Preparation and Swelling Kinetic Analysis of Poly (HPMC-co-AA-co-AM) Super Absorbent Resin

Super absorbent resin(SAR)is prepared by aqueous high temperature polymerization using hydroxypropyl methylcellulose(HPMC)as monomer backbone material,acrylic acid(AA)and acrylamide(AM)as the graft copolymer monomer,potassium persulfate(KPS)as the initiator to generate free radicals,and N,N`-methylenebisacrylamide(MBA)as cross-linking agent for cross-linking reaction.Simutaneously,the influence of individual factors on the water absorption is investigated,and these factors are mainly AA,AM,KPS,MBA,HPMC,and reaction temperature.The optimized conditions are obtained by the experiment repeating for several times.The water absorption multiplicity and salt absorption multiplicity under the conditions are 782.4 and 132.5 g/g,respectivity.Furthermore,the effects of different temperatures and salt concentrations on its water absorption,as well as the swelling kinetics of SAR are studied.It is indicated the water-absorbing swelling process is mainly caused by the difference in water osmotic pressure and Na+concentration inside and outside the cross-linked molecular structure of the resin,which is not only consistent with the quasi-secondary kinetic model,but also with the Fick diffusion model.

Lyophilization Process of Hydroxypropyl Tetrahydropyrantriol Liposomes

[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.

乙酰化羟丙基糯玉米淀粉对速冻汤圆品质的影响

为提高速冻汤圆的食用品质,以乙酰化羟丙基糯玉米淀粉(acetylated hydroxypropyl waxy corn starch,AHWCS)作为品质改良剂,探究其对速冻汤圆的蒸煮、质构特性和感官品质的影响。结果表明,当添加质量分数为20%时,在蒸煮特性方面速冻汤圆失重率为9.95%、蒸煮损失率为0.93%、冻裂率为13.33%,均为最低;汤汁透光率为7.43%,为最高。在质构特性方面,硬度、咀嚼性较低,质地松软,弹性最高。在感官品质方面,汤圆表面光滑、色泽鲜亮、口感柔软、有浓厚的糯米清香味,感官评分最高,为90.67分,汤圆品质最佳。因此,添加适当比例的AHWCS可有效改善速冻汤圆的品质,这为其在速冻食品中的应用提供了基础。

PREPARATION AND STRUCTURE OF FIVE DERIVATIVES OF β-(1→3)-D-GLUCAN ISOLATED FROM PORIA COCOS SCLEROTIUM

A new solvent of cellulose (1.5 mol/L NaOH/0.5 mol/L urea aqueous solution) was used as one of the homogeneous reaction media of polysaccharides for methylation, hydroxyethylation and hydroxypropylation. A water insoluble β -(1—>3)-D-glucan, sample PCS3- isolated from fresh sclerotium of Poria cocos was sulfated in dimethyl sulfoxide (Me 2 SO), carboxymethylated in NaOH, isopropanol solution, as well as methylated, hydroxyethylated and hydroxypropylated in the new solvent system, respectively, to obtain five water-soluble derivatives coded as S-PCS3- C- PCS3- M-PCS3- HE-PCS3- and HP-PCS3- Their chemical structure and distribution of substitution were characterized by infrared spectroscopy (IR), elementary analysis (EA), 1 H-NMR, 13 C-NMR, 2D-COSY, 2D-TOCSY and 2D- 1 H-detected 1H 13C HMQC spectra. The results reveal that the relative reactivity of hydroxyl groups of the β -(1-?3)-D-glucan is in the order C-6 > C-4 > C-2 on the whole. The substitution of the samples S-PCS3- C-PCS3- and M-PCS3- occurred mainly at C-6 position and secondly at C-4 and C-2 positions, and that of HE-PCS3- occurred at C-6 and C-4 positions and of HP-PCS3- almost completely occurred at C-6 position. The degrees of substitution (DS) obtained from 13 C-NMR range from 0.23 to 1.27. The water solubility of the derivatives is in the order S-PCS3- >C-PCS3- >M-PCS3- >HE-PCS3- >HP-PCS3- This work provides a novel and nonpolluting process for the methylation, hydroxyethylation and hydroxypropylation of β -(1—>3)-D-glucan.

