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OBJECTIVE：To study the effects of different penetration enhancers on in vitro transdermal permeation of Flavaspidic acid BB cream. METHODS ：Flavaspidic acid BB cream was prepared ，containing 11 kinds of different penetration enhancers as 1％ azone，2％ azone，3％ azone，4％ azone，1％ menthol，1％ propylene glycol ，1％ oleic acid ，1％ azone+1％ menthol，1％ azone+1％ propanediol，1％ azone+1％ oleic acid or 1％ menthol+1％ propanediol. Modified Franz diffusion cell was adopted using abdominal skin of isolated male rat as transdermal barrier. The content of flavaspidic acid BB was determined by UPLC. The accumulative transdermal amount （Q24 h）and percutaneous permeability （Jss）within 24 h were calculated ；and compared with Flavaspidic acid BB cream without transdermal enhancer ，the enhancement ratio （ER）was calculated. RESULTS ： Q24 h of Flavaspidic acid BB cream with above 11 kinds of transdermal enhancers were （82.96±7.15），（80.17±0.66），（78.22± 1.87），（73.53±1.24），（35.65±2.23），（34.02±1.73），（42.68±2.66），（33.94±1.37），（34.16±1.54），（46.78±1.21），（43.66±1.69） μg/cm2，respectively. Jss value were （5.26±0.10），（4.69±0.12），（4.45±0.45），（4.00±0.06），（3.74±0.33），（3.23±0.18）， （3.73±0.53），（3.14±0.47），（3.54±0.11），（3.98±0.34），（4.34±0.14）μg（/ cm2·h），respectively. ER were 2.055，1.831，1.738， 1.564，1.462，1.263，1.456，1.227，1.385，1.557，1.698，respectively. CONCLUSIONS ：All of the above transdermal absorption enhancers can enhance the percutaneous absorption of Flavaspidic acid BB cream ，among which ，1％ azone is the best.
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This experiment was aimed to screen the absorption enhancer for intranasal administration preparations of paeoniflorin. In this study, HPLC method for determination of paeoniflorin in perfusion liquid was established and the improved model of nasal perfusion in rats was used to screen out the species and amounts of absorption enhancer. In order to avoid the influence of the secretion and absorption of nasal cavity on the volume of perfusion fluid, the residual dose was calculated by using the volume correction method. Linear regression was carried out between the logarithm to the percentage of the residual dose and the corresponding time, and the slope of the regression line was exactly the absorption rate constant. Experimental results showed that hydroxypropyl-β-cyclodextrin and water-soluble azone can significantly improve the nasal absorption of paeoniflorin. Furthermore, water-soluble azone had the highest absorption rate constant and the best promoting penetration effect on intranasal administration preparations of paeoniflorin. It was also found that when the mass concentration of water-soluble azone in the perfusion liquid increased from 5 g•L⁻¹ to 20 g•L⁻¹, the absorption rate constant was gradually increased and peaked at 20 g•L⁻¹. When the mass concentration was increased to 30 g•L⁻¹, the absorption rate constant was decreased, indicating that the best mass concentration of water-soluble azone was 20 g•L⁻¹.
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PAMAM dendrimer is one of the most widely studied dendrimers in recent years, which has a large number of functional groups on the surface and cavities inside, specific three-dimensional structure and good biocompatibility, permeability and stability. It has been widely applied in drug and gene carrier fields and may become a new absorption enhancer. In order to study the absorption enhancing effects of PAMAM dendrimers, liquiritin was selected as the model drug, with the protection of spleen and liver, detoxification and other functions, but it had not been widely used in clinical application because of its difficult absorption, first pass effect, and low bioavailability. This topic was based on the two main determinants (solubility and permeability) of intestinal absorption in the body, researched the physicochemical properties of liquiritin, analyzed the transport volume of liquiritin with or without PAMAM dendrimers by using Caco-2 cell model, and analyzed the cytotoxicity of PAMAM dendrimers on Caco-2 cells by MTT experiments. These results showed that 0.1% of the G4 generation PAG can promote the absorption of liquiritin safely and effectively, and it was suitable for further development into a new type of pharmaceutical excipients.
