CN-122005824-A - Intelligent Rosa roxburghii source delivery system and preparation method and application thereof

Abstract

The invention provides an intelligent Rosa roxburghii tratt source delivery system, a preparation method and application thereof. The system is formed by self-assembly of the Rosa roxburghii endogenous components through physical field programming induction, and simultaneously meets the requirements of (1) Cu 2+ /Mn 2+ mol ratio of 1:5.5-1:6.5 and Cu 2+ /Sr 2+ mol ratio of 1:0.45-1:0.51, (2) Zeta potential-5 to +5 mV, conductivity <10 mu S/cm, (3) release rate <10% in simulated gastric fluid and release rate >80% in simulated intestinal fluid for 2 hours, and (4) single administration MTD (methyl thiazolyl tetrazolium) is more than or equal to 5.0 g/kg based on solid matters. The system has near neutral Zeta potential and extremely low conductivity, is stable in long-term storage, can synergistically reduce serum uric acid, transaminase and blood sugar, and has kidney protection effect at the same time of efficiently reducing uric acid. The invention also provides a green preparation method of the system and application of the system in multiple fields.

Inventors

• HUANG FUYANG
• LUO JUNXUAN
• HUANG WEI

Assignees

• 沁届本草智造(广东横琴)科技有限公司

Dates

Publication Date

20260512

Application Date

20260228

Claims (14)

1. 1. The intelligent Rosa roxburghii source delivery system is characterized in that the system is formed by self-assembly of Rosa roxburghii endogenous components through physical field programming induction, and simultaneously meets the following conditions: (a) Has a characteristic chemical fingerprint that the molar ratio of copper ions (Cu 2+ ) to manganese ions (Mn 2+ ) in the system is 1:5.5 to 1:6.5, and the molar ratio of copper ions (Cu 2+ ) to strontium ions (Sr 2+ ) is 1:0.45 to 1:0.51; (b) Has a characteristic physical fingerprint that the Zeta potential of the system as a whole in an aqueous dispersion is from-5 mV to +5 mV and the electrical conductivity is less than 10 μS/cm; (c) The system has the characteristic functional fingerprint that the characteristic polyphenol active ingredient encapsulated in the system is used as a tracer, the cumulative release rate of the characteristic polyphenol active ingredient in vitro simulated gastric fluid after being incubated for 2 hours is less than 10 percent, the cumulative release rate of the characteristic polyphenol active ingredient in vitro simulated gastric fluid after being incubated for 2 hours is more than 80 percent, the pH of the characteristic polyphenol active ingredient in vitro simulated gastric fluid is 1.2, and the pH of the characteristic polyphenol active ingredient in vitro simulated gastric fluid is 6.8.
2. 2. The intelligent delivery system of Rosa roxburghii source according to claim 1, wherein the characteristic safety fingerprint is further satisfied that the maximum tolerated dose MTD of single administration in terms of solid matter is not less than 5.0 g/kg.
3. 3. The intelligent delivery system of claim 1 or 2, wherein the system comprises nanoscale liposomes formed by self-assembly of endogenous components, and a copper-manganese-strontium-polyphenol coordination structure core encapsulated inside the liposomes.
4. 4. A method of making the intelligent delivery system of a rosa roxburghii source of claim 1, comprising the steps of: (a) Providing a Rosa roxburghii material slurry; (b) Introducing the Rosa roxburghii raw material slurry into a differential pressure suspension vibration type intelligent regulation reactor, wherein the reactor is configured to establish and maintain a net driving differential pressure (delta P) by cooperatively regulating and controlling a feeding pressure (P 1 ) and a back pressure (P 2 ), and the Rosa roxburghii raw material slurry is treated for 1 to 2 times by controlling the feeding pressure P 1 to be in the range of 50 MPa to 200 MPa and controlling the net driving differential pressure delta P to be in the range of 5 MPa to 30 MPa; (c) Standing the system treated in the step (b) for 1 to 3 days at a temperature of between 0 and 4 ℃ to obtain the intelligent Rosa roxburghii source delivery system; wherein no exogenous chemical additive is introduced during the treatment of step (b).
5. 5. The method according to claim 4, wherein in step (b) the Zeta potential of the treated intermediate product immediately shown in the aqueous dispersion is in the range of-10 mV to +10 mV by controlling the net driving pressure difference Δp.
6. 6. A composition comprising the intelligent delivery system of a rosa roxburghii tratt source of any one of claims 1 to 3, and a food or pharmaceutical acceptable carrier.
7. 7. Use of a rosa roxburghii tratt-derived intelligent delivery system according to any one of claims 1 to 3 or of a composition according to claim 6 for the preparation of a product for reducing serum uric acid.
8. 8. Use of a rosa roxburghii-derived intelligent delivery system according to any of claims 1 to 3 or of a composition according to claim 6 for the preparation of a product for reducing serum transaminase.
9. 9. Use of a rosa roxburghii-derived intelligent delivery system according to any of claims 1 to 3 or of a composition according to claim 6 for the preparation of a product for protecting renal function and reducing serum creatinine.
10. 10. Use of a rosa roxburghii tratt-derived intelligent delivery system according to any one of claims 1 to 3 or the composition according to claim 6 for the preparation of a product for assisting in lowering blood sugar.
11. 11. Use of a rosa roxburghii-derived intelligent delivery system according to any of claims 1 to 3 or of a composition according to claim 6 for the preparation of a product for assisting in the reduction of serum triglycerides.
12. 12. Use of a rosa roxburghii-derived intelligent delivery system according to any of claims 1 to 3 or of a composition according to claim 6 for the preparation of a product for the synergistic improvement of hyperuricemia and liver injury.
13. 13. Use according to any one of claims 7 to 12, wherein the product comprises a pharmaceutical or health food; the product has the functions of preventing, assisting in treating or treating hyperuricemia, gout or nonalcoholic fatty liver disease.
14. 14. Use of a smart delivery system of rosa roxburghii origin as claimed in any of claims 1 to 3 or of the composition of claim 6 for the preparation of a product for regulating metabolic functions; the regulating metabolism includes regulating at least two selected from blood glucose, blood lipid, uric acid, liver function index or kidney function index.