Pharmacokinetics and Biodegradation Performance of a Hydroxypropyl Chitosan Derivative

Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical and pharmaceutical fields. However, it is not yet known about its pharmacokinetics and biodegradation performance, which are crucial for its clinical applications. In order to lay a foundation for its further applications and exploitations, here we carried out fluorescence intensity and GPC analyses to determine the pharmacokinetics mode of fluorescein isothiocyanate-labeled HP-chitosan(FITC-HP-chitosan) and its biodegradability. The results showed that after intraperitoneal administration at a dose of 10 mg per rat, FITC-HP-chitosan could be absorbed rapidly and distributed to liver, kidney and spleen through blood. It was indicated that FITC-HP-chitosan could be utilized effectively, and 88.47% of the FITC-HP-chitosan could be excreted by urine within 11 days with a molecular weight less than 10 k Da. Moreover, our data indicated that there was an obvious degradation process occurred in liver(< 10 k Da at 24 h). In summary, HP-chitosan has excellent bioavailability and biodegradability, suggesting the potential applications of hydroxypropyl-modified chitosan as materials in drug delivery, tissue engineering and biomedical area.

Graft Copolymerization of Ethyl Acrylate onto Hydroxypropyl Methylcellulose Using Potassium Persulfate as Initiator

With potassium persulfate (KPS) as initiator, graft copolymerization of ethyl acrylate (EA) onto water-soluble hydroxypropyl methylcellulose (HPMC) was investigated in aqueous medium. Effects of monomer concentration, initiator concentration, matrix concentration, and reaction temperature on the percentage of grafting (G) and grafting efficiency (G_E) were studied. The results show that G and G_E values both increase with the the increase of EA concentration and KPS concentration; when raising HPMC concentration from 0.12 mmol/L to 0.47 mmol/L, G decreases, while G_E increases;and when raising reaction temperature from 50 ℃ to 65 ℃,G increases, but G_E decreases. In addition, the graft copolymers were characterized by Fourier transform infrared (FTIR) spectra and transmission electron microscopy (TEM) methods.

Hydration Heat Effect of Cement Pastes Modified with Hydroxypropyl Methyl Cellulose Ether and Expanded Perlite

Hydration heat effect of cement pastes and mechanism of hydroxypropyl methyl cellulose ether （HPMC） and expanded perlite in cement pastes were studied by means of hydration exothermic rate, hydration heat amount, FTIR and TG-DTG. The results show that HPMC can significantly delay the hydration induction period and acceleration period of cement pastes. As mixing amount increased, hydration induction period of cement pastes enlarged and accelerated period gradually went back. At the same time, the amount of hydration heat gradually decreased. Expanded perlite had worse delay effects and less change of hydration heat amount of cement pastes than HPMC. HPMC changed the structure of C-S-H during cement hydration. The more amount of HPMC, the more obvious effect. However, EXP had little influence on the structure of C-S-H. At the same age, the content of Ca （OH）2 in cement pastes gradually decreased as the mixing amount increase of HPMC and expanded perlite, and had better delay effect than that single-doped with HPMC or expanded perlite when HPMC and expanded nerlite were both dooed in cement pastes.

Rheological and drag reduction properties of hydroxypropyl xanthan gum solutions

Hydroxypropyl xanthan gum(HXG) was prepared from xanthan gum(XG) and propylene oxide under alkaline condition. Rheological and drag reduction properties of different concentrations of aqueous HXG and XG solution were studied. The micro-structure network of HXG and XG solutions was investigated by Cryo-FESEM. The results showed that HXG and XG solutions could exhibit shear thinning property. The apparent viscosity of6 g·L-1HXG solution was 1.25 times more than that of 6 g·L-1XG solution. The storage modulus G′ and the loss modulus G″ of HXG solutions were greater than those of XG solutions, and thixotropic and viscoelastic properties were more significant in HXG solutions. The HXG and XG solutions reduced the pressure drop of straight pipe, and the maximum drag reduction of 1 g·L-1HXG and XG in smooth tube reached 72.8% and 68.1%, respectively. Drag reduction rate was increased as the concentration increased. The HXG solution may become a new polymeric drag reducer.

Properties of Novel Reactive Transfer Printing of Silk

The novel reactive transfer printing of silk was carried out through a hot-press adhesion and steaming. The special transfer paper was prepared by coating the paste mainly containing hot-melt adhesive hlgh-substituted hydroxypropyl cellulose （H-HPC） and printing thickener earboxymethyl cellulose （CMC）. The effects of each ingredient in the paste on color yield of the prints and dye penetration were investigated. The major results indicate that, color yield is chiefly governed by the adhesion extent imparted by H-HPC, the type of fixing alkaline agent, and the content of urea. Trichloroacetic acid （TCAA） as the fixing alkaline agent and adding 5% urea can enhance the color depth obviously. Dye penetration depends on the coating quantity on the transfer paper, the contents of urea and dicyandiamide. The printed silk possesses a higher color yield, color fastness of grade 3 or above, clear sharpness, and good handle when the paste contains 3 % H-HPC, 0. 7 % CMC, 3 % TCAA, 5 % urea, 3 % dicyandiamide, and 0. 5 % physical sorbent nano-silica.

