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@#In order to guarantee the quality of traditional Chinese medicines (TCMs), the crystallization transformation of complex extracts of TCMs and the influence of solid form on their physicochemical properties were studied.The extract of total flavonoids from Pueraria lobata was taken as a model.Crystallization transformation happened when lofting under different conditions, and the intrinsic dissolution tests were carried out.It was found that humidity was the key factor to induce crystallization of total flavonoids from Pueraria lobata.The greater the wettability was, the more the crystallization was.The dissolution rate of total flavonoids from Pueraria lobata with the most crystallization amount significantly decreased by 96.51% compared to the sample without crystallization.After further simulating the preparation process of total flavonoids from Pueraria lobata, it was found that the wet granulation process with introduced water would also lead to crystallization and reduced dissolution rate.As for all crystallization samples, there was an inversely proportional relationship between the dissolution rates and the amount of crystallization.The risk of crystallization existed both in the storage and preparation process of TCM extracts.Crystallization would significantly affect the dissolution rate, and thus the quality of TCM products.In this study, the crystallization transformation of amorphous complex TCM extracts was discovered, and the effect of the crystallization transformation on its dissolution behavior was systematically studied, which provides a new research idea for assuring the quality of TCM products and promoting the improvement of TCM preparation level.
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Objective: To prepare magnolol solid dispersions (Mag-SD), magnolol phospholipids complex (Mag-PC) and magnolol solid lipid nanoparticles (Mag-SLN), and compare their effects on the pharmacokinetics in vivo. Methods: Solvent evaporation method was used to prepare Mag-SD and Mag-PC. Their existential state of Mag in Mag-SD and Mag-PC were analyzed by X-ray power diffraction (XRPD). High pressure homogenization method was employed to prepare Mag-SLN, its particle size and Zeta potential were also studied. The dissolution in vitro of Mag-SD, Mag-PC and Mag-SLN were also studied compared to magnolol suspension. SD rats in each group were administered intragastrically with magnolol, Mag-SD, Mag-PC and Mag-SLN, respectively. The concentration of magnolol in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. The pharmacokinetic behavior and bioavailability of magnolol, Mag-SD, Mag-PC and Mag-SLN were also compared. Results: The results of XRPD indicated that magnolol showed an amorphous state in Mag-SD and Mag-PC. The average particle size and Zeta potential of Mag-SLN was (161.37 ± 3.77) nm and (-29.16 ± 1.83) mV, respectively. The results of dissolution in vitro indicated that the cumulative dissolution of magnolol was 30.6% within 12 h. Mag-SD, Mag-PC and Mag-SLN enhanced its cumulative dissolution to 96.3%, 76.4% and 45.9%, respectively. The results of pharmacokinetics in vivo showed that Cmax, AUC0-t and AUC0-∞ of Mag-SD, Mag-PC and Mag-SLN were enhanced greatly compared to magnolol suspension. Mag-PC, Mag-SD and Mag-SLN increased its Cmax from (429.67 ± 53.12) ng/mL to (533.62 ± 59.01), (721.73 ± 103.44) and (1 063.21 ± 108.22) ng/mL, respectively. The bioavailability of Mag-SD, Mag-PC and Mag-SLN were enhanced to 1.38, 2.12 and 3.45 times, respectively. Conclusion: Mag-SD, Mag-PC and Mag-SLN could promote the absorption of magnolol in SD rats notably. In addition, Mag-SLN could give a better effect on the bioavailability.
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Irbesartan (IBS) is a tetrazole derivative and antihypertensive drug that has two interconvertible struc-tures, 1H-and 2H-tautomers. The difference between them lies in the protonation of the tetrazole ring. In the solid-state, both tautomers can be isolated as crystal forms A (1H-tautomer) and B (2H-tautomer). Studies have reported that IBS is a polymorphic system and its forms A and B are related monotropically. These reports indicate form B as the most stable and less soluble form. Therefore, the goal of this contribution is to demonstrate through a complete solid-state characterization, thermodynamic study and dissolution properties that the IBS forms are desmotropes that are not related monotropically. However, the intention is also to call attention to the importance of conducting strict chemical and in solid-state quality controls on the IBS raw materials. Hence, powder X-ray diffraction (PXRD) and Raman spectroscopy (RS) at ambient and non-ambient conditions, differential scanning calorimetry (DSC), hot stage microscopy (HSM), Fourier transform infrared (FT-IR) and scanning electron microscopy (SEM) techniques were applied. Furthermore, intrinsic dissolution rate (IDR) and structural stability studies at 98％relative humidity (RH), 25 ?C and 40 ?C were conducted as well. The results show that in fact, form A is approximately four-fold more soluble than form B. In addition, both IBS forms are stable at ambient conditions. Nevertheless, structural and/or chemical instability was observed in form B at 40 ?C and 98％RH. IBS has been confirmed as a desmotropic system rather than a polymorphic one. Consequently, forms A and B are not related monotropically.