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@#In this paper, silymarin nanoemulsions(SM-NE)were prepared based upon PC/Tween 80 system, and adsorption of lactoferrin(LF)absorbed onto the surface of silymarin nanoemulsions via electrostatic interaction resulted in the formation of lactoferrin-modified silybin nanoemulsions(LF-SM-NE). SM-NE and LF-SM-NE were characterized in terms of the shape, diameter, zeta potential, and entrapment efficiency. In addition, in vivo absorption of SM-NE and LF-SM-NE following oral dosing was investigated by the application of LC-MS/MS in the determination of silymarin in blood sample. The results showed that the saturated adsorption of Lf at the surface of the SM-NE occurred at LF concentration of 0. 15 mg/mL and the incubation time of 4 h. LF-SM-NE were spherical with average particle size of(257±5. 9)nm, zeta potential of -(33. 1±1. 5)mV, entrapment efficiency(96. 9±1. 9)% and drug loading(3. 90±0. 12)%. Compared with those of SM-NE, LF-SM-NE significantly increased drug levels of LF in rats were observed after dosing of LF-SM-NE, and both of cmax and AUC were increased by approximately 2-fold. In summary, LF-SM-NE could improve oral drug absorption of LF in rats. The approach of enhancement in oral absorption of the nanoemulsions shows a promise for the application.
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Aim: To investigate the enhancement of enhancers on matrine in vitro and in vivo. Methods: The permeability of matrine across rat intestine was determined by non-everted intestinal sacs model in vitro, and the in vivo activity was assayed in a model of acute liver injury in mice. Sodium deoxycholate (SDC) was selected as the enhancer Candidate. Results: Among the tested absorption enhancers, only polysorbate 80 (Tween 80) and SDC showed to be capable of increasing the transport of matrine through small intestinal mucosa in rats.Enhancement ratios of 1.6 was observed for 0.5% SDC solutions with the best absorption enhancement for matrine in vitro, it was chosen to conduct hepatoprotective study in vivo. In mice with acute liver injury, combination of matrine with 0.5% SDC demonstrated considerably more activity than matrine along after oral administration. Conclusion: The results indicated that the absorption of matrine could be significantly improved by the absorption enhancer.
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OBJECTIVE: To optimize the formulation of ketamine hydrochloride for intranasal administration that was of effective anesthetic effect.METHODS: Using ketamine hydrochloride injection as basic preparation,various nasal absorption enhancer or viscosity modifiers(0.5%,1% and 2% azone,EDTA,carbomer,2-hydroxypropyl-?-cyclodextrin,carboxymethyl cellulose) were added to make different nasal drops.After intranasal administration,the anesthetic effect was evaluated to find the optimum formulation.The behavior of anesthetic induction period and anesthetic index were used to evaluate the anesthetic effect.RESULTS: The perfect anesthetic effect was achieved when the formulation was prepared by adding 1% azone in ketamine hydrochloride injection(at a dose of 10 mg?kg-1).The anesthetic time was long.The muscle relaxing time,eyelid reflecting disappearing time,pain disappearing time and righting reflecting disappearing time were(21.4?7.1) min,(11.4?4.6) min,(15.6?5.7) min and(12.0?4.8) min,respectively.CONCLUSIONS: Optimal formulation of ketamine hydrochloride for intranasal administration was obtained when 1% azone was added as an absorption enhancer.
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Aim Effect of various absorption enhancers on the insulin colonic absorption was investigated. Methods The hypoglycemic effect was examined after colon delivery of INS SOL co administered with various absorption enhancers and the pharmacological bioavailability (PA) was calculated. Results INS SOL (5 U?kg -1 ) containing eucalyptol, sodium caprate, sodium deoxycholate and menthol significantly decreased the blood glucose level ( P
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0.1%EDTA≈5% HP ? CD≈1%lecithin. Conclusion: The three methods have good correlation.
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AIM To investigate the hypoglycemic effect of buccally delivered insulin solution (INS SOL) in normal rats. METHODS The hypoglycemic response was examined after buccal delivery of INS SOL co administered with various absorption enhancers. The pharmacological bioavailability (PA) was used to evaluate the absorption enhancement of INS SOL from the buccal cavity under various conditions compared with subcutaneous injection. RESULTS In the absence of enhancers, the PA was low(6 8%) after buccal delivery of INS SOL. However, the concomitant administration of sodium lauryl phosphate, sodium deoxycholate, Brij78 as well as lecithin appeared to be more effective in increasing the hypoglycemic effects of insulin. INS SOL (5 ??kg -1 ) containing 5% Brij 78 had the highest PA of 33%. CONCLUSION The use of proper absorption enhancers is useful for improving the buccal absorption of insulin.