Medicine containing aspirin, its preparation method, pharmaceutical composition and application
A technology of aspirin and drugs, applied in the field of aspirin-containing drugs, and its preparation field, can solve the problems of limited clinical application of small molecule drug aspirin delivery reliability, contradiction between toxicity and transfection activity design itself, difficult connection and non-toxic degradation, etc. Achieve high reliability, improve stability, and reduce the chance of contact
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[0152] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned aspirin-containing medicine, which comprises the following steps: providing any of the above-mentioned nucleic acid nanoparticles; Loaded on nucleic acid nanoparticles to obtain aspirin-containing medicines.
[0153] When physically linked, aspirin is usually physically intercalated between the GC base pairs. When the connection is made by covalent connection, aspirin usually chemically reacts with the amino group outside the G ring to form a covalent connection. The aspirin-containing medicine prepared by the above-mentioned method can have better targeting ability after being modified by the target head, can deliver aspirin stably, and has high reliability.
[0154] In a preferred embodiment, the step of physically connecting aspirin includes: mixing and stirring aspirin, nucleic acid nanoparticles and a first solvent to obtain a premixed syste...
Embodiment 1
[0178] 1. RNA and DNA nanoparticle carriers:
[0179] (1) The base sequences of the three polynucleotides constituting the RNA nanoparticles are shown in Table 1:
[0180] Table 1:
[0181]
[0182]
[0183] (2) Three polynucleotide base sequences of DNA nanoparticles
[0184] The DNA adopts the same sequence as the RNA described above, except that T replaces U. Among them, the molecular weight of the a chain is 8802.66, the molecular weight of the b chain is 8280.33, and the molecular weight of the c chain is 9605.2.
[0185] The a, b and c chains of the above RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0186] Second, the self-assembly experimental steps:
[0187](1) Mix and dissolve RNA or DNA single-stranded a, b, c in DEPC water or TMS buffer at a molar ratio of 1:1:1;
[0188] (2) heating the mixed solution to 80°C / 95°C (wherein the RNA assembly temperature is 80°C, and the DNA assembly temperatur...
Embodiment 2
[0199] 1. 7 groups of short-sequence RNA nanoparticle carriers:
[0200] (1) The base sequences of the three polynucleotides that make up the 7 groups of RNA nanoparticles are shown in Tables 2 to 8 respectively:
[0201] Table 2: R-1
[0202]
[0203] Table 3: R-2
[0204]
[0205]
[0206] Table 4: R-3
[0207]
[0208] Table 5: R-4
[0209]
[0210] Table 6: R-5
[0211]
[0212]
[0213] Table 7: R-6
[0214]
[0215] Table 8: R-7
[0216]
[0217] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0218] Second, the self-assembly experimental steps:
[0219] (1) Mix and dissolve RNA single strands a, b, and c simultaneously in DEPC water or TMS buffer at a molar ratio of 1:1:1;
[0220] (2) heating the mixed solution to 80°C, keeping the temperature for 5min and then slowly cooling to room temperature at a rate of 2°C / min;
[0221]...
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