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Study of a Gelrite/Alginate-based in Situ Gelling Ophthalmic Delivery System for Matrine

Author: LiuYueJiang
Tutor: WuChunJie
School: Chengdu University of Traditional Chinese Medicine
Course: Pharmacy
Keywords: Matrine Ocular drug delivery system Quality Control In vitro release Chorioallantoic membrane Penetration enhancers Bioavailability Experimental ophthalmia
CLC: R283
Type: Master's thesis
Year: 2010
Downloads: 118
Quote: 0
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Abstract


The ideal ocular administration system, it should be administered in the form of eyedrops, do not cause blurred vision or produce eye irritation; having a suitable viscosity can resist dilution of the tear, and not after the administration of rapid loss; have longer ocular residence time, can improve the bioavailability of the drug. This article selected ion-sensitive polymer polysaccharides gellan gum (Gelrite) as a gel matrix, in situ, and sodium alginate (Alginate) as a tackifier were prepared matrine ophthalmic gel. Screening prescription single factor, viscosity and gelling capacity for the evaluation of indicators initially identified prescription. Investigated the impact of different temperature, ionic strength and shear rate and rheological properties of the gel the viscosity was measured with a rotary viscometer. Establish a gel content determination method for the determination of the gel in vitro release, combined with the isolated rabbit corneal penetration experiments to study the law of preparations in vitro release and whether sustained release characteristics. Single and multiple dose experiments, evaluation Matrine eye situ gel rabbit eye irritation. The tear elimination kinetics experiments investigated whether matrine gel drugs eye residence time can be extended to improve its bioavailability. The chorioallantoic membrane irritant irritant experimental quantitative evaluation gel in vitro rabbit corneal penetration penetration enhancers screening tests, combined with the chick embryo. Centrifugal, high temperature, low temperature, light and acceleration experiments examine preparations traits, ph value and matrine content changes, to evaluate the stability of the drug. Rabbits experimental the ophthalmia model, examine the preliminary Pharmacodynamic of matrine situ gel. Screening to determine the best prescription for: Matrine 1% mannitol 5%, 0.2% gellan gum and sodium alginate 0.6%. Gel viscosity decreased with increasing shear rate, showing pseudoplastic fluid nature. With the increase of the ion concentration, the viscosity of the gel first rose and then dropped, the appropriate viscosity gel, matrine situ gel formation in a physiological environment. Matrine detectable concentration in the range of 10 ~ 60μg/ml inside a good relationship. High, medium, low concentrations average recovery was 97.4%, RSD 1.7% day RSD was 1.29%. Three batches the matrine situ gel content were 98.2%, 99.4%, and 98.5% of the labeled amount. Matrine eye drops compared of matrine gel in the rabbit cornea extend the residence time, have a good slow-release effect, non-irritating to rabbit eyes. Situ gel chorioallantoic membrane irritating, and 1% propylene glycol is ideal penetration enhancers. The preparation of centrifugal and light stable, high temperature instability, it is recommended to save in a cool place. Rabbit ocular inflammation symptoms of matrine situ gel caused by pepper tincture was inhibited with the saline group, a significant difference (P lt; 0.05), the efficacy sustained up to 48h. The reasonable formulation of design, the process is simple, sensitive and accurate method of quality control, good stability; pharmacological experiments show that, in situ gel can extend the drug in rabbit eyes residence time, improve the bioavailability of matrine and rabbits experiment ophthalmia has a good effect; rabbit eye irritant experimental and chorioallantoic membrane experimental results show that matrine situ gel is safe.

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CLC: > Medicine, health > Chinese Medicine > Of Pharmacy > Chinese medicine processing,preparation
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