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The aim of this work was to develop, optimize and characterize a silymarin-laden polyvinylpyrrolidone (PVP)-polyethylene glycol (PEG) polymeric composite to resolve low aqueous solubility and dissolution rate problem of the drug. A number of silymarin-laden polymeric formulations were fabricated with different quantities of PVP K-30 and PEG 6000 by the solvent-evaporation method. The effect of PVP K-30 and PEG 6000 on the aqueous solubility and dissolution rate was investigated. The optimized formula-tion and its constituents were characterized using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) techniques. Both the PEG 6000 and PVP K-30 positively affected the aqueous solubility and dis-solution rate of the drug. In particular, a formulation consisting of silymarin, PVP K-30 and PEG 6000 (0.25/1.5/1.5, w/w/w) furnished the highest solubility (24.3972.95 mg/mL) and an excellent dissolution profile (～100％ in 40 min). The solubility enhancement with this formulation was ～1150-fold as com-pared to plain silymarin powder. Moreover, all the constituents existed in the amorphous state in this silymarin-laden PVP-PEG polymeric composite. Accordingly, this formulation might be a promising tool to administer silymarin with an enhanced effect via the oral route.
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Objective: To prepare astragaloside IV self-emulsifying drug release system (astragaloside IV SMEDDS), and investigate its intestinal absorption characteristics in rats. Methods: According to the solubility and compatibility of astragaloside IV in different oil phases, surfactants and cosurfactants, the prescription composition of astragaloside IV SMEDDS was determined. The dosage range of each component in the ideal microemulsion region was drawn by pseudo-ternary phase diagram, and the microstructure, particle size distribution and in vitro drug release of astragaloside IV SMEDDS after water dispersion were evaluated. The stability of astragaloside IV SMEDDS diluted with simulated human physiological body fluid was investigated, and the intestinal absorption kinetics of astragaloside IV self-microemulsion in rats was investigated by intestinal reflux test in rats. Results: The prescription of astragaloside IV SMEDDS was composed of Capmul MCM, Tween-80, and Transcutol H. Astragaloside IV SMEDDS was prepared by water dispersion to form a light blue emulsion microemulsion, and the uniform size of the microemulsion could be observed under transmission electron microscope, and the microemulsion was prepared by selecting a certain amount of astragaloside IV in any prescription dosage in the microemulsion formation region. The light blue emulsion microemulsion could be observed under transmission electron microscope. The average particle size of astragaloside IV SMEDDS was (45.4 ± 5.8) nm; The dissolution rate of astragaloside IV in the three dissolution media was significantly increased, and the microemulsion formed by astragaloside IV had good physical stability in simulated human physiological liquid. The absorption rate of astragaloside IV microemulsion in the whole intestine of rats was significantly higher than that of astragaloside IV suspension. Conclusion: The preparation of astragaloside IV into SMEDDS can increase the dissolution rate of the drug, enhance the absorption of the drug in the intestinal tract, which is expected to improve the oral bioavailability of astragaloside IV.
