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Preparation of Ivermectin and Terbinafine Cyclodextrin Inclusion Complex

Author: ZhangHaiLiang
Tutor: LiYinQian
School: Northwest University of Science and Technology
Course: Basic Veterinary Science
Keywords: Ivermectin Terbinafine Cyclodextrin Inclusion Complex
CLC: TQ461
Type: Master's thesis
Year: 2009
Downloads: 92
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Abstract


The ivermectin (Ivermectin, IVM) is good to get rid of the the livestock digestive tract nematodes and ectoparasites drugs, special Terbinafine (Terbinafine TBF) better antifungal drugs effective in the treatment of livestock, combined internal and external parasites and fungi mixed infections. Due to both poor water solubility, bioavailability, limiting their clinical application. Cyclodextrin as a new water-soluble additives, commonly used to increase the solubility and bioavailability of the guest molecules. This article discusses the process of ivermectin and terbinafine made of cyclodextrin inclusion complexes, identification and quality standard system. Test content and results are as follows. 1.IVM and TBF cyclodextrin inclusion complexes by comparing the grinding method, ultrasonic method and saturated aqueous solution method the package combined effect of the preparation method to determine the polishing prepared IVM inclusion ultrasound prepared TBF inclusion complex. By orthogonal test and variance analysis, optimization of the inclusion complex preparation programs: IVM main object of the mass ratio of 3:1, inclusion temperature 55 ℃, inclusion time of 2 h; TBF main object of the mass ratio of 1 : 1, inclusion temperature 25 ° C, the inclusion time 1 h. The results show that the inclusion complex prepared by the above conditions are good solubility and stability. Cyclodextrin inclusion 2.IVM and TBF identification and determination in order to further examine the effect of the inclusion complex internal structure and the inclusion by the phase solubility method, thin layer chromatography, UV spectrophotometry, infrared analysis to identify inclusion in the main guest molecules to form inclusion complexes of 1:1. By UV spectrophotometer inclusion content of the standard curve equation, IVM A = 0.0361C-0.0116 (R2 = 0.9998, n = 6), the TBF as A = 0.0226-0.0171-C (R2 = 0.9996, n = 6) show that the method is stable and accurate. Cyclodextrin inclusion security and stability of 3.IVM-TBF stability tests show that the inclusion complex heat, moisture, light stability. The combination of the two drugs inclusion compatibility reaction. Karber method to simplify the determination of ivermectin - terbinafine cyclodextrin inclusion (ivermectin) mice were injected subcutaneously with LD50 was 33.98 mg / kg. The rabbit quadriceps stimulation test showed that ivermectin - terbinafine cyclodextrin inclusion complex may be administered. The 4.IVM-TBF cyclodextrin inclusion complex clinical effect observed through clinical trials, the IVM-TBF cyclodextrin inclusion complex of goat gastrointestinal nematode eggs negative rate of 90.91%, the egg reduction rate of 98.07%, kill on the sheep lice drive the total effective rate was 93.75%, the hair ringworm total effective rate was 100%.

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