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Compound medicine as well as preparation method and application thereof

A compound and drug-based technology, which is applied in the field of medicine, can solve problems such as ineffective phosphorus reduction and gastrointestinal discomfort, and achieve the effects of avoiding gastrointestinal adverse reactions, good targeted curative effect, and simple preparation process

Inactive Publication Date: 2018-01-19
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Silam is a non-specific binding agent with extensive adsorption, so the effect of reducing phosphorus is not obvious; lanthanum carbonate is specific to phosphorus, so it can strongly bind phosphate, but studies have shown that long-term use of lanthanum carbonate It may be deposited in the gastric mucosa of patients and cause pathological changes of chronic gastritis and gastric ulcer. At the same time, many patients switch to other phosphorus binders due to gastrointestinal discomfort caused by taking lanthanum carbonate

Method used

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  • Compound medicine as well as preparation method and application thereof
  • Compound medicine as well as preparation method and application thereof
  • Compound medicine as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1). Micronize 1g of lanthanum carbonate powder, add it to 10-25g of ethyl acetate solution, and disperse it ultrasonically. The ultrasonic power is 100-200W, and the dispersion time is 30min;

[0036] (2). Dissolve 1.5g PLGA in 100-300g ethyl acetate solution, heat and stir to mix evenly to form a solution;

[0037] (3). The mixture obtained in (1) is uniformly dispersed in the solution described in (2), heated, stirred and mixed to form a primary emulsion;

[0038](4). Dissolve 0.6g of polyvinyl alcohol in 100-300mg of water, then add 1.5-5g of NaCl, heat and mix to form a polyvinyl alcohol solution;

[0039] (5). Add the emulsion formed in (3) into the polyvinyl alcohol solution described in (4), stir mechanically at a speed of 4500r·min-1, and stir for 6h to form a S / O / W type double emulsion.

[0040] (6). Stir the emulsion obtained in (5) to volatilize ethyl acetate, solidify into balls, and then centrifuge, wash, and dry to obtain the PLGA drug-loaded microsphere...

Embodiment 2

[0042] Preparation of compound drugs:

[0043] (1). Micronize 0.5g of lanthanum carbonate powder, add it to 1-3ml of ethyl acetate solution, and disperse it ultrasonically. The ultrasonic power is 100-200W, and the dispersion time is 30min;

[0044] (2). Dissolve 1g PLA in 12-40ml ethyl acetate solution, heat and stir to mix evenly to form a solution;

[0045] (3). The mixture obtained in (1) is uniformly dispersed in the solution described in (2), heated, stirred and mixed to form a primary emulsion;

[0046] (4). Dissolve 0.8g of polyvinyl alcohol in 100-300mL of water, then add 1.5-5g of NaCl, heat and mix to form a polyvinyl alcohol solution;

[0047] (5). Then add the emulsion formed in (3) into the polyvinyl alcohol solution described in (4), stir mechanically at a speed of 4500r min-1, and stir for 6h to form a S / O / W complex

[0048] (6). Stir the emulsion obtained in (5) to volatilize ethyl acetate, solidify into balls, and then centrifuge, wash, and dry to obtain th...

Embodiment 3

[0050] This example investigates the protective effect of PLGA on lanthanum carbonate in an acidic environment.

[0051] Group A is mixed with 500mg of lanthanum carbonate powder (minimum dosage for patients with mild symptoms, up to 3.75g at one time) and 500ml of dilute hydrochloric acid with pH=2 (a person can secrete 500ml of gastric juice in one meal),

[0052] Group B was mixed with PLGA-wrapped composite dosage form containing the same amount of lanthanum carbonate and 500ml of dilute hydrochloric acid with pH = 2. After 4 hours, it was found that the pH of the liquid in group A was equal to 7, and the lanthanum carbonate powder precipitated at the bottom of the beaker without obvious Change; the PH value of the liquid in group B hardly rose, and powder settled at the bottom of the beaker, and its amount was more than that in group A.

[0053] Thereby, explain that lanthanum carbonate powder is dissolved in acid, and PLGA has played protective effect to lanthanum carbon...

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Abstract

The invention relates to a compound medicine as well as a preparation method and an application thereof. The compound medicine is an effective combination of an auxiliary material polymer shell and aneffective component in the shell, wherein the effective component is a phosphorus binding agent, and the auxiliary material polymer shell is PLGA (poly(lactic-co-glycolic acid) or an other polymer material. The medicine can be used as a medicine for specifically adsorbing phosphorus. Compared with the prior art, the compound medicine has the advantages that the excellent phosphate adsorption performance of lanthanum carbonate is fully used, advantages of being non-toxic, rich in ester bonds and freely soluble in lipid of the polymer material are developed, and the compound nano-medicine of PLGA / lanthanum carbonate which is high in biocompatibility and easy to discharge is prepared. The method has simple preparation process and easily controllable conditions; compared with lanthanum carbonate chewable dosage forms which are used for many years, the compound medicine is more suitable for treating hyperphosphatemia.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound medicine and its preparation method and application. Background technique [0002] Hyperphosphatemia mainly occurs in patients with chronic renal failure (Chronic renal disease, CKD). It means that the serum phosphorus level exceeds the upper limit of normal value (>1.45mmol / L) set by the laboratory. Excessive blood phosphorus can cause vascular calcification, which is a strong predictor of cardiovascular disease mortality, and cardiovascular disease is the main cause of death in CKD patients. Relevant studies have shown that for every 1mg / dl increase in blood phosphorus level, the risk of death in CKD patients increases by 18%, and more than 50% of end-stage renal disease dies from cardiovascular diseases; young dialysis patients develop vascular calcification decades earlier than normal people 14 / 16 of dialysis patients aged 20-30 have vascular calcification, an...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K33/24A61P3/12
Inventor 朱玉
Owner TONGJI UNIV
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