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Objective: Hot-melt extrusion technique was applied to prepare magnolol solid dispersions, which can improve the in vitro solubility of magnolol and the in vivo bioavailability in rats. Methods: Four kinds of excipients, such as PS-630, HPC, EPO, and Soluplus, which were compatible with magnolol were used to prepare solid dispersions of different drug loadings by solubility parameter calculation. The prepared solid dispersion was characterized by differential scanning calorimetry (DSC), X-ray diffraction analysis (XRPD) and infrared spectroscopy (IR) using in vitro dissolution as an indicator; UPLC-MS/MS was used to evaluate the pharmacokinetic behavior of rats after oral administration of magnolol solid dispersion. Results: The in vitro dissolution test showed that the solid dispersion prepared by the 1:6 drug loading of PS-630, HPC, and EPO can significantly improve the dissolution of magnolol, and the drug was dispersed in the carrier in an amorphous state. The in vivo bioavailability test showed that the Cmax of magnolol in the solid dispersion prepared by PS-630 and HPC was about five times and 2.3 times that of the monomer, respectively, and the AUC0-t was increased about 37.22% and 70.88%, respectively. There was no increase in the EPO system. Conclusion: Hot melt extrusion technology can be successfully applied to improve the in vitro dissolution and in vivo bioavailability of the poorly soluble drug magnolol.
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OBJECTIVE： To prepare Capsaicin solid dispersion， to optimize its formulation and characterize the dispersion. METHODS： Capsaicin solid dispersion was prepared by melting method using P188 or PEG4000 as carrier. Using 60 min accumulative dissolution rate in vitro as index， orthogonal test was used to optimize type of carrier， drug ratio and stirring time. Validation test was conducted. The stability of Capsaicin solid dispersion within 0， 30， 180 d was investigated at 40 ℃ under the relative humidity of 75％， and X-ray diffraction （XRD） was used to analyze whether there were peaks. Capsaicin solid dispersion was characterized by differential scanning calorimetry （DSC） and XRD. RESULTS： The optimized formula included P188-PEG4000 as carrier， capsaicin-P188-PEG 4000 mass ratio of 1 ∶ 5 ∶ 3， stirring for 20 min. Accumulative dissolution rate in vitro of Capsaicin solid dispersion was 84.6％ within 60 min （n＝3）， and the preparation kept stable within 180 d [RSD of content was 3％ （n＝3）； XRD showed that there was no peak]. The phase characteristics showed that capsaicin was highly dispersed in the amorphous or molecular state in carrier. CONCLUSIONS： The optimized technology can be used to prepare Capsaicin solid dispersion， and improves more than 80％ dissolution rate in vitro at 60 min. It is stable， simple and feasible.
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Tadalafil (TD), a phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, has a low oral bioavailability due to its extremely poorly aqueous solubility. The aim of this study was to enhance its solubility and dissolution by coamorphization with dapoxetine (DP), a selective serotonin reuptake inhibitor to manage premature ejaculation. Coamorphous TD-DP (molar ratio, 1:1) was prepared by solvent-evaporation method and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR). The supersaturated dissolution of TD from coamorphous TD-DP was investigated in various aqueous media and compared to that of crystalline TD. In addition, physical stability of coamorphous system was also evaluated under the conditions of 40℃/75% relative humidity (RH) and 25℃/60% RH for 90 days. DSC thermogram and PXRD pattern indicated the formation of the coamorphous TD-DP. In comparison to original TD crystal, the dissolution of TD from coamorphous system were significantly enhanced in various media (water, 0.01 mol·L-1 HCl and pH 4.5 phosphate buffer). In addition, no crystallization phenomenon of the prepared coamorphous system was observed until 90 days' storage under 25℃/60% RH. However, when temperature and humidity were increased to 40℃/75% RH, the coamorphous TD-DP was recrystallized easily.
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In current study, adefovir dipivoxil (AD)-acetaminophen (AP) cocrystal (molar ratio, 1:1) was prepared by slow evaporation from acetonitrile, followed by physicochemical characterizations using differential scanning calorimetry, powder X-Ray diffraction and Fourier transform infrared spectroscopy. Molecular modeling showed that the phosphoester group of AD was connected with the amide group of AP through hydrogen bonds. In comparison to crystalline AD, the solubility and dissolution rate of AD from AD-AP cocrystal were significantly enhanced by 1.5-fold and 1.6-fold, respectively. In addition, based on the rat single-pass intestinal perfusion study, the permeabilities of AD in various intestinal sections (i.e., duodenum, jejunum, ileum and colon) were significantly improved (e.g., about 3-fold enhancement in duodenum) after cocrystallization with AP by inhibiting P-glyprotein mediated efflux of AD, which will benefit absorption in vivo and subsequent oral bioavailability of poorly permeable drug AD.
