The gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulations

Abstract The objective of the study was to evaluate the gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulation. Mucilage was extracted from the fruits of Dillenia indica using established methods and characterized by rheology and swelling. Emulsion (F1) was prepared using the continental emulsification method. Gelling agents (2 %w /v) were prepared by dispersing in distilled water with constant stirring at a moderate speed using a magnetic stirrer. F1 was added to the gel (0-75 %w /w) to obtain emulgel formulations and evaluated using viscosity, globule size, pH, release profiles and kinetic modeling. Data were expressed as mean ± SD, and similarity factor (f2) was used to compare all formulations. Formulation viscosity was significantly higher with carbopol than with Dillenia; globule sizes increased with concentration of gelling agents, and pH reduced as the concentration of Dillenia increased. All formulations showed controlled release properties with t80 ranging between 114 and 660 min. The release was governed by Korsmeyer-Peppas model. Formulation F5 prepared with 50 % Dillenia showed highest similarity to F4 prepared with 75 %w /w carbopol. Dillenia indica demonstrated acceptable gelling properties comparable with that of carbopol and could be improved for use in emulgel formulations.

Formulation development and pharmacokinetic studies of long acting in situ depot injection of risperidone

Abstract Risperidone is an atypical antipsychotic drug widely prescribed all over the world due to its clinical advantages. The currently available long acting marketed depot formulation of risperidone is a microsphere based preparation using poly-[lactide-co-glycolide] (PLGA) as drug release barrier. It is however, a cold chain product due to thermal instability of PLGA at room temperature. After beginning the depot injection therapy it is administered every two weeks but associated with another drawback of about 3 weeks lag time due to which its tablets are also administered for three weeks so as to attain and maintain therapeutic drug concentration in the body. The present work attempts to develop a long acting depot delivery system of risperidone for once a month administration based on the combination of sucrose acetate isobutyrate and polycaprolactone dissolved in benzyl benzoate to provide an effective drug release barrier for one month without any lag time and which can be stored at room temperature precluding the requirement of cold supply chain. The developed depot formulation showed a sustained in vitro drug release profile with 88.95% cumulative drug release in 30 days with little burst release. The in vivo pharmacokinetic studies of the developed formulation conducted on rats showed attainment of mean peak plasma drug concentration of 459.7 ng/mL in 3 days with a mean residence time of 31.2 days, terminal half-life of 20.6 days, terminal elimination rate constant of 0.0336 per day, and a good in vitro- in vivo correlation.

Comparative study of oral ivermectin, topical permethrin and benzyl benzoate in the treatment of scabies

Background: Efficacy of these modalities as shown by various investigations are inconsistent and ambiguous. Thus, evidence based effective treatment option is warranted. Aim of the study was to compare the efficacy of oral ivermectin, topical permethrin and benzyl benzoate in the treatment of uncomplicated scabies.Methods: Patients with confirmed diagnosis of scabies were included in this study. One hundred and ninety-five subjects were included in this investigation as per inclusion and exclusion criteria laid down. Equal numbers of patients were randomly allocated to one of the three treatment groups. Efficacy of three groups [oral ivermectin (Group A), topical permethrin (Group B) and benzyl benzoate (Group C)] of drugs was compared in terms of improvement in clinical grading of disease (%) and improvement in clinical grading of pruritus (%) during follow up visits.Results: Those subjects receiving topical permethrin, at 1st follow up 56.9% showed cure rate which increased to 89.2% at 2nd follow up with respect to clinical improvement in pruritus. Maximum relief in severity of pruritus at the end of 6th week was reported by 58(89.2%) patients receiving group B treatment modality followed by 52 patients (80%) in arm A. Regarding efficacy of three treatment groups in terms of improvement in severity of lesion at the end of 6 weeks, maximum number of patients 57(87.7%), receiving group B treatment reported improvement which is better than other two treatment groups.Conclusions: maximum number of patients receiving topical Permethrin treatment reported improvement better than other Oral Ivermectin therapy and topical benzyl benzoate. Oral ivermectin may serve a good alternative for managing scabies under certain conditions like poor compliance to topical scabicides.

Volatile constituents of Atalantia roxburghiana Hook. f., Tetradium trichotorum Lour. and Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) from Vietnam / Compuestos volátiles de Atalantia roxburghiana Hook. f., Tetradium trichotorum Lour. y Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) provenientes de Vietnam

The chemical constituents of essential oils obtained by hydrodistillation of the leaves of Atalantia roxburghiana Hook. f. and Tetradium trichotomum Lour., as well as the leaves and fruits of Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) are being reported. The essential oils were analysed by using gas chromatography (GC) and gas chromatography coupled with mass spectrometry (GC-MS). Sabinene (36.9%) was the most singly abundant compound in the leaf of A. roxburghiana. The major constituents present in the leaf oil of T. trichotorum were (E)-ß-ocimene (24.8%), α-pinene (10.4%), (Z)-ß-ocimene (9.4%) and ß-caryophyllene (8.0%). On the other hand, while α-pinene (17.5%), ß-caryophyllene (15.5%) and caryophyllene oxide (10.6%) occurred in higher proportion in the leaf of M. oligophlebia, the fruit oil was dominated by benzyl benzoate (16.8%), (E, E)-farnesol (8.3%) and ß-caryophyllene (6.0%).

