was investigated according to the paddle over disk method in ChP2010. Terbinafine hydrochloride released continuously for 10 h from the film. Improved Franz type diffusion cells were used in vitro transdermal studies by the application of excised minipigs skins. No penetration of drug into the receptor medium across the skin existed and so it could imply the safety for local application. It was found that(93. 05±5. 66)% of drug stayed on the skin surface while(1. 15±0. 85)% entered into the skin, which was beneficial for the treatment of superficial skin fungal infection.
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OBJECTIVE:To study the effects of Clebopride(CBP)bioadhensive sustained-release tablets on experimental gas-tric ulcer and gastrointestinal motility disorder. METHODS:Gastric ulcer rat model was induced by ethanol and aspirin,and then divided into model group (normal saline),common tablet (CBP tablet 0.072 mg/kg) and sustained-release tablet high-dose and low-dose groups (CBP bioadhensive sustained-release tablet 0.072,0.036 mg/kg);normal rats were included in normal control group (normal saline);they were given relevant medicine intragastrically,twice a day for sustained-release tablet,three times a day for other. Ulcer area were observed 2 and 4 days after medication to calculate healing rate of ulcer(n=6). Gastrointestinal mo-tility disorder mice model was induced by atropine,and then divided into model group (normal saline),common tablet group (CBP tablet 0.1 mg/kg)and sustained-release tablet high-dose,medium-dose and low-dose groups(CBP bioadhensive sustained-re-lease tablet 0.1,0.05,0.025 mg/kg);normal mice were included in normal control group(normal saline);they were given rele-vant medicine intragastrically,once a day,for consecutive 3 days. The rate of gastric emptying and small intestinal propulsion were detected (n=6). RESULTS:Compared with normal control group,ulcer area of rats increased in model group;compared with model group,that of rats decreased in common tablet group and sustained-release tablet high-dose,low-dose groups,with statisti-cal significance (P<0.01);healing rates of gastric ulcer were 32.35%-48.24% 2 days after medication,and those were above 70% 4 days after medication. Compared with normal control group,the rate of gastric emptying and small intestinal propulsion in mice decreased in model group;compared with model group,those of mice increased in common tablet group and sustained-re-lease tablet high-dose,medium-dose,low-dose groups. The effects of sustained-release tablet high-dose and medium-dose groups were better than that of common tablet group;those difference had statistical significance (P<0.01 or P<0.05). CONCLU-SIONS:CBP bioadhensive sustained-release tablets have im-provement effects against gastric ulcer of rats and gastrointesti-nal motility disorder of mice.
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OBJECTIVE: To investigate the absorption kinetics of Panax notoginseng saponins (PNS) in rat small intestines and the effects of bioadhesive materials on the absorptive kinetics and appearance permeability. METHODS: HPLC was used to determine the concentrations of Panax notoginseng saponins. An in situ single pass intestinal perfusion was used to investigate the absorption of Panax notoginseng saponins in rat small intestines (duodenum and jejunum-ileum). RESULTS: In duodenum and jejunum-ileum, Panax notoginseng saponins at different concentrations (0.5-2 mg · mL-1) had no significant effect on the absorptive kinetics and appearance permeability of small intestines (P > 0.05), respectively. Some bioadhesive materials (include chitosan, carbomer 934P, 941P, Konjac glucan and HPMC K4M) could promote the absorption of Panax notoginseng saponins in small intestines, this effect was more obvious in duodenum area. HPMC K15M has no effect on the PNS absorption in small intestines(P > 0.05), pectin could even delay the absorption to some extent. CONCLUSION: Panax notoginseng saponins has a poor absorption in small intestines, the passive diffusion mechanism take great part in its transport progress. Some bioadhesive materials could enhance the permeability of Panax notoginseng saponins on the small intestine wall.
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<b>Introduction: </b>Brenta’s silt-clay (BrentaKer<sup>®</sup>, EGAP, Italy) is a natural sediment containing minerals pertaining to Italian Dolomite Alps mountains, which is extracted from the catchment area of Brenta river. Particle-size distribution, mineralogical, chemical, tensiometric investigations with some observational findings open to new perspectives for its application in beauty & wellness field. On these basis, surface energy evaluations of tensiometric affinity with the skin by TVS modelling [1] and in-vivo clinical studies of anti-acne properties of Brenta’s silt-clay were performed.<BR><b>Objectives:</b> The aim of this work was to evaluate the properties of the Brenta’s silt-clay in anti-acne cosmetic treatments. These properties were hypothesized on the basis of its tensiometric affinity for the skin, as determined by the Bio-adhesive TVS index [1].<BR><b>Materials and Methods: </b> Surface energy studies were performed by contact angle method, using the DSA10-Kruss tensiometer (diiodomethane, FomblinHC/25<sup>®</sup>PFPE, glycerine as liquid tests). Bio-adhesive TVS index levels were originated from overlapping Brenta’s silt-clay and skin’s tensiometric prints. 10 healthy volunteers with mild-moderate facial acne vulgaris with a maximum of 20 comedones, 50 papules and pustules, without nodules or cysts were enrolled [2]. A mud composed by 15g of γ-rays irradiated Brenta’s silt-clay (Oroscare, EGAP, Italy) and 10g of water was prepared and applied on the areas of the face to be treated (15 minutes, twice a week, 30 days). Number of a) comedones, papules and pustules, (b) quantity of sebum (Sebumeter-CK), (c) pH (pH-Meter-CK), and (d) soothing effect evaluated by skin’s colour (Mexameter-CK) were analysed at baseline (T0), after 15 (T15) and 30 (T30) days.<BR><b>Results:</b> In three subjects, the Bio-adhesive TVS index showed maximal affinity between Brenta’s silt-clay (DC=17.8±4 mN/m, PC=32.0±4.6 mN/m, SFE=49.8 mN/m) and untreated skin (DC=13.5±4.1, PC=19.67±13.4, SFE=33.2±16.2), indicating that the surface energy of Brenta’s silt-clay was higher than that of the skin and suggesting its capability to modify skin’s selective permeability. In T0-T30 period the number of papules significantly decreased from 11.3±3, 83 to 10.6±3, 74 (p=0.033). In the same period, the number of postules decreased from to 2.5±1.5 to 1.9±2.02 (p=0.055) whereas the papular colorimetric measurement diminished from 618±13.5 to 613.0±6.80 (p=0.046). Sebum values significantly decreased both in T0-T15 (-28.7%, p=0.027) and in T0-T30 (-32.7%, p=0.017) periods. Finally, significant changing of pH and colorimetric measurements on healthy skin were not observed.<BR><b>Conclusions: </b>In subjects with mild to moderated facial acne vulgaris, a mask based on Brenta’s silt-clay regulates the sebum, reduces papular inflammatory, maintains cutaneous physiological conditions, suggesting its efficacy in anti-acne treatment. Bio-adhesive TVS index analysis suggests that this efficacy is probably related to its capability to modify skin’s selective permeability.