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Novel Oral Microspheres Of Insulin With Protease Inhibitor Protecting From Enzymatic Degradation

M. Morishita, I. Morishita, K. Takayama, Y. Machida, T. Nagai
Published 1992 · Chemistry

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Abstract Eudragit L100 insulin microspheres (IMS) containing a protease inhibitor were prepared for an oral dosage form of insulin. The efficiencies of insulin incorporation of IMS containing trypsin inhibitor (TI), chymostatin (CS), Bowman-Birk inhibitor (BBI) and aprotinin (AP) amounted to approx. 80% and did not differ among the preparations. In a release study, the more than 90% of insulin remaining after treatment of simulated gastric fluid was released in a medium of simulated intestinal fluid during the initial 60 min. The protective efficiency of the various preparations toward three digestive enzymes (pepsin, trypsin and α-chymotrypsin) was investigated under the chosen experimental conditions. Strong insulin protective efficiency towards pepsinic degradation was observed in all preparations. The highest efficiencies towards each trypsinic and α-chymotrypsinic degradation were achieved with IMS containing TI and IMS containing CS, respectively. IMS containing AP was less resistant to trypsinic and α-chymotrypsinic degradation compared with IMS containing TI towards trypsin and IMS containing CS towards α-chymotrypsin, but was slightly more effective than IMS containing BBI towards both enzymes. On the other hand, complete insulin degradation after respective enzymatic incubation was observed in IMS without inhibitor. These results indicated that IMS containing protease inhibitor could be prepared and would be able to protect insulin from proteolytic degradation.
This paper references
10.1016/0378-5173(86)90023-2
Trials of rectal insulin suppositories in healthy humans
Nishihata Toshiaki (1986)
10.1111/J.1399-3011.1985.TB02155.X
The Bowman-Birk inhibitor. Trypsin- and chymotrypsin-inhibitor from soybeans.
Y. Birk (1985)
10.1111/j.2042-7158.1985.tb03064.x
Promoting effect of the new chymotrypsin inhibitor FK‐448 on the intestinal absorption of insulin in rats and dogs
S. Fujii (1985)
10.2337/diab.22.6.459
Absorption of Insulin from Perfused Rabbit Small Intestine in Vitro
M. Shichiri (1973)
10.1016/0378-5173(86)90069-4
Targeted enteral delivery of insulin to rats
E. Touitou (1986)
10.1016/0168-3659(84)90017-8
Powder dosage form of insulin for nasal administration
Nagai Tsuneji (1984)
10.1016/0006-2952(87)90411-4
Absorption of protein via the intestinal wall. A quantitative model.
E. Ziv (1987)
Controlled release microspheres based on Eudragit L100 for the oral administration of erythromycin.
I. Morishita (1991)
10.1016/0014-5793(76)80016-6
Oral administration of insulin by encapsulation within liposomes
H. M. Patel (1976)
10.2337/diab.37.2.246
New Approach for Oral Administration of Insulin With Polyalkylcyanoacrylate Nanocapsules as Drug Carrier
C. Damgé (1988)
10.1016/0024-3205(82)90673-7
The absorption of insulin from various regions of the rat intestine.
M. Kidron (1982)
10.2337/diab.32.11.1040
Insulin Administered Intranasally as an Insulin-Bile Salt Aerosol: Effectiveness and Reproducibility in Normal and Diabetic Subjects
A. Moses (1983)
Comparison of nasal, rectal, buccal, sublingual and intramuscular insulin efficacy and the effects of a bile salt absorption promoter.
B. Aungst (1988)
10.1002/MED.2610060205
Topical mucosal adhesive dosage forms
T. Nagai (1986)
10.7164/ANTIBIOTICS.23.425
GHYMOSTATIN, A NEW GHYMOTRYPSIN INHIBITOR PRODUCED BY ACTINOMYGETES
H. Umezawa (1970)
10.1016/0378-5173(90)90030-8
Intestinal mucosal transport of insulin
R. J. Schilling (1990)
10.1016/S0140-6736(89)92954-1
ORAL DELIVERY OF INSULIN
YoughW. Cho (1989)
10.1016/S0022-3476(71)80202-0
Intestinal absorption of insulin in patients with fibrocystic disease.
M. Balsam (1971)
10.2337/diab.20.8.552
Insulin Across Respiratory Mucosae by Aerosol Delivery
F. W. Wigley (1971)
10.1016/0378-5173(88)90116-0
Blood glucose control in diabetic rats by transdermal iontophoretic delivery of insulin
Liu Jue-Chen (1988)



