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Objective: To optimize preparation of mitochondrial targeting hyperoside liposomes (DLD/Hyp-Lip), and study its stability in fetal bovine serum, in vitro release behavior and mitochondrial targeting. Methods: DLD/Hyp-lip was prepared by film dispersion method. Single factor experiment was carried out with entrapment efficiency and drug loading as indexes to investigate the effects of the ratio of phospholipids to hyperoside (Hyp) and DSPE-PEG (distearoyl phosphoethanolamine-polyethylene glycol) to DLD on DLD/Hyp-Lip. The formulation of DLD/Hyp-Lip was further optimized by central composite design response surface methodology. The appearance, size and potential of liposomes were observed by transmission electron microscope and particle size analyzer. The stability and drug release rate of liposomes in fetal bovine serum were evaluated by serum stability test and in vitro drug release test. The drug delivery system was evaluated by mitochondrial targeting. Results: The optimal formula of DLD/ Hyp-Lip was as follows: the ratio of total phospholipids to hyperoside was 12.50:1, the ratio of total phospholipids to cholesterol was 6.00:1, and the dosage ratio of DSPE-PEG to DLD was 3:5, the encapsulation efficiency was (95.57 ± 0.56) %, the drug loading was (8.55 ± 0.57) %. The prepared liposomes had good appearance, the particle size of the lip was (124.9 ± 3.4) nm, and the potential was (-6.2 ± 1.9) mV. It was stable in fetal bovine serum and accumulated in vitro release medium for 24 h. Mitochondrial targeting experiments showed that DLD/Hyp-Lip could promote the accumulation of drugs in the mitochondria. Conclusion: This method is simple and convenient, and can accurately and effectively optimize the preparation process of DLD/Hyp-Lip. The prepared DLD/Hyp-Lip has high encapsulation efficiency, small particle size, uniform distribution and good sustained-release effect, which lays the foundation for further in vivo research of DLD/Hyp-Lip. DLD/Hyp-Lip with hyperoside has good mitochondrial targeting of liver cancer cells and is a potentially efficient mitochondrial targeted drug delivery system for liver cancer cells.
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In order to increase the solubility of essential oil in compound licorice microemulsion and improve the efficacy of the decoction for treating chronic eczema, this experiment intends to prepare the decoction into microemulsion. The essential oil was used as the oil phase of the microemulsion and the extract was used as the water phase. Then the microemulsion area and maximum ratio of water capacity was obtained by plotting pseudo-ternary phase diagram, to determine the appropriate types of surfactant and cosurfactant, and Km value-the mass ratio between surfactant and cosurfactant. With particle size and skin retention of active ingredients as the index, microemulsion prescription was optimized by D-optimal design method, to investigate the release behavior of the optimized prescription. The results showed that the microemulsion was optimal with tween-80 as the surfactant and anhydrous ethanol as the cosurfactant. When the Km value was 1, the area of the microemulsion region was largest while when the concentration of extract was 0.5 g·mL⁻¹, it had lowest effect on the particle size distribution of microemulsion. The final optimized formulation was as follows: 9.4% tween-80, 9.4% anhydrous ethanol, 1.0% peppermint oil and 80.2% 0.5 g·mL⁻¹ extract. The microemulsion prepared under these conditions had a small viscosity, good stability and high skin retention of drug; in vitro release experiment showed that microemulsion had a sustained-release effect on glycyrrhizic acid and liquiritin, basically achieving the expected purpose of the project.
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Objective To optimize the best prescription of Yuanhu Zhitong Oral Disintegrating Tablets (YZODT). Methods Using the single factor test, the prescription of the tablets was optimized by central composite design-response surface methodology (CCD-RSM) with the tablet wetting time and the disintegration time limit as evaluation index, so as to determine the best preparation process. Results The dosages of the optimized prescription of MCC, L-HPC, and PVPP were 30%, 15%, and 5%, respectively. The average disintegration time of the optimized YZODT was 42.89 s, and the deviation from the predicted value was 3.27%. Conclusion The optimized YZODT has the advantages of fast disintegration, moderate hardness, convenient use, and simple process.
