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Hard capsule

a hard capsule and capsule technology, applied in the field of hard capsules, can solve the problems of poor solubility, low absorbability of alimentary canal, prone to drop or fluctuation, etc., and achieve the effect of excellent stability

Inactive Publication Date: 2005-08-25
HOSHI NOBORU +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006] The present inventors carried out assiduous studies to attain the above object, and as a result discovered that a hard capsule that is made mainly of a polymer or copolymer obtained by polymerizing or copolymerizing at least one polymerizable vinyl monomer in the presence of polyvinylalcohol and / or a derivative thereof has excellent stability even when filled with a solvent for dissolving a sparingly soluble therapeutic ingredient, and moreover is also excellent in terms of general properties that a hard capsule should possess such as water solubility.
[0045] Note that, as with a normal hard gelatin capsule or cellulose derivative capsule, colorants such as dyes and pigments, opacifying agents, fragrances and so on can if required be added to the hard capsule of the present invention as appropriate from within ranges such that the effects of the present invention are not impeded.
[0049] Pharmaceutical contrivances such as making the filling operation easier or preventing leakage of the filling from out of the hard capsule can be achieved by adding a thickener for the above-mentioned solvent. There are no particular limitations on the thickener, so long as it is one mentioned in pharmaceutics textbooks or the like or one that is commonly used, for example light silicic acid anhydride, a vegetable oil, or a cellulose derivative.
[0051] In addition to a pharmaceutical preparation for oral administration, the hard capsule of the present invention can also be used as an inhalant or as a pharmaceutical preparation for rectal administration. Moreover, in addition to drugs for medical treatment, the hard capsule of the present invention can also be used in the fields of drugs / chemicals for animals or plants, cosmetics, and foodstuffs. Furthermore, the hard capsule of the present invention can also be filled with reagents or the like for assaying or synthesis, and used with an object of simplifying handling thereof.

Problems solved by technology

Many active substances (i.e. therapeutic ingredients) of medicines have poor solubility in water; with such substances, the absorbability from the alimentary canal is low, and hence the utilizability, the expression of therapeutic effects and so on are prone to dropping or fluctuating.
However, these solvents are generally liquids, and hence making tablets is difficult, and moreover the pharmaceutical form ultimately put onto the market is developed separately.
However, there is a drawback in that if a conventional gelatin hard capsule is filled with polyethylene glycol having a degree of polymerization of 400 (PEG 400), then moisture in the capsule skin migrates into the solvent, and the capsule may split (Pharmaceutical Technology Europe, October, 84, 86, 88-90, 1998).

Method used

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Examples

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Effect test

synthesis example 1

[0055] 75 parts by weight of PVA-SH (degree of polymerization 500, degree of hydrolysis 88%, made by Kuraray Co., Ltd.) was completely dissolved in 237 parts by weight of ion-exchange water at 95° C. Next, the amounts of methacrylic acid and methyl methacrylate shown in Table 1 below were added, and after purging with nitrogen gas 3 parts by weight of t-butyl hydroperoxide was added and reaction was carried out, thus producing compounds E-1001, E-1002, E-1003 and E-1004. An aqueous solution of 15 to 20% of each of the components was prepared, and approximately 0.1 mm films were produced using a casting method. The solubilities (water solubility, solubility at pH 1.2, solubility at pH 6.8, solubility in PEG 400) and strengths (bending angle (RH 65%, dry state)) of the films produced are shown in Table 1.

[0056] In the water solubility tests, a piece of film of size 20 mm square was immersed in 10 ml of water, gentle shaking was carried out, and it was ascertained whether or not the f...

synthesis example 2

[0058] 75 parts by weight of PVA-SH (degree of polymerization 500 and 1500 mixed together, both degree of hydrolysis 88%, made by Kuraray Co., Ltd.) was completely dissolved in 237 parts by weight of ion-exchange water at 95° C. Next, the amounts of acrylic acid and methyl methacrylate shown in Table 2 below were added, and after nitrogen substitution 3 parts by weight of t-butyl hydroperoxide was added and reaction was carried out, thus producing compounds E-2001, E-2002, E-2003, E-2004, E-2005 and E-2006. The mixing proportions of the PVA-SH of degree of polymerization 500 and the PVA-SH of degree of polymerization 1500 were 50:50 (E-2001), 50:50 (E-2002), 45:55 (E-2003), 40:60 (E-2004), 20:80 (E-2005) and 10:90 (E-2006). An aqueous solution of 15 to 20% of each of the components was prepared, and approximately 0.1 mm films were produced using a casting method. The solubilities and strengths of the films produced were measured as in Synthesis Example 1, and are shown in Table 2. ...

synthesis example 3

[0059] 75 parts by weight of PVA-SH (degree of polymerization 500 and 1500 mixed together in a ratio of 1:9, both degree of hydrolysis 88%, made by Kuraray Co., Ltd.) was completely dissolved in 237 parts by weight of ion-exchange water at 95° C. The amounts of methacrylic acid and methyl methacrylate shown in Table 3 below were then added thereto, and after nitrogen substitution 3 parts by weight of t-butyl hydroperoxide was added and reaction was carried out, thus producing compounds E-3001, E-3002, E-3003. An aqueous solution of 15 to 20% of each of the components was prepared, and approximately 0.1 mm films were produced using a casting method. The solubilities and strengths of the films produced were measured as in Synthesis Example 1, and are shown in Table 3.

TABLE 3Polymer composition ratios and film propertyvalues for Synthesis Example 3E-3001E-3002E-3003CompositionPVA-SH757575MAA7.5105MMA17.51520Film solubilityWater solubilityYesYesYespH 1.2 solubilityYesYesYespH 6.8 solu...

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Abstract

A method of manufacturing a hard capsule made mainly of a polymer or copolymer obtained includes polymerizing or copolymerizing at least one polymerizable vinyl monomer in the presence of polyvinyl alcohol and / or a derivative thereof. Unlike conventional hard capsules, this hard capsule can be filled with a solvent (e.g., polyethylene glycol) for a sparingly soluble drug ingredient.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This is a continuation of U.S. patent application Ser. No. 10 / 362,114, filed Feb. 19, 2003, which is the U.S. National Phase under 35 U.S.C. § 371 of International Application PCT / JP01 / 07244, filed Aug. 24, 2001, which claims priority to Japanese Patent Application No. 2000-259830, filed Aug. 29, 2000, the disclosure of which is incorporated herein by reference in their entirety. The International Application was not published under PCT Article 21(2) in English.BACKGROUND OF THE INVENTION [0002] 1. Field of the Invention [0003] The present invention relates to a hard capsule that is made mainly of a polymer or copolymer obtained by polymerizing or copolymerizing at least one polymerizable vinyl monomer in the presence of polyvinylalcohol and / or a derivative thereof. [0004] 2. Description of the Related Art [0005] Many active substances (i.e. therapeutic ingredients) of medicines have poor solubility in water; with such substances, the a...

Claims

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Application Information

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IPC IPC(8): A61J3/07A61K9/48A61K47/32
CPCA61J3/071A61K9/4816Y10T428/1352Y10S514/962A61K47/32A61J3/07
Inventor HOSHI, NOBORUSHIMAMOTO, TOSHIOSUGIYAMA, SHIGERU
Owner HOSHI NOBORU
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