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Long-acting slow-release pharmaceutical preparation and preparation method thereof

A slow-release drug and long-acting technology, which is applied in drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of inconvenient clinical use and poor patient compliance

Active Publication Date: 2017-09-29
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For example, Risperidal Consta (Hengde), a marketed long-acting antipsychotic developed based on the technology disclosed in patent CN1137756, uses PLGA with a molecular weight of about 150 kDa as the carrier and risperidone as the API. The release of the drug, followed by a drug release stagnation period of about 3 weeks, so patients still need to rely on oral administration of tablets within 3 weeks after injection of the microspheres to achieve the therapeutic effect, which is inconvenient for clinical use and poor patient compliance

Method used

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  • Long-acting slow-release pharmaceutical preparation and preparation method thereof
  • Long-acting slow-release pharmaceutical preparation and preparation method thereof
  • Long-acting slow-release pharmaceutical preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] (1) Dissolve 7.5g PLGA (20000Da, 0.22dL / g, lactide / glycolide=100 / 0, COOH, COOH represents the terminal carboxyl group, the same below) in 30mL of dichloromethane, and then 2.5g of entecavir Add to the PLGA solution to dissolve to obtain the inner oil phase;

[0065] (2) Dissolving polyvinyl alcohol in purified water to a concentration of 1% and a volume of 2.4 L, then cooling to 4-8°C to obtain an external aqueous phase;

[0066] (3) Inject the internal oil phase obtained in step (1) into the external water phase of step (2) through a membrane emulsifier (average pore size is about 50 μm) to form an emulsion, then stir for 10 hours to harden the particles, collect the particles by filtration, and obtain ultra-pure Washing with water and freeze-drying for 50 hours gave long-acting slow-release entecavir microspheres with a drug loading rate of 22.59% and a geometric particle size of 28-105 μm.

[0067] The obtained microspheres were tested for their drug loading rate (H...

Embodiment 2

[0069] (1) Dissolve 7g of PLGA (23000Da, 0.27dL / g, 90 / 10, COOH) in 31.5mL of dichloromethane, then add 3g of anastrozole into the PLGA solution to dissolve to obtain an internal oil phase;

[0070] (2) dissolving polyvinyl alcohol in purified water to a concentration of 1% and a volume of 2.5 L, then cooling to 4-8°C to obtain an external aqueous phase;

[0071] (3) Mix the internal oil phase obtained in step (1) with the external water phase of step (2) to form an emulsion through a static mixer (L / D=30-50), then stir for 10 hours to harden the particles, collect the particles by filtration, Washing with ultrapure water, freeze-drying for 50 hours, to obtain long-acting sustained-release anastrozole microspheres with a drug loading rate of 27.11% and a geometric particle size of 32-110 μm.

Embodiment 3

[0073] (1) Dissolve 6.5g of PLGA (22000Da, 0.25dL / g, 88 / 12, COOH) in 42mL of dichloromethane, then add 3.5g of paliperidone into the PLGA solution and dissolve to obtain an internal oil phase;

[0074] (2) Dissolving polyvinyl alcohol in purified water to a concentration of 1.5% and a volume of 3.4 L, and then cooling to 4-8°C to obtain an external aqueous phase;

[0075] (3) Mix the internal oil phase (peristaltic pump 70rpm) obtained in step (1) with the external water phase (screw pump 4m / s) obtained in step (2) to form an emulsion through a pipeline homogenizer, and then continue to stir for 10 hours to make the particles After hardening, the microparticles were collected by filtration, washed with ultrapure water, and freeze-dried for 50 hours to obtain long-acting sustained-release paliperidone microspheres with a drug loading rate of 32.08% and a geometric particle size of 25-95 μm.

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Abstract

The invention discloses a long-acting slow-release pharmaceutical preparation. The pharmaceutical preparation contains the following components in percentage by weight: 25%-60% of a water-insoluble or sparingly-soluble drug and 40%-75% of a high-molecular polymer. After the pharmaceutical preparation is subjected to one time of intramuscular injection administration, the rate of a maximum plasma concentration to a minimum plasma concentration in a main release period is less than 5; the slope of a linear trend line of a cumulative release curve is less than 8 under an in-vitro simulated release condition; the daily release amount is less than 8.5%; and the simulated release condition is a buffer solution with the temperature of 37+ / -0.5 DEG C and the pH of 6.8-8.4. The prepared long-acting slow-release pharmaceutical preparation has the beneficial effects that an obvious release delay period or a burst release phenomenon are avoided after the administration, the steady state plasma concentration can be rapidly achieved, the plasma concentration with a relatively small fluctuation range can be maintained in several weeks or longer through once administration, and the pharmaceutical preparation can take effect rapidly and has good compliance with a patient.

Description

technical field [0001] The invention belongs to the field of long-acting sustained-release pharmaceutical preparations, and in particular relates to a long-acting sustained-release pharmaceutical preparation with fast onset of action, small day-to-day release rate differences, and small blood drug concentration fluctuations and a preparation method thereof. Background technique [0002] In the process of continuous constant-rate administration (such as intravenous infusion) or fractional constant-dose administration of the drug, the blood drug concentration will gradually increase, and a stable and effective blood drug concentration can be reached after 4 to 5 half-lives. At this time, the drug is absorbed The speed and elimination speed reach a balance, and the blood drug concentration is relatively stable at a certain level. At this time, the blood drug concentration is called the steady-state blood drug concentration, also known as the plateau value. [0003] In the dosin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K45/00A61P25/18A61P25/28A61P31/12A61P35/00A61P25/36
CPCA61K9/0002A61K9/5146A61K9/5153A61K45/00A61K47/34
Inventor 赖树挺郑阳曹付春连远发刘锋
Owner AC PHARMA CO LTD
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