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Summary for Patent: 5,631,021
|Title:||Method for producing microcapsule|
|Abstract:||A microcapsule produced by preparing a water-in-oil emulsion comprising an inner aqueous layer containing said water-soluble drug and a drug retaining substance therefor and an oil layer containing a polymer substance, then thickening or solidifying said inner aqueous layer to a viscosity of not lower than about 5000 centiposes and finally subjecting the resulting emulsion to in water drying gives prolonged release of water-soluble drug.|
|Inventor(s):||Okada; Hiroaki (Osaka, JP), Ogawa; Yasuaki (Osaka, JP), Yashiki; Takatsuka (Hyogo, JP)|
|Assignee:||Takeda Chemical Industries, Ltd. (Osaka, JP)|
1. A prolonged release microcapsule for injection, which is produced by redispersing a spherical microcapsule having an average diameter of 2 to 200 .mu.m, comprising particles
containing a water-soluble drug, the particles being dispersed in a spherical microcapsule matrix composed of a polymer of lactic acid and glycolic acid having a comonomer ratio within the range of about 100/0 to 50/50 and an average molecular weight
within the range of about 5,000 to 200,000, in an excipient selected from the group consisting of mannitol, sorbitol, lactose and glucose and then solidifying, wherein, the water-soluble drug is a polypeptide of the formula (I)
wherein R.sub.1 is His, Tyr, Trp or p-NH.sub.2 -Phe; R.sub.2 is Tyr or Phe; R.sub.3 is Gly or a D-amino acid residue; R.sub.4 is Leu, Ile or Nle; and R.sub.5 is Gly-NH-R.sub.6 or NH-R.sub.6, wherein R.sub.6 is H or a lower alkyl group which may optionally be substituted by OH, or a salt thereof, and the resulting microcapsule, upon reconstitution in a vehicle for injection, provides greater stability than if no redispersing step is performed.
2. A microcapsule as claimed in claim 1, wherein the water-soluble drug is (Pyr)Glu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NH-C.sub.2 H.sub.5.
3. A microcapsule as claimed in claim 1, wherein the comonomer ratio is 75/25.
4. A microcapsule as claimed in claim 1, wherein the excipient is mannitol.
5. An injectable preparation comprising a therapeutically effective amount of the microcapsule as claimed in claim 1.
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