Thymopentin oral microsphere preparation and preparation method thereof

A technology of microspheres and preparations, applied in pharmaceutical formulations, peptide/protein components, medical preparations containing active ingredients, etc. The effect of bioavailability

Active Publication Date: 2010-06-09
北京博恩特药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of the poor stability of thymopentin, it is easily degraded and inactivated by gastric acid and various digestive enzymes in the gastrointestinal tract; at the same time, due to the strong water solubility and poor fat solubility of thymopentin, combined with the The biofilm barrier formed by the tight association on the surface greatly hinders the absorption of thymopentin from the gastrointestinal tract, making its oral bioavailability extremely low
At present, the main route of clinical administration of thymopentin is intravenous or subcutaneous injection, and the dosing interval is mostly once a day or every other day. For patients who need long-term treatment, frequent injections will bring a lot of pain and inconvenience. poor

Method used

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  • Thymopentin oral microsphere preparation and preparation method thereof
  • Thymopentin oral microsphere preparation and preparation method thereof
  • Thymopentin oral microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0144] Embodiment 1: Thymopentin Oral Microspheres

[0145] Thymopentin 0.5kg

[0146] Gelatin 0.4kg

[0147] Lactide-glycolide copolymer 9kg

[0148] Dichloromethane 30L

[0149] Polyvinyl alcohol-124 10kg

[0150] Aprotinin 0.05kg

[0151] Sodium glycocholate 0.2kg;

[0152] Thymopentin, gelatin, aprotinin, and sodium glycocholate were dissolved in 5L of water for injection to make an aqueous solution as the water phase W 1 Dissolve the lactide-glycolide copolymer in 30l of dichloromethane to make a 30% lactide-glycolide copolymer dichloromethane solution as the oil phase 0; use it uniformly at 4°C Pulp machine 10000rpm high-speed vibration and emulsification for 3 minutes, mix the oil and water two phases evenly to make W I / 0 phase, 10kg polyvinyl alcohol-124 was dissolved in 500L water for injection to make a concentration of 2% polyvinyl alcohol-124 aqueous solution, as the water phase W 2 ; Emulsify with a homogenizer at 10,000 rpm for 5 minutes at 4°C, and 1 / 0 ...

Embodiment 2

[0153] Embodiment 2: Thymopentin oral microsphere tablet

[0154] Thymopentin 0.4kg

[0155] Gelatin 0.2kg

[0156] Lactide-glycolide copolymer 4kg

[0157] Dichloromethane 20L

[0158] Polyvinyl Alcohol-124 5kg

[0159] Aprotinin 0.15kg

[0160] Sodium glycocholate 1.5kg;

[0161] Dissolve thymopentin, gelatin, aprotinin, and sodium glycocholate in 2L of water for injection to make an aqueous solution as the water phase W 1 ; Dissolve lactide-glycolide copolymer in 20L dichloromethane to make a 20% lactide-glycolide copolymer dichloromethane solution as oil phase 0; Pulp machine 7000rpm high-speed vibration and emulsification for 2 minutes, mix the oil and water two phases evenly to make W I / 0 phase, dissolve polyvinyl alcohol-124 in 480L water for injection to make a 1% aqueous solution of polyvinyl alcohol-124, and emulsify it with a homogenizer at 14000 rpm for 4 minutes at 3°C, and mix with the previous W 1 / 0 phase is emulsified and included to obtain W 1 / 0 / W ...

Embodiment 3

[0162] Embodiment 3: Thymopentin oral microsphere capsule

[0163] Thymopentin 0.7kg

[0164] Gelatin 1.3kg

[0165] Lactide-glycolide copolymer 16kg

[0166] Dichloromethane 40L

[0167] Polyvinyl alcohol-124 21kg

[0168] Aprotinin 0.03kg

[0169] Sodium glycocholate 0.5kg;

[0170] Dissolve thymopentin, gelatin, aprotinin, and sodium glycocholate in 7L water for injection to make an aqueous solution as the water phase W 1 ; Dissolve lactide-glycolide copolymer in 40L dichloromethane to make a 40% lactide-glycolide copolymer dichloromethane solution as oil phase 0; Pulp machine 14000rpm high-speed vibration and emulsification for 4 minutes, mix the oil and water two phases evenly to make W 1 / 0 phase, polyvinyl alcohol-124 was dissolved in 700L water for injection to make a concentration of 3% polyvinyl alcohol-124 aqueous solution, as the water phase W 2 ; Emulsify at 5°C with a homogenizer at 7000rpm for 7 minutes at high speed, with the former W 1 / 0 phase is emu...

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Abstract

The invention discloses a thymopentin oral microsphere preparation and a preparation method thereof. The oral microsphere preparation comprises the following raw materials: thymopentin, gelatin, a lactide-glycolide copolymer, dichloromethane, polyvinylalcohol-124, an aprotinin or trypsin inhibitor, and sodium glycyl-cholate or deoxysodium cholate or sodium caprate. The thymopentin oral microsphere preparation has high bioavailability, can replace injection administration without reducing clinical curative effects and overcomes a lot of pains and inconvenience of patients caused by frequent injections.

Description

field of invention [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a thymopentin oral microsphere preparation and a preparation method thereof. Background technique [0002] Thymopentin (TP-5) is composed of five amino acids including arginine, lysine, aspartic acid, valine and tyrosine, and its chemical name is N-[N-[Nα-[Nα- L-arginyl-L-lysine]-L-α-aspartyl]-L-valyl]-L-tyrosine, a potent thymopoietin II in thymus secretion part. [0003] Thymopentin is a cellular immune regulation drug, which has the function of inducing T cell differentiation, promoting the maturation and activation of T lymphocyte subsets; Thymopentin can enhance the phagocytosis of macrophages, enhance the immune function of red blood cells, and increase the (NK) activity, increase the production level of interleukin-2 (IL-2) and receptor expression level, promote the production of γ-interferon in peripheral blood mononuclear cells, and en...

Claims

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Application Information

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IPC IPC(8): A61K38/08A61K9/16A61K47/42A61P37/04A61P1/16
Inventor 王永辉冯前进郭光明周晓庆
Owner 北京博恩特药业有限公司
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