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

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

CN101721677AActive Publication Date: 2010-06-09北京博恩特药业有限公司
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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

Patent Timeline
09 Jun 2010
Publication
CN101721677A
IPC
A61K38/08; A61K9/16; A61K47/42; A61P37/04; A61P1/16
Inventors
王永辉; 冯前进