Se muestran los constituyentes químicos de los aceites esenciales obtenidos, por hidrodestilación, de las hojas de Atalantia roxburghiana Hook. f. y de Tetradium trichotomum Lour., así como de las hojas y frutos de Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae). Los aceites esenciales fueron analizados por Cromatografía de Gases (CG) y por Cromatografía de Gases acoplada a Espectrometría de Masas (CG-EM). El compuesto más abundante en las hojas de A. roxburghiana es el sabineno (36.9%); mientras que los mayoritarios en el aceite de las hojas de T. trichotomum fueron (E)-ß-ocimeno (24.8%), α-pineno (10.4%), (Z)-ß-ocimeno (9.4%) y ß- cariofileno (8.0%). En las hojas de M. oligophlebia los compuestos más abundantes fueron α-pineno (17.5%), ß-cariofileno (15.5%) y óxido de cariofileno (10.6%); sin embargo, en el aceite obtenido del fruto fueron benzoato de bencilo (16.8%), (E, E)-farnesol (8.3%) y ß- cariofileno (6.0%).

Simultaneous Determination of Six Active Constituents in Shexiang Baoxin Pills by GC-MS / 中国药师

Objective: To develop a GC-MS method for the simultaneous determination of six active constituents ( borneol, isoborneol, cinnamaldehyde, cinnamic acid, muscone and benzyl benzoate) in Shexiang Baoxin pills. Methods: A gas chromatogra-phy-mass spectrography (GC-MS) method was adopted using a DB-5 capillary column (30 m × 0. 25 mm,0. 1 μm). The column tem-perature was raised as the following program:the initial temperature was 70℃, maintained for 2 min, raised the temperature (5℃· min-1) to 150℃, maintained for 4 min and then raised the temperature (20℃·min-1) to 260℃, and maintained for 3 min. The range of mass-to-electric charge ratio was 10 to 425. Results:The calibration curves of borneol, isoborneol, cinnamaldehyde, cinnam-ic acid, muscone and benzyl benzoate were linear within the range of 0.022-22.000 μg·ml-1(r=0.999 6),0.024-24.000 μg· ml-1(r=0.999 6),0.028-28.000μg·ml-1(r=0.999 8),0.034-34.000μg·ml-1(r=0.999 6),0.040-40.000μg·ml-1(r=0.999 7) and 0.050-50. 000 μg·ml-1 (r =0.999 9), respectively. The average recovery was 97.20%, 97.40%, 97.53%, 99. 60%, 98. 78% and 98. 27% and RSD was 0. 89%, 1. 18%, 1. 52%, 1. 49%, 0. 79% and 1. 74%(n=6), respectively. Con-clusion:The method is accurate, suitable, convenient and reproducible, which can be used for the quality control of multi components in Shexiang Baoxin pills.

Chemical constituents from the leaves of Broussonetia papyrifera / 药学学报

To separate and identify the chemical constituents from the leaves of Broussonetia papyrifera (Linn.) Vent, various columns including Diaion HP-20, Toyopearl HW-40C, Sephadex LH-20, silica gel were employed for the isolation and purification of compounds from the leaves of B.papyrifera. The structures of the compounds were elucidated by their physiochemical characteristics and spectral data. Nineteen compounds were isolated from the leaves of B.papyrifera and their structures were identified as apigenin (1), apigenin-7-O-β-D-glucopyranoside (2), chrysoerid-7-O-β-D-glucopyranoside (3), apigenin-7-O-β-D-glucopyranuronide (4), vitexin-7-O-β-D-glucopyranoside (5), luteolin (6), 5,7,4′-trihydroxyl-6-C-[a-L-rhamnopyranosyl(1→2)]-β-D-glucopyranosyl flavone (7), 5,7,4′-trihydroxyl-8-C-[a-L-rhamnopyranosyl(1→2)]-β-D-glucopyranosyl flavone (8), saponaretin (9), vitexin (10), benzyl benzoate-2,6-di-O-β-D-glucopyranoside (11), (2R,3R,5R,6S,9R)-3-hydroxy-5,6-epoxy-β-ionol-2-O-β-D-glucopyranoside (12), (2R,3R,5R,6S,9R)-3-hydroxyl-5,6-epoxy-acetyl-β-ionol-2-O-β-D-glucopyranoside (13), ficustriol (14), (6S,9S)-roseoside (15), 3β-hydroxy-5α,6α-epoxy-β-ionone-2α-O-β-D-glucopyranoside (16), icariside B1 (17), sammangaoside A (18), 3-hydroxy-5α,6α-epoxy-β-ionone (19). Compounds 11, 12 and 13 are new compounds, the others are isolated from this genus Broussonetia for the first time.

A fatal case of benzyl benzoate poisoning.

We present a case of benzyl benzoate ingestion in a 38 years old Thai woman whose presenting symptom was coma and severe metabolic acidosis. The amount ingested was 360ml of 25%W/V benzyl benzoate. It did not contain any alcohol or acid substance. Standard textbooks and other reference books do not mention severe symptoms caused by ingestion of given this substance and gastric lavage is the only recommendation. Should there be another method used to induce elimination of benzyl benzoate-hemodialysis?