An osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and a preparation method thereof

A technology of hydroxycamptothecin and solid dispersion, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc. Release and other issues, to achieve the effect of sustained drug release, improved bioavailability, and stable drug release

Inactive Publication Date: 2009-03-04
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the extremely low solubility of hydroxycamptothecin, the osmotic pump tablet of the above form still cannot achieve constant release of the drug.

Method used

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  • An osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and a preparation method thereof
  • An osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and a preparation method thereof
  • An osmotic pump controlled release tablet of solid dispersion of hydroxy camptothecin and a preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0034] Among them, the hydroxycamptothecin solid dispersion is prepared by mixing hydroxycamptothecin with a mass ratio of 1:2-1:30 with a polymer carrier, and the preparation method includes: a melting method, a solvent-melting preparation co-precipitation method and Spray drying method, etc.

[0035] The core of the single-layer osmotic pump tablet is prepared according to the following process: the solid dispersion of hydroxycamptothecin, the excipients for controlled release and other excipients are crushed and sieved, and the binders and lubricants in the other excipients After the materials are uniformly mixed, a soft material is made with a binder, sieved and granulated, dried at 50°C, sieved again to be granulated, and lubricant is added to form a tablet core.

[0036] The core of the push-pull osmotic pump tablet is prepared according to the following process: the solid dispersion of hydroxycamptothecin, the excipients for controlling release and other excipients are pulv...

Embodiment 1

[0039] Example 1: Preparation of hydroxycamptothecin double-layer osmotic pump tablets

[0040] Using film coating technology, wet granulation and tableting, laser drilling is performed on the coating film of the drug-containing layer as a drug release hole. Among them, the preparation of the hydroxycamptothecin solid dispersion adopts the solvent-melting method.

[0041] The composition of the solid dispersion of hydroxycamptothecin is (mass percentage):

[0042] Hydroxycamptothecin 17%

[0043] Polyethylene glycol 6000 83%

[0044] (The mass ratio of hydroxycamptothecin to polyethylene glycol 6000 is 17:83).

[0045] The content of every 100 osmotic pump tablets is as follows:

[0046] The composition of the drug-containing layer of the tablet core is:

[0047] Hydroxycamptothecin solid dispersion 9g

[0048] Polyoxyethylene 50 4g

[0049] Sodium chloride 4g

[0050] Lactose 3g

[0051] Magnesium stearate 0.05g

[0052] The composition of the push layer is:

[0053] Polyoxyethyl...

Embodiment 2

[0064] Example 2: Preparation of hydroxycamptothecin double-layer osmotic pump tablets

[0065] As in Example 1, hydroxycamptothecin was prepared as a double-layer osmotic pump tablet. In this example, the preparation of the hydroxycamptothecin solid dispersion adopts the co-precipitation method.

[0066] The composition of the solid dispersion of hydroxycamptothecin is (mass percentage):

[0067] Hydroxycamptothecin 14%

[0068] Polyvinylpyrrolidone (K30) 86%

[0069] (The mass ratio of hydroxycamptothecin to polyvinylpyrrolidone is 7:43)

[0070] The content of every 100 osmotic pump tablets is as follows:

[0071] The composition of the drug-containing layer of the tablet core is:

[0072] Hydroxycamptothecin solid dispersion 9g

[0073] Polyoxyethylene 50 4g

[0074] Sodium chloride 4g

[0075] Lactose 3g

[0076] Magnesium stearate 0.05g

[0077] The composition of the push layer is:

[0078] Polyoxyethylene 550 4g

[0079] Hydroxypropyl methylcellulose 1g

[0080] Sodium chl...

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Abstract

A tablet of the dispersed hydroxy camptothecine solid released under the control of osmotic pump is composed of a tablet core containing dispersed hydroxy camptothecine solid, release controlling auxiliaries, and carrier and a perforated coated layer. Its preparing process includes preparing tablet core, coating and perforating.

Description

Technical field [0001] The invention relates to the technical field of preparations, to be precise, it is a controlled-release preparation that uses solid dispersion solubilization technology and osmotic pump technology to achieve zero-order release of hydroxycamptothecin. Background technique [0002] Hydroxycamptothecin (HCPT) is a cell cycle specific drug. Studies have found that it has a targeted and selective inhibitory effect on DNA topoisomerase I, thereby inhibiting cancer cell DNA replication and transcription. It has no cross-resistance with other commonly used anticancer drugs, its anticancer effect is equivalent to 30 times that of camptothecin and its toxicity is significantly lower than that of camptothecin. Clinically, it is mostly used for digestive system cancers such as stomach cancer, esophageal cancer, liver cancer, etc.; it also has a good effect on oral cavity, cervical and facial cancers. Hydroxycamptothecin is a water-insoluble and poorly soluble drug with...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/30A61K31/475A61K47/34A61K47/38A61K47/26A61P35/00A61K47/10A61K47/32
Inventor 陈欢欢蒋国强朱德权江盛阳丁富新
Owner TSINGHUA UNIV
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