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Koumine sustained-release preparation and preparation method thereof

A technology of hook kiss element and sustained-release preparation, which is applied to anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc. The effect of stable concentration, reduction of dosing times, and reduction of fluctuation of blood drug concentration

Active Publication Date: 2013-05-15
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The invention can overcome the disadvantages of poor absorption, large fluctuation of blood drug concentration and many administration times in common preparations

Method used

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  • Koumine sustained-release preparation and preparation method thereof
  • Koumine sustained-release preparation and preparation method thereof
  • Koumine sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: pharmacokinetic test of kelkinin in rats

[0035] 1.1 Drugs and reagents

[0036] Gelnectin was provided by our laboratory with a purity of 99.1%; methanol was chromatographically pure and was purchased from Sinopharm Chemical Reagent Co., Ltd.; ammonia was analytically pure and was purchased from Shantou Xilong Chemical Factory Co., Ltd.; ethyl acetate was purchased from Sinopharm Group Chemical Reagent Co., Ltd.

[0037] 1.2 Instruments

[0038] Angilent1100 high performance liquid chromatography (Angilent, USA); TGL-16C desktop high-speed centrifuge (Shanghai Anting Scientific Instrument Factory); KQ-200DB numerical control ultrasonic instrument (Kunshan Ultrasonic Instrument Co., Ltd.); WH-2 micro Vortex mixer (Shanghai Huxi Analytical Instrument Factory).

[0039] 1.3 Animals

[0040] SD male rats, weighing 250-300 g, were purchased from Shanghai Slack Experimental Animal Co., Ltd. Raise them in the animal room for three days before the experimen...

Embodiment 2

[0046] Embodiment 2: Determination test of apparent oil-water partition coefficient of keloids

[0047] 2.1 Drugs and reagents

[0048] Gelnectin was provided by our laboratory with a purity of 99.1%; methanol was chromatographically pure and purchased from Sinopharm Chemical Reagent Co., Ltd.; n-butylamine, hydrochloric acid, sodium hydroxide, dipotassium hydrogen phosphate, sodium dihydrogen phosphate, n-octanol All were of analytical grade and purchased from Sinopharm Chemical Reagent Co., Ltd.

[0049] 2.2 Instruments

[0050] Angilent1100 high performance liquid chromatography (Angilent, USA); WH-2 micro-vortex mixer (Shanghai Huxi Analytical Instrument Factory); RHS-4CT pH meter (Shanghai Dapu Instrument Co., Ltd.).

[0051] 2.3 Method

[0052] Prepare HCl solution with pH 1.0 and 3.0, phosphate buffer solution with pH 6.8 and 7.4, and NaOH solution with pH 9.0, respectively. Take an appropriate volume of n-octanol, pure water, and the above-mentioned solutio...

Embodiment 3

[0058] Example 3: In vivo intestinal absorption kinetics test of kelezin in rats

[0059] 3.1 Drugs and reagents

[0060] Gelnectin was provided by our laboratory with a purity of 99.1%; methanol was chromatographically pure and purchased from Sinopharm Chemical Reagent Co., Ltd.; the rest of the reagents were analytically pure and were purchased from Sinopharm Chemical Reagent Co., Ltd.

[0061] Preparation of K-R solution: 7.8g of NaCl, 0.35g of KCl, NaHCO per 1L of buffer 3 1.37g, NaH 2 PO 4 .2H 2 O 0.32g, MgCl 2 0.02g, CaCl 2 0.37g, glucose 1.4g (add just before use), adjust the pH value to 6.8 with 1mol / L phosphoric acid.

[0062] Preparation of perfusate: prepare the perfusion solution with the required concentration with freshly prepared K-R solution for the drug to be investigated.

[0063] 3.2 Instruments

[0064] Agilent 1100 high performance liquid chromatography (Angilent, USA); ZNCL-S magnetic stirrer (Gongyi Yuhua Instrument Co., Ltd.); PHS-407 precisi...

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Abstract

The invention discloses a Koumine sustained-release preparation and a preparation method thereof. The Koumine sustained-release preparation comprises by weight: 0.1%-5% of Koumine, 10-60% of a sustained-release material, and the balance other medicine acceptable carrier. The Koumine sustained-release preparation disclosed in the invention can improve the bioavailability of medicines and delay the release of Koumine from medicinal preparations, reduces the peak valley phenomenon of medicine absorption, is in favor of maintaining a stable plasma concentration so as to achieve a sustained release effect, and is more conducive to treatment of diseases. Repeated tests show that the sustained-release preparation provided in the invention has good repeatability and feasibility. And the preparation method provided in the invention has a simple process and good reliability.

Description

technical field [0001] The invention relates to an oral sustained-release and controlled-release pharmaceutical preparation, in particular to an oral sustained-release preparation of kelezin. Background technique [0002] hook kiss ( Gelsemium elegans Benth.) is the whole herb of Strychophyllum chinensis. Our country has a long history of research on hook kisses. It has been recorded in "Shen Nong's Materia Medica" and "Compendium of Materia Medica". Chinese hook kisses are abundant in Fujian, Zhejiang, Guangdong and other places. Physiological and pharmacological activities, such as inhibition of respiratory center, anti-tumor, anti-inflammation, relaxation of smooth muscle, mydriasis, inhibition of platelet aggregation, etc., folks use hook kisses to treat various pains, especially chronic neuropathic pain and cancer pain. In the 1960s, the No. 422 Hospital and No. 416 Hospital of the Navy formulated the "Zhi Tong Ling" injection with the total alkaloids of Gelensis, and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/22A61K9/52A61K31/439A61P29/00A61P19/02A61P35/00
Inventor 俞昌喜苏燕评范振东许盈杨渐廖凯君
Owner FUJIAN MEDICAL UNIV
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