This paper is referenced by
10.1007/978-81-322-1160-0_13
Zinc Oxide Nanomaterials as Amylase Inhibitors and for Water Pollution Control
Rohini Kitture (2014)
10.1016/0378-5173(94)00386-J
Using microemulsion formulations for oral drug delivery of therapeutic peptides
J. M. Sarciaux (1995)
10.1016/S0378-5173(96)04832-6
Synthesis and evaluation of a modified mucoadhesive polymer protecting from α-chymotrypsinic degradation
A. Bernkop-Schnürch (1997)
proteínas : III . Aplicação à insulina
Catarina M. Silva (2006)
10.1007/978-3-642-59990-3_3
Proteins as Drugs: Analysis, Formulation and Delivery
C. Middaugh (1999)
10.1007/0-306-46803-4_13
Insulin formulation and delivery.
J. Brange (1997)
10.3109/02652048.2012.742159
Microencapsulation techniques to develop formulations of insulin for oral delivery: a review
F. Cárdenas-Bailón (2013)
10.22028/D291-22771
In vitro characterization of the novel solubility enhancing excipient Soluplus
M. Linn (2011)
10.1002/JPS.2600830606
Oral administration of insulin in solid form to nondiabetic and diabetic dogs.
E. Ziv (1994)
10.1016/J.IJPHARM.2006.08.002
In vitro study of polyoxyethylene alkyl ether niosomes for delivery of insulin.
A. Pardakhty (2007)
10.1016/0169-409X(93)90046-7
Nano- and microparticles for the delivery of polypeptides and proteins
P. Couvreur (1993)
10.1080/10837450802089123
Optimization and In Vivo Evaluation of an Oral Dual Controlled-Release Tablet Dosage Form of Insulin and Duck Ovomucoid
V. Agarwal (2008)
10.1016/J.JDDST.2016.10.012
Development and evaluation of insulin-loaded cationic solid lipid nanoparticles for oral delivery
J. Hecq (2016)
10.1055/s-0031-1296163
In vitro and in vivo evaluation of insulin microspheres containing protease inhibitor.
M. Jelvehgari (2011)
10.1016/J.IJPHARM.2007.05.015
Peroral delivery of insulin using chitosan derivatives: a comparative study of polyelectrolyte nanocomplexes and nanoparticles.
Anchalee Jintapattanakit (2007)
10.1080/10717540590968891
Niosomes with Sorbitan Monoester as a Carrier for Vaginal Delivery of Insulin: Studies in Rats
Meiying Ning (2005)
SYNTHESIS AND CHARACTERIZATION OF NEW DEXTRAN-BASED HYDROGELS AND THEIR USE IN DRUG DELIVERY
(2004)
10.22270/UJPR.V3I6.221
ORAL DRUG DELIVERY OF INSULIN IN DIABETES MELLITUS: AN ATTRACTIVE ALTERNATE TO OVERCOME INVASIVE ROUTE
P. Mathur (2019)
DEVELOPMENT AND CHALLENGES FACING FOR INSULIN ORAL DELIVERY
Venkatachalam Senthil (2013)
10.1016/j.xphs.2019.12.012
Propylene glycol caprylate as a novel potential absorption enhancer for improving the intestinal absorption of insulin: efficacy, safety and absorption-enhancing mechanisms.
Hiroki Ukai (2019)
10.1590/S1516-93322003000100003
Administração oral de peptídios e proteínas: III. Aplicação à insulina
Catarina M. Silva (2003)
10.3109/03639045.2015.1044904
Development and evaluation of chitosan and chitosan derivative nanoparticles containing insulin for oral administration
J. Hecq (2015)
10.2147/IJN.S67947
Novel PLGA-based nanoparticles for the oral delivery of insulin
S. Malathi (2015)
10.1517/13543776.10.9.1357
The use of multifunctional polymers for non-invasive peptide and protein application
A. Bernkop-Schnürch (2000)
Lymphatic transport of orally administered drugs.
L. Reddy (2002)
10.1002/PEN.11006
High speed imaging of drop formation from low viscosity liquids and polymer melts in spinning disk atomization
Y. Senuma (2002)
10.4172/2167-0501.1000143
Recent Advancements in Diabetes Pharmacotherapy
M. A. Woldu (2014)
10.3109/03639049709150544
Development and analysis of a polymer protecting from luminal enzymatic degradation caused by α-chymotrypsin
A. Bernkop-Schnürch (1997)
10.1016/0378-5173(93)90418-F
Enteral insulin delivery by microspheres in 3 different formulations using Eudragit L100 and S100
I. Morishita (1993)
10.1007/978-1-4899-1207-7
Targeting of Drugs 4
G. Gregoriadis (1994)
Oral delivery of proteins: Preparation and characterization of an oral dual-controlled release formulation of insulin and ovomucoid
V. Agarwal (2001)
10.1007/978-4-431-65883-2_14
Controlled Drug Delivery Formulation with Safe Polymers
T. Nagai (1996)
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