OBJECTIVETo prepare diazepam transdermal gel and to assess its bioavailability.

METHODSUsing Carbopol 934 as a gel matrix, the diazepam transdermal gel was prepared with glycerol as the humectant and azone as penetration enhancer. The penetration rate of diazepam through excised rabbit skin was measured by Franz diffusion cell and HPLC method. Using diazepam tablets as control, the relative bioavailability of diazepam gel was determined in rabbits.

RESULTSThe transdermal flux of diazepam gel was 39.26 g/cm(2)/h and the bioavailability of diazepam gel was 36.25%.

CONCLUSIONDiazepam gel prepared in the study would be developed as a novel transdermal preparation.

Administration, Cutaneous ; Animals ; Biological Availability ; Diazepam ; administration & dosage ; pharmacokinetics ; Drug Compounding ; Gels ; pharmacokinetics ; Rabbits ; Skin Absorption

The clinical efficacy and safety of topical propranolol hydrochloride gel in the treatment of superficial infantile hemangiomas (IHs) were assessed. Fifty-one cases of IHs from Oct. 2010 to Sept. 2011 were subjected to the topical propranolol hydrochloride gel intervention in Fuzhou General Hospital of Nanjing Military Commands, China. Changes in size, texture, color, peak systolic velocity of the hemangiomas, resistance index and adverse effects were observed. The results were evaluated by using Achauer system, and responses of IHs to pranpronolol were considered scale II (poor) in 4 patients (17.24%), scale II (moderate) in 18 patients (24.14%), scale III (good) in 22 patients (44.83%) and scale IV (excellent) in 7 patients (13.79%). The response of superficial hemangiomas was significantly better than other hemangiomas (P<0.05), and no differences in response were found among different primary sites (P>0.05). Our study indicates that topical application of 3% propranolol hydrochloride gel is effective and safe in treating IHs.
Female ; Gels ; administration & dosage ; Hemangioma ; drug therapy ; Humans ; Infant ; Infant, Newborn ; Male ; Propranolol ; administration & dosage

Administration, Topical ; Cinnamomum zeylanicum ; Episiotomy ; methods ; Female ; Gels ; administration & dosage ; Humans ; Phytotherapy ; methods ; Plant Preparations ; administration & dosage ; Pregnancy

Child, Preschool ; Female ; Gels ; Hemangioma ; drug therapy ; Humans ; Infant ; Male ; Propranolol ; administration & dosage ; adverse effects

Based on the previous study of compound liquorice microemulsion, this paper aims to prepare the compound liquorice microemulsion gel and investigate its pharmacodynamics of chronic eczema. The type, dosage and adding method of gel matrix, and formula dosage of humectant were optimized by single factor method to obtain the formula and preparation technique of the gel. With glycyrrhizic acid, glycyrrhetin and oxymatrine used as evaluation indexes, the Franz diffusion cell method was adopted to monitor the in vitro release profile of the gel. Eczema model of delayed-type hypersensitivity in mice was chosen to detect the ear swelling rate, degree of inflammatory cell infiltration of ear pieces, and pathological changes of ear pieces, so as to investigate the therapeutic effect of the microemulsion gel. The preparation process of the compound liquorice microemulsion gel was stable. The release of glycyrrhizin and oxymatrine was most consistent with the Hixcon-Crowell kinetic model, while the release of glycyrrhizic acid was most consistent with the Ritger-Peppas kinetic model. The pharmacodynamics studies proved that compound liquorice microemulsion gel could significantly reduce the ear swelling rate in mice, with good anti-inflammatory effect as well as the ability to resist the pathological changes of chronic eczema and inhibit the infiltration of dermal inflammatory cells. Therefore, the preparation process of compound liquorice microemulsion gel is feasible, with stable drug release and a significant therapeutic effect on chronic eczema.
Administration, Cutaneous ; Animals ; Drug Liberation ; Emulsions ; Gels ; Glycyrrhiza ; Mice ; Skin Absorption

To evaluate the traits and rheological properties of thermosensitive in situ gel of Yihuang Decoction and its common gel for vaginal use, and predict the release behavior of Yihuang Decoction in situ gel in vitro. Poloxamer was used as thermosensitive material to prepare Yihuang Decoction vaginal in situ gel, and Yihuang Decoction common gel was prepared with carbopol. Then the differences of the two gels before and after diluting with vaginal fluid were compared. The rheological parameters of Yihuang Decoction in situ gel and its common gel were determined with Anton Paar MCR102 rheometer. In addition, berberine hydrochloride was selected as an index component to evaluate the in vitro release properties of Yihuang Decoction vaginal thermosensitive in situ gel. Yihuang Decoction vaginal thermosensitive in situ gel was Newtonian fluid under low-temperature conditions, which was yellow and transparent. After reaching the gelling temperature of 24.5 ℃, it became semi-solid, pseudoplastic fluid. The gelling temperature was predicted to be 37 ℃, and the phase transition time was 30 s after diluting with simulated vaginal fluid. However, the rheological properties of Yihuang Decoction common gel had no significant changes with temperature. Compared with in situ gel, the color of common gel was darker and more translucent. Besides, its mobility was stronger after diluting with simulated vaginal fluid. The in vitro release study showed that the kinetic behavior of berberine hydrochloride in Yihuang Decoction vaginal thermosensitive in situ gel was matched with the Higuchi equation. Through simulation of vaginal administration, physical properties and dynamic rheological parameters were used to intuitively and scientifically evaluate the two gels. Compared with the common gel, the thermosensitive in situ gel could quickly attached to the vaginal mucosa and release drug, and thus was more suitable for developing vaginal administration of Yihuang Decoction, which also provides references for studying new vaginal preparation of Yihuang Decoction.
Administration, Intravaginal ; Drugs, Chinese Herbal/chemistry* ; Female ; Gels/chemistry* ; Humans ; Poloxamer ; Rheology ; Temperature ; Viscosity

OBJECTIVETo screen the formulations of cryptotanshinone gel for treatment of topical diseases such as acne.