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To illustrate the intrinsic dissolution rate(IDR) involved in biopharmaceutics classification system of Chinese materia medica(CMMBCS), investigate the effect of artificial multicomponent environment on IDR of berberine, by using a non-disintegrating disk, and summarize related rules by using the obtained data. Progressive levels design was used to investigate the effects of single component environment (puerarin, baicalin, and glycyrrhizic acid); double-component environment(puerarin+baicalin, puerarin+ glycyrrhizic acid, baicalin+glycyrrhizic acid); and triple-component environment(puerarin+baicalin+glycyrrhizic acid) on IDR of berberine, laying a foundation for further researches on the absorption mechanism of multiple components.
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Objective: To prepare bepotastine besilate film-coated tablets, determine the dissolution rate by HPLC, and evaluate the similarity of dissolution curves for self-made tablets and the original tablets. Methods: Bepotastine besilate tablets were prepared by using microcrystalline cellulose, hydroxypropyl cellulose, mannitol, aspartame and magnesium stearate as the accessories. Bepotas-tine besilate film-coated tablets were prepared by using OpadryⅡpremixed spray-coating liquid. The formulation was screened with the angle of repose, disintegration time, content uniformity and dissolution rate as the indices. The coating material amount was screened with the dissolution rate as the index. Results: The optimal formulation of bepotastine besilate film-coated tablet contained bepotastine besilate 5 mg,mannitol 43 mg,microcrystalline cellulose 21. 5mg,aspartame 0. 5 mg,magnesium stearate 0. 5 mg and hydroxypropyl cellulose 15 mg. The optimal weight of coating material was 5% . The self-made tablets and the original tablets had similar dissolution behavior in 4 media including water, hydrochloric acid(pH 1. 2), acetate buffer solution(pH 4. 5) and phosphate buffer solution(pH 6. 8). Conclusion:The self-made tablets have similar dissolution behavior in vitro with the original tablets, and their quality is similar.
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OBJECTIVE: To investigate the effects of different dose compatibility of Scutellaria baicalensis-Rheum palmatum-Coptis chinensis based on Sanhuang Xiexin decoction (shorted for Xiexin decoction) on dissolution rate of baicalin and baicalein, and to provide reference for studying chemical mechanism of TCM compound dose composition compatibility. METHODS: HPLC method was used to determine the contents of baicalin and baicalein. By fixing the dose of S. baicalensis (3 g), using the dose of R. palmatum and C. chinensis as factors, dissolution rate of baicalin and baicalein as response value, two-factor and five-level central composite test was designed. The optimal dose compatibility of S. baicalensis-R. Palmatum-C. chinensis was optimized by response surface method, and compared with the dissolution rate of baicalin and baicalein in classic dose Xiexin decoction (S. baicalensis 3 g, R. Palmatum 6 g, C. chinensis 3 g). RESULTS: When the doses of S. baicalensis, R. palmatum, C. chinensis were 3, 1. 76, 0. 17 g, total dissolution rate of baicalin and baicalein was the highest in extract. The average total dissolution rate of baicalin and baicalein in validation test was 21. 89％ (RSD=0. 46％, n=3),and the relative error was 2. 88％ with the predicted value of 22. 54％. Compared with the classical dose of Xiexin decoction, the total dissolution rate of baicalin and baicalein in the optimum dose of S. baicalensis-R. Palmatum-C. chinensis in extract was increased by 47. 21％. CONCLUSIONS: The different dose compatibility of S. baicalensis-R. Palmatum-C. chinensis based on Xiexin decoction influence the dissolution of baicalin and baicalein to certain extent. When the doses of S. baicalensis, R. palmatum, C. chinensis are 3, 1. 76, 0. 17 g, dissolution rate of baicalin and baicalein are higher than that of classic dose.
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Objective: To optimize the preparation process of tetrandrine dropping pills (TDP) and investigate the in vitro dissolution rate. Methods: Plackett-Burman experimental design was used to screen the critical factors in the preparation process of TDP from the ratio of matrix, ratio of matrix to drug, dropping temperature, dropping rate, dropping distance, and condensate temperature. The forming rate and weight variation of TDP were used as the evaluation index, the parameters in the preparation process of TDP were optimized by using the Box-Behnken response surface method. Moreover, the in vitro dissolution rate of TDP was compared with tetrandrine tablets by rotating basket method. Results: The Plackett-Burman experimental design results showed that the ratio of matrix, dropping temperature and condensate temperature had a significant effect on the forming rate of TDP. The optimum preparation parameters by Box-Behnken response surface method were as follows: the ratio of matrix was 2.6∶1, dropping temperature was 82.4 ℃ and condensation temperature was 7.5 ℃ with high forming rate, good roundness, stable weight, and fast drug dissolution rate of TDP. Conclusion: The quality of TDP by experimental design method can meet the requirements and can be further amplified.
