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Improvements relating to pharmaceutical compositions

A composition and mixture technology, which is applied in the direction of drug combination, bulk delivery, nanocapsules, etc., can solve the problems of not being able to prepare nano-dispersions, not teaching and providing nano-dispersions, etc.

Inactive Publication Date: 2011-11-09
IOTA NANOSOLUTIONS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In EP-1741424 it is not taught to provide nanodispersions and the method described therein cannot prepare nanodispersions

Method used

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  • Improvements relating to pharmaceutical compositions
  • Improvements relating to pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0193] 0.10 g loratadine and 0.70 g hypromellose phthalate (HPMCP) were dissolved in 80 ml ethanol / acetone mixture (50% by volume); 0.10 g pluronic F127 and 0.10 g Mannitol was dissolved in 20 ml of distilled water. The aqueous solution was then added to the ethanol / acetone mixture and stirred using a magnetic bar to form a homogeneous solution. The solution was spray dried using a Buchi Mini B-290 spray dryer with an inlet temperature of 150°C and a liquid feed rate of 2.5 ml / min. A free-flowing white powder was obtained.

[0194] The dried powder samples were redispersed in phosphate buffer solution (pH=7.2) and nanoparticle size was measured using a Malvern Nano-S. A particle size measurement of 385±21 nm (at 5 mg / ml concentration) was obtained (after viscosity correction).

Embodiment 2

[0196] Dissolve 0.10 g loratadine and 0.80 g hypromellose phthalate (HPMCP) in 80 ml ethanol / acetone mixture (50% by volume); dissolve 0.10 g pluronic F127 in 10 ml distilled water . The aqueous solution was then added to the ethanol / acetone mixture and stirred using a magnetic bar to form a homogeneous solution. The mixture was spray dried using a Buchi Mini B-290 spray dryer with an inlet temperature of 150°C and a liquid feed rate of 2.5 ml / min. A free-flowing white powder was obtained.

[0197] The dried powder samples were redispersed in phosphate buffer solution (pH=7.2) and nanoparticle size was measured using a Malvern Nano-S. (uncorrected viscosity) gave a particle size measurement of 429±8 nm (at 5 mg / ml concentration).

Embodiment 3

[0198] Example 3 (Dissolution Test of Example 1):

[0199] 100 mg (equivalent to 10 mg of loratadine) of the spray-dried powder from Example 1 were dispersed in 900 ml of a dissolution medium (distilled water, pH=2.2 HCl solution or pH=7.2 phosphate buffer solution, respectively), Overhead paddle stirring at 50 rpm, (dissolution medium) temperature 37°C. Aliquots of each solution were withdrawn at 5 minutes, 10 minutes, 20 minutes, etc. using a pipette (1 ml Eppendorf pipette). The dispersion was then diluted with ethanol for detection of UV properties (1 ml of ethanol was added to 1 ml of the dispersion). The dissolution of Example 1 in different media is summarized in Table 1.

[0200] Table 1

[0201]

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Abstract

The present invention provides a substantially solvent-free nano-dispersion of an active in a carrier, wherein the carrier comprises an enteric carrier soluble at intestinal pH, but insoluble at stomach pH, and wherein the enteric carrier comprises at least 50% by weight of the nano-dispersion; and processes for the preparation of a substantially solvent-free nano-dispersion of an active in a carrier.

Description

technical field [0001] The present invention relates to improvements in enteroprotective pharmaceutical compositions. Background technique [0002] Enteric coatings are widely used for a variety of purposes, including protecting acid-sensitive pharmaceutical actives from gastric acid or protecting the gastric mucosa from drugs that cause irritation and / or damage to the stomach lining. [0003] For enteric coating agents, use cellulosic types (including cellulose acetate phthalate (CAP), cellulose acetate trimellitate (CAT), hydroxypropyl methylcellulose phthalate (HPMCP) , hydroxypropyl methylcellulose acetate succinate (HPMCAS) and carboxymethyl ethyl cellulose (CMEC)), vinyl types (including polyvinyl acetate phthalate (PVAP)), and acrylic types (including copolymers of methacrylic acid and ethyl acrylate). [0004] Taking HPMCP as an example, the pH threshold for rapid disintegration of HPMCP can be controlled by changing the phthaloyl content. Thus, it is ensured that...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16
CPCA61K9/1652A61K9/5161A61K9/1694A61P37/08A61P43/00
Inventor D·安格斯D·J·邓卡夫A·J·福斯特S·P·兰纳德王东
Owner IOTA NANOSOLUTIONS