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Novel dosage form of sinomenine medicament or hydrochlorate thereof and preparation technique thereof

A technology of sinomenine and hydrochloride, which is applied in the field of sinomenine or its hydrochloride enteric-coated controlled-release tablet and its preparation technology, can solve the toxic and side effects, low bioavailability, and cannot meet clinical needs And other issues

Active Publication Date: 2009-03-04
HUNAN ZHENGQING PHARM GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the existing sinomenine preparations mainly include enteric-coated film-coated tablets, sinomenine gel matrix sustained-release tablets twice a day, and injections, etc. Due to the constraints of various factors, the existing dosage forms are far from being suitable for clinical needs.
Due to the low bioavailability and short half-life of sinomenine when administered orally, clinical treatment of rheumatism and rheumatoid diseases requires long-term medication. Due to its strong histamine release effect, a large dose can cause some patients to develop Scalp and face itching, flushing, pain, aggravated swelling, accompanied by rash, sweating, occasional abdominal pain, gastric discomfort, etc.; the blood concentration of sinomenine ordinary enteric-coated tablets is very low for a period of time at the beginning, and then rapidly release, the blood concentration suddenly rises, and there is an obvious peak; compared with other common preparations, sinomenine hydrochloride gel matrix sustained-release tablets have the characteristics of stable blood concentration in the body, fewer administration times, and longer duration of drug effects. , but the clinical application found that its toxic and side effects are also obvious, mainly manifested as severe gastrointestinal allergic reactions, especially the stimulation of gastric mucosa; general topical preparations are difficult to penetrate the skin into the lesion, and it is difficult to obtain a satisfactory therapeutic effect

Method used

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  • Novel dosage form of sinomenine medicament or hydrochlorate thereof and preparation technique thereof
  • Novel dosage form of sinomenine medicament or hydrochlorate thereof and preparation technique thereof
  • Novel dosage form of sinomenine medicament or hydrochlorate thereof and preparation technique thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0220] Example 1: Preparation of matrix-type enteric-coated controlled-release tablets

[0221] 1. Tablet core composition

[0222] Sinomenine 60.0kg Hypromellose 100.0kg

[0223] Starch 40.0kg Dextrin 60.0kg

[0224] Lactose 90.0kg 70% ethanol solution 40L

[0225] Magnesium Stearate 3.5kg

[0226] 2. Enteric coating ingredients

[0227] Kalekang Yakeyi Enteric Coating Prepowder 52.5kg Purified Water 210L;

[0228] Pass the sinomenine raw material through an 80-mesh sieve, pass each auxiliary material through an 80-mesh sieve, mix according to the proportion, add 70% ethanol solution, make a soft material, granulate with a 20-mesh sieve, dry at 40°C for 2 hours, granulate, add 1 % magnesium stearate, mixed evenly, and pressed into tablets to obtain the skeleton tablet core; weighed the prescribed amount of Kalecon Yakeyi enteric-coated pre-coated powder, dispersed in purified water and stirred evenly, and prepared into enteric-coated prepowder with a solid content of 20%...

Embodiment 2

[0229] Example 2: Preparation of film-controlled enteric-coated controlled-release tablets

[0230] 1. Tablet core composition

[0231] Sinomenine 60.0kg Ethylcellulose 52.1kg

[0232] Microcrystalline cellulose 39.1kg Lactose 198.8 parts by weight

[0233] 3% Hypromellose Aqueous Solution 40L Magnesium Stearate 3.5kg

[0234] 2. Enteric-coated film-controlled ingredients

[0235] Acrylic RS 10.16kg Acrylic RL 1.84kg

[0236] Hypromellose Phthalate 3.19kg Diethyl Phthalate 6.0L

[0237] Talc powder 3kg 80% ethanol 150L;

[0238] Pass the sinomenine raw material through an 80-mesh sieve, pass each auxiliary material through an 80-mesh sieve, mix according to the proportion, add 3% hypromellose aqueous solution, make soft material, granulate with a 20-mesh sieve, dry at 40°C for 2 hours, and dry granules, add 1% magnesium stearate, mix well, and press into tablets to get the skeleton tablet core; weigh the prescribed amount of enteric-coated film-controlled coating ingredien...

Embodiment 3

[0239] Example 3: Preparation of matrix-type enteric-coated controlled-release tablets

[0240] 1. Tablet core composition

[0241] Sinomenine 120kg Hypromellose 100kg

[0242] Starch 10kg Dextrin 60kg

[0243] Lactose 60kg 70% ethanol solution 50L

[0244] Magnesium Stearate 5kg

[0245] 2. Enteric coating ingredients

[0246] Kalekon Yakeyi Enteric Coating Prepowder 60kg Purified Water 290L;

[0247] Pass the sinomenine raw material through an 80-mesh sieve, pass each auxiliary material through an 80-mesh sieve, mix according to the proportion, add 70% ethanol solution, make a soft material, granulate with a 20-mesh sieve, dry at 40°C for 2 hours, granulate, add 1 % magnesium stearate, mixed evenly, and pressed into tablets to obtain the skeleton tablet core; weighed the prescribed amount of Kalecon Yakeyi enteric-coated pre-coated powder, dispersed in purified water and stirred evenly, and prepared into enteric-coated prepowder with a solid content of 20%. Dissolve th...

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Abstract

The invention discloses a sinomenine or an enteric-coated controlled-release tablet of hydrochloride thereof. The prepared enteric-coated controlled-release tablet hardly releases the drug in artificial simulated gastric juice, but can slowly and smoothly release the drug in artificial simulated intestinal juice; the sustained release time of the drug can achieve more than 12 hours or even 24 hours; the enteric-coated controlled-release tablet is taken once or twice daily, the plasma drug concentration in vivo is smooth, and the peak-valley phenomenon of the plasma drug concentration is reduced; as the prepared enteric-coated controlled-release tablet hardly releases the drug in stomach, the contacted concentration of the drug with the gastric mucosa is small, the stimulation of the stomach caused by the drug is alleviated. As the prepared enteric-coated controlled-release tablet sustainedly slowly releases the drug in intestinal tract, the times of the drug administration are reduced, and the patient compliance is improved, thereby being applicable to the needs of the clinical development.

Description

technical field [0001] The invention relates to a new drug dosage form of sinomenine or its hydrochloride, in particular to a sinomenine or its hydrochloride enteric-coated controlled-release tablet and a preparation process thereof. Background technique [0002] Sinomenine (sinomenine) is the main active ingredient in the rhizomes of Chinese medicine Fangjiaceae plants such as Qingfengteng and Xunfengteng. At present, its hydrochloride is mainly used clinically. Sinomenine hydrochloride is a long needle-like crystal with a melting point of 233°C , easily soluble in water and dilute sodium hydroxide, soluble in ethanol, insoluble in chloroform and ether, and the equilibrium solubility in water, 0.1mol / L hydrochloric acid, pH6.8 phosphate buffer solution is 42.57, 23.73, 58.84 mg / ml. Sinomenine has pharmacological effects such as anti-inflammation, immunosuppression, analgesia, lowering blood pressure, anti-arrhythmia, anti-allergy, releasing histamine, and affecting gastroi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61K9/22A61K9/38A61K47/38A61P29/00A61P9/06
Inventor 吴飞驰向大雄仇萍滕健刘伟肖建波
Owner HUNAN ZHENGQING PHARM GRP CO LTD
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