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Objective To prepare and characterize ursolic acid nanoparticles (UANs), and to investigate its improvement of equilibrium solubility and dissolution rate. Methods UANs were prepared by emulsion solvent evaporation method, and followed by freeze-drying. The organic phase was trichloromethane containing 30% ethanol, the aqueous phase is ultrapure water, poloxamer 188 was as surfactant and cryoprotectant. The optimal conditions for preparing nanoparticles were screened out using single-factor experiment. The particle size was used as the basis for optimization experiment. The following six main parameters had significant influences on particle size were picked out, including the concentration of poloxamer 188, volume ratio of organic to water phase, homogenate speed and homogenate time, as well as homogenization pressure and cycles. And then, dynamic light scattering equipment was used to analyze the mean particle size, the morphology of UANs powder obtained was presented by scan electronic micro-scope (SEM). The UANs weather and how changes in surface chemical character and physical structure was estimated by using X-ray diffraction (XRD) and differential scanning calorimetry (DSC). The equilibrium solubility study and dissolution test were carried on raw ursolic acid (UA) and UANs. Results The optimal conditions of preparation UANs: 0.05% of poloxamer 188, 1:4 of volume ratio of organic to water phase, 7 000 r/min of homogenate speed for 2 min and a homogenization pressure of 50.0 MPa for 6 times. Based on the optimal conditions, the mean particle size was (157.5 ± 28.0) nm and Zeta potential of (20.33 ± 1.67) mV. Particle distribution of UANs illustrated that UA had been nanoscale with uniform particle size distribution. SEM showed that UANs were nearly spherical. By the XRD and DSC, we could acquaint UA in UANs had the same chemical structure as the raw UA but had been amorphous state. The result of solubility test figured that the equilibrium solubility of UANs was 13.48 times in SGF, 11.79 times in SIF and 23.99 times in deionized water than raw UA. The dissolution rate of UANs prepared by ESE method has been up to 14.72 times in SGF and 74.35 times in SIF. Conclusion This study indicates that the emulsion solvent evaporation method has an array of valued on improving water solubility of UA, and it will have benefit on enhancing oral bioavailability.
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Objective: To improve the dissolution of Salviae Miltiorrhizae Radix et Rhizoma (SMRR) and Paeoniae Radix Alba (PRA) in Tongmai Dasheng Tablets (TDT), and to construct a good powder dispersion. Methods: SMRR, PRA, and Placenta Hominis (PH) were crushed by common method and ultramicro method using calgon as a dispersant to prepare 19 powder dispersion samples. The particle size distribution, infrared spectrum, dispersion, specific surface area, and porosity of the powder dispersions were investigated. The contents of salvianolic acid B and paeoniflorin were measured by HPLC, and the dissolution of salvianolic acid B and paeoniflorin in different powder dispersions was evaluated. Results: Infrared spectrum results showed that superfine pulverization, mixed comminution or adding the auxiliary pulverizing cannot produce new substances in medicinal powder. The dissolution rate of salvianolic acid B and paeoniflorin in the mixed ultramicro powder dispersions of SMRR and PRA was the highest, salvianolic acid B 83.57%, RSD 2.03%, paeoniflorin 80.75%, RSD 0.61%. Conclusion: The dissolution rate is affected not only by the specific surface area of the powder but also by the dispersity of the powder. In order to improve the dissolution rate of active ingredients in powder, it is important to increase the specific surface area of the powder and improve the dispersity of the powder. In the mixed powder of SMRR, PRA, and PH, the dissolution rate of salvianolic acid B and paeoniflorin was lower than that of the mixed powder of SMRR and PRA. Hence, PH was smashed alone, and then mixed with the other two kinds of medicinal powder.