Buccal administration of mucoadhesive blend films saturated with propranolol loaded nanoparticles

The aims of this study were to prepare and characterize hydroxypropyl methylcellulose(HPMC)/polycarbophil(PC) mucoadhesive blend films saturated with propranolol hydrochloride(PNL)-loaded nanoparticles to improve permeability of drugs that undergo firstpass metabolism. An ionic cross-linking method and film casting technique was used to prepare nanoparticles and mucoadhesive blend films, respectively. Increasing concentrations of PNL(70, 80, 90 mg/film) in HPMC/PC blend films containing PNL-loaded nanoparticles(PN-films) and HPMC/PC blend films containing PNL(80 mg/film) without nanoparticles(PPfilms) were prepared to test swelling, mucoadhesiveness, release, permeation and physicochemical properties. Scanning electron microscope(SEM) images showed a partially smooth surface with a wrinkled occurrence and spherically shaped, well-dispersed nanoparticles on the surface of PN-films containing PNL 80 mg/film(PN-films-80). The size of the nanoparticles on the surface of PN-films-80 was around 100 nm, which was similar to the nanoparticle size observed using light scattering technique. The swelling index(SI)of all PN-films and PP-films increased greatly in the first period time(10–20 min) and reached swelling equilibrium at 20 min and 30 min, respectively. For the PN-films, the concentration of PNL influenced the mucoadhesive properties and tended to be higher when the amount of PNL increased. Immediate release of all blend film formulations was found in early time points(10–30 min). After 120 min, the release of PN-films-70 was lower than the other PNfilms. Permeation studies using porcine buccal mucosa showed that inclusion of nanoparticles in the films increased the permeability of PNL compared to PP-films. Therefore, buccal administration of mucoadhesive blend films containing PNL-loaded nanoparticles could be a promising approach for drugs that undergo first-pass metabolism.

Thermal and structural studies of poly (vinyl alcohol) and hydroxypropyl cellulose blends

Polymers and polymeric composites have steadily reflected their importance in our daily life. Blending poly(vinyl alcohol) (PVA) with a potentially useful natural biopolymers such as hydroxypropyl cellulose (HPC) seems to be an interesting way of preparing a polymeric blends. In the present work, blends of PVA/HPC of compositions (100/0, 90/10, 75/25, 50/50, 25/75, and 0/100 wt/wt%) were prepared to be used as bioequivalent materials. Thermal analyses [differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA)], and X-ray diffraction (XRD) were employed to characterize and reveal the miscibility map and the structural properties of such blend system. The obtained results of the thermal analyses showed variations in the glass transition temperature (Tg) indicating the miscibility of the blend systems. Moreover, the changes in the melting temperature (Tm), shape and area were attributed to the different degrees of crystallinity and the existence of polymer-polymer interactions between PVA and HPC molecules. The X-ray diffraction (XRD) analysis showed broadening and sharpening of peaks at different HPC concentrations with PVA. This indicated changes in the crystallinity/amorphosity ratio, and also suggested that the miscibility between the amorphous components of homo-polymers PVA and HPC is possible. The results showed that HPC doped in PVA film can improve the thermal stability of the film under investigation, leading to interesting technological applications.

Synthesis of Hydroxypropyl Guar Gum by Phase Transfer Catalysis

HGG (Hydroxypropyl guar gum) was synthesized by phase transfer catalysis for the first time. The effects of alkalinity, phase transfer catalyst, etherification, pH value, temperature, reaction time and stirring speed were investigated. An optimal synthetic reaction technology was established, namely, dose of guar gum is 100 g, propylene oxide 40-50 g, HTAC (hexadecyl trimethyl ammonium chloride ) 1.3-1.7 g, pH value 10-10.5, temperature 45-50℃, and reaction time 3-4 hours. The result shows that the improved HGG has high viscosity. Its dissolution speed, content of insoluble residue, colloid light transparency and stability are apparently superior to guar flour.