Description

Intelligent Rosa roxburghii source delivery system and preparation method and application thereof Technical Field The invention relates to the technical fields of biological medicines, functional foods and advanced biological materials, in particular to an intelligent delivery system of a roxburgh rose source, which is derived from natural plants, has unique endogenous identification and intelligent response functions and is applied to multiple fields of regulating the metabolic function of organisms, and preventing and assisting in treating metabolic syndrome and related diseases. Background With the aging of the global population and the change of life style, the prevalence of metabolic syndrome with obesity, hyperglycemia, hypertension, dyslipidemia, hyperuricemia and the like as core components is rapidly rising, and has become a serious public health challenge. These metabolic disorders are causal to form complex network pathophysiological association, and present a great challenge to the current single-target-based chemotherapy, which often accompanies side effects such as liver and kidney function injury, and thus, long-term safe and effective comprehensive management is difficult to realize. Under the background, the development of a multi-target and high-safety comprehensive regulation scheme from plant resources with homology of medicine and food becomes an important direction. Rosa roxburghii (Rosa roxburghii Tratt.) is rich in vitamin C, superoxide dismutase (SOD), polyphenols, flavone and microelements, and has antioxidant, antiinflammatory and metabolism regulating effects. However, the natural active ingredients have the common problems of low oral bioavailability and poor stability, and the efficacy of the natural active ingredients is restricted. Existing delivery technologies rely mostly on synthetic carriers, present safety risks and do not meet the "clean tag" technology trend. A further technical challenge is that the long term physical stability of colloidal dispersions is highly dependent on the higher Zeta potential (absolute value is typically >20-30 mV) based on the general awareness of classical DLVO theory. This knowledge has largely limited the search for the construction of novel delivery systems with near neutral Zeta potential and long term stability, taking advantage of the intrinsic nature of the natural components. Thus, there is an urgent need in the art for an innovative system with high stability, intelligent delivery and multiple metabolic regulation functions, which can overcome the above-mentioned drawbacks, and which is constructed by green processes using natural components. Disclosure of Invention It should be noted that the invention is one of the series of applications of the same applicant under the inventive concept of the differential pressure suspension vibration type intelligent regulation reactor and the physical field programming method thereof submitted on the same day. The reactor establishes and maintains a net driving pressure difference (delta P) by cooperatively regulating and controlling the feeding pressure (P 1) and the back pressure (P 2), so that an energy mode programmable physical field can be generated in a processing cavity of the reactor, and the reactor is particularly suitable for inducing a complex natural system to carry out directional self-assembly. The primary aim of the invention is to provide an intelligent Rosa roxburghii source delivery system. The key technical problems are solved by 1) directly converting complex natural systems such as roxburgh rose into an intelligent delivery system with stable structure and definite function on the premise of green and no chemical addition; 2) breaking the teaching strip of 'high potential stabilization', constructing and verifying natural products based on a new stable paradigm, 3) endowing the system with the capability of accurately responding to physiological environments, realizing the efficient delivery of active ingredients, 4) systematically verifying the comprehensive regulation potential of the system on multiple metabolic disorders and the excellent safety thereof, and providing a core technology and a material foundation for developing next-generation natural source health products. In order to achieve the above object of the present invention, the following technical solutions are specifically adopted: In a first aspect, an intelligent delivery system (CRG-DDS) of a roxburgh rose source is provided, which is formed by self-assembly of endogenous components of the roxburgh rose through physical field programming induction, and simultaneously meets the following conditions: (a) Has a characteristic chemical fingerprint that the molar ratio of copper ions (Cu 2+) to manganese ions (Mn 2+) in the system is 1:5.5 to 1:6.5, and the molar ratio of copper ions (Cu 2+) to strontium ions (Sr 2+) is 1:0.45 to 1:0.51; (b) Has a characteristic physical fingerprint that the Zeta potential o