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Clnidipine dropping pill

A technology of dipine dripping pills and cilnidipine, which is applied in the direction of organic active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve the problems of small dissolution rate, affecting the clinical efficacy of drugs, and low bioavailability, and achieves Quick onset, improve the effect of human bioavailability

Inactive Publication Date: 2005-12-21
苑振亭
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because cilnidipine is insoluble in water, the dissolution rate of conventional oral preparations such as tablets and capsules is small and the absorption is poor, resulting in low bioavailability, which often affects the clinical efficacy of the drug

Method used

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  • Clnidipine dropping pill

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Prescription 1000 capsules

[0015] Cinidipine 2.5g

[0016] Macrogol 4000 8g

[0017] Macrogol 6000 4.5g

[0018] Mint essence 0.1g

[0019] Preparation: Weigh and mix cilnidipine and polyethylene glycol evenly, heat to 70°C, stir and melt to dissolve the medicine completely; then add peppermint flavoring agent and mix well. Use a dropper with a diameter of 1mm to drop the drug solution into liquid paraffin at -10°C, solidify for 30 to 40 minutes, and then filter, wash, dry, and pack to obtain the product. Each drop pill weighs 15mg and contains 2.5mg of cilnidipine.

Embodiment 2

[0021] Prescription 1000 capsules

[0022] Cinidipine 5g

[0023] Macrogol 6000 20g

[0024] Sucrose Fatty Acid Ester 5g

[0025] Orange essence 0.2g

[0026] Preparation: Weigh cilnidipine, polyethylene glycol, and sucrose fatty acid ester and mix evenly, heat to 70°C, stir and melt to dissolve the drug completely; then add orange essence and corrective agent, and mix well. Use a dropper with a diameter of 2mm to drop the drug solution in liquid paraffin at -10°C, solidify for 30 to 40 minutes, and then filter, wash, dry, and pack to obtain the product. Available example 1 method preparation. Each drop pill weighs 30mg and contains 5mg of cilnidipine.

Embodiment 3

[0028] Prescription 1000 capsules

[0029] Cinidipine 5g

[0030] Poloxamer 188 25g

[0031] Orange essence 0.2g

[0032] Preparation: Weigh cilnidipine and poloxamer 188, heat at 60°C, stir and melt to dissolve the medicine completely; then add orange essence and corrective agent, and mix well. Use a dropper with a diameter of 2mm to drop the drug solution into methyl silicone oil at -10°C, cure for 30 to 40 minutes, then filter, wash, dry, and pack. Available example 1 method preparation. Each drop pill weighs 30mg and contains 5mg of cilnidipine.

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Abstract

The present invention relates to a senidipine dripping pills preparation for curing hypertension and angina pectoris and its preparation method. Said invention uses medicine senidipine and dripping pill matrix, mixes them and utilizes dripping pill preparation technique to make dripping pills. The ratio range of medicine and dripping matrix is 1:100-1:1, the dripping pill matrix is water soluble material, can be mixture of both two or more than two of polyethylene glycol, sodium stearate, poloxamer and monostearate. Besides, said invention also provides the concrete steps of its preparation method.

Description

Technical field: [0001] The invention relates to a cilnidipine drop pill for treating hypertension and angina pectoris and a preparation method thereof, belonging to the technical field of western medicine preparations. Background technique: [0002] The general name of the main drug involved in the present invention: cilnidipine; English name: cilnidipine b; chemical name: (E)-(±)-1,4-dihydro-2,6-dimethyl-4-(3- Nitrophenyl)-3,5-pyridinedicarboxylic acid-2-methoxyethyl, 3-phenyl-2-propenyl ester; molecular formula: C 27 h 28 N 2 o 7 ; Molecular weight: 492.19; Structural formula: see figure. [0003] [0004] Cilnidipine is a cardiovascular drug widely used clinically and belongs to the class of calcium channel antagonist drugs. Wang Yao is used for the treatment of patients with hypertension and angina pectoris. At present, the specifications of cilnidipine used clinically are tablets of 5 mg and 10 mg. Because cilnidipine is insoluble in water, conventional oral ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422
Inventor 苑振亭丁平田
Owner 苑振亭