Preparation Process of Hydroxypropyl Tetrahydropyrantriol Liposomes

[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Using particle size distribution and encapsulation rate as evaluation indicators, the effects of hydration time, ratio of organic phase to aqueous phase, granulation method, as well as thin film dispersion and reverse evaporation methods on liposomes preparation were investigated, and the optimal preparation method was selected. Single factor experiments were used to screen the drug phospholipid ratio, ultrasound time, and phospholipid cholesterol ratio, and the preparation process was optimized through orthogonal experiments. [Results] The optimal process of preparing hydroxypropyl tetrahydropyrantriol liposomes was as below: 1 : 10 of drug phospholipid ratio, 6 min of ultrasound time, 4 : 1 of phospholipid cholesterol ratio, (60.94%±7.24%) of entrapment efficiency, (86.44±6.08) nm of particle size, (0.195±0.077) of PDI. [Conclusions] The optimal preparation process of hydroxypropyl tetrahydropyrantriol liposomes selected by orthogonal experiment could effectively improve the encapsulation efficiency of hydroxypropyl tetrahydropyranotriol and reduce particle size. Moreover, the method was stable and reliable.

Regulating the Function of Nanocomposite Made from Hydroxypropyl Methyl Cellulose with Bacterial Cellulose Nanocrystal

Hydroxypropyl methyl cellulose(HPMC)-based hybrid nanocomposites reinforced with bacterial cellulose nanocrystals(BCNC) were prepared and characterized.The HPMC nanocomposites exhibited good thermal stability,with a thermogravimetric peak temperature of around 346℃.The addition of BCNC did not significantly affect the thermal degradation temperature or improve the transparency of HPMC nanocomposites.However,the addition of BCNC favorably affected the light scattering properties of the nanocomposites and enhanced mechanical properties such as tensile stress and Young's modulus from 65 MPa and 1.5 GPa up to 139 MPa and 3.2 GPa,respectively.The oxygen permeability of the HPMC nanocomposites also increased with increase in the amount of BCNC added.

Development and evaluation of Panax notoginseng saponins contained in an in situ pHtriggered gelling system for sustained ocular posterior segment drug delivery

Objective:This study aimed to lay the foundation for the research on Panax notoginseng saponins(PNS)in pH-sensitive in situ gel and the development and improvement of related preparations.Methods:We used Carbopol■940,a commonly used pH-sensitive polymer,and the thickener hydroxypropyl methylcellulose(HPMC E4M)as an ophthalmic gel matrix to prepare an ophthalmic in situ gel of PNS.In addition,formula optimization was performed by assessing gelling capability with the results of in vitro release studies.In vitro(corneal permeation,rheological,and stability)and in vivo(ocular irritation and preliminary pharmacokinetics in the vitreous)studies were also performed.Results:The results demonstrated that the in situ gelling systems containing PNS showed a sustained release of the drug,making it an ideal ocular delivery system for improving posterior ocular bioavailability.Conclusions:This study lays the foundation for the research of PNS contained in an in situ pH-triggered gel as well as the development and improvement of related preparations.It concurrently traditional Chinese medicine with a contemporary in situ gelling approach to provide new directions for the treatment of posterior ocular diseases such as diabetic retinopathy.

Nicotine transdermal patch for smoking cessation using combination of hydrophilic and hydrophobic polymers as matrix film formers

One of the most popular nicotine replacement therapies (NRTs)available in the market nowadays is the nicotine patches, which provide a source of nicotine to reduce the withdrawal symptoms experienced when smoking is stopped. Nicotine transdermal patch to satisfy addicted smoker’s cravings as oninvasive, self medicated therefore patient compliance and less frequent administration than oral was investigated to contain2 layers;backing layer, adhesive with drug layer.

Evaluation of CC2 as a Decontaminant in Various Hydrophilicand Lipophilic Formulations Against Sulphur Mustard