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OBJECTIVE: To strengthen pharmacist intervention in prescribing behavior of doctors, so as to further standardize prescribing behavior.METHODS: Through the review of the advantages and disadvantages of the relevant laws, education training and assessment system for prescription intervention in the USA, a deep analysis was made in combination with the Chinese system and the characteristics of the medical staff.RESULTS: A new clinical pathway was introduced to standardize the intervention of doctors′ prescriptions, so as to improve the level of diagnosis and treatment and the environment for medical treatment in China.CONCLUSION: Improving pharmacists′ professional accomplishment and introducing Internet model and intelligent medical technology can improve the linkage among clinical, community medical institutions and social pharmacies, and also enhance the feasibility and reliability of Internet prescription drug purchase intervention. Promote the closed-loop connection and continuous upgrading of the pharmaceutical industry chain, gradually realize the standardization model of diagnosis and treatment, and then promote the results of the overall medical level.
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@#To prepare a budesonide rectal thermogel. The gel solution was prepared by cold method, and the gelation temperature of the gel solution was determined by reverse tube method. The amount of poloxamer 407(P407), poloxamer 188(P188)and hydroxy propyl methyl cellulose(HPMC)was optimized by central composite design/response surface method. The in vivo gelation character was investigated after rectal administration of the budesonide thermogel into the rat, and the in vitro drug release from the gel was examined by the Franz diffusion cell method. Finally, the optimal formulation includes 0. 002% budesonide, 0. 93% HPMC, 2. 00% P188, and 18. 31% P407. It is preferable to obtain the appropriate formulation for budesonide rectal in situ thermogel, which can achieve wide distribution and adhesion to the rectum, as well as long-term drug release.
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Objective To investigate the effect of the optimal prescription of huiru yizeng on rats with hyperplasia of mammary gland and hyperprolactinemia. Methods Fifty-six female Wistar rats were randomly divided into 7 groups (n=8), including normal control group, model control group, sodium chloride group, bromocriptin group, rupi sanjie group, the original prescription group and optimizing prescription group. Rat model of mammary gland hyperplasia with hyperprolactinemia was replicated in 6 groups but not the normal control group. The successfully established experimental rats were given corresponding drugs by intragastric gavage. After 30 days, the levels of the estradiol, progesterone, and prolactin were detected, and the pathomrphology of glandular tissue was observed. Results Prolactin levels of model control group, the original prescription group and optimize prescription group were (69.47 ±6.08), (53.13 ±10.59), and (28.41 ±6.37) pg·mL-1, respectively . Compared with that in the model control group, the contents of prolactin in both the optimal prescription group and the original prescription group were reduced, but the optimal prescription group was better (P<0. 01). In the original prescription group, the lobules of mammary gland showed a few of hyperplasia, the individual alveoli and duct showed a slight hyperplasia, and a small amount of secretions was found in the duct. The degree of the hyperplasia was alleviated in the optimal prescription group similar to that observed in the normal control group, which showed that there was no hyperplasia in the lobules of mammary gland or no secretions in the duct. Conclusion The therapeutic effects of the optimal prescription are much better than the original prescription, which can effectively lower the level of prolactin, adjust the balance among the prolactin , estrogen and progesterone, and alleviate the pathological hyperplasia of mammary glands in the model rats.
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Objective To optimize the prescription of preparation technology of Xiaoer Qingfei Dispersible Tablets. Methods The filler, disintegrant, adhesive, lubricant, and drug loading were screened by single factor tests. The combined application proportion of three disintegrating agents, PVPP, CMS-Na, and L-HPC, were optimized by orthogonal test. Results The best prescription of preparation technology of dispersible tablets:microcrystalline cellulose as filler;silica gel powder as lubricant;75%alcohol as the adhesive;PVPP, L-HPC, and CMS-Na as combined disintegrants (L-HPC∶PVPP∶CMS-Na=4∶3∶6). The disintegration time of prepared dispersible tablets was less than 3 minutes, and all through the No.2 sieve. Dispersible uniformity was in accordance with the provisions. Conclusion Xiaoer Qingfei Dispersible Tablets prepared by the optimized preparation process are stable and feasible, and suitable for clinical application.
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OBJECTIVE: To optimize the formulation of aspirin ointment. METHODS: With cumulative permeation quantity within 6 h and shin irritation as indexes, the method of central composite design was used to optimize the formulation of aspirin ointment, taking the most important three ingredients including sodium lauryl sulfale(X1), sodium citrate (X2) and triethanolamine (X3) as the study subjects. RESULTS: The optimized formulation of aspirin ointment was composed of 1.41% sodium lauryl sulfate, 3.5% sodium citrate and 3.0% triethanolamine. Three batches of aspirin ointment were prepared using the optimized formulation, for which the average cumulative permeation quantity within 6 h was 990.18 μg · cm-2, and no obvious shin irritation was observed. CONCLUSION: Central composite design is successfully used lo optimize the formulation of aspirin ointment.