METHODDifferent cryptotanshinone gels incorporating various penetration enhancers at different concentrations were prepared using carbopol 934L as matrix. The steady transdermal fluxes and drug retention amounts in skin of the gels were investigated on single chamber diffusion cells using excised rat abdomen skin as model and 40% polyethylene glycol-400 saline as releasing media. The optimal formulation would be the gel which had the maximum drug retention amount/ transdermal drug flux ratio.

RESULTThe promotion effects of menthol at different concentrations were as follows: 5% > 3% > 1%, and the effects on drug retention amount in skin were followed as: 5% approximately equal 3% > 1%; The promotion effects of a zone at different concentrations were as follows: 5% approximately equal 3% > 1%, and the effects on drug retention amount in skin were as follows: 5% > 3% approximately equal 1%. Combination of enhancers showed no superior effects compared to single uses. 5% azone had the maximum retention amount/ transdermal flux ratio.

CONCLUSIONThe optimal formulation was the cryptotanshinone gel containing 5% azone.

Administration, Topical ; Animals ; Chemistry, Pharmaceutical ; Gels ; Male ; Permeability ; Phenanthrenes ; administration & dosage ; chemistry ; metabolism ; Rats ; Rats, Sprague-Dawley ; Skin ; metabolism

The purpose of this study was to prepare tetramethylpyrazine hydrochloride transdermal gel and to study its permeation ability in vitro. The skin permeation ability was evaluated by Valian-Chien permeation cells with isolated rat skin. The concentration of tetramethylpyrazine in samples was determined by HPLC. The optimal formulation was composed with 5% azone, 5% peppermint oil, 8% sodium carboxymethylcellulose and 8% tetramethylpyrazine hydrochloride. The accumulative permeation amount of the gel was (6 731.87 +/- 102.31) microg x cm(-2) in 12 h,and the permeation rate was (535.02 +/- 33.89) microg x cm(-2) x h(-1). The release profile in vitro was in line with zero-order formulation. Tetramethylpyrazine hydrochloride gel prepared in the study would be developed as a novel transdermal preparation.
Administration, Cutaneous ; Animals ; Chemistry, Pharmaceutical ; Gels ; In Vitro Techniques ; Male ; Permeability ; Pyrazines ; administration & dosage ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

The present study aimed to compare the clinical efficacy of a 0.4% carbomer gel and 1% carboxymethyl cellulose (CMC) containing artificial tears in treatment of dry eye patients. Sixty subjects with mean age of 45.89 years who had symptoms and signs of dry eye were enrolled in this prospective, investigator-masked and stratified random sampling study. The subjects were divided into two parallel groups with 30 subjects (60 eyes) in each group. One group received carbomer gel, and the other group received 1% CMC containing artificial tears. Subjects received the drops 3 to 4 times or more per day for 3 months. At the first visit time, the precorneal residence time of these two drops was measured. The efficacy was assessed by comparing the subjective symptoms (ocular dryness, foreign body sensation, burning sensation and pain), and the objective test results of tears breakup time, Schirmer's test and corneal fluorescein staining prior to the study and after the treatment. As a result, the ocular residence time of carbomer gel was significantly longer than that of 1% CMC (P<0.001). Most of the primary subjective symptoms and objective test results were improved after treatment in both carbomer gel group and 1% CMC group. As to the improvement of each symptom and objective test result, carbomer gel was more effective than 1% CMC group (P<0.01). In conclusion, carbomer gel had longer precorneal residence time and was more effective than 1% CMC in the treatment of patients with dry eyes.
Acrylic Resins/*administration & dosage ; Carboxymethylcellulose Sodium/*administration & dosage ; Dry Eye Syndromes/*drug therapy ; Gels/*administration & dosage ; Ophthalmic Solutions/administration & dosage ; Prospective Studies

To evaluate in vitro release and transdermal behaviors of Huoxue Zhitong gel, modified Franz diffusion cell methods was applied to investigate in vitro transdermal absorption of Huoxue Zhitong gel and the content of paeonolan in receptor fluid composed of PEG400%-95% ethanol-water (l:3:6)were determined by HPLC. The results were processed and different equations were fitted. The release law were in accordance with Weibull equation and the fitting equation was In[-1/(1 - Q)] = -0.790 51nt - 1.7012 (r = 0.9809). In 8 hours, cumulative release of paeonol was 85. 18% and the release rate was 2.827 µg . cm-2 h-1. Transdermal actions were consistent with zero-level model fit and the fitting equation was Q(t) = 1.7579t + 0. 7213 (r = 0.9991). In 8 hours, cumulative transdermal rate and transmission rate of paeonol was 54. 85%, 1. 820 µg . cm-2 h-1. So the Huoxue Zhitong gel had a good release and transdermal properties.
Acetophenones ; administration & dosage ; pharmacokinetics ; Administration, Cutaneous ; Animals ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Gels ; Mice ; Skin Absorption