| Radiation enteritis (RE) is a common complication of abdominal and pelvic tumor patients after radiotherapy, the domestic and international data show that the diarrhea, bloody diarrhea, vomiting and other symptoms in threat to disease patient health at the same time also seriously reduce the quality of life of the patients. So they suffer physical and mental torture. Radix Scutellariae is benefit for heat clearing and detoxifyin and its effective components named baicalin (BAI) has anti bacteria, anti inflammation, heat clearing and detoxifying effect, and this coincide with the treatment of traditional Chinese medicine in the treatment of RE of the principle of detoxification, dampness, heat, treatment. However, due to the fat soluble, poor water solubility of the BAI and the conventional dosage forms used for rectal lesion site will appear poor compliance, a sense of foreign body, short retention time and other issues, resulting in the treatment unable to be completed. So the Bai of liposome thermo sensitive hydrogel (BAI-LIP-TSG) binary formulation, with liposome's lipophilic hydrophilic nature to carrier Bai, using temperature sensitive gel (TSG) can produce phase transition characteristic to improve the conventional dosage forms in rectal administration system, combination to improve the drug in the rectum for drug delivery system of biological utilization degree, in order to provide new preparation of baicalin liposome thermo sensitive gel in the practice and provide exquisite theory. Paper contents are as follows:1. This study establish a method to measure the content of BAI by HPLC method, to determine the solubility of BAI and the partition coefficient of BAI to be preformulation research, which showed that BAI was a fat water insoluble (logP-1.42) material. Make the BAI system for liposome, using the lipophilic and hydrophilic features to overcome the defects of poor solubility of BAI.2. In the preparation of the prescription and process optimization, take Bai liposomes by reverse evaporation method, making the OD value for the comprehensive evaluation index of drug loading and encapsulation rate, testing BAI liposome preparation process and recipe optimization through the central composite design, preparation of BAI liposomal zeta potential for (-45.5 ± 2.4)MV, the particle size is (159.2 ± 4.23) nm, and this condition for preparing BAI liposome stability evaluation proves good.3. Use the same method to optimize and verify the temperature sensitive gel matrix prescription. BAI in different dosage forms was investigated through the intestinal mucosa. The rectal mucosa BAI temperature sensitive gel through lipid was higher than that in other forms. Using the dialysis bag method for the determination of BAI in different preparations in vitro release, and determine the best effect of sustained release BAI-LIP-TSG.4. The evaluation of BAI-LP-TSG quality, safety, stability and retention time show that BAI-LP-TSG has good stability, non irritating, average retention time but ordinary thermosensitive hydrogel 1.09 times.This study combines baicalin liposomes and temperature sensitive gel combined binary preparation for rectal administered for the treatment of RE for the first time, which can not only delay Bai release and prolong the endorectal retention time, but so it can enable the medicine to fully contact with radioactive enteritis lesions and improve treatment effect. Moreover, due to the characteristics from the dosage form in front of the phase transition temperature as a liquid, after administration, transformation into a semi solid body, breaking through the conventional rectal administration of biological agents utilization which is low and the patients complied with the bottleneck, and good preparation stability, no irritation of the rectal mucosa. Therefore it is expected to improve rate of cure, to provide a new basis for rectum giving medicine in treating reflux esophagitis (RE). |
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