Objective To evaluate CC2 (N, N’-dichloro-bis [2, 4, 6-trichlorophenyl] urea) invarious hydrophilic and lipophilic formulations as a personnel decontaminant for sulphurmustard (SM). Methods Twenty percent of CC2 was prepared as a suspension or ointmentwith various chemical agents and its stability was evaluated by active chlorine assay. Theefficacy was evaluated in mice by recording the mortality after applying 29 LD50 of SM (LD50 =8.1 mg/kg dermally) and decontaminating it after 2 min with 200 mg of the formulation.Studies were also carried out with 10% and 20% CC2 in acacia and hydroxypropyl cellulose,and the suspensions were stored in polyethylene containers. The stability of the suspensionswas evaluated by active chlorine assay. The efficacy was evaluated by recording themortality after applying 29 LD50 of SM in mice and 12 LD50 of SM in rats (LD50 = 2.4 mg/kgdermally), and decontaminating it with the formulations. LD50 by different routes andprimary skin irritation test of CC2 were also carried out. Results CC2 reacted with peanutoil and neem oil, and was unstable in povidone iodine and Fuller’s earth. Good stability wasachieved with petroleum jelly, honey, polyvinyl pyrrolidone, calamine lotion, acacia andhydroxypropyl cellulose. Though CC2 was stable in lipophilic formulations, it did notprotect the animals. The hydrophilic formulations particularly acacia and hydroxypropylcellulose gave very good protection and was stable in the polyethylene containers for aperiod of 1 year. The efficacy of 20% CC2 was better than 10% CC2. The oral and dermalLD50 of CC2 was found to be above 5.0 g/kg. CC2 was also found to be nonirritant.Conclusion Twenty percent of CC2 in hydroxypropyl cellulose is better with respect tostability, efficacy and ease of decontamination. CC2 is also a safe chemical.

Preparation of silymarin nanocrystals using a novel high pressure crystallization technique and evaluation of its dissolution and absorption properties

Oral bioavailability of drug is limited by the factors such as the membrane permeability, the solubility, the dissolution rate and so on (1)In case of a poorly water-soluble drug, its solubility and dissolution rate is a critical factor for its oral bioavailability.Among various techniques for enhancing solubility or dissolution properties, physical modification of drug products such as reducing the particle size is one of common approaches [2].

Development and bioequivalence study of potassium chloride extended release tablets

The purposes of this study are to prepare the generic extended release tablet of potassiumchloride(PC) 600 mg and to compare the absorption of potassium ion from the experimen-tal tablets to that of Kaleorid? LP 600 mg(Leo Pharmaceutical Products, Denmark). Car-nauba wax was used as retardant in the matrix core tablets. The core tablets were coatedwith blends of ethyl cellulose(EC) and hydroxypropyl methyl cellulose(HPMC) to modulatethe drug release. Results of a selective two-level, three-factor experiment design revealedthat a blend of 41.75% of EC and 58.25% of HPMC at 4.5% weight gained could produce thecoated tablets having dissolution profiles similar to those of Kaleorid?. A two-treatment,two-period, two-sequence crossover bioequivalence study was carried out on 24 healthyvolunteers to compare the absorption of potassium ion from experimental tablets to thatfrom Kaleorid?. The potassium ion in the urine was measured by a selective electrode of theADVIA 1650 system(Bayer) and used to calculate cumulative urinary excretion and urinaryexcretion rate. Results of 90 percent confidence interval analysis showed that the limits fornatural log-transformed cumulative urinary potassium excretion(Ln Ae 0-24) of test productwere in the range of 3.73–3.79 mEq, corresponding to 99.08%–100.92% of Kaleorid ?, respec-tively, and the limits for natural log-transformed maximal potassium excretion rate( R max) oftest product were in the range of 1.72–1.82 mEq/h, corresponding to 97.34%–102.66% of refer-ence product, respectively. Both of them fell within the bioequivalence interval(80%–125%)of reference product, proving that experimental product is bioequivalent to Kaleorid ?.

Development,characterization and solubility enhancement of comparative dissolution study of second generation of solid dispersions and microspheres for poorly water soluble drug

The poor dissolution characteristics of water-insoluble drugs are a major challenge for pharmaceutical scientists.Reduction of the particle size/increase in the surface area of the drug is a widely used and relatively simple method for increasing dissolution rates.The objective of this study was to improve solubility,release and comparability of dissolution of a poorly soluble drug using two different types of formulations(solid dispersions and microspheres).Hydrochlorothiazide was used as a model drug.The solid dispersions and microspheres were prepared by solvent evaporation method using ethyl cellulose,hydroxypropyl methylcellulose in different drug-to-carrier ratios(1:1,1:2 w:w).The prepared formulations were evaluated for interaction study by Fourier transform infrared spectroscopy,differential scanning calorimetry,percentage of practical yield,drug loading,surface morphology by scanning electron microscopy,optical microscopy and in-vitro release studies.The results showed no interaction between the drug and polymer,amorphous state of solid dispersions and microspheres,percentage yield of 42.53%to 78.10%,drug content of 99.60%to 99.64%,good spherical appearance in formulation VI and significant increase in the dissolution rate.