Propofol flexible nano-liposome patch and application thereof
A flexible and nano-liposome technology of propofol, applied in the field of medicine, can solve the problems of strengthening, unsatisfactory effect, slow conditioning effect, etc., achieves enhanced curative effect, avoids liver first-pass effect and gastrointestinal inactivation, and has good effect. Effect
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Embodiment 1
[0077] Embodiment 1, the preparation embodiment of propofol flexible nano liposome patch
[0078] The invention screens and verifies the dosage range and preparation process of various excipients in the formulation of the propofol-free flexible nano liposome patch. The present invention is described in detail below in conjunction with embodiment, but not limited to following example.
[0079] One, the preparation example of propofol flexible nano liposome
[0080] (1) Propofol flexible nanoliposomes prepared with different ratios of phospholipids
[0081] Example 1.1 Prescription:
[0082]
[0083] Preparation:
[0084] Step 1: Dissolve 1g of propofol, 21g of dipalmitoylphosphatidylcholine, 7g of dipalmitoylphosphatidylglycerol and 5g of cholesterol in absolute ethanol, stir to dissolve, and then depressurize the resulting solution in a water bath at 60°C Remove the organic solvent to prepare a uniform liposome film containing propofol;
[0085]Step 2: Add 20g of sodiu...
Embodiment 2
[0130] Embodiment 2, the preparation embodiment of propofol flexible nano-liposome patch
[0131] (1) Propofol flexible nano-lipid body temperature-sensitive gel patch
[0132] Example 2.1 Prescription:
[0133]
[0134] Preparation:
[0135] Step 1: Dissolve 1g of propofol, 21g of dipalmitoylphosphatidylcholine, 7g of dipalmitoylphosphatidylglycerol and 5g of cholesterol in absolute ethanol, stir to dissolve, and then depressurize the resulting solution in a water bath at 60°C Remove the organic solvent to prepare a uniform liposome film containing propofol;
[0136] Step 2: Add 20g of sodium cholate into water to fully dissolve. After the dissolution is complete, slowly add it dropwise to the liposome film obtained in step 1 under the protection of nitrogen, and disperse at a high speed for 5 minutes under the condition of 10000r / min to elute the phospholipid film And fully swell and hydrate, then adjust the pH to 7.0 with 0.1mol / L NaOH or HCL, and then carry out extru...
Embodiment 3
[0175] Embodiment 3, the quality research of propofol flexible nano-liposome patch
[0176] (1) Particle size and potential detection of propofol flexible nanoliposomes
[0177] A dynamic light scintillation particle size / potential meter was used to detect the particle size and potential of the propofol flexible nanoliposomes prepared in the above three examples, and the results are shown in Table 1.
[0178] Table 1 The particle size of propofol flexible nanoliposomes
[0179]
[0180] *PdI: Polydispersion index polydispersity index (used to measure the particle size distribution range)
[0181] It can be seen from Table 1 that the particle sizes obtained by the above three prescriptions and preparation processes all meet the requirements, and the particle size distribution diagrams are shown in figure 2 , 3 , 4.
[0182] The present invention continued to detect the potential of Example 2.4. The test results are attached Figure 5 As shown, the average value of its...
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