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Study on the Nanosuspensions of a Long-acting Derivative of Riboflavin

Author: LiGuangLong
Tutor: JinYiGuang；DuLiNa
School: Henan University
Course: Pharmacy
Keywords: Nanotechnology Nano- suspensions Long riboflavin Riboflavin Stability
CLC: R94
Type: Master's thesis
Year: 2009
Downloads: 323
Quote: 1
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Abstract

Currently, more than 40% of the drug candidate exists the problem of poor solubility, poor solubility of the drug has also caused lower bioavailability, which often resulted in a variety of excellent development of the drug candidate is discarded. Insoluble drug delivery problems become pharmacy research a huge challenge. To solve the above problem, paper Select riboflavin long (long-acting derivative of riboflavine) as a model drug of nano-suspension (nanosuspensions) of injection, long-term physical and chemical properties of riboflavin is special, a typical The characteristics of poorly soluble drugs, specifically as follows: 1. preformulation studies: the use of UV spectrophotometry long riboflavin, examine its solubility and partition coefficient, the results indicate that long-term water partition coefficient representing riboflavin molecule large, is a lipophilic side amphiphilic molecule, suitable for preparing a water-based nano-suspension. 2 prescription screening and process optimization: After formulation and preparation process after the screening of the preparation process was improved by solvent selected long-acting injection riboflavin prepared nano suspension. Long-term riboflavin obtained nanoparticles were nanotube structure, particle size of about 280nm, Zeta potential-24.5mv, frozen and freeze-dried nanoparticles will not destroy the structure, and lyophilized to give long-lasting riboflavin nano powders, injectable prior to the aqueous dispersion to obtain a uniform and stable nano-suspension. 3 assay development: to establish a long-term, respectively, and riboflavin riboflavin vivo HPLC analysis method, method is sensitive and accurate. Long-term in vitro riboflavin HPLC conditions: mobile phase was methanol - water (87:13, v / v), flow rate 1.0ml/min, t _R = 6.66min riboflavin in vitro HPLC conditions as: methanol -1.0% HAc (45:55, v / v), detection wavelength 267 nm; acting as riboflavin body HPLC conditions: methanol - water (84:16, v / v), flow rate 1.0 ml / min detection wavelength 269 nm; riboflavin vitro HPLC conditions: methanol -1.0% HAc (40:60, v / v), detection wavelength 267 nm. 4 Properties: high-speed centrifugation does not affect the size of nanoparticles, nano long riboflavin suspension susceptible to a particle size of buffer salts, but its size does not affect the animal plasma. Suspension was sterilized by boiling a slight impact on the stability, autoclaves would undermine the stability of particle structure and affect the preparation, lyophilized powder Co ^{60 Irradiation does not affect the stability of the preparation. Acting in a neutral environment nanosuspension riboflavin (pH7.4) stable, acidic and alkaline conditions susceptible to degradation, the main degradation product of riboflavin. Long-term suspension of riboflavin in various biological systems nanometer (enzymes, plasma) are degraded in the degradation rate is greater than the buffer salt system, healthy human plasma degradation t _1/2 is 286.17h, to provide a basis for long-term in vivo release. 5 Stability: The long-term suspension of riboflavin nano influencing factors were investigated, lyophilized powder type is selected as the final preparations to determine packaging brown vial rubber stopper sealed aluminum cap for the current acceleration and temperature experiments show that long-term stay like riboflavin nano powder has good stability. 6 Pharmacodynamics: Pharmacodynamics established two SD rats, methylamine methotrexate (MTX) model mainly on long-term preventive effect of riboflavin results showed that no significant stress response in rats administered For high dose MTX injection caused a significant preventive effect of angular cheilitis; prepared animal feed and build without riboflavin riboflavin deficiency model to study long-term therapeutic effect of riboflavin nano-suspensions, the results show that the long-term Riboflavin nano suspension has obvious long-lasting effect, a single dose may be for 30 days or more, the monitoring of treatment group were better than riboflavin deficient group, has a good therapeutic effect. In this paper a new formulation techniques, successfully prepared with good physical and chemical stability, a high concentration of riboflavin nm long suspension, which has good in vitro degradation, may be lyophilized, and can be well dispersed with water, solutions having a special properties of the pharmaceutical preparations using conventional problems.}

Study on the Nanosuspensions of a Long-acting Derivative of Riboflavin

Abstract

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