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Objective Solid dispersion of curcumin and piperine compositions (CUR-PIP SD) was prepared to increase the in vitro dissolution rate and the oral bioavailability of CUR and PIP. Methods The CUR-PIP SD was prepared by a solvent evaporation method with dissolution rate as index. The characterization of CUR-PIP SD was evaluated by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), and the resulting SD was evaluated by in vitro dissolution assay. UPLC-MS/MS was used to determine the plasma concentrations of CUR and PIP in rats after ig administration. Results In vitro dissolution experiments showed that the dissolution rate of CUR and PIP in SD were both greatly improved compared with that of raw materials. Oral bioavailability of CUR in the SD was 2.71 times of that of the drug substance (P < 0.05), and PIP was increased to 2.68 times (P < 0.05). Conclusion The SD prepared with PVP K30 can effectively increase the in vitro dissolution and bioavailability of CUR and PIP.
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Objective To prepare luteolin solid dispersions (Lut-SD) and luteolin phospholipids complex solid dispersions (Lut-PC-SD), and compare the effects of two kinds of solid dispersions on the bioavailability in vivo. Methods PVP K30 was employed as carrier, and solvent evaporation method was used to prepare Lut-SD and Lut-PC-SD. Their existential state of luteolin in solid dispersions was analyzed by X-ray power diffraction (XRPD). The solubility and dissolution rate were also studied. SD rats in each group were administered intragastrically with Lut, Lut-SD, and Lut-PC-SD, respectively. Their blood samples were collected at different time intervals. Diosmetin was used as internal standard, the concentration of Lut in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. Results The results of XRPD indicated that Lut showed an amorphous state in Lut-SD and Lut-PC-SD. The solubility of Lut was enhanced from (61.09 ± 0.09) μg/mL to (365.33 ± 0.38) μg/mL and (401.14 ± 0.19) μg/mL by Lut-SD and Lut-PC-SD, repectively. The dissolution of Lut was also improved greatly by the two kinds of solid dispersions. Compared to Lut, the bioavailability of Lut-SD and Lut-PC-SD was enhanced to 150.10% and 204.52%, repectively. Conclusion Lut-SD and Lut-PC-SD both could enhance the bioavailability of Lut in SD rats notably. In addition, Lut-PC-SD could give a better effect.
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The mesoporous silica nanoparticles (MSN) in different pore size and sirolimus (SRL) loaded self-microemulsifying drug delivery system (SMEDDS) were prepared. The results in morphology were collected by scanning electron microscope, transmission electron microscope, small-angle X-ray diffraction, and N2 adsorption-desorption. The results showed that the prepared MSN has ordered nanochannels with a pore size of 6.3, 8.1, 10.8 nm, respectively. The particle size of SRL-SMEDDS were measured by particle sizing system, which was 20.6±1.3 nm. The stirring method was developed to prepare SRL-SMEDDS-MSN. It was found that the optimal ratio of SRL-SMEDDS to MSN was 2:1, while the drug loading rate was near 0.83%, and the flow properties of SRL-SMEDDS-MSN were of good condition. The differential scanning calorimetry results proving a molecular or amorphous dispersed state of SRL in MSN while the suspension experiment has shown great reconstitution properties of SRL-SMEDDS-MSN. There is no significant influence on maximum drug release rate of different pore size of SRL-SMEDDS-MSN in 250 mL water within 2 h, while the results of the first 40 min have an obvious difference. Above all, MSN might provide a new strategy for the solidification of SMEDDS.
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The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods. Appropriate amount of lubricant and disintegrating agent was added into part of the mixed powder, and then the granules were prepared by using extrusion granulation and high shear granulation. The granules dissolution behavior was evaluated by using equilibrium dissolution quantity and dissolution rate constant of the hypericin as the indicators. Then the effect of physical properties on dissolution behavior was analyzed through the stepwise regression analysis method. The equilibrium dissolution quantity of hypericin and adsorption heat constant in hawthorn leaves were positively correlated with the monolayer adsorption capacity and negatively correlated with the moisture absorption rate constant. The dissolution rate constants were decreased with the increase of Hausner rate, monolayer adsorption capacity and adsorption heat constant, and were increased with the increase of Carr index and specific surface area. Adsorption heat constant, monolayer adsorption capacity, moisture absorption rate constant, Carr index and specific surface area were the key physical properties of hawthorn leaf granule to affect